BARBITURATES

OFFICIAL NAMES: Methohexital (Brevital), thiamylal (Surital), thiopental (Pentothal), pentobarbital (Nembutal), secobarbital (Seconal), amobarbital (Amytal), bubalbital (Florinal, Fioricet), butabarbital (Butisol), talbutal (Lotusate), aprobarbital (Alurate), amobarbital and secobarbital (Tuinal), phenobarbital (Luminal), mephobarbital (Mebaral)

STREET NAMES: Barbs, downers, red devils, Mexican reds, red birds, blue devils, blue heavens, goof balls, yellow jackets, block busters, reds, blues, pinks, Christmas trees, Amys, rainbows, purple hearts

DRUG CLASSIFICATIONS: Schedule II, III, IV; depressant

OVERVIEW

Barbiturates are among the drugs classified as central nervous system (CNS) depressants. These drugs depress or slow down the activity of nerves that control emotions and bodily functions such as breathing. Barbiturates are prescribed as a sedative that calms the patient or as a hypnotic that helps a person sleep. Other uses include epilepsy treatment and anesthesia before surgery.

Barbiturates are compounds derived from barbituric acid, a substance discovered in 1863 by German chemist Adolf von Baeyer. The year after von Baeyer's discovery, German scientists von Mering and Fischer synthesized the first barbiturate. Production began on the drug called barbital, and medical practices began using it in treatment in 1882.

In 1903, barbital with the brand name of Veronal was marketed as a sleeping pill. Before that time, remedies for insomnia included drinking alcohol or taking bromides, chloral hydrate, or opiates.

In 1912, phenobarbital was introduced under the trade name Luminal. Since 1912, several thousand barbituric acid derivatives have been synthesized. At the beginning of the twenty-first century, only about 12 were on the market.

During the 1930s, many Americans received barbiturate prescriptions to help them sleep or relax. However, people discovered that barbiturates produced an intoxicating effect similar to that produced by drinking alcohol. People took barbiturates to get drunk. They combined the pills with alcohol to become more intoxicated.

The sedative becomes a "thrill pill"

German chemists knew in the 1900s that barbiturates could be addictive. However, people who took barbiturates did not always exhibit symptoms of drug dependence or withdrawal. By the 1940s, the addictive nature of barbiturates alarmed groups ranging from the American Medical Association (AMA) to the United States Food and Drug Administration (FDA).

The 1938 Food, Drug, and Cosmetic Act gave regulatory powers to the FDA. The federal agency used those powers to restrict access to drugs that had a potential for abuse or misuse. The FDA placed barbiturates and amphetamines in that category of drugs that could only be obtained with a prescription from a doctor or dentist. In several decades, the federal government would classify barbiturates and amphetamines as the most abused prescription drugs in the country.

During the 1940s, research indicated that barbiturates produced intoxication and were addictive. People showed signs of withdrawal when they stopped taking barbiturates.

The AMA began warning people about barbiturate abuse in articles with titles like "1,250,000 Doses A Year." That article appeared in a 1942 issue of Hygeia, an AMA magazine published for a general audience.

Warnings about the dangers of nonprescription use of barbiturates did not have the intended effect. Instead of taking precautions about barbiturates, people wanted to try the drug that some called a "thrill pill."

A popular drug combination

The barbiturate became one half of a polydrug habit that became acceptable throughout America. People took barbiturates to sleep at night. In the morning, the barbiturate might make them feel sleepy, so they took an amphetamine.

Amphetamines are central nervous system stimulants. People called them "uppers" because amphetamines gave them energy. Amphetamines cut a person's appetite, so people also used them as diet pills. In the evening a person still "up" from an amphetamine took a "downer" (barbiturate) to sleep at night. In the morning, the drug-taking cycle would start again.

Polydrug use was so widespread by the 1950s that the federal government classified barbiturates and amphetamines as the most abused drugs in the country. The abuse problem grew even though barbiturates were prescription drugs.

Prescription abuse

The FDA discovered the scope of the abuse problem after a 1948 Supreme Court ruling gave the agency the authority to investigate drug sales at the pharmacy level. According to an FDA report, barbiturate transactions included:

• A prescription refilled 61 times, with three refills after the patient died from barbiturate intoxication.
• A Kansas City woman obtained 40 refills for a prescription. Her doctor prescribed refills. Other refills came by mail order. The woman died from barbiturate intoxication.
• The staff at a Tennessee drug store could not explain what happened to more than 180,000 barbiturates sent to the store by manufacturers and wholesalers.

According to the FDA report, enforcement action during the 1940s and 1950s centered primarily on pharmacies. Those involved in the illegal sales of barbiturates included pharmacists as well as drug store owners and employees.

As pharmacies complied with the law, the FDA targeted black market sales of barbiturates from 1960 through 1965. Meanwhile, a new generation discovered barbiturates.

Drug use during the 1960s

During the 1960s, youths began to experiment with drugs on a wider scope. Middle-class and upper-class youths discovered that it was easy to obtain barbiturates; they often found them in their parents' medicine chests.

A United States Senate Subcommittee heard about the severity of the problem from a Dr. Sidney Cohen. He said that 10 billion barbiturate doses would be produced in 1969. That figure represented an 800% increase in the amount produced in 1942, according to the 1972 Consumers Union Report on Licit and Illicit Drugs.

The 1970s bring restricted access to barbiturates

According to the FDA, barbiturate abuse continued during the 1970s and 1980s. However, the adoption of the federal Comprehensive Drug Abuse Prevention and Control Act in 1970 would limit access to highly addictive drugs like barbiturates. The act placed barbiturates on a list of controlled substances that were subject to abuse. The act limited the number of prescriptions a person could receive. It also set annual quotas for the amount of drugs that pharmaceutical companies could manufacture.

As access to barbiturates was limited, benzodiazepines were promoted as a safer alternative. Benzodiazepines went on the market during the 1960s and were thought to be less addictive than barbiturates.

With barbiturates less available, drug abusers turned to other illegal substances during the 1970s and 1980s. One indication of drug demand was the record of drugs seized by the United States Customs Service. Customs confiscated greater quantities of marijuana, heroin, and cocaine. As a result, Customs recorded seizures of each drug separately.

Barbiturates in the late twentieth century

At the close of the twentieth century, the DEA reported that barbiturates represented about 20% of all depressant prescriptions in the United States. Uses ranged from epilepsy treatment to assisted suicide in Oregon. In 1997, Oregon voters approved the Death with Dignity Act, which allows doctors to prescribe lethal dosages of barbiturates to terminally ill people.

Furthermore, the late 1990s brought concerns about benzodiazepines, the drugs thought to be a safe alternative to barbiturates. Benzodiazepines produced side effects similar to those produced by barbiturates. These included the risk of addiction when high doses were taken. Benzodiazepines accounted for 30% of all prescriptions for controlled substance, according to the DEA.

CHEMICAL/ORGANIC COMPOSITION

Barbiturates are compounds derived from barbituric acid. These drugs are classified in four categories that are defined by the amount of time that it takes for barbiturate to produce results and how long those results last.

The ultrashort-acting barbiturates methohexital, thiamylal, and thiopental produce unconsciousness within several minutes. These drugs are used for anesthesia before surgery.

Short and intermediate-acting barbiturates take effect within 15 to 40 minutes. The effects of these barbiturates last from five to six hours. These medications are prescribed for sedation or to help people sleep. The barbiturates in this category are amobarbital, pentobarbital, secobarbital, bubalbital, butabarbital, talbutal, and aprobarbital.

Mephobarbital and phenobarbital are long-acting barbiturates that take effect within approximately one to two hours. These effects last approximately 12 hours.

According to the United States Drug Enforcement Agency (DEA), drug abusers favor short and intermediate-acting barbiturates. Barbiturate users often refer to the pills they take in terms of the color of the capsule. These street names include blues or blue devils for Amytal; reds, red birds; and red devils for Seconal; yellow jackets for Nembutal; purple hearts for Luminal; and rainbows and Christmas trees for Tuinal.

INGESTION METHODS

In the United States, barbiturates are manufactured in various forms. Most barbiturates come in pills and capsules that patients swallow. Some barbiturates are manufactured as an elixir, a liquid form of the drug that patients swallow.

Other barbiturates are manufactured as a powder that is injected into the patient's vein. In addition, pentobarbital is manufactured as a suppository that is inserted in the rectum. Pentobarbital is also available in capsule, tablet, elixir, and injection dosages. Phenobarbital is produced in capsule, tablet, injection, and elixir dosages.

Amobarbital is manufactured in pill, capsule, and injection dosages. Butabarbital is manufactured in capsule, tablet, and elixir dosages. Secobarbital is produced in capsule and injection dosages.

Aprobarbital is an elixir, mephobarbital is a tablet, and the drug containing secobarbital and amobarbital is a capsule. Legally prescribed barbiturates and those used in medical procedures are used in the form that the drug is produced. Some drug abusers will inject powder from capsules or ground-up tablets.

THERAPEUTIC USE

Barbiturates produce forms of central nervous system depression. Reactions to these drugs range from mild sedation (producing sleep) to a coma. Doctors may prescribe barbiturates as sedatives to calm patients' nerves, reduce tension or help them sleep. The drugs are also used as an anticonvulsant to control epileptic seizures.

In addition, the sleep-producing action of barbiturates is used to relax and partially anesthetize patients before some surgical procedures. Before some major brain surgeries, barbiturates (usually pentobarbital or thiopental) are used to temporarily induce coma in an effort to protect the brain; these drugs can reduce the metabolic rate of brain tissue and control cerebral blood flow.

Ultrashort-acting barbiturates

The ultrashort-acting barbiturates methohexital (Brevital), thiamylal (Surital), and thiopental (Pentothal) are administered as an anesthetic before surgery. The barbiturate is injected into the patient's vein to induce anesthesia. The patient then receives a longer-acting anesthetic like nitrous oxide. The drugs are used in hospital settings and are not subject to abuse, according to the DEA.

Short-acting and intermediate-acting barbiturates

The barbiturates in these categories are pentobarbital (Nembutal), secobarbital (Seconal, Amatyl), a combination of amobarbital and secobarbital (Tuinal), bubalbital (Florinal, Fioricet), butabarbital (Butisol), talbutal (Lotusate), and aprobarbital (Alurate).

Short-acting and intermediate barbiturates are prescribed as sedatives and sleeping pills. In addition, veterinarians use pentobarbital to anesthetize animals. This barbiturate is also used to euthanize or put animals to sleep.

Long-acting barbiturates

The long-acting barbiturates phenobarbital (Luminal) and mephobarbital (Mebaral) are used medically to help a patient sleep. Another use is day-long sedation, a procedure that treats tension and anxiety. Furthermore, long-acting barbiturates are used with other drugs in the treatment of convulsive conditions like epilepsy.

Phenobarbital is the oldest antiepileptic drug in common use and has a solid efficiency record for the control of seizure. However, due to some side effects (hypertension, depression, dizziness, rash, memory lapses) and drug interactions (primarily other anticonvulsants), phenobarbital is now generally used as a second-line treatment.

Assisted suicide

After Oregon voters in 1997 approved the Death with Dignity Act, terminally ill people could receive prescriptions for lethal dosages of drugs so that they could end their lives. To be eligible for the Death with Dignity drugs, the person needed a diagnosis of less than six months to live. That diagnosis would be verified by two physicians, who would also determine that the person was competent when the decision was made.

