A-Z Drug Facts > Tranylcypromine Sulfate

Tranylcypromine Sulfate

Pronouncation: (tran-ill-SIP-row-meen SULL-fate)
Class: MAO inhibitor

Trade Names:
Parnate
- Tablets 10 mg

Pharmacology

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Tranylcypromine blocks activity of enzyme MAO, thereby increasing monoamine (eg, epinephrine, norepinephrine, serotonin) concentrations in CNS.

Pharmacokinetics

Absorption

Tranylcypromine appears to be well absorbed following oral administration of 30 mg/day. T _max is 3 h; however, max inhibition of MAO occurs within 5 to 7 days. There is a rapid onset of activity.

Metabolism

Tranylcypromine is metabolized with the release of the active metabolite. In activation is primarily by acetylation.

Elimination

The drug is excreted in 24 h.

Onset

Onset of action is from 48 h to 3 wk.

Special Populations

Slow acetylators

Slow acetylators may yield exaggerated effects after standard dosing.

Indications and Usage

Treatment of reactive depression.

Unlabeled Uses

Bulimia; treatment of panic disorders with associated agoraphobia.

Contraindications

Hypersensitivity to MAO inhibitors; pheochromocytoma; CHF; abnormal liver function; history of liver disease; severe renal function impairment; cerebrovascular defect; concurrent use of another MAO inhibitor, tricyclic or SSRI antidepressants, dextromethorphan, or CNS depressants (eg, alcohol), meperidine, sympathomimetic drugs (eg, amphetamines, dopamine, pseudoephedrine), or related drugs (eg, methyldopa, levodopa), buspirone, cheese or food with high tyramine content; cardiovascular disease; hypertension; history of headache; patients older than 60 yr (possibility of cerebral sclerosis).

Dosage and Administration

Adults

PO 10 mg 3 times daily initially; if no improvement after 2 wk, titrate up to 60 mg/day in 10 mg/day increments at intervals of 1 to 3 wk.

Storage/Stability

Store tablets at room temperature in a tightly closed container.

Drug Interactions

Amine-containing foods

May cause severe hypertension or hemorrhagic strokes.

Anorexiants

May cause exaggerated pharmacologic effects (eg, severe headaches, hypertension, hyperpyrexia) of anorexiants (eg, amphetamines, related compounds).

CNS depressants

May enhance CNS effects.

Dextromethorphan

Concurrent use has been associated with severe reactions (eg, hyperpyrexia, hypotension, death).

Fluoxetine, fluvoxamine, nefazodone, paroxetine, sertraline, trazodone, venlafaxine

Although data are limited, interactions comparable to those of tricyclic antidepressants and tranylcypromine may occur.

Guanethidine

MAO inhibitors may antagonize antihypertensive effect. Insulin and sulfonylureas may enhance hypoglycemic action.

Levodopa

May cause hypertensive reactions.

Meperidine

May lead to severe reactions, including agitation, convulsions, diaphoresis, fever, respiratory depression, and vascular collapse.

Sympathomimetics

May cause severe headache, hypertensive crisis, and hyperpyrexia.

Tricyclic antidepressants, busipirone, carbamazepine, CNS stimulants, cyclobenzaprine, maprotiline, tyramine

May lead to potentially fatal reactions, including seizures and hypertensive crisis, mental status changes, hyperthermia.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Orthostatic hypotension; edema; hypertensive crisis; palpitations; tachycardia.

CNS

Dizziness; headache; sleep disturbances; tremors; hyperreflexion; manic symptoms; muscle twitching; convulsions; vertigo; confusion; memory impairment; toxic delirium; hypomania; coma.

Dermatologic

Rash; sweating; photosensitivity.

EENT

Blurred vision; glaucoma; dry mouth.

GI

Constipation; nausea; diarrhea; anorexia; abdominal pain.

Genitourinary

Sexual dysfunction; urinary retention; incontinence.

Hematologic

Anemia; leukopenia; agranulocytosis; thrombocytopenia.

Hepatic

Fatal progressive necrotizing hepatocellular damage; elevated serum transaminases; hepatitis.

Metabolic

Weight gain; hypermetabolic syndrome (eg, fever, tachycardia, rapid breathing, rigidity, metabolism, acidosis, coma); hypernatremia.

Precautions

Pregnancy

Category undetermined.

Lactation

Excreted in breast milk.

Children

Not recommended for patients under 16 yr.

Elderly

Use with caution; older patients may suffer more morbidity than younger patients.

Diabetes

May alter glucose control.

Epilepsy

May lower seizure threshold.

Depression

May aggravate coexisting symptoms such as anxiety and agitation.

Hyperthyroidism

Use with caution because of increased sensitivity to pressor amines.

Suicidal patients

Strict supervision may be necessary in patients at risk.

Overdosage

Symptoms

Excitement, hypotension, dizziness, movement disorders, irritability, insomnia, weakness, severe headache, anxiety, restlessness, drowsiness, coma, convulsions, flushing, hypertension, sweating, tachypnea, acidosis, hyperpyrexia, tachycardia, cardiorespiratory arrest, incoherence, agitation, mental confusion, shock.

Patient Information

• Advise patient that antidepressants restore depressed people to normal moods.
• Inform patient and family that it may be 3 to 4 wk before a noticeable improvement in mood is noted.
• Instruct patient to take the medication at the same time every day.
• Advise patient not to take any other medications, including otc or prescription medications without checking with their health care provider first. This medication interacts with a large number of other medications.
• Teach patient to avoid sudden position changes to prevent orthostatic hypotension.
• Instruct patient and family on how to take BP. If the BP is markedly higher than normal, they should notify the health care provider.
• Warn patient that eating foods that contain tyramine or tryptophan while taking this medication can produce hypertensive crisis which is potentially fatal. These foods include, but are not limited to, protein foods that are aged or fermented such as cheeses, pickled herring, liver, hard sausage, pods of broad beans, beer, red wine, yeast extract, yogurt, ginseng, soy sauce, bananas, raisins, and avocados. Arrange for a consultation with a dietitian.
• Instruct patient to ingest caffeine and chocolate only in small amounts.
• Inform patient to avoid the use of alcohol and other recreational drugs.
• Advise patient to use caution while driving or performing other tasks requiring mental alertness until effect is determined.
• Instruct patient to stop taking the medication and notify the health care provider immediately if any of the following occurs: severe headache, chest pain, rapid heart beat, eye pain or photophobia, severe sweating, stiff neck, nausea, or vomiting.

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