Maprotiline
Maprotiline
Definition
Maprotiline is an antidepressant. It is a member of the tetracyclic antidepressant family of compounds and is administered orally. In the United States, it is sold under the trade name Ludiomil.
Purpose
Maprotiline is an antidepressant intended for use by people with depressive neurosis and bipolar syndrome. It is also occasionally used for the relief of anxiety associated with depression .
Description
Maprotiline elevates mood. The precise pharmacological mode of action is not fully understood but it is thought to inhibit the reuptake of the neurotransmitter norepinephrine at nerve endings in the brain . It is prescribed in 25-, 50-, and 75-mg tablets.
Recommended dosage
The recommended initial dosage of maprotiline is typically 75 mg, given by mouth in three 25-mg administrations, although some patients may start with an initial dose of 25 mg. The initial dosage should bemaintained for at least two weeks. Therapeutic results may be observed in three to seven days. Typically, initial administration may have to be continued for two to three weeks before results are observed.
The recommended total dosage is 150 mg per day. Dosage should be increased 25 mg at a time. The maximum daily dosage for people with severe depression is 225 mg.
Precautions
Maprotiline should be discontinued or educed in dosage prior to surgery. This is due to the potential for interactions with anesthetic agents.
Maprotiline may promote seizure activity. Of all the cyclic antidepressants it probably causes the highest incidence of seizures and has thus fallen out of favor with most psychiatrists. Also for this reason, it should not be combined with other neuroleptics (antipsychotics) that can also cause seizures. The drug increases the effect of alcohol and should not be taken with products containing alcohol or barbiturates People taking monoamine oxidase inhibitors (MAOIs), such as Parnate (tranylcypromine ) and Nardil (phenelzine ), should not take maprotiline.
The possibility of suicide is a component of depression. A minimal number of doses should be dispensed at any one time to minimize the potential for use as a suicide agent. Because the drug may lower the threshold for a manic episode among people with bipolar disorders, it should be used only with caution and under close supervision.
Side effects
The most commonly reported side effect of maprotiline is dry mouth. Slightly more than one person in five (22%) experiences this effect. Approximately 16% of users experience drowsiness, 8% report dizziness, and 6% report nervousness and constipation. Other less common reported side effects include anxiety, agitation, insomnia , blurred vision, tremor, weakness, fatigue , nausea, and headache with blurred vision. Other rare side effects are similar to those experienced by people who use tricyclic antidepressants. These include abnormally high or low blood pressure, tachycardia, and syncope. Hallucinations , disorientation,
KEY TERMS
Barbiturates —A class of medications (including Seconal and Nembutal) that causes sedation and drowsiness. They may be prescribed legally, but may also be used as drugs of abuse.
Bipolar syndrome —An abnormal mental condition characterized by periods of intense elation, energy, and activity followed by periods of inactivity and depression.
Guanethidine —An antihypertensive drug used to treat high blood pressure.
Hallucination —A false sensory perception. A person experiencing a hallucination may “hear” sounds or “see” people or objects that are not really present. Hallucinations can also affect the senses of smell, touch, and taste.
Manic —Referring to mania, a state characterized by excessive activity, excitement, or emotion.
Monoamine oxidase inhibitors —A group of antidepressant drugs that decrease the activity of monoamine oxidase, a neurotransmitter found in the brain that affects mood.
Norepinephrine —A neurotransmitter in the brain that acts to constrict blood vessels and raise blood pressure. It works in combination with serotonin.
Physostigmine —A short-acting drug that enhances levels of a substance (acetylcholine) between neurons in the brain.
Syncope —A brief lapse of consciousness caused by a temporarily insufficient flow of blood to the brain.
Tachycardia —A pulse rate above 100 beats per minute.
and mania have been reported, as have vomiting, diarrhea, and gastric distress.
Interactions
Cimetidine and fluoxetine reduce the elimination of maprotiline, thus increasing its plasma concentration. Barbiturates and phenytoin increase the elimination of maprotiline, thus decreasing its plasma concentration. Cardiovascular toxicity has been reportedwhenmaprotiline is used simultaneously with thyroid-replacement medications such as levothyroxine, and maprotiline blocks the pharmacological effect of guanethidine.