Secobarbital was prescribed to 67 out of 70 patients during 1998 through 2000, according to an Oregon Public Health Services report.

USAGE TRENDS

Passage of the federal Controlled Substances Act in 1970 restricted access to barbiturates. That action led to an eventual decline in the use and abuse of one of the most widely prescribed drugs of the twentieth century.

Scope and severity

In 1977, pharmacists filled approximately 7.9 million prescriptions for Luminal (phenobarbital), according to the National Institute of Drug Abuse (NIDA). NIDA estimated that approximately 1.7 million Nembutal prescriptions were filled, along with an estimated 1.5 million Seconal prescriptions, and 375,000 Amytal prescriptions.

NIDA research included estimates of deaths linked to use of a barbiturate. The federal agency estimated that 250 deaths were related to secobarbital, the same number for pentobarbital, 110 phenobarbital fatalities, and 30 deaths were connected to amobarbital.

At the start of the twenty-first century, the United States Drug Enforcement Agency said that barbiturates accounted for 20% of depressant prescriptions. Barbiturate use had declined so much that researchers no longer compiled separate statistics about the drug. Instead, barbiturates were placed in the sedative category that included tranquilizers.

Age, ethnic, and gender trends

During the 1950s, barbiturates were popular with the middle and upper classes. By the 1960s, barbiturate users spanned the generations from youths to older adults. However, recent surveys of illicit drug abuse illustrated the sharp decline in barbiturate abuse. In the National Household Survey on Drug Abuse for 2000, sedatives were placed in a category of psychotherapeutic drugs. This category included pain relievers, tranquilizers, stimulants, and pain relievers.

The survey conducted by the Substance Abuse and Mental Health Services Administration (SAMHSA) focused on the 14 million Americans who were current illicit drug users. Current use was defined as having used the drug the month before the survey. Those surveyed were age 12 and older.

Of that total, 1.8% of men and 1.7% of women had taken a psychotherapeutic drug for nonmedical reasons during the month before the survey. Of youths between the ages of 12 and 17, 7.7% of girls and 3.3% of girls were "likely" to use a illicit psychotherapeutic drugs.

Typically, women are more likely then men to receive barbiturate prescriptions because they are more likely to seek help for anxiety, depression, and insomnia. Barbiturates are also widely prescribed to older adults. Elderly persons use these drugs as sedatives, and again women receive the majority of the prescriptions.

MENTAL EFFECTS

The mental effects of barbiturates depend on the amount of the drug taken and the strength of the dosage. Generally, a person falls asleep when taking a prescribed dosage at bedtime.

Intoxication

A person experiences intoxication after taking a larger dose of a barbiturate. A mild state of intoxication brings a feeling of euphoria (happiness) that frequently leads to increased self-esteem and a lowering of inhibitions.

As intoxication increases, the person exhibits behavior similar to that displayed by a person intoxicated by alcohol. The person may be short-tempered, aggressive, and possibly violent. Other possible symptoms are impaired judgement and mood swings.

Upon waking, the person may experience "hangover" sensations that include dizziness. The person may still be sleepy and behave in a clumsy manner. Depression may be experienced.

Dependence

Barbiturate use can lead to both psychological and physical dependence. Psychological addiction can occur quickly. Signs of drug dependence include relying on the drug for a desired effect. The addicted abuser believes he or she must take a barbiturate to sleep, relax, or have a feeling of well-being. As the person relies emotionally on the drug, continued use of barbiturates leads to physical dependence.

As people develop tolerance for barbiturates, they may think they need more of the drug or a higher dosage to get the desired effect. This can lead to an overdose, which results from a person taking a larger than prescribed dose of a drug. Psychological symptoms of a barbiturate overdose include extreme drowsiness, intense confusion, and impaired judgement.

PHYSIOLOGICAL EFFECTS

Barbiturates act on the central nervous system, and use of these drugs can bring about changes ranging from mild sedation to a coma. Furthermore, an overdose or an attempt to withdraw abruptly from barbiturates can be fatal.

Short-term effects

Barbiturates help a person to sleep. However, this slumber differs from normal sleep. Barbiturate use decreases the amount of the dream phase of sleep known as the rapid eye movement (REM) stage. This phase of sleep is necessary for maintaining good health.

Barbiturates produce reactions similar to those of alcohol. A person may experience "hangover" symptoms including headache and dizziness. They may still feel tired and less alert as well. A person experiencing these symptoms should not drive or operate machinery. These hangover symptoms may last for hours.

Like alcohol, barbiturates are intoxicating. During the stage after mild intoxication, the person's speech may be slurred. The person may stagger and lose muscular control. Other symptoms of intoxication include irritability, shallow breathing, and fatigue.

At-risk groups

Older adults and pregnant women should consider the risks associated with barbiturate use. When a person ages, the metabolization rate for drugs decreases. As a result, people over age 65 are at higher risk of the harmful effects of barbiturates. There is also greater risk for drug dependence.

When barbiturates are taken during pregnancy, the drug passes through the mother's bloodstream and through the placenta into the fetus. After the baby is born, it may experience withdrawal symptoms and have trouble breathing. Other withdrawal symptoms include troubled sleep patterns, fever, and irritability. Furthermore, nursing mothers who take barbiturates may transmit the drug in their breast milk.

Harmful side effects

An individual using CNS depressants like barbiturates can develop a tolerance for the drugs. Over time, the body becomes used to the presence of barbiturates in the system. When this happens, the prescribed dose of the drug does not produce a desired result and the individual may take more pills or stronger dosages of barbiturates. A tolerance to that level can develop, requiring even more barbiturates or a stronger dosage. As tolerance continues to increase, the individual may take a fatal dose in their attempt to get the desired effect.

Overdose occurs when a drug is consumed in a dose that is greater than the body can handle. Symptoms of an overdose include intense tiredness, confusion, irritability, and fever or a low body temperature. The person may experience shortness of breath, sleepiness or difficulty getting to sleep, and weakness. Other signs of overdose are slurred speech, a slow heartbeat, and uncommon eye movements.

An overdose may be triggered by drinking alcohol or taking a drug like an amphetamine while using barbiturates. In an effect called synergy, the two drugs intensify the effects of each other. As a result, the prescribed dose of one drug could be fatal if taken with another drug.

The amount of a fatal dosage of barbiturate will vary with the individual. However, the lethal dose is usually 10 to 15 times as large as a usual dose. A fatal overdose starts with cardiovascular collapse followed by respiratory depression. The person then falls into a coma and dies.

Long-term health effects

Barbiturates are addictive. A person may develop a physical dependency after taking more than 400 mg of pentobarbital or secobarbital a day over an approximately 90-day period.

Long-term use of other barbiturates can also lead to physical and psychological dependence. Symptoms of dependence include the feeling that a person cannot relax or sleep without taking a barbiturate. Another sign of addiction is a tendency to increase the dosage.

People at risk of barbiturate abuse and addiction include alcoholics and abusers of opiates, sedative-hypnotics, and amphetamines.

Withdrawal

When a person stops taking barbiturates, the body begins to adapt to the lack of drugs in the system. If a person has used barbiturates in large doses or for an extended period of time, a physician should be consulted about the withdrawal process.

Onset of withdrawal symptoms usually begin eight to 16 hours after the last pill was taken. Symptoms may last up to 15 days if the person was a long-term barbiturate user or took large doses of the drug.

During this time, the person feels weak, dizzy, and anxious. Withdrawal brings tremors and shakes. The person may hallucinate, experience delusions, or become violent and hostile. Withdrawal symptoms generally diminish over time.

In some cases, withdrawal symptoms can be fatal, so a person cannot just stop taking barbiturates. The physician will establish a plan of gradual withdrawal from barbiturates.

REACTIONS WITH OTHER DRUGS OR SUBSTANCES

From the 1940s on, people took amphetamines, the highly addictive drugs referred to as "uppers," during the day. They used amphetamines to increase their energy and to relieve the effects of barbiturates. Those effects could include sleepiness and hangover symptoms.

By evening, people who still experienced the effects of the amphetamines turned to "downers," the street name for barbiturates. People took downers to slow down and sleep. In the morning, the drug-taking cycle started again. The person took an upper to counteract the effects of the downer.

Barbiturates are frequently taken in combination with amphetamines. Amphetamines are highly addictive drugs known as "uppers" since they increase energy. They are used to counteract the "downer" effect of barbiturates that induce sleep. This cycle is very dangerous. Both types of drug are addictive and can lead to tolerance. The combination of amphetamine use during the day and barbiturate use as night results in a synergy of the two drugs, which lowers the amount of the drug that is fatal. There is also synergy when a person uses barbiturates and consumes alcohol.

The person combining drugs does not know what dosage of the combination will be lethal. As a result, someone using a barbiturate could die after taking a prescribed dose of an amphetamine.

Barbiturates and other medications

Medications can cause adverse reactions for the person taking barbiturates. Tranquilizers and antihistamines depress the brain's control over breathing. This could increase the chance of respiratory failure when someone uses barbiturates.

Barbiturates may counteract the effects of birth control pills that contain estrogen. A woman taking those oral contraceptives may become pregnant after taking barbiturates.

TREATMENT AND REHABILITATION

Barbiturates act so powerfully on the nervous system that a person must gradually withdraw from these drugs. To suddenly stop taking barbiturates could result in serious medical complications or death. This withdrawal process, known as detoxification, is part of the treatment process for people dependent on barbiturates.

Medically supervised detoxification reduces the risk of death as the person's body adapts to reduced amounts of barbiturates. This treatment starts with the person receiving the usual amount of the barbiturate and then less and less of the drug over time. The person still endures withdrawal symptoms. However, the more serious symptoms may be less severe.

To lessen the REM rebound effect, it is recommended that a person reduce barbiturate consumption by one therapeutic dosage over a period of five or six days, according to Physicians' Desk Reference. Another method is to take two doses instead of three for a week.

Detoxification may occur in a hospital, or treatment may be given on an outpatient basis. Counseling is also part of the treatment regimen. After the person is successfully treated for physical addiction, he or she must follow through with psychological rehabilitation.

Behavioral treatment helps a person avoid barbiturates by providing guidance about how to function without drugs and how to cope with cravings. The behavior-modification treatments can be set up as one-on-one counseling sessions, group therapy, family counseling, or other types of therapies. For the person wanting to remain drug-free, ongoing support can be found in 12-step programs and other groups that meet regularly.

PERSONAL AND SOCIAL CONSEQUENCES

Barbiturates harm more people than those who take them. People who drive while intoxicated by barbiturates risk the lives of others. A pregnant woman who takes barbiturates passes the drugs along to her unborn baby. After the baby is born, the infant will have to undergo withdrawal from the barbiturate.

Barbiturates can also affect relationships. The drugs have been compared to alcohol in terms of the intoxicating effects. Both drugs produce a euphoric feeling during the mild intoxication stage. People may enjoy being around the person at that point.

As the intoxication increases, the person may become belligerent. He or she may provoke an argument. There is a possibility of violence. Judgement is impaired, so the person might make an unsafe decision like trying to drive home.

Some people who abuse barbiturates do not worry about driving under the influence. The reason is not because they are confident about their ability to drive, but because they know that police will not smell alcohol on their breath.

