Tranylcypromine Sulfate

Trade Names:
Parnate
- Tablets 10 mg

Pharmacology

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Tranylcypromine blocks activity of enzyme MAO, thereby increasing MAO (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. Its 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 may yield exaggerated effects after standard dosing.

Indications and Usage

Treatment of major depressive episodes without melancholia.

Unlabeled Uses

Prevention of migraine; social anxiety disorders; panic disorders; bipolar depression; Alzheimer and Parkinson disease if patients are unresponsive or unable to take other agents.

Contraindications

Hypertension; cerebrovascular defects; cardiovascular disease; history of headache, liver disease or abnormal LFTs; presence of pheochromocytoma; in combination with other MAOIs or dibenzazepine-related entities (eg, cyclobenzaprine), antihypertensives (eg, guanethidine, methyldopa, reserpine), diuretics, antihistamines, sedatives, anesthetics (eg, general anesthesia, cocaine, local anesthesia-containing sympathomimetic vasoconstrictors), antiparkinson agents (eg, benztropine, trihexyphenidyl), tricyclic antidepressants (eg, amitriptyline), levodopa, serotoninergics (eg, fluoxetine, dexfenfluramine), tryptophan, bupropion, buspirone, sympathomimetics (eg, amphetamine), dextromethorphan, or caffeine; in combination with cheese or other foods with high tyramine content; in combination with CNS depressants (eg, alcohol, meperidine) or hypotensive agents (eg, dopamine).

Dosage and Administration

PO Usual effective dose is 30 mg/day in divided doses. If there are no signs of improvement within 2 wk, the dosage may be increased in 10 mg/day increments at intervals of 1 to 3 wk (max, 60 mg/day).

Storage/Stability

Store at 59° to 86°F.

Drug Interactions

Severe hypertension or hemorrhagic stroke may occur in patients taking tranylcypromine when these foods are ingested.

Coadministration is contraindicated.

Hypoglycemia may be potentiated and recovery delayed by tranylcypromine.

Hypotensive effect may be inhibited by tranylcypromine. Coadministration is contraindicated.

Effect may be potentiated by tranylcypromine. Coadministration is contraindicated.

Risk of serious and life-threatening reactions may be increased by tranylcypromine. Coadministration is contraindicated.

Risk of toxicity may be increased by tranylcypromine. Coadministration is contraindicated.

Risk of increased blood pressure may be increased by tranylcypromine. Coadministration is contraindicated.

Risk of severe side effects (eg, hyperpyrexia, muscle rigidity, seizures) may be increased by tranylcypromine. Coadministration is contraindicated.

Hypertensive crisis may be precipitated. Coadministration is contraindicated.

Risk of serotonin syndrome occurrence may be increased. Coadministration is contraindicated.

Risk of delirium, including agitation, disorientation, and visual hallucinations, may be increased.

Hypertensive reactions may occur. Coadministration is contraindicated.

Serum levels may be elevated, increasing the risk of cardiotoxicity. Coadministration is contraindicated.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Palpitation, tachycardia.

CNS

Agitation, anxiety, dizziness, drowsiness, headache, insomnia, manic symptoms, numbness, overstimulation, paresthesia, restlessness, tremor, weakness; akinesia, ataxia, confusion, disorientation, memory loss (postmarketing).

Dermatologic

Alopecia, skin rash; flare-up of cystic acne, scleroderma, urticaria (postmarketing).

EENT

Blurred vision, tinnitus.

GI

Abdominal pain, anorexia, constipation, diarrhea, dry mouth, nausea; fissures at corner of mouth (postmarketing).

Genitourinary

Impotence, retarded ejaculation, urinary retention; urinary frequency, urinary incontinence (postmarketing).

Hematologic-Lymphatic

Agranulocytosis, anemia, leukopenia, thrombocytopenia.

Hepatic

Hepatitis.

Metabolic-Nutritional

SIADH.

Musculoskeletal

Muscle spasm, myoclonic jerks.

Miscellaneous

Chills, edema.

Precautions

Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established.

Elderly

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

Anginal pain

Tranylcypromine may suppress anginal pain, which would otherwise serve as a warning of myocardial ischemia.

Anxiety/Agitation

May aggravate coexisting symptoms, such as anxiety and agitation.

Bipolar disorder

Because antidepressants may increase the likelihood of precipitation of a mixed/manic episode in patients at risk of bipolar disorder, screen patients prior to initiating treatment to determine if they are at risk for bipolar disorder.

Diabetes

May alter glucose control.

Epilepsy

May lower seizure threshold.

Hypertensive crisis

Hypertensive crisis, which may be fatal, is the most important reaction associated with tranylcypromine administration. Discontinue treatment immediately upon occurrence of palpitation or frequent headaches.

Hyperthyroidism

Use with caution because of increased sensitivity to pressor amines.

Hypotension

May occur.

Myelography

Discontinue tranylcypromine at least 48 h before myelography and do not resume for at least 24 h post procedure.

Overdosage

Symptoms

Agitation, anxiety, coma, dizziness, drowsiness, hyperpyrexia, hypertension, hypotension, incoherence, insomnia, mental confusion, movement disorders, restlessness, severe headache, shock, weakness.

Patient Information

• 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 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 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 health care provider immediately if any of the following occurs: chest pain, eye pain or photophobia, nausea, rapid heart beat, severe headache, severe sweating, stiff neck, or vomiting.
• Advise patients and family to be alert for the emergence of agitation, irritability, and unusual changes in behavior as well as the emergence of suicidality, and to report such symptoms immediately to health care provides.

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