An increased risk of seizures has been reported with the simultaneous use of physostigmine and maprotiline. Asimilar effect is observed when maprotiline is taken simultaneously with phenothiazine compounds.
See alsoAnxiety and anxiety disorders; Bipolardisorder; Depression and depressive disorders.
Resources
BOOKS
Foreman, John C., and Torben Johansen. Textbook of Receptor Pharmacology. 2nd ed. Boca Raton, FL: CRC Press, 2002.
Page, Clive P., and Michael Murphy. Integrated Pharmacology. St. Louis: Mosby-Year Book, 2002.
Preston, John D., John H. O’Neal, and Mary C. Talaga. Handbook of Clinical Psychopharmacology for Therapists. 4th ed. Oakland, CA: New Harbinger Publications, 2004.
PERIODICALS
Arenas, M. Carmen, and others. “Are the Effects of the Antidepressants Amitriptyline, Maprotiline, and Fluoxetine on Inhibitory Avoidance State-Dependent?” Behavioural Brain Research 166.1 (Jan. 2006): 150-58.
Mayers, Andrew G., and David S. Baldwin. “Antidepressants and Their Effect on Sleep.” Human Psychopharmacology: Clinical and Experimental 20.8 (Dec. 2005): 533-59.
Rambelomanana, S., and others. “Antidepressants: General Practitioners’ Opinions and Clinical Practice.” Acta Psychiatrica Scandinavica 113.6 (June 2006): 460-67.
ORGANIZATIONS
American Academy of Clinical Toxicology. 777 East Park Drive, P.O. Box 8820, Harrisburg, PA 17105-8820. Telephone: (717) 558-7750. Web site: <http://www.clintox.org/index.html>
American Academy of Family Physicians. 11400 Tomahawk Creek Parkway, Leawood, KS 66211-2672. Telephone: (913) 906-6000. Web site: <http://www.aafp.org/>.
American Medical Association. 515 N. State Street, Chicago, IL 60610. Telephone: (312) 464-5000. Web site: <http://www.ama-assn.org/>.
American Psychiatric Association. 1400 K Street NW, Washington, DC 20005. Telephone: (888) 357-7924. Web site: <http://www.psych.org/>.
American Society for Clinical Pharmacology and Therapeutics. 528 North Washington Street, Alexandria, VA 22314. Telephone: (703) 836-6981.
American Society for Pharmacology and Experimental Therapeutics. 9650 Rockville Pike, Bethesda, MD 20814-3995. Telephone: (301) 530-7060. Web site: <http://www.aspet.org/>.
L.Fleming Fallon, Jr., MD, Dr.P.H.
Ruth A. Wienclaw, PhD
Maprotiline
Maprotiline
Definition
Maprotiline is an oral antidepressant. It is a member of the tetracyclic antidepressant family of compounds. In the United States, it is sold under the trade name Ludiomil.
Purpose
Maprotiline is an antidepressant intended for use by persons with depressive neurosis and bipolar syndrome. It is also occasionally used for the relief of anxiety associated with depression.
Description
Maprotiline elevates mood. The precise pharmacological mode of action is not fully understood but it is thought to inhibit the reuptake of the neurotransmitter norepinephrine at nerve endings in the brain . It is prescribed in 25-, 50-, and 75-mg tablets.
Recommended dosage
The recommended initial dosage of maprotiline is 75 mg, given by mouth in three 25-mg administrations. The initial dosage should be maintained for at least two weeks. Therapeutic results maybe observed in three to seven days. Typically, initial administration may have to be continued for two to three weeks before results are observed.
The recommended total dosage is 150 mg per day. Dosage should be increased 25 mg at a time. The maximum daily dosage in severely depressed persons is 225 mg. The elderly may require a total initial dosage of 25 mg per day.
Precautions
Maprotiline should be discontinued or reduced in dosage prior to surgery. This is due to the potential for interactions with anesthetic agents.
Maprotiline may promote seizure activity: of all the cyclic antidepressants it probably causes the highest incidence of seizures and has thus fallen out of favor with most psychiatrists. Also for this reason, it should not be combined with other neuroleptics (antipsychotics) that can also cause seizures. The drug increases the effect of alcohol and should not be taken with products containing alcohol or barbiturates . Persons taking monoamine oxidase inhibitors (MAOIs), such as Parnate (tranylcypromine ) and Nardil (phenelzine ), should not take maprotiline.
