No

Antidepressant, Monoamine Oxidase Inhibitor

Treatment of major depressive episode without melancholia

C

Hypersensitivity to tranylcypromine; uncontrolled hypertension; pheochromocytoma; hepatic or renal disease; cerebrovascular defect; cardiovascular disease; concurrent use of sympathomimetics (and related compounds), CNS depressants, ethanol, meperidine, bupropion, buspirone, guanethidine, and serotonergic drugs (including SSRIs) - do not use within 5 weeks of fluoxetine discontinuation or 2 weeks of other antidepressant discontinuation; general anesthesia, local vasoconstrictors; spinal anesthesia (hypotension may be exaggerated). Foods which are high in tyramine, tryptophan, or dopamine, chocolate, or caffeine.

Safety in children <16 years of age has not been established; use with caution in patients who are hyperactive, hyperexcitable, or who have glaucoma, suicidal tendencies, hyperthyroidism, or diabetes; avoid use of meperidine within 2 weeks of phenelzine use. Toxic reactions have occurred with dextromethorphan. Hypertensive crisis may occur with tyramine, tryptophan, or dopamine-containing foods. Should not be used in combination with other antidepressants. Hypotensive effects of antihypertensives (beta-blockers, thiazides) may be exaggerated. Use with caution in depressed patients at risk of suicide. May cause orthostatic hypotension (especially at dosages >30 mg/day) - use with caution in patients with hypotension or patients who would not tolerate transient hypotensive episodes - effects may be additive when used with other agents known to cause orthostasis (phenothiazines). Has been associated with activation of hypomania and/or mania in bipolar patients. May worsen psychotic symptoms in some patients. Use with caution in patients at risk of seizures, or in patients receiving other drugs which may lower seizure threshold. Discontinue at least 48 hours prior to myelography. Use with caution in patients receiving disulfiram. Use with caution in patients with renal impairment.

Cardiovascular: Orthostatic hypotension, edema

Central nervous system: Dizziness, headache, drowsiness, sleep disturbances, fatigue, hyper-reflexia, twitching, ataxia, mania

Dermatologic: Rash, pruritus

Endocrine & metabolic: Decreased sexual ability (anorgasmia, ejaculatory disturbances, impotence), hypernatremia, hypermetabolic syndrome

Gastrointestinal: Xerostomia, constipation, weight gain

Genitourinary: Urinary retention

Hematologic: Leukopenia

Hepatic: Hepatitis

Neuromuscular & skeletal: Weakness, tremor, myoclonus

Ocular: Blurred vision, glaucoma

Miscellaneous: diaphoresis

Symptoms of overdose include tachycardia, palpitations, muscle twitching, seizures, insomnia, transient hypotension, hypertension, hyperpyrexia, coma

Competent supportive care is the most important treatment for an overdose with a monoamine oxidase (MAO) inhibitor. Both hypertension or hypotension can occur with intoxication. Hypotension may respond to I.V. fluids or vasopressors, and hypertension usually responds to an alpha-adrenergic blocker. While treating the hypertension, care is warranted to avoid sudden drops in blood pressure, since this may worsen the MAO inhibitor toxicity. Muscle irritability and seizures often respond to diazepam, while hyperthermia is best treated antipyretics and cooling blankets. Cardiac arrhythmias are best treated with phenytoin or procainamide.

CYP2A6 and 2C19 enzyme inhibitor

MAOIs may inhibit the metabolism of barbiturates and prolong their effect

MAOIs in combination with dexfenfluramine, sibutramine, meperidine, fenfluramine, and dextromethorphan may cause serotonin syndrome; these combinations are best avoided

MAOIs in combination with amphetamines, other stimulants (methylphenidate), metaraminol, and decongestants (pseudoephedrine) may result in severe hypertensive reaction; these combinations are best avoided

Foods (eg, cheese) and beverages (eg, ethanol) containing tyramine, should be avoided in patients receiving an MAOI; hypertensive crisis may result

MAOIs inhibit the antihypertensive response to guanadrel or guanethidine; use an alternative antihypertensive agent

MAOIs in combination with levodopa and reserpine may result in hypertensive reactions; monitor

MAOIs in combination with lithium have resulted in malignant hyperpyrexia; this combination is best avoided

MAOIs may increase the pressor response of norepinephrine; monitor

MAOIs may prolong the muscle relaxation produced by succinylcholine via decreased plasma pseudocholinesterase

Tramadol may increase the risk of seizures and serotonin in patients receiving an MAOI

MAOIs may produce hypoglycemia in patients with diabetes; monitor

MAOIs may produce delirium in patients receiving disulfiram; monitor

Thought to act by increasing endogenous concentrations of epinephrine, norepinephrine, dopamine and serotonin through inhibition of the enzyme (monoamine oxidase) responsible for the breakdown of these neurotransmitters

Onset of action: 2-3 weeks are required of continued dosing to obtain full therapeutic effect

Duration: May continue to have a therapeutic effect and interactions 2 weeks after discontinuing therapy

Half-life: 90-190 minutes

Time to peak serum concentration: Within 2 hours

Elimination: In urine

Adults: Oral: 10 mg twice daily, increase by 10 mg increments at 1- to 3-week intervals; maximum: 60 mg/day

Alcohol: Avoid use

Food: Avoid tyramine-containing foods

Blood pressure, blood glucose

glucose

Attempts should be made to avoid use of vasoconstrictor due to possibility of hypertensive episodes with monoamine oxidase inhibitors

Orthostatic hypotension in >10% of patients; meperidine should be avoided as an analgesic due to toxic reactions with MAO inhibitors

Take exactly as directed (do not increase dose or frequency); may take 2-3 weeks to achieve desired results; may cause physical and/or psychological dependence. Take in the morning to reduce the incidence of insomnia. Avoid excessive alcohol, caffeine, and other prescription or OTC medications not approved by prescriber. Avoid tyramine-containing foods (eg pickles, aged cheese, wine); see prescriber for complete list of foods to be avoided. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). You may experience drowsiness, dizziness, or blurred vision (use caution when driving or engaging in tasks requiring alertness until response to drug is known); anorexia or dry mouth (small frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help); constipation (increased exercise, fluids, or dietary fruit and fiber may help); diarrhea (buttermilk, yogurt, or boiled milk may help); orthostatic hypotension (use caution when climbing stairs or changing position from lying or sitting to standing); or altered sexual ability (reversible). Report persistent excessive sedation; muscle cramping, tremors, weakness, or change in gait; chest pain, palpitations, rapid heartbeat, or swelling of extremities; vision changes; or worsening of condition. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Breast-feeding is not recommended.

Assist with ambulation during initiation of therapy; monitor blood pressure closely, patients should be cautioned against eating foods high in tyramine or tryptophan (cheese, wine, beer, pickled herring, dry sausage)

Tablet, as sulfate: 10 mg

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