In some ways, the effects of barbiturates are predictable. Prolonged barbiturate use can shorten a person's attention span. The person may suffer memory loss. Both conditions would make it difficult for a person to do well in school or perform on a job.

In addition, barbiturates make a person tired, anxious, and depressed. The person who took barbiturates to feel better finds that the drugs only deepen the depression.

As a person takes more or higher doses of a barbiturate, he or she does not know if that dose will be fatal. And with increased tolerance, the difference diminishes between an intoxicating dose and a fatal dose.

Furthermore, the method of withdrawing from barbiturates is not as simple as stopping completely. Barbiturates slow the brain's activity, so there could be a rebound when a person stops taking the drug. This rebound activity could lead to seizures and other harmful consequences.

LEGAL CONSEQUENCES

When barbiturates first went on the market during the 1930s, people in the United States did not need a prescription to buy them. Lawmakers soon realized that barbiturates were addictive. Some states adopted laws that banned the sale of nonprescription barbiturates. The federal government took similar action after the Food and Drug Administration gained regulatory power in1938. That set the stage for a 40-year battle against barbiturate abuse.

Legal history

The federal Food, Drug, and Cosmetics Act of 1938 gave regulatory powers to the Food and Drug Administration (FDA). Pharmaceutical companies apply to the FDA for approval to manufacture a new drugs. The approval process includes research, testing, and hearings. Once a drug is approved, the FDA determines whether a prescription is required.

FDA regulations about prescription drugs apply to how the manufacturer promotes or advertises the medications. Unless specified by other regulations such as the Controlled Substances Act (CSA), there are no restrictions on the condition for which the doctor prescribes the pill, the dosage prescribed, or the amount of time that the patient will take the pill.

Federal guidelines, regulations, and penalties

The Controlled Substances Act (CSA) portion of the 1970 Comprehensive Drug Abuse Prevention and Control Act classified drugs in five categories based on the effect of the drug, its medical use, and potential for abuse. Schedule I contains drugs like heroin, which have no medical use but may be used in research. It is the most tightly controlled category.

Schedule II drugs have a high potential for abuse. They are accepted for medical use with restrictions. These drugs may lead to severe psychological or physical dependence. Barbiturates in this category are amobarbital (Amytal), pentobarbital (Nembutal), and secobarbital (Seconal, Tuinal).

Schedule III drugs have less of a potential for abuse than drugs in Schedules I and II. The drugs have a medical use. Abuse of these drugs may lead to "moderate or low psychological dependence or high psychological dependence," according to the CSA. Barbiturates in this category are aprobarbital (Alurate) butabarbital (Busitol, Bubatel), and butibal (Fiorinal). A prescription may be filled up to five times during the six months after the first prescription was written.

Schedule IV drugs have a low abuse potential as compared to Schedule III drugs. These substances have an accepted medical use. They could lead to limited psychological or physical dependence, according to the CSA. The Schedule IV barbiturates are barbital (Veronel), mephobarbital (Mebaral), and phenobarbital (Luminal). Five prescription refills are allowed during the six months after the patient received the first prescription.

Penalties. Federal law prohibits the possession, use, and distribution of illegal drugs. The Controlled Substances Act established tighter controls on the manufacture and distribution of drugs like diet pills. Limits were set on the amounts of Schedule II pills that could be manufactured.

Procedure for the legal distribution of pills included the requirement of a written prescription for Schedule II drugs. An exception is made in emergencies.

For Schedule III and IV drugs, the prescription may be written or called into the pharmacy. Both the health care practitioner and pharmacist are required to keep records when prescriptions are filled for controlled drugs.

Trafficking. Trafficking is the illegal distribution of controlled drugs. Federal penalties for this crime can include fines and imprisonment. Sentencing is based on factors such as whether the trafficker is a first-time offender. Penalties are higher for a second offense. In addition, if the illegal distribution of a Schedule II drug results in death or serious injury, the convicted offender faces a prison term of from 20 years to life.

In cases where there is no serious injury or death, the penalties for a first-time offense are:

• Schedule II: Trafficking 100 grams or more of methamphetamine carries a prison term of from 10 years to life and a fine of up to $4 million.
• Schedule III drugs: Trafficking any quantity of these drugs is punishable by up to five years in prison and a maximum fine of $250,000.
• Schedule IV drugs: Illegally distributing any quantity of these drugs carries a prison term of up to three years and a fine of up to $250,000.

Penalties for drug abusers. The federal penalty for the first-time offense of illegally possessing a controlled substance is up to one year in prison and a fine of from $1,000 to $100,000. Penalties are generally doubled for a second offense.

In some cases, a person may not receive a prison sentence. The Anti-Drug Abuse Act of 1988 imposes a civil penalty on the minor drug offender, the person possessing a small quantity of an illegal controlled substance. Possession of this quantity known as a "personal use amount" carries a fine of up to $10,000.

Drug laws in the United Kingdom. In the United Kingdom, substances are regulated by the 1971 Misuse of Drugs Act and the 1986 Medicines Act. The 1971 act placed drugs in categories of A, B, or C. The A category contains the most dangerous drugs. The least dangerous drugs are in Category C.

The 1986 act established five medical schedules that are based on factors such as the therapeutic value of the drug. Another consideration is whether a prescription is required. Schedule 1 is the most strictly controlled category.

Barbiturates are a Class B drug unless the barbiturate is used in an injectable form. It then becomes a Class A drug.

The maximum penalty for possession of a Class B drug is five years of prison, an unlimited fine (of any amount), or prison and a fine. The maximum fine for supply (trafficking) is a 14-year prison term, an unlimited fine, or both penalties.

For Class A drugs, the penalty for possession is seven years in prison, an unlimited fine, or both. The supply penalty for this class, which includes cocaine and heroin, is life imprisonment, an unlimited fine, or both penalties.

See also Amphetamines; Antidepressants; Benzodiazepine; Diet pills; Tranquilizers

RESOURCES

Books

Breacher, Edward M., et al. The Consumers Union Report on Licit and Illicit Drugs. Boston: Little Brown & Co., 1972.

Dorsman, Jerry. How to Quit Drugs for Good. Rocklin, CA: Prima Publishing, 1998.

Hughes, Richard and Robert Brewin. The Tranquilizing of America. New York: Harcourt Brace Jovanovich, 1979.

Medical Economics. Physicians' Desk Reference 2001. Montvale, NJ: Medical Economics, 2001.

Wolfe, Sidney. Worst Pills, Best Pills. New York: Pocket Books,1999.

Organizations

National Institute on Drug Abuse (NIDA), National Institutes of Health, 6001 Executive Blvd., Room 5213, Bethesda, MD, USA, 20892-9561, (301) 443-1124, (888) 644-6432, <http://www.nida.nih.gov>.

U.S. Drug Enforcement Administration, 2401 Jefferson Davis Highway, Alexandria, VA, USA, 22201, (800) 882-9539, <http://www.dea.gov>.

U.S. Food and Drug Administration (FDA), 560 Fishers Lane, Rockville, MD, USA, 20857-0001, (888) 463-6332, <http://www.fda.gov>.

Liz Swain

Barbiturates

What Kind of Drug Is It?

Barbiturates (pronounced bar-BIH-chuh-rits) are drugs that act as depressants and are used as sedatives or sleeping pills. Because they are depressants, they are often called "downers." According to Lawrence Clayton in Barbiturates and Other Depressants, "Any depressant will kill if taken in a large enough quantity." Accidental overdose can occur quite easily among barbiturate users.

The effects of barbiturates are very similar to those of alcohol and include increased feelings of relaxation, sleepiness, and a decrease in inhibitions. Barbiturates are habit-forming drugs and should not be used on an everyday basis. They can cause depression in high doses and addiction when taken over a long period of time.

Overview

Barbiturates have an extremely high potential for abuse. Ever since their introduction in the early 1900s, barbiturates have been considered addictive drugs. Barbiturates slow down both the mind and the body. In his book A Brief History of Drugs: From the Stone Age to the Stoned Age, Antonio Escohotado pointed to their "high capacity to produce numbness" by putting the user in a state somewhere between drunkenness and sleep. Aside from those effects, he continued, is their "almost inevitable ability to kill in high doses: a detail that converted these drugs into the most common means of committing suicide" from the 1940s through the 1960s.

Discovered in the 1860s

The story of barbiturates began "when a chemist combined animal urine and acid from apples," explained Clayton. That chemist was German professor and future Nobel prizewinner Adolf von Baeyer (1835–1917). The substance he created became known as barbituric (bar-bih-CHUR-ik) acid. It received its name because Baeyer first produced it on St. Barbara's Day (a day of religious recognition observed each year on December 4) of 1863.

Official Drug Name: Amobarbital (AMM-oh-BAR-bit-al; Amytal), aprobarbital (AH-pro-BAR-bit-al; Alurate), barbital (BAR-bit-al; Veronal), butabarbital (BYOOT-uh-BAR-bit-al; Butisol), butalbital (byoo-TAHL-bit-al; Fioricet and Fiorinal), mephobarbital (MEFF-oh-BAR-bit-al; Mebaral), pentobarbital (PENT-oh-BAR-bit-al; Nembutal), phenobarbital (FEEN-oh-BAR-bit-al; Luminal), secobarbital (SEK-oh-BAR-bit-al; Seconal), secobarbital with amobarbital (Tuinal), thiopental (THY-oh-PENN-tal; Pentothal).

Also Known As: Barbs, downers, and sleeping pills (general names). Certain barbiturates have their own street names, often based on the color of the pill: blues or blue dolls for Amytal; purple hearts for Luminal; rainbows for Tuinal; reds, red birds, or red devils for Seconal; yellows or yellow jackets for Nembutal.

Drug Classifications: Schedule II, III, IV; depressant

Following Baeyer's discovery, two German researchers, Dr. Joseph von Mering (1849–1908) and Nobel prizewinner Emil Hermann Fischer (1852–1919), produced barbital, the first barbiturate. Barbiturates are compounds derived from barbituric acid. Doctors recognizedbarbital'ssleep-enhancingeffectsasfar back as 1882. More than twenty years later, in 1903, barbital was marketed as a sleeping pill under the brand name Veronal. The second barbiturate, phenobarbital, arrived on the scene in 1912 under the name Luminal. Since then, several thousand barbituric acid-type drugs have been synthesized. At the beginning of the twenty-first century, only about twelve were still being used.

Barbiturates were found to reduce the activity of nerves that control emotions and bodily functions such as breathing. Because of the drugs' soothing effects, they were commonly prescribed as sedatives for nearly fifty years. Other uses include epilepsy treatment and anesthesia before surgery.

Intoxicating Effects Lead to Abuse

During the 1930s, many Americans received barbiturate prescriptions to help them sleep or relax. Barbiturates quickly gained a reputation as an intoxicant, a substance that makes users seem drunk. People began taking barbiturates as recreational drugs. They also began the dangerous practice of combining the pills with alcohol to increase the intoxication.

The 1938 Food, Drug, and Cosmetic Act gave authority over drug production to the U.S. Food and Drug Administration (FDA). The federal agency used those powers to restrict access to drugs that had a potential for abuse or misuse. The use of barbiturates without a medical doctor's prescription became illegal in the United States. But that didn't keep the drugs from becoming more and more popular throughout the 1940s.

