Tranylcypromine sulfate
Tranylcypromine sulfate (Parnate)
Tranylcypromine sulfate
(tran-ill-SIP-roh-meen)
Pregnancy Category: C Parnate (Rx)


Classification: Antidepressant, monoamine oxidase inhibitor


Action/Kinetics: A MAO inhibitor with a rapid onset of activity. Due to inhibition of MAO, the concentration of epinephrine, norepinephrine, and serotonin increases in storage sites throughout the nervous system. This increase has been alleged to be the basis for the antidepressant effects. MAO activity recovers in 3-5 days after drug withdrawal. No orthostatic hypotensive effect; slight anticholinergic and sedative effects. t1/2: 2.4-2.8 hr.


Uses: Treatment of major depressive episode without melancholia. Not a first line of therapy; is used when clients have failed to respond to other drug therapy. Investigational: Alone or as an adjunct to treat bulimia, obsessive compulsive disorder, and manifestations of psychotic disorders. Also, treatment of social phobia, seasonal affective disorders, adjunct to treat multiple sclerosis, and to treat idiopathic orthostatic hypotension (e.g., Shy-Drager syndrome) refractory to conventional therapy.


Contraindications: Use in those with a confirmed or suspected CV defect or in anyone with CV disease, hypertension, or history of headache. In the presence of pheochromocytoma. History of liver disease or in those with abnormal liver function. Use in combination with a large number of other drugs, especially other MAO inhibitors, tricyclic antidepressants, serotonin-reuptake inhibitors, buspirone, sympathomimetics, meperidine, CNS depressants (e.g., alcohol and narcotics), hypotensive drugs, excessive caffeine, and dextromethorphan (see Drug Interactions). Use with tyramine-containing foods (see Drug Interactions).


Special Concerns: Assess benefits versus risks before using during pregnancy and lactation. Use with caution in clients taking antiparkinson drugs, in impaired renal function, in those with seizure disorders, in diabetics, in hyperthyroid clients, and in those taking disulfiram. Geriatric clients may be more sensitive to the drug.


Side Effects: CNS: Anxiety, agitation, headaches (without elevation of BP), manic symptoms, restlessness, insomnia, weakness, drowsiness, dizziness, significant anorexia. GI: Dry mouth, nausea, diarrhea, abdominal pain, constipation. CV: Tachycardia, edema, palpitation. GU: Impotence, urinary retention, impaired ejaculation. Musculoskeletal: Muscle spasm, tremors, myoclonic jerks, numbness, paresthesia. Hematologic: Anemia, leukopenia, agranulocytosis, thrombocytopenia. Miscellaneous: Blurred vision, chills, impotence, hepatitis, skin rash, impaired water excretion, tinnitus.


Overdose Management: Symptoms: Insomnia, restlessness, anxiety, agitation, mental confusion, incoherence, hypotension, dizziness, weakness, drowsiness, shock, hypertension with severe headache. Rarely, hypertension accompanied by twitching or myoclonic fibrillation of skeletal muscles with hyperprexia, generalized rigidity, and coma. The toxic effects may be delayed or prolonged following the last dose of the drug; thus, observe closely for at least a week. Treatment: Gastric lavage, if performed early. General supportive measures. Treat hypertensive crisis using phentolamine 5 mg IV. External cooling to treat hyperprexia. Standard measures to treat circulatory shock. Myoclonic effects may be relieved by using barbiturates; however, tranylcypromine may prolong the effects of barbiturates.


Drug Interactions: Alcohol / Possibility of excitation, seizures, delirium, hyperpyrexia, circulatory collapse, coma, death Anesthetics, general / Hypotensive effect; use together with caution Antidepressants, tricyclic / Concomitant use excitation, sweating, tachycardia, tachypnea, hyperpyrexia, disseminated intravascular coagulation, delirium, tremors, convulsions, death. Antihypertensive drugs / Exaggerated hypotensive effects Beta-adrenergic blocking drugs / Exaggerated hypotensive effects Buspirone / Elevated BP Dextromethorphan / Brief episodes of psychosis or bizarre behavior Ephedra / See Sympathomimetic drugs below Fluoxetine / Possibility of hyperthermia, rigidity, myoclonic movements, death Ginseng / Risk of headache, mania, or tremors MAO Inhibitors / Concomitant use of tranylcypromine with other MAO inhibitors may cause a hypertensive crisis or severe seizures. Discontinue the MAO inhibitor at least 7-10 days before initiating a new drug. However, such combinations have been used together successfully Meperidine / See Narcotics Narcotics / Possibility of excitation, seizures, delirium, hyperpyrexia, circulatory collapse, coma, death St. John's wort / Do not use with tranylcypromine Scotch broom herb / Risk of hypertensive crisis Selective serotonin reuptake inhibitors /See Fluoxetine Sympathomimetic drugs--amphetamine, cocaine, dopa, ephedrine, epinephrine, metaraminol, methyldopa, methylphenidate, norepinephrine, phenylephrine, phenylpropanolamine. Many OTC cold products, hay fever medications, and nasal decongestants contain one or more of these drugs / All peripheral, metabolic, cardiac, and central effects are potentiated for up to 2 weeks after termination of MAO inhibitor therapy. Symptoms include acute hypertensive crisis with possible intracranial hemorrhage, hyperthermia, coma, and possibly death Thiazide diuretics / Exaggerated hypotensive effects Tryptophan / Possibility of behavioral and neurologic effects, including disorientation, confusion, amnesia, delirium, agitation, hypomania, ataxia, myoclonus, hyperreflexia, shivering, ocular oscillation,and Babinski signs Tyramine-rich foods--beer, broad beans, certain cheeses (Brie, cheddar, Camembert, Stilton), Chianti wine, chicken livers, caffeine, cola beverages, figs, licorice, liver, pickled or kippered herring dry sausage (Genoa salami, hard salami, pepperoni, Lebanon bologna), tea, cream, yogurt, yeast extract, and chocolate / Possible precipitation of hypertensive crisis, including severe headache, hypertension, intracranial hemorrhage, death Yeast, Brewer's / BP


How Supplied: Tablets: 10 mg.


Dosage
¢Tablets Major depressive syndrome without melancholia.
Individualize the dose. Usual effective dose: 30 mg/day given in divided doses. If there are no signs of improvement in 2 weeks, the dose can be increased by 10 mg/day at intervals of 1 to 3 weeks, up to a maximum of 60 mg/day.