tranylcypromine sulfate

tranylcypromine sulfate

[tran′əlsip′rəmēn]

a monoamine oxidase inhibitor that acts as an antidepressant.

indications It is prescribed in the treatment of severe reactive or endogenous mental depression without melancholia and has an unlabeled use for the treatment of post-traumatic stress disorder.

contraindications Cerebrovascular or cardiovascular diseases, paranoid schizophrenia, liver dysfunction, alcoholism, pheochromocytoma, or known hypersensitivity to this drug prohibits its use. It is not given to children under 16 years of age.

adverse effects Among the most serious adverse effects are severe hypertensive episodes that can be precipitated by ingestion of foods rich in tyramine or by concurrent administration of many sympathomimetic drugs. Common side effects include headache, vertigo, dry mouth, blurred vision, and orthostatic hypotension.

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tranylcypromine sulfate (tran´lsī´-prmēn´),

n brand name: Parnate;
drug class: antidepressant, monoamine oxidase inhibitor (MAOI);
action: increases concentrations of endogenous norepinephrine, serotonin, and dopamine in central nervous system (CNS) storage sites;
use: treatment of depression (when uncontrolled by other means).

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tranylcypromine sulfate

Parnate

Pharmacologic class: MAO inhibitor

Therapeutic class: Antidepressant

Pregnancy risk category C

FDA Boxed Warning

• Drug may increase risk of suicidal thinking and behavior in children and adolescents with major depressive disorder and other psychiatric disorders. Risk must be balanced with clinical need, as depression itself increases suicide risk. With patient of any age, observe closely for clinical worsening, suicidality, and unusual behavior changes when therapy begins. Advise family and caregivers to observe patient closely and communicate with prescriber as needed.
• Drug isn't approved for use in pediatric patients.

Action

Unknown. Thought to increase concentrations of serotonin, epinephrine, and norepinephrine in CNS by inhibiting effects of MAO.

Availability

Tablets: 10 mg

⊘Indications and dosages

➣ Depression

Adults: 10 mg P.O. t.i.d., increased if needed by 10 mg P.O. daily at intervals of 1 to 3 weeks. Maximum dosage is 60 mg daily.

Contraindications

• Hypersensitivity to drug or other MAO inhibitors
• Pheochromocytoma
• Heart failure or other cardiovascular disease
• Confirmed or suspected cerebrovascular disorder
• Severe renal impairment
• Hypertension
• History of hepatic disease or elevated liver function tests
• History of headache
• Upcoming elective surgery
• Concurrent use of other MAO inhibitors, dibenzazepine derivatives, CNS depressants, anesthetics, antihypertensives, bupropion, sympathomimetics, selective serotonin reuptake inhibitors (SSRIs), or dextromethorphan
• Consumption of caffeine, certain cheeses, and other foods with high tryptophan or tyramine content

Precautions

Use cautiously in:
• seizure disorders, diabetes mellitus, hyperactivity, schizophrenia, severe depression, suicidal attempt or ideation
• pregnant or breastfeeding patients
• children.

Administration

☞ Don't stop therapy suddenly. Dosage must be tapered.

Route	Onset	Peak	Duration
P.O.	Unknown	1-3.5 hr	10 days

Adverse reactions

CNS: dizziness, headache, hyperreflexia, tremor, mania, hypomania, confusion, impaired memory, hypersomnia or insomnia, weakness, fatigue, drowsiness, restlessness, increased anxiety, myoclonic movements, suicidal behavior or ideation (especially in child or adolescent)

CV: orthostatic hypotension, tachycardia, palpitations, syncope, paradoxical hypertension, hypertensive crisis

EENT: blurred vision

GI: nausea, diarrhea, constipation, GI disturbances, abdominal pain, dry mouth, anorexia

GU: urinary retention, impaired ejaculation, erectile dysfunction

Hematologic: anemia, agranulocytosis, leukopenia, thrombocytopenia

Musculoskeletal: muscle twitching

Other: weight gain, chills, edema

Interactions

Drug-drug. Anesthetics, antihypertensives, bupropion, CNS depressants, dextromethorphan, dibenzazepine derivatives, other MAO inhibitors, SSRIs, sympathomimetics: potentially fatal reactions

Beta-adrenergic blockers: bradycardia

Carbamazepine: hypertensive crisis, severe seizures, coma, circulatory collapse

Hypoglycemics: potentiation of hypoglycemic response

Levodopa: hypertensive reactions

Methylphenidate: increased risk of hypertensive crisis

Sulfonamides: sulfonamide or tranylcypromine toxicity

Thiazide diuretics: exaggerated hypotension

Drug-diagnostic tests. Transaminases: increased levels

Drug-food. Foods containing high caffeine, tyramine, or tryptophan content: hypertension

Drug-herbs. Cacao: vasopressor effects

Ephedra (ma huang): severe reactions, including hypertensive crisis

Ginseng: tremor, headache, mania

Licorice: increased tranylcypromine activity

L-tryptophan: serotonin syndrome (overreactive reflexes, high body temperature, jaw clenching, sweating, drowsiness, euphoria, and even death)

Drug-behaviors. Alcohol use: increased CNS effects

Patient monitoring

☞ Monitor vital signs and cardiovascular status carefully. Stay alert for indications of impending hypertensive crisis (palpitations, frequent headaches). Keep phentolamine at hand to lower blood pressure if needed.
• Monitor CBC and liver function tests.
☞ Observe patient closely for suicidal ideation and drug hoarding.

Patient teaching

☞ Instruct patient or caregiver to immediately report rapid heartbeat and frequent headaches (possible symptoms of hypertensive crisis).
• Advise patient to read food labels carefully and to avoid foods high in tyramine, tryptophan, and caffeine.
• Tell patient drug causes serious interactions with many common drugs. Instruct him to tell all prescribers he's taking it.
☞ Teach patient or caregiver to recognize and immediately report increasing depression or suicidal ideation (especially in child or adolescent).
• Advise patient to avoid alcohol and herbal remedies, because serious reactions may occur.
☞ Caution patient not to stop therapy suddenly. Dosage must be tapered.
• Instruct patient to move slowly when sitting up or standing, to avoid dizziness from sudden blood pressure drop.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration, vision, and alertness.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.