At that time, researchers in the United States and the United Kingdom began noticing a disturbing trend. Over the years, the production of barbiturates had grown from thousands to millions of doses per year. Higher rates of barbiturate production and consumption seemed to coincide with a growing number of deaths from barbiturate poisoning. As late as 1964, Joel Fort, author of "The Problem of Barbiturates in the United States of America," argued against the wide availability of barbiturates. "Despite conclusive evidence to the contrary," he wrote, "many physicians in the United States appear to think and act as though barbiturates are completely harmless drugs that can be prescribed in unlimited quantities." His report was prepared for the United Nations Office on Drugs and Crime.

Downers and Uppers

The pairing of barbiturates with amphetamines became a significant problem throughout the United States in the 1940s and 1950s. It all began when record numbers of people started taking barbiturates to help them sleep at night. To counteract the grogginess and lack of energy they suffered the next morning, users would take amphetamines to help them wake up. Amphetamines are stimulants or "uppers." At night, users still "up" from an amphetamine high would take "downers," or barbiturates, to rid themselves of their extra energy and get to sleep. The next day the drug-taking cycle would start again. The regular use of barbiturates with amphetamines was so widespread by the 1950s that the U.S. government classified them as the most abused drugs in the country.

New Generation, New Drugs

During the 1960s, a new generation of young people began experimenting with a wide variety of mind-altering substances. Barbiturates were among the drugs abused by these new users, mainly because the pills were widely available and frequently used by the generation that came before them—their parents. According to the 1972 Consumers Union Report on Licit and Illicit Drugs, 10 billion barbiturate doses were scheduled for production in 1969 alone. That figure represented an 800-percent increase in the amount produced twentyseven years earlier in 1942.

Prescription Abuse

In 1948, the Supreme Court of the United States gave the Food and Drug Administration (FDA) permission to investigate pharmacies' records of barbiturate prescriptions. The results showed a shocking pattern of abuse. In one case a single prescription for barbiturates was refilled sixty-one times. The last three of those refills were approved after the patient had already died from a barbiturate overdose. In another incident, more than 180,000 barbiturates simply disappeared from a Tennessee drug store. Records indicated that drug manufacturers had sent the pills to the store, but the staff at the store was unable to explain where they went.

Soon after these discoveries were made public, pharmacies began complying with laws regarding the sale and refill of prescription barbiturates. Illegal transactions made by pharmacists, drug store owners, and drug store employees dropped dramatically. This led to the growth of a black market—a market in which barbiturates are supplied and sold illegally—beginning in the 1960s.

Passage of the Controlled Substances Act (CSA) in 1970 restricted access to barbiturates in the United States. Another category of anti-anxiety drugs, the benzodiazepines (pronounced ben-zoh-die-AZ-uh-peenz), were promoted as a safer alternative to

Drugs and Fame

"Until recently," wrote Paul M. Gahlinger in Illegal Drugs: A Complete Guide to Their History, Chemistry, Use, and Abuse, "about 3,000 people a year died from barbiturates, about half of them suicides." Film star and sex symbol Marilyn Monroe died of an overdose on August 5, 1962, after taking nearly fifty Nembutal tablets. The popular blonde had appeared in such films as Some Like It Hot, How to Marry a Millionaire, Bus Stop, and Gentlemen Prefer Blondes. Her death was controversial as it was deemed a suicide. But many of her fans insisted that she would never take her own life.

Other celebrity deaths can be attributed to barbiturate use as well. Electric guitarist Jimi Hendrix died of suffocation brought on by a barbiturate overdose on September 18, 1970. Hendrix thrilled audiences with his performance at Woodstock in 1969. Among his popular songs were "Purple Haze," "All Along the Watchtower," and an electrifying guitar rendition of "The Star Spangled Banner."

Barbiturates may have played a role in the death of Elvis Presley, the King of Rock 'n' Roll, as well. He died on August 16, 1977, of a drug overdose. A mixture of methaqualone, morphine, codeine, and several barbiturates were found in his system at the time of his death. (Entries on

each of these drugs are available in this encyclopedia.) Remembered for his many movies, he recorded such hits as "Hound Dog," "Jailhouse Rock," "Love Me Tender," "Don't Be Cruel," and "Return to Sender." Each year, thousands of people visit his former home, Graceland, in Memphis, Tennessee.

barbiturates. Prescriptions for benzodiazepines rose because health providers considered them less addictive than barbiturates, with a lower risk of accidental overdose among users. As barbiturates became harder to obtain, drug abusers turned to other illegal substances during the 1970s and 1980s. U.S. Drug Enforcement Administration (DEA) reports indicate that the use of marijuana, heroin, and cocaine began to rise after 1970.

What Is It Made Of?

Barbiturates are compounds derived from barbituric acid, a substance made from carbon, hydrogen, nitrogen, and oxygen. The uric acid portion of the name is taken from the main ingredient in urine, which provides the basis for barbituric acid.

Barbiturate users often refer to the pills they take in terms of the color of the capsule. These street names include blues or blue dolls for Amytal; reds, red birds, or red devils for Seconal; yellows or yellow jackets for Nembutal; purple hearts for Luminal; and rainbows for Tuinal.

How Is It Taken?

In the United States, barbiturates are manufactured in various forms. Most barbiturates come in pills and capsules that patients swallow. Some are available as liquids that are swallowed. Others are produced in injectable forms. Some abusers have been known to mix up their own injectable liquid barbiturates by crushing pills and combining the powdered drug with water.

Drugs made from barbituric acid are classified in one of four categories: ultrashort-, short-, intermediate-, or long-acting. These categories are defined by the amount of time that it takes for the barbiturate to produce effects in the user and how long those effects last.

DEA reports indicate that drug abusers favor short- and intermediate-acting barbiturates. These types of barbiturates take effect within fifteen to forty minutes of being swallowed, and their depressant effects last from five to six hours. Drugs in this category include amobarbital, aprobarbital, butabarbital, pentobarbital, and secobarbital.

Are There Any Medical Reasons for Taking This Substance?

For many years, barbiturates were used as daytime sedatives. Since the discovery of another type of anti-anxiety drug called benzodiazepine, which is considered safer, barbiturates are not prescribed for this purpose as frequently as they once were.

When combined with an aspirin or nonaspirin pain reliever and caffeine, the barbiturate butalbital is effective in treating severe pain. It is sometimes prescribed to relieve the pain associated with migraine headaches.

As of 2005, barbiturates were used primarily for presurgical and surgical anesthesia. They were being administered to patients in operating rooms under an anesthetist's care. They also continued to be used in the treatment of certain types of epilepsy.

Usage Trends

Reactions to barbiturates range from mild sedation to coma and even death. Doctors may prescribe barbiturates as sedatives to calm patients' nerves, reduce tension, or help them sleep. The drugs are also used as an anticonvulsant to control epileptic seizures. The sleep-producing action of barbiturates is used to relax and partially anesthetize patients before some surgical procedures.

At the close of the twentieth century, the DEA reported that barbiturates represented about 20 percent of all depressant prescriptions in the United States.

The "Death with Dignity" Debate

The use of barbiturates in assisted suicides in Oregon has fueled a storm of controversy throughout the United States. In 1997 Oregon became the only state in the nation to permit assisted suicide. Oregon voters approved the Death with Dignity Act, allowing doctors to prescribe lethal doses of barbiturates, most often secobarbital, to terminally ill people.

The terms of the act defined terminally ill people as those individuals estimated to have fewer than six months to live. That diagnosis had to be verified by two physicians, who would also determine whether the terminally ill person was competent to make such a decision. "During the six years since the Oregon law took effect," wrote Jim Barnett in a 2004 article for the

Oregonian, "171 Oregonians have died by doctorassisted suicide."

The administration of President George W. Bush has fought against the Death with Dignity Act since 2001. Opponents of the assisted suicide law argue that the state of Oregon is breaking federal laws that govern the use of controlled substances. However, supporters of the Death with Dignity law believe that it represents the will of the people—the voters of Oregon. They contend that the act treats the terminally ill with compassion and dignity by allowing them the right to end their lives humanely. As of mid-2005, the U.S. Supreme Court had not ruled on the issue of assisted suicide in Oregon.

Barbiturate Use Down Since the Mid-1980s, Says SAMHSA

Recent surveys of illicit drug abuse showed a sharp decline in barbiturate abuse since the mid-1980s. The National Survey on Drug

Use and Health (NSDUH), formerly known as the National Household Survey on Drug Abuse, is a carefully calculated assessment of American drug use. It is conducted by the Substance Abuse and Mental Health Services Administration (SAMHSA) and obtains information on nine different categories of illicit drug use. As of 2005, the latest results available were from the 2003 survey. All of the respondents to the survey were over the age of twelve. They were asked to report "only uses of drugs that were not prescribed for them or drugs they took only for the experience or feeling they caused." Over-the-counter drugs and legitimate uses of prescription drugs were not included.

According to the 2003 NSDUH summary, prescription-type sedatives were placed in a category called "psychotherapeutic drugs." This category also included tranquilizers, pain relievers, and stimulants. About 300,000 Americans over the age of twelve reported using sedatives without a prescription. The authors of the survey noted that "the number of first-time sedative users rose steadily during the late 1960s and early 1970s, and then declined during the early 1980s, remaining below 250,000 per year since 1984." The 2003 estimates were all similar to the corresponding estimates for 2002.

Monitoring the Future Results

The results of the 2004 Monitoring the Future (MTF) study were released to the public on December 21, 2004. Conducted by the University of Michigan (U of M), it was sponsored by research grants from the National Institute on Drug Abuse (NIDA). Like the NSDUH results regarding sedative use from 2002 and 2003, the MTF survey results indicate that barbiturate use among twelfth-grade students held steady between 2003 and 2004.

Effects on the Body

Barbiturates are classified as ultrashort-, short-, intermediate-, and long-acting, depending on how quickly they act and how long their effects last. Ultrashort barbiturates such as thiopental (Pentothal) produce unconsciousness within about a minute of intravenous (iv) injection. These drugs are used to prepare patients for surgery; other general anesthetics like nitrous oxide are then used to keep the patient from waking up before the surgery is complete. Because Pentothal and other ultrashort-acting barbiturates are typically used in hospital settings, they are not very likely to be abused, noted the DEA.

Abusers tend to prefer short-acting and intermediate-acting barbiturates. The most commonly abused are amobarbital (Amytal), pentobarbital (Nembutal), and secobarbital (Seconal). A combination of amobarbital and secobarbital (called Tuinal) is also highly abused. Short-acting and intermediate-acting barbiturates are usually prescribed as sedatives and sleeping pills. These pills begin acting fifteen to forty minutes after they are swallowed, and their effects last from five to six hours. Veterinarians use pentobarbital to anesthetize animals before surgery; in large doses, it can be used to euthanize animals.

Long-acting barbiturates such as phenobarbital (Luminal) and mephobarbital (Mebaral) are prescribed for two main reasons. When taken at bedtime, they help treat insomnia. When taken during the day, they have sedative effects that can aid in the treatment of tension and anxiety. These same effects have been found helpful in the treatment of convulsive conditions like epilepsy. Long-acting barbiturates take effect within one to two hours and last twelve hours or longer.