The possibility of suicide is a component of depression. A minimal number of doses should be dispensed at any one time to minimize the potential for use as a suicide agent. Because the drug may lower the threshold for a manic episode among persons with bipolar disorders , it should be used only with caution and under close supervision.
Side effects
The most commonly reported side effect of maprotiline is dry mouth. Slightly more than one person in five (22%) experiences this effect. Approximately 16% of users experience drowsiness, dizziness is reported by 8%, and nervousness and constipation by 6%. Other less common side effects include anxiety, agitation, insomnia , blurred vision, tremor, weakness, fatigue , nausea, and headache with blurred vision are also reported. Other rare side effects are similar to those experienced by users of tricyclic antidepressants. These include abnormally high or low blood pressure, tachycardia, and syncope. Hallucinations , disorientation, and mania have been reported, as have vomiting, diarrhea, and gastric distress.
Interactions
Cimetidine and fluoxetine reduce the elimination of maprotiline, thus increasing its plasma concentration. Barbiturates and phenytoin increase the elimination of maprotiline, thus decreasing its plasma concentration. Cardiovascular toxicity has been reported when maprotiline is used simultaneously with thyroid-replacement medications such as levothyroxine, and maprotiline blocks the pharmacological effect of guanethidine.
An increased risk of seizures has been reported with the simultaneous use of physostigmine and maprotiline. A similar effect is observed when maprotiline is taken simultaneously with phenothiazine compounds.
See also Anxiety and anxiety disorders; Bipolar disorder; Bipolar disorders; Depression and depressive disorders
Resources
BOOKS
Adams, Michael and Norman Holland. Core Concepts in Pharmacology. Philadelphia: Lippincott-Raven, 1998.
Foreman, John C. and Torben Johansen. Textbook of Receptor Pharmacology. 2nd ed. Boca Raton, FL: CRC Press,2002.
Page, Clive P., and Michael Murphy. Integrated Pharmacology. St. Louis: Mosby-Year Book, 2002.
Von Boxtel, Chris J., Budiono Santoso, and I. Ralph Edwards. Drug Benefits and Risks: International Textbook of Clinical Pharmacology. New York: John Wiley and Sons,2001.
PERIODICALS
Martenyi F., M. Dossenbach, K. Mraz, and S. Metcalfe. "Gender differences in the efficacy of fluoxetine and maprotiline in depressed patients: a double-blind trial of antidepressants with serotonergic or norepinephrinergic reuptake inhibition profile." European Journal of Neuropsychopharmacology 11, no. 3 (2001): 227-232.
Normann C., K. Lieb, and J. Walden. "Increased plasma concentration of maprotiline by coadministration of risperidone." Journal of Clinical Psychopharmacology 22, no. 1 (2002): 92-93.
Pisani F., G. Oteri, C. Costa, G. Di Raimondo, and R. Di Perri. "Effects of psychotropic drugs on seizure threshold." Drug Safety 25, no. 2 (2002): 91-110.
ORGANIZATIONS
American Academy of Clinical Toxicology. 777 East Park Drive, PO Box 8820, Harrisburg, PA 17105-8820. Telephone: (717) 558-7750. Fax: (717) 558-7845. Web site: <http://www.clintox.org/index.html>.
American Academy of Family Physicians. 11400 Tomahawk Creek Parkway, Leawood, KS 66211-2672. Telephone:(913) 906-6000. Web site: <http://www.aafp.org/>.
American Medical Association. 515 N. State Street, Chicago, IL 60610. Telephone: (312) 464-5000. Web site: <http://www.ama-assn.org/>.
American Psychiatric Association. 1400 K Street NW, Washington, DC 20005. Telephone: (888) 357-7924. Fax(202) 682-6850. Web site: <http://www.psych.org/>.
American Society for Clinical Pharmacology and Therapeutics. 528 North Washington Street, Alexandria, VA 22314. Telephone: (703) 836-6981. Fax: 703-836-5223.
American Society for Pharmacology and Experimental Therapeutics. 9650 Rockville Pike, Bethesda, MD 20814-3995. Telephone: (301) 530-7060. Fax: (301) 530-7061. Web site: <http://www.aspet.org/>.
L. Fleming Fallon, Jr., M.D., Dr.P.H.