Similar to Alcohol

recreational users report that a barbiturate high makes them feel "relaxed, sociable, and good-humored," according to an Independent article. Users typically describe feelings of decreased anxiety, a loss of inhibitions, and an increased sense of confidence. Physical effects include slowed breathing and a lowering of both blood pressure and heart rate.

Like alcohol, barbiturates are intoxicating. During the stage after mild intoxication, the user's speech may be slurred and a loss of coordination may become noticeable. Stumbling and staggering are common. Other symptoms include shallow breathing, fatigue, frequent yawning, and irritability.

When taken in high doses, barbiturates can cause serious side effects, including "unpredictable emotional reactions and mental confusion," noted the Independent. Judgment becomes severely impaired and the user may experience mood swings.

The mental effects of barbiturates generally depend on the amount of the drug taken and the strength of the dosage. Generally, a person falls asleep when taking a prescribed dosage at bedtime. But barbiturates remain in the system for a long time. "At normal doses," explained Cynthia Kuhn and her coauthors in Buzzed: The Straight Facts about the Most Used and Abused Drugs from Alcohol to Ecstasy, "the major concern is that they can have sedative effects that outlast their sleep-inducing properties…. Driving, flying an airplane, or other activities requiring muscle coordination can be impaired for up to a day after a single dose." Some barbiturates can be detected in a user's urine sample days or even weeks after the drug was consumed.

Truth Serum

Thiopental is a barbiturate that is marketed under the name Sodium Pentothal, but it is probably best known as "truth serum." When dissolved in water, it can be swallowed or administered by intravenous injection. In large doses, it is one of three drugs used in the United States to execute prisoners on death row. In lower doses, it is sometimes used as a truth serum.

Drug experts claim that truth serum does not force people to tell the truth. It merely decreases their inhibitions, making them more likely to be "caught off guard" when questioned by authorities. People being questioned may slip up and expose a lie or give more information on a subject or event than they intended.

Dependence, Tolerance, and Overdose

Barbiturate use can lead to both psychological and physical dependence. Psychological addiction can occur quickly. Signs of drug dependence include relying on a drug regularly for a desired effect. The addicted abuser believes he or she must take a barbiturate to sleep, relax, or just get through the day. Continued use of barbiturates leads to physical dependence.

As people develop a tolerance for barbiturates, they may need more of the drug or a higher dosage to get the desired effect. This can lead to an overdose, which results when a person takes a larger-than-prescribed dose of a drug. "People who get in the habit of taking sleeping pills every night to fall sleep," noted Andrew Weil and Winifred Rosen in From Chocolate to Morphine, "might start out with one a night, progress to two, then graduate to four to get the same effect. One night the dose they need to fall asleep might also be the dose that stops their breathing." Generally, barbiturate overdoses "occur because the effective dose of the drug is not too far away from the lethal dose," explained Dr. Eric H. Chudler on the Neuroscience for Kids Web site.

Symptoms of an overdose typically include severe weakness, confusion, shortness of breath, extreme drowsiness, an unusually slow heartbeat, and darting eye movements. The amount of a fatal dosage of barbiturate varies from one individual to another. However, the lethal dose is usually ten to fifteen times as large as a usual dose. An overdose affects the heart and the respiratory system. The user then falls into a coma and dies.

Clayton pointed out that barbiturates "can have a 'multiplying' effect when taken with other depressants. For example, if someone drinks alcohol and takes a barbiturate, the effect may be ten times stronger than either one taken separately." According to Weil, "many people have died because they were ignorant of this fact."

Older adults and pregnant women should consider the risks associated with barbiturate use. When a person ages, the body becomes less able to rid itself of barbiturates. As a result, people over the age of sixty-five are at higher risk of experiencing the harmful effects of barbiturates, including drug dependence and accidental overdose. When barbiturates are taken during pregnancy, the drug passes through the mother's bloodstream to her fetus. After the baby is born, it may experience withdrawal symptoms and have trouble breathing. In addition, nursing mothers who take barbiturates may transmit the drug to their babies through breast milk.

Reactions with Other Drugs or Substances

People who abuse inhalants run a very high risk of overdose if they consume barbiturates while on an inhalant high. opiates are also especially dangerous when combined with barbiturates. Barbiturates should not be mixed with alcohol or other drugs, including tranquilizers, muscle relaxants, antihistamines, cold medicines, allergy medicines, and certain pain relievers. The use of barbiturates by people suffering from depression may pose an increased risk of suicide. Children or adults diagnosed with attention-deficit/hyperactivity disorder (adhd) may experience increased excitability rather than a calming effect when given barbiturates. In addition, these drugs may lower the effectiveness of birth control pills that contain estrogen. Unless they use a barrier-type form of birth control, women taking oral contraceptives may become pregnant while taking barbiturates.

Treatment for Habitual Users

When addicted users stop taking barbiturates, their bodies must adapt to the lack of drugs in their systems. This process is known as withdrawal. If the users have taken barbiturates in large doses or for an extended period of time, a physician should be consulted about the withdrawal process. An attempt to withdraw abruptly from barbiturates can be fatal.

Withdrawal symptoms usually begin eight to sixteen hours after the last pill was taken. Symptoms in users with a long history of barbiturate use may last up to fifteen days, but the severity of the symptoms decreases as the body rids itself of the drug. During withdrawal, users feel anxious, weak, dizzy, and nauseated. They may also experience shakes, tremors, and even seizures. In addition, users could possibly have hallucinations and become violent or hostile.

Dream Time

Barbiturates bring on sleep in people who take them. This slumber, however, differs from normal sleep. Barbiturate use decreases the amount of dream time during sleep known as the rapid eye movement (REM) stage. This phase of sleep is necessary for maintaining good health.

In some cases, withdrawal symptoms can be deadly. A physician must establish a plan of gradual withdrawal from this type of drug, usually decreasing the dosage by about 10 percent each day over a ten-day to two-week period. The withdrawal process may occur in a hospital, or treatment may be given on an outpatient basis. Either way, counseling is vital. Users who are treated successfully for their physical addiction must follow through with psychological rehabilitation. Behavioral treatment helps former users avoid barbiturates so

they can remain drug free even when faced with cravings. Long-term support can be found in twelve-step programs and other support groups that meet regularly.

Consequences

Barbiturates are used to treat anxiety, sleeplessness, muscular tension, and pain. Their calming effect has a serious downside, though. Barbiturates lessen the brain's control over breathing. Respiratory failure is the primary cause of death in cases of barbiturate overdose. Gahlinger pointed out that "since barbiturates reduce the amount of oxygen reaching the brain, the overdosing person who survives may be left with permanent brain damage."

Barbiturate users can develop a tolerance for the drug. As the body becomes used to the presence of barbiturates in the system, the prescribed dose of the drug may lose its effectiveness. Habitual users may find themselves taking more and more pills in stronger and stronger dosages to achieve the effect they once attained on a low dosage of the drug. This cycle often leads to accidental overdose.

Prolonged barbiturate use can shorten a person's attention span and result in memory loss. Both conditions would make it difficult for a person to do well in school or perform on a job. In addition, barbiturates affect the judgment of those who use them, increasing the likelihood of risky behavior. Users of barbiturates are sometimes tempted to drive while drunk because they know that police will not smell alcohol on their breath.

Taking barbiturates to ease depression "is probably the riskiest way of using them," cautioned Weil. Although these drugs may improve the user's mood temporarily, "over time they often increase anxiety and depression, encouraging further drug-taking in a downward spiral that can end in suicide."

The Law

When barbiturates first became available in the United States, they could be purchased without a prescription. It did not take long, however, for lawmakers to realize that barbiturates were addictive. On their own, some state governments adopted laws in the mid-1930s that banned the sale of nonprescription barbiturates. In 1938, the U.S. government stepped in, passing the U.S. Food, Drug, and Cosmetics Act. This act gave the FDA regulatory power over new drugs, including barbiturates. This means that drug companies would have to apply to the FDA for approval to manufacture such drugs. Once approved, the FDA would determine whether a new drug would require a medical doctor's prescription.

For more than thirty years, until the passage of the Controlled Substances Act (CSA) of 1970, barbiturates were still widely abused. Under the stiffer terms of the CSA, barbiturates became controlled substances. In other words, their use is regulated by certain federal laws. The CSA called for the assignment of all controlled drug substances into one of five categories called schedules. These schedules are based on a substance's medicinal value, possible harmfulness, and potential for abuse and addiction. Schedule I is reserved for the most dangerous drugs that have no recognized medical use.

Various barbiturates fall into three different schedules: Schedule II, Schedule III, and Schedule IV. Drugs in all of these categories cannot be obtained legally without a medical doctor's prescription. Schedule II drugs are dangerous substances with genuine medical uses that also have a high potential for abuse and addiction. They are accepted for medical use with restrictions. These drugs may lead to severe psychological or physical dependence. Barbiturates in this category include amobarbital (Amytal), pentobarbital (Nembutal), and secobarbital (Seconal and Tuinal).

Schedule III drugs have less of a potential for abuse than drugs placed in Schedules I and II. The drugs have real medical uses, but their abuse can still lead to psychological addiction or psychological dependence in those who take them. Barbiturates in this category include aprobarbital (Alurate), butabarbital (Butisol), and butalbital (Fiorinal and Fioricet).

Schedule IV drugs have a low abuse potential when compared to Schedule III drugs. These substances have an accepted medical use, but some patients risk developing a psychological dependence on them. Schedule IV barbiturates include barbital (Veronal), mephobarbital (Mebaral), and phenobarbital (Luminal).

Fines and Jail Time

Possessing barbiturates without a prescription is against the law and can result in up to a year's imprisonment and/or thousands of dollars in fines. The length of the jail sentence and the amount of the fine are increased when a person is convicted of a second or third offense of barbiturate possession. People convicted of distributing or selling barbiturates face lengthy prison terms and fines in the millions of dollars. Selling drugs is a dangerous business for both the buyer and the seller. Illegally distributed Schedule II drugs can kill or seriously injure a user. In cases such as these, the distributor or seller of the substance is considered partially responsible for the user's death and could end up with a lifetime jail sentence.

In the United Kingdom, drugs are regulated by the 1971 Misuse of Drugs Act and the 1986 Medicines Act. The 1971 act placed drugs in three classes: A, B, or C. The most dangerous drugs are called Class A drugs; the least dangerous drugs are in the C category.

Most barbiturates are considered Class B drugs throughout the United Kingdom. If they are used in an injectable form, however, they jump to a Class A rating. The maximum penalty for possession of a Class B drug under UK law is five years of prison, an unlimited fine, or a combination of jail time and a fine. Penalties for supplying or distributing Class B drugs are higher. For Class A drugs, the penalty for possession is seven years in prison, an unlimited fine, or both. The supply penalty for this class could land a seller in jail for life.

For More Information

Books

Brecher, Edward M., and others. The Consumers Union Report on Licit and Illicit Drugs. Boston: Little Brown & Co., 1972.

Clayton, Lawrence. Barbiturates and Other Depressants. New York: Rosen Publishing Group, 1994.

Escohotado, Antonio. A Brief History of Drugs: From the Stone Age to the Stoned Age. Rochester, VT: Park Street Press, 1999.

Gahlinger, Paul M. Illegal Drugs: A Complete Guide to Their History, Chemistry, Use, and Abuse. Las Vegas, NV: Sagebrush Press, 2001.

Hughes, Richard, and Robert Brewin. The Tranquilizing of America. New York: Harcourt, 1979.

Hyde, Margaret O., and John F. Setaro. Drugs 101: An Overview for Teens. Brookfield, CT: Twenty-first Century Books, 2003.

Kuhn, Cynthia, Scott Swartzwelder, Wilkie Wilson, and others. Buzzed: The Straight Facts about the Most Used and Abused Drugs from Alcohol to Ecstasy, 2nd ed. New York: W.W. Norton, 2003.

Schull, Patricia Dwyer. Nursing Spectrum Drug Handbook. King of Prussia, PA: Nursing Spectrum, 2005.

Silverman, Harold M. The Pill Book, 11th ed. New York: Bantam, 2004.

Weil, Andrew, and Winifred Rosen. From Chocolate to Morphine. New York: Houghton Mifflin, 1993, rev. 2004.

Wolfe, Sidney. Worst Pills, Best Pills. New York: Pocket Books, 1999.

Periodicals

Barnett, Jim. "Feds Push Challenge to Assisted Suicide Law." Oregonian (November 10, 2004).

Johnson, Kevin, and Richard Willing. "Ex-CIA Chief Revitalizes 'Truth Serum' Debate." USA Today (April 26, 2002).

Schodolski, Vincent J. "U.S. Seeks to Bury Oregon Suicide Law." Knight Ridder/Tribune News Service (November 27, 2004): p. K6995.

"Sex, Drugs, and Rock 'n' Roll." Independent (January 28, 1996): p. 8.

Weathermon, Ron, and David W. Crabb. "Alcohol and Medication Inter-actions." Alcohol Research & Health, vol. 23, no. 1 (1999): pp. 40-54.

Web Sites

"2003 National Survey on Drug Use and Health (NSDUH)." U.S. Department of Health and Human Services, Substance Abuse and Mental Health Services Administration.http://www.oas.samhsa.gov/nhsda.htm (accessed June 30, 2005).

"Barbiturates." Neuroscience for Kids.http://faculty.washington.edu/chudler/barb.html and http://faculty.washington.edu/chudler/neurok.html (both accessed June 30, 2005).

"Barbiturates." U.S. Department of Justice, Drug Enforcement Administration.http://www.usdoj.gov/dea/concern/barbiturates.html (accessed June 30, 2005).

Fort, Joel. "The Problem of Barbiturates in the United States of America." United Nations Office on Drugs and Crime.http://www.unodc.org/unodc/bulletin/bulletin_1964-01-01_1_page004.html (accessed June 30, 2005).

Glatt, M. M. "The Abuse of Barbiturates in the United Kingdom." United Nations Office on Drugs and Crime.http://www.unodc.org/unodc/bulletin/bulletin_1962-01-01_2_page004.html (accessed June 30, 2005).

Monitoring the Future.http://www.monitoringthefuture.org/ and http://www.nida.nih.gov/Newsroom/04/2004MTFDrug.pdf (both accessed June 30, 2005).

"Prescription Drugs: Abuse and Addiction." National Institute on Drug Abuse (NIDA) Research Report Series.http://www.drugabuse.gov/ResearchReports/Prescription/ (accessed June 30, 2005).

See also: Alcohol; Benzodiazepine; Tranquilizers

BARBITURATES

Barbiturates refer to a class of general central nervous system depressants that are derived from barbituric acid, a chemical discovered in 1863 by the Nobel Prize winner in chemistry (1905) Adolf von Baeyer (1835-1917). Barbituric acid itself is devoid of central depressant activity; however, German scientists Emil Hermann Fischer and Joseph von Mering made some modifications to its structure and synthesized barbital, which was found to possess depressant properties. Scientists had been looking for a drug to treat anxiety and nervousness but without the dependence-producing effects of Opiate drugs such as Opium, Codeine, and Morphine. Other drugs such as bromide salts, Chloral Hydrate, and paraldehyde were useful sedatives, but they all had problems such as toxicity or they left such a bad taste in patients' mouths that they preferred not to take them. Fischer and von Mering noted that barbital produced sleep in both humans and animals. It was introduced into chemical medicine in 1903 and was soon in widespread use.

By 1913, the second barbiturate, Phenobarbi-Tal, was introduced into medical practice. Since that time, more than 2,000 similar chemicals have been synthesized but only about 50 of these have been marketed. Although the barbiturates were quickly used to treat a number of disorders effectively, their side effects were becoming apparent. The chief problem, an overdose, can result in respiratory depression, which can be fatal. By the mid-1950s, more than 70 percent of admissions to a poison-control center in Copenhagen, Denmark, involved barbiturates. Additionally, it became apparent that the barbiturates were subject to abuse, which could lead to dependence, and that a serious withdrawal syndrome could ensue when the drugs were abruptly discontinued. In the 1960s, the introduction of a safer class of hypnotic drugs, the Benzodiazepines reduced the need for barbiturates.

Barbiturates are dispensed in distinctly colored capsules making them very easy to identify by the lay public. In fact, users within the drug culture often refer to the various barbiturates by names associated with their physical appearance. Examples of these names include blue birds, blue clouds, yellow jackets, red devils, sleepers, pink ladies, and Christmas trees. The term goofball is often used to describe barbiturates in general. All barbiturates are chemically similar to barbital, the structure of which is shown in Figure 1.

All barbiturates are general central nervous system depressants. This means that sedation, sleep, and even anesthesia will develop as the dose is increased. Some barbiturates also are useful in reducing seizure activity and so have been used to treat some forms of epilepsy. The various barbiturates differ primarily in their onset and duration of action, ability to enter the brain, and the rate at which they are metabolized. These differences are achieved principally by adding or subtracting atoms to the two branches on position #5 in Figure 1. The barbiturates are classified on the basis of their duration of action, which ranges from ultrashort-acting to long-acting. The onset of action of the ultrashort-acting barbiturates occurs in seconds and lasts a few minutes. The short-acting compounds take effect within a few minutes and can last four to eight hours, while the intermediate- and long-acting barbiturates can take almost an hour to take effect but last six to twelve hours. Table 1 lists the common barbiturates, their trade names, typical route of administration, and plasma half-life. The plasma half-life is a measure of how long the drug remains in the blood, but not how long the effects last, although it does provide a general indication of when to expect the effects to wane (a half-life of five hours means that one-half of the drug will be removed from the system in five hours; one-half of the remaining drug will be removed during the next five hours, etc.).

EFFECTS ON THE BODY AND THERAPEUTIC USES

Barbiturates affect all excitable tissues in the body. However, Neurons are more sensitive to their effects than other tissues. The depth of central nervous system depression ranges from mild sedation to coma and depends on many factors including which drug is used, its dose, the route of administration, and the level of excitability present just before the barbiturate was taken. The most common uses for the barbiturates are still to promote sleep and to induce anesthesia. Barbiturate-induced sleep resembles normal sleep in many ways, but there are a few important differences. Barbiturates reduce the amount of time spent in rapid eye movement or REM sleep—a very important phase of sleep. Prolonged use of barbiturates causes restlessness during the late stages of sleep. Since the barbiturates remain in our bodies for some time after we awaken, there can be residual drowsiness that can impair judgment and distort moods for some time after the obvious sedative effects have disappeared. Curiously, some people are actually excited by barbiturates, and the individual may even appear inebriated. This paradoxical reaction often occurs in the elderly and is more common after taking phenobarbital.

The general use of barbiturates as hypnotics (Sleeping Pills) has decreased significantly, since they have been replaced by the safer benzodiazepines. Phenobarbital and butabarbital are still available, however, as sedatives in a number of combination medications used to treat a variety of inflammatory disorders. These two drugs also are used occasionally to antagonize the unwanted overstimulation produced by ephedrine, Amphetamine, and theophylline.

Since epilepsy is a condition of abnormally increased neuronal excitation, any of the barbiturates can be used to treat convulsions when given in anesthetic doses; however, phenobarbital has a selective anticonvulsant effect that makes it particularly useful in treating grand mal seizures. This selective effect is shared with mephobarbital and metharbital. Thus, phenobarbital is often used in hospital emergency rooms to treat convulsions such as those that develop during tetanus, eclampsia, status epilepticus, cerebral hemorrhage, and poisoning by convulsant drugs. The benzodiazepines are, however, gradually replacing the barbiturates in this setting as well.

It is not completely understood how barbiturates work but, in general, they act to enhance the activity of GABA on GABA-sensitive neurons by acting at the same receptor on which GABA exerts its effects (see Figure 2). GABA is a Neurotransmit-Ter that normally acts to reduce the electrical activity of the brain; its action is like a brake. Thus, barbiturates enhance the braking effects of GABA to promote sedation. There is an area in the brain called the reticular activating system, which is responsible for maintaining wakefulness. Since this area has many interconnecting or polysynaptic neurons, it is the first to succumb to the barbiturates, and that is why an individual becomes tired and falls asleep after taking a barbiturate.

PHARMACOKINETICS AND DISTRIBUTION

The ultrashort-acting barbiturates differ from the other members of this class mainly by the means by which they are inactivated. Methohexital and its relatives are very soluble in lipids (i.e., fatty tissue). The brain is composed of a great deal of lipid; when the ultrashort-acting barbiturates are given intravenously, they proceed directly to the brain to produce anesthesia and unconsciousness. After only a few minutes, however, these drugs are redistributed to the fats in the rest of the body so their concentration is reduced in the brain. Thus, recovery from IV barbiturate anesthesia can be very fast. For this reason, drugs such as methohexital and thiopental are used primarily as intravenous anesthetic agents and not as sedatives.

The other longer-acting barbiturates must be metabolized by the liver into inactive compounds before the effects wane. Since these metabolites are more soluble in water, they are excreted through the kidneys and into the urine. As is the case with most drugs, metabolism and excretion is much quicker in young adults than in the elderly and infants. Plasma half-lives are also increased in pregnant women because the blood volume is expanded due to the development of the placenta and fetus.

TOLERANCE, DEPENDENCE, AND ABUSE

Repeated administration of any number of drugs results in eventual compensatory changes in the body. These changes are usually in the opposite direction of those initially produced by the drug such that more and more drug is needed to achieve the initial desired effect. This process is called Tolerance. There are two basic mechanisms for tolerance development: tissue tolerance and metabolic or pharmacokinetic tolerance. Tissue tolerance refers to the changes that occur on the tissue or cell that is affected by the drug. Metabolic tolerance refers to the increase in the processes that metabolize or break down the drug. This process generally occurs in the liver. Barbiturates are subject to both types of tolerance development.

Tolerance does not develop equally in all effects produced by barbiturates. Barbiturate-induced respiratory depression is one example. Barbiturates reduce the drive to breathe and the processes necessary for maintaining a normal breathing rhythm. Thus, while tolerance is quickly developing to the desired sedative effects, the toxic doses change to a lesser extent. As a result, when the dose is increased to achieve the desired effects (e.g., sleep), the margin of safety actually decreases as the dose comes closer to producing toxicity. A complete cessation of breathing is often the cause of death in barbiturate poisoning (Rall, 1990).

If tolerance develops and the amount of drug taken continues to increase, then Physical Dependence can develop. This means that if the drug is suddenly stopped, the tissues' compensatory effects become unbalanced and withdrawal signs appear. In the case of barbiturates, mild signs of withdrawal include apprehension, insomnia, excitability, mild tremors, and loss of appetite. If the dose was very high, more severe signs of withdrawal can occur, such as weakness, vomiting, decrease in blood pressure regulatory mechanisms (so that pressure drops when a person rises from a lying position, called orthostatic hypotension), increased pulse and respiratory rates, and grand mal (epileptic) seizures or convulsions. Delirium with fever, disorientation, and Hallucinations may also occur. Unlike withdrawal from the opioids, withdrawal from central nervous system depressants such as barbiturates can be life threatening. The proper treatment of a barbiturate-dependent individual always includes a slow reduction in the dose to avoid the dangers of rapid detoxification.

Few, if any, illegal laboratories manufacture barbiturates. Diversion of licit production from pharmaceutical companies is the primary source for the illicit market. Almost all barbiturate users take it by mouth. Some try to dissolve the capsules and inject the liquid under their skin (called skin-popping) but the toxic effects of the alcohols used to dissolve the drug and the strong alkaline nature of the solutions can cause lesions of the skin. Intravenous administration is a rare practice among barbiturate abusers.

Many barbiturate users become dependent to some degree during the course of treatment for insomnia. This type of problem is called iatrogenic, because it is initiated by a physician. In some instances the problem will be limited to continued use at gradually increasing doses at night, to prevent insomnia that is in turn due to withdrawal. However, some individuals who are susceptible to the euphoric effects of barbiturates may develop a pattern of taking increasingly larger doses to become intoxicated, rather than for the intended therapeutic effects (for example, to promote sleepiness). To achieve these aims, the person may obtain prescriptions from a number of physicians and take them to a number of pharmacists—or secure their needs from illicit distributors (dealers). If the supply is sufficient, the barbiturate abuser can rapidly increase the dose within a matter of weeks. The upper daily limit is about 1,500 to 3,000 milligrams; however, many can titrate their daily dose to the 800 to 1,000 milligram range such that the degree of impairment is not obvious to others. The pattern of abuse resembles that of ethyl (drinking) Alcohol, in that it can be daily or during binges that last from a day to many weeks at a time. This pattern of using barbiturates for intoxification is more typically seen in those who, from the beginning, obtain barbiturates from illicit sources rather than those who began by seeking help for insomnia.

Barbiturates are sometimes used along with other drugs. Often, the barbiturate is used to potentiate, or boost, the effects of another drug upon which a person is physically dependent. Alcohol and Heroin are commonly taken together in this way. Since barbiturates are "downers," they also are used to counteract the unwanted overstimulation associated with stimulant-induced intoxication. It is not uncommon for stimulant abusers (on Cocaine or amphetamines) to use barbiturates to combat the continued "high" and the associated motor disturbances associated with heavy and continued cocaine use. Also, barbiturates are used to ward off the early signs of withdrawal from alcohol.

Treatment for barbiturate dependence is often conducted under carefully controlled conditions, because of the potential for severe developments, such as seizures. Under all conditions, a program of supervised withdrawal is needed. Many years ago, pentobarbital was used for this purpose and the dose was gradually decreased until no drug was given. More recently, phenobarbital or the benzodiazepines—Chlordiazepoxide and diazepam—have been used for their greater margin of safety. The reason that the benzodiazepines sometimes work is because the general central nervous system depressants—barbiturates, alcohol, and benzodiazepines—develop cross-dependence to one another. Thus a patient's barbiturate or alcohol withdrawal signs are reduced or even eliminated by diazepam.

(See also: Addiction: Concepts and Definitions ; Withdrawal )

BIBLIOGRAPHY

CsÁky, T. Z. (1979). Cutting's handbook of pharmacology: The actions and uses of drugs, 6th ed. New York: Appleton-Century Crofts.

Henningfield, J. E., & Ator, N. A. (1986). Barbiturates: Sleeping potion or intoxicant? In The encyclopedia of psychoactive drugs. New York: Chelsea House.

Mendelson, J. H., & Mello, N. K. (1992). Medical diagnosis and treatment of alcoholism. New York: McGraw-Hill.

Rall, T. W. (1990). Hypnotics and sedatives: Ethanol. In A. G. Gilman et al. (Eds.), Goodman and Gilman's the pharmacological basis of therapeutics, 8th ed. New York: Pergamon.

Winger, G., Hoffman, F.G., & Woods, J. H. (1992). A handbook of drugs and alcohol abuse: the biomedical aspects, 3rd ed. New York: Oxford University Press.

Scott E. Lukas

Barbiturates

Recommended dosage

Precautions

Special conditions

Allergies

Pregnancy

Breastfeeding

Other medical conditions

Use of certain medicines

Side effects

Interactions

Resources

Barbiturates are a group of medicines known ascentral nervous system (CNS) depressants. Derived from barbituric acid, barbiturates were first prepared by German organic chemist Adolf von Baeyer (1835–1917) in 1864. They were first introduced to the public at the beginning of the twentieth century. Also known as sedative-hypnotic drugs, barbiturates make people very relaxed, calm, and sleepy. These drugs are sometimes used to help patients relax before surgery. Some barbiturates may also be used to control seizures (convulsions). Although barbiturates have been used to treat nervousness and sleep problems, they have generally been replaced by other medicines for these purposes.

These medicines may become habit-forming and should not be used to relieve everyday anxiety and tension or to treat sleeplessness over long periods.

Description Barbiturates are available only with a physician’s prescription and are sold in capsule, tablet, liquid, and injectable forms. Some commonly used barbiturates are phenobarbital (Barbita) and secobarbital (Seconal).

Recommended dosage

Recommended dosage depends on the type of barbiturate and other factors such as the patient’s age and the condition for which the medicine is being taken. Check with the physician who prescribed the drug or the pharmacist who filled the prescription for the correct dosage.

Always take barbiturates exactly as directed. Never take larger or more frequent doses, and do not take the drug for longer than directed. If the medicine does not seem to be working, even after taking it for several weeks, do not increase the dosage. Instead, check with the physician who prescribed the medicine.

Do not stop taking this medicine suddenly without first checking with the physician who prescribed it. It may be necessary to taper down gradually to reduce the chance of withdrawal symptoms. If it is necessary to stop taking the drug, check with the physician for instructions on how to stop.

Precautions

See a physician regularly while taking barbiturates. The physician will check to make sure the medicine is working as it should and will note unwanted side effects.

Because barbiturates work on the central nervous system, they may add to the effects of alcohol and other drugs that slow the central nervous system, such as antihistamines, cold medicine, allergy medicine, sleep aids, medicine for seizures, tranquilizers, some pain relievers, and muscle relaxants. They may also add to the effects of anesthetics, including those used for dental procedures. The combined effects of barbiturates and alcohol or other CNS depressants (drugs that slow the central nervous system) can be very dangerous, leading to unconsciousness or even death. Anyone taking barbiturates should not drink alcohol and should check with his or her physician before taking any medicines classified as CNS depressants.

Taking an overdose of barbiturates or combining barbiturates with alcohol or other central nervous system depressants can cause unconsciousness and even death. Anyone who shows signs of an overdose or a reaction to combining barbiturates with alcohol or other drugs should get emergency medical help immediately. Signs include:

• Severe drowsiness,
• Breathing problems,
• Slurred speech,
• Staggering,
• Slow heartbeat,
• Severe confusion, and
• Severe weakness.

Barbiturates may change the results of certain medical tests. Before having medical tests, anyone taking this medicine should alert the health care professional in charge.

People may feel drowsy, dizzy, lightheaded, or less alert when using these drugs. These effects may even occur the morning after taking a barbiturate at bedtime. Because of these possible effects, anyone who takes these drugs should not drive, use machines or do anything else that might be dangerous until they have found out how the drugs affect them.

Barbiturates may cause physical or mental dependence when taken over long periods. Anyone who shows these signs of dependence should check with his or her physician right away:

• The need to take larger and larger doses of the medicine to get the same effect;
• A strong desire to keep taking the medicine; and
• Withdrawal symptoms, such as anxiety, nausea or vomiting, convulsions, trembling, or sleep problems, when the medicine is stopped.

Children may be especially sensitive to barbiturates. This may increase the chance of side effects such as unusual excitement.

Older people may also be more sensitive that others to the effects of this medicine. In older people, barbiturates may be more likely to cause confusion, depression, and unusual excitement. These effects are also more likely in people who are very ill.

Special conditions

People with certain medical conditions or who are taking certain other medicines can have problems if they take barbiturates. Before taking these drugs, be sure to let the physician know about any of these conditions.

Allergies

Anyone who has had unusual reactions to barbiturates in the past should let his or her physician know before taking the drugs again. The physician should also be told about any allergies to foods, dyes, preservatives, or other substances.

Pregnancy

Taking barbiturates during pregnancy increases the chance of birth defects and may cause other problems such as prolonged labor and withdrawal effects in the baby after birth. Pregnant women who must take barbiturates for serious or life-threatening conditions should thoroughly discuss with their physicians the benefits and risks of taking this medicine.

Breastfeeding

Barbiturates pass into breast milk and may cause problems such as drowsiness, breathing problems, or slow heartbeat in nursing babies whose mothers take the medicine. Women who are breastfeeding should check with their physicians before using barbiturates.

Other medical conditions

Before using barbiturates, people with any of these medical problems should make sure their physicians are aware of their conditions:

• Alcohol or drug abuse,
• Depression,
• Hyperactivity (in children),
• Pain,
• Kidney disease,
• Liver disease,
• Diabetes,
• Overactive thyroid,
• Underactive adrenal gland,
• Chronic lung diseases such as asthma or emphysema,
• Severe anemia, and
• Porphyria.

Use of certain medicines

Taking barbiturates with certain other drugs may affect the way the drugs work or may increase the chance of side effects.

Side effects

The most common side effects are dizziness, light-headedness, drowsiness, and clumsiness or unsteadiness. These problems usually go away as the body adjusts to the drug and do not require medical treatment unless they persist or interfere with normal activities.

KEY TERMS

Adrenal glands— Two glands located next to the kidneys. The adrenal glands produce the hormones epinephrine and norepinephrine and the corticosteroid (cortisone-like) hormones.

Anemia— A condition in which the level of hemoglobin falls below normal values due to a shortage of mature red blood cells. Common symptoms include pallor, fatigue, and shortness of breath.

Central nervous system— The brain and spinal cord components of the nervous system that control the activities of internal organs, movements, perceptions, thoughts, and emotions.

Hallucination— A sensory experience of something that does not exist outside the mind. A person can experience a hallucination in any of the five senses. Hallucinations usually result from drugs or mental disorders.

Hypnotic— A medicine that causes sleep. Porphyria—A disorder in which porphyrins build up in the blood and urine.

Porphyrin— A type of pigment found in living things, such as chlorophyll, which makes plants green, and hemoglobin, which makes blood red.

Sedative— Medicine that has a calming effect and may be used to treat nervousness or restlessness.

Seizure— A sudden attack, spasm, or convulsion.

Withdrawal symptoms— A group of physical or mental symptoms that may occur when a person suddenly stops using a drug to which he or she has become dependent.

More serious side effects are not common, but may occur. If any of the following side effects occur, check with the physician who prescribed the medicine immediately:

• Fever,
• Muscle or joint pain,
• Sore throat,
• Chest pain or tightness in the chest,
• Wheezing,
• Skin problems, such as rash, hives, or red, thickened, or scaly skin,
• Bleeding sores on the lips,
• Sores or painful white spots in the mouth, and
• Swollen eyelids, face, or lips.

In addition, check with a physician as soon as possible if confusion, depression, or unusual excitement occur after taking barbiturates.

Patients who take barbiturates for a long time or at high doses may notice side effects for some time after they stop taking the drug. These effects usually appear within 8 to 16 hours after the patient stops taking the medicine. Check with a physician if these or other troublesome symptoms occur after stopping treatment with barbiturates:

• Dizziness, lightheadedness or faintness,
• Anxiety or restlessness,
• Hallucinations,
• Muscle twitches or trembling hands,
• Nausea and vomiting,
• Seizures (convulsions),
• Sleep problems, nightmares, or increased dreaming.
• Vision problems,
• Weakness.

Other side effects may occur. Anyone who has unusual symptoms during or after treatment with barbiturates should get in touch with his or her physician.

Interactions

Birth control pills may not work properly when taken while barbiturates are being taken. To prevent pregnancy, use additional or additional methods of birth control while taking barbiturates.

Barbiturates may also interact with other medicines. When this happens, the effects of one or both of the drugs may change or the risk of side effects may be greater. Anyone who takes barbiturates should let the physician know all other medicines he or she is taking. Among the drugs that may interact with barbiturates are:

• Other central nervous system (CNS) depressants such as medicine for allergies, colds, hay fever, and asthma; sedatives; tranquilizers; prescription pain medicine; muscle relaxants; medicine for seizures; sleep aids; barbiturates; and anesthetics.
• Blood thinners.
• Adrenocorticoids (cortisone-like medicines).
• Antiseizure medicines such as valproic acid (Depakote and Depakene), and carbamazepine (Tegretol).

The list above does not include every drug that may interact with barbiturates. Be sure to check with a physician or pharmacist before combining barbiturates with any other prescription or nonprescription (over-the-counter) medicine.

Resources

BOOKS

Derkins, Susie. Barbiturates and Your Central Nervous System: The Incredibly Disgusting Story. New York: Rosen Central, 2001.

Klaassen, Curtis D. Casarett and Doull’s Toxicology 6th ed. Columbus: McGraw-Hill, Inc., 2001.

O’Neil, Maryadele J. Merck Index: An Encyclopedia of Chemicals, Drugs, & Biologicals. 13th ed. Whitehouse Station, NJ: Merck & Co., 2001.

PERIODICALS

Kiefer, D.M. “Chemistry Chronicles: Miracle Medicines.” Today’s Chemist 10, no. 6 (June 2001): 59-60.

Nancy Ross-Flanigan

Barbiturates

Definition

Barbiturates are medicines that act on the central nervous system and cause drowsiness and can control seizures.

Purpose

Barbiturates are in the group of medicines known as central nervous system depressants (CNS). Also known as sedative-hypnotic drugs, barbiturates make people very relaxed, calm, and sleepy. These drugs are sometimes used to help patients relax before surgery. Some may also be used to control seizures (convulsions). Although barbiturates have been used to treat nervousness and sleep problems, they have generally been replaced by other medicines for these purposes.

These medicines may become habit forming and should not be used to relieve everyday anxiety and tension or to treat sleeplessness over long periods.

Description

Barbiturates are available only with a physician's prescription and are sold in capsule, tablet, liquid, and injectable forms. Some commonly used barbiturates are phenobarbital (Barbita) and secobarbital (Seconal).

Recommended dosage

Recommended dosage depends on the type of barbiturate and other factors such as the patient's age and the condition for which the medicine is being taken. Check with the physician who prescribed the drug or the pharmacist who filled the prescription for the correct dosage.

Always take barbiturates exactly as directed. Never take larger or more frequent doses, and do not take the drug for longer than directed. If the medicine does not seem to be working, even after taking it for several weeks, do not increase the dosage. Instead, check with the physician who prescribed the medicine.

Do not stop taking this medicine suddenly without first checking with the physician who prescribed it. It may be necessary to taper down gradually to reduce the chance of withdrawal symptoms. If it is necessary to stop taking the drug, check with the physician for instructions on how to stop.

Precautions

See a physician regularly while taking barbiturates. The physician will check to make sure the medicine is working as it should and will note unwanted side effects.

Because barbiturates work on the central nervous system, they may add to the effects of alcohol and other drugs that slow the central nervous system, such as antihistamines, cold medicine, allergy medicine, sleep aids, medicine for seizures, tranquilizers, some pain relievers, and muscle relaxants. They may also add to the effects of anesthetics, including those used for dental procedures. The combined effects of barbiturates and alcohol or other CNS depressants (drugs that slow the central nervous system) can be very dangerous, leading to unconsciousness or even death. Anyone taking barbiturates should not drink alcohol and should check with his or her physician before taking any medicines classified as CNS depressants.

KEY TERMS

Adrenal glands— Two glands located next to the kidneys. The adrenal glands produce the hormones epinephrine and norepinephrine and the corticosteroid (cortisone-like) hormones.

Anemia— A lack of hemoglobin—the compound in blood that carries oxygen from the lungs throughout the body and brings waste carbon dioxide from the cells to the lungs, where it is released.

Central nervous system— The brain and spinal cord.

Hallucination— A false or distorted perception of objects, sounds, or events that seems real. Hallucinations usually result from drugs or mental disorders.

Hypnotic— A medicine that causes sleep.

Porphyria— A disorder in which porphyrins build up in the blood and urine.

Porphyrin— A type of pigment found in living things, such as chlorophyll, that makes plants green and hemoglobin which makes blood red.

Sedative— Medicine that has a calming effect and may be used to treat nervousness or restlessness.

Seizure— A sudden attack, spasm, or convulsion.

Withdrawal symptoms— A group of physical or mental symptoms that may occur when a person suddenly stops using a drug to which he or she has become dependent.

Taking an overdose of barbiturates or combining barbiturates with alcohol or other central nervous system depressants can cause unconsciousness and even death. Anyone who shows signs of an overdose or a reaction to combining barbiturates with alcohol or other drugs should get emergency medical help immediately. Signs include:

• severe drowsiness
• breathing problems
• slurred speech
• staggering
• slow heartbeat
• severe confusion
• severe weakness

Barbiturates may change the results of certain medical tests. Before having medical tests, anyone taking this medicine should alert the health care professional in charge.

People may feel drowsy, dizzy, lightheaded, or less alert when using these drugs. These effects may even occur the morning after taking a barbiturate at bedtime. Because of these possible effects, anyone who takes these drugs should not drive, use machines or do anything else that might be dangerous until they have found out how the drugs affect them.

Barbiturates may cause physical or mental dependence when taken over long periods. Anyone who shows these signs of dependence should check with his or her physician right away:

• the need to take larger and larger doses of the medicine to get the same effect
• a strong desire to keep taking the medicine
• withdrawal symptoms, such as anxiety, nausea or vomiting, convulsions, trembling, or sleep problems, when the medicine is stopped

Children may be especially sensitive to barbiturates. This may increase the chance of side effects such as unusual excitement.

Older people may also be more sensitive that others to the effects of this medicine. In older people, barbiturates may be more likely to cause confusion, depression, and unusual excitement. These effects are also more likely in people who are very ill.

Special conditions

People with certain medical conditions or who are taking certain other medicines can have problems if they take barbiturates. Before taking these drugs, be sure to let the physician know about any of these conditions:

ALLERGIES. Anyone who has had unusual reactions to barbiturates in the past should let his or her physician know before taking the drugs again. The physician should also be told about any allergies to foods, dyes, preservatives, or other substances.

PREGNANCY. Taking barbiturates during pregnancy increases the chance of birth defects and may cause other problems such as prolonged labor and withdrawal effects in the baby after birth. Pregnant women who must take barbiturates for serious or life-threatening conditions should thoroughly discuss with their physicians the benefits and risks of taking this medicine.

BREASTFEEDING. Barbiturates pass into breast milk and may cause problems such as drowsiness, breathing problems, or slow heartbeat in nursing babies whose mothers take the medicine. Women who are breastfeeding should check with their physicians before using barbiturates.

OTHER MEDICAL CONDITIONS. Before using barbiturates, people with any of these medical problems should make sure their physicians are aware of their conditions:

• alcohol or drug abuse
• depression
• hyperactivity (in children)
• pain
• kidney disease
• liver disease
• diabetes
• overactive thyroid
• underactive adrenal gland
• chronic lung diseases such as asthma or emphysema
• severe anemia
• porphyria

USE OF CERTAIN MEDICINES. Taking barbiturates with certain other drugs may affect the way the drugs work or may increase the chance of side effects.

Side effects

The most common side effects are dizziness, light-headedness, drowsiness, and clumsiness or unsteadiness. These problems usually go away as the body adjusts to the drug and do not require medical treatment unless they persist or interfere with normal activities.

More serious side effects are not common, but may occur. If any of the following side effects occur, check with the physician who prescribed the medicine immediately:

• fever
• muscle or joint pain
• sore throat
• chest pain or tightness in the chest
• wheezing
• skin problems, such as rash, hives, or red, thickened, or scaly skin
• bleeding sores on the lips
• sores or painful white spots in the mouth
• swollen eyelids, face, or lips

In addition, check with a physician as soon as possible if confusion, depression, or unusual excitement occur after taking barbiturates.

Patients who take barbiturates for a long time or at high doses may notice side effects for some time after they stop taking the drug. These effects usually appear within 8-16 hours after the patient stops taking the medicine. Check with a physician if these or other troublesome symptoms occur after stopping treatment with barbiturates:

• dizziness, lightheadedness or faintness
• anxiety or restlessness
• hallucinations
• vision problems
• nausea and vomiting
• seizures (convulsions)
• muscle twitches or trembling hands
• weakness
• sleep problems, nightmares, or increased dreaming

Other side effects may occur. Anyone who has unusual symptoms during or after treatment with barbiturates should get in touch with his or her physician.

Interactions

Birth control pills may not work properly when taken while barbiturates are being taken. To prevent pregnancy, use additional or additional methods of birth control while taking barbiturates.

Barbiturates may also interact with other medicines. When this happens, the effects of one or both of the drugs may change or the risk of side effects may be greater. Anyone who takes barbiturates should let the physician know all other medicines he or she is taking. Among the drugs that may interact with barbiturates are:

• Other central nervous system (CNS) depressants such as medicine for allergies, colds, hay fever, and asthma; sedatives; tranquilizers; prescription pain medicine; muscle relaxants; medicine for seizures; sleep aids; barbiturates; and anesthetics.
• Blood thinners.
• Adrenocorticoids (cortisone-like medicines).
• Antiseizure medicines such as valproic acid (Depakote and Depakene), and carbamazepine (Tegretol).

The list above does not include every drug that may interact with barbiturates. Be sure to check with a physician or pharmacist before combining barbiturates with any other prescription or nonprescription (over-the-counter) medicine.

Resources

PERIODICALS

Miller, Norman S. "Sedative-Hypnotics: Pharmacology and Use." Journal of Family Practice 29 (December 1989): 665.