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Indications and Dosage
Oral
Depression Adult: Initially, 10 mg in the morning and in the afternoon. May increase afternoon dose to 20 mg after a wk if response is inadequate or alternatively, an additional 10 mg may be given at midday. Gradually reduce for maintenance, usually 10 mg daily, once response is obtained.
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Contraindications
Porphyria, actual or suspected cerebrovascular disease, severe CV disease, actual or suspected phaeochromocytoma, hyperthyroidism, blood dyscrasias, liver damage. Concomitant use w/ indirectly acting sympathomimetic amines or similar anti-obesity agents, ephedrine or phenylpropanolamine, levodopa or dopamine, pethidine and closely related narcotic analgesics, nefopam, dextromethorphan, buspirone, bupropion, fluvoxamine, TCAs, SSRIs, selective norepinephrine reuptake inhibitors (SNRIs) and other MAOIs and cheese or other foods w/ high-tyramine content (w/in 2 wk after stopping treatment); meperidine (w/in 2 or 3 wk after stopping treatment).
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Special Precautions
Patient w/ epilepsy, DM, hyperthyroidism, CV disease in whom physical activity should be regulated, history of drug or alcohol dependence. Avoid abrupt withdrawal. Withdraw treatment at least 2 wk before elective surgery. Not intended for use in bipolar depression. Renal impairment. Pregnancy and lactation.
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Adverse Reactions
Insomnia, postural HTN, drowsiness, dizziness, fatigue, dry mouth, blurred vision, headache, diarrhoea, nausea, vomiting, sleep disturbance, rash, overstimulation (e.g. agitation and anxiety, developing rarely into hypomanias). Rarely, hepatocellular damage, jaundice, hallucinations, blood dyscrasias.
Potentially Fatal: Suicidal thinking and behaviour, hypertensive crisis. |
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Patient Counseling Information
May impair ability to drive or operate machinery.
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Monitoring Parameters
Monitor blood glucose, BP, renal and hepatic function, heart rate, mental status.
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Overdosage
Symptoms: Hyperpyrexia, convulsions, tremor. Management: Induce vomiting and/or gastric lavage together w/ supportive and symptomatic treatment. May use external cooling for hyperpyrexia. Hypotension may be treated by fluid replacement, or w/ norepinephrine (in severe cases). HTN may be relieved by slow inj of phentolamine mesylate. Pancuronium w/ mechanical ventilation may reverse muscle spasm and pyrexia. β-adrenergic receptor blockers may also be used.
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Drug Interactions
May antagonise the action of guanethidine. Hyperactivity may occur w/ reserpine. Risk of central excitation w/ methyldopa. May potentiate the action of oral hypoglycaemic agents or insulin, anticholinergic antiparkinsonism drugs, narcotic analgesics (except pethidine). Possible additive effects w/ other hypotensive agents. May lower seizure threshold w/ metrizamide. Risk of neuromotor syndrome w/ L-tryptophan.
Potentially Fatal: Risk of severe hypertensive reactions w/ indirectly acting sympathomimetic amines (e.g. amphetamine, fenfluramine or other similar anti-obesity agents), ephedrine or phenylpropanolamine, levodopa or dopamine. May potentiate the action of pethidine and narcotic analgesics (e.g. meperidine), nefopam, dextromethorphan. Increased BP w/ buspirone. Possible overdosage may occur w/ other MAOIs. Increased risk of HTN and CNS excitation w/ TCAs. Risk of serotonin syndrome w/ fluvoxamine. Serious reactions (e.g. hyperthermia, rigidity, myoclonus, autonomic instability w/ possible fluctuations in vital signs, mental status changes) w/ SSRIs and SNRIs. May enhance the hypertensive effect of bupropion. |
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Food Interaction
May enhance the adverse/toxic effect w/ alcohol. Risk of serious hypertensive reaction w/ cheese or other foods w/ high-tyramine content.
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Action
Description: Tranylcypromine increases epinephrine, norepinephrine and serotonin concentration in storage sites throughout the nervous system through inhibition of the enzyme, monoamine oxidase.
Onset: 2 days to 3 wk (continued dosing). Duration: Up to 10 days following discontinuation. Pharmacokinetics: Absorption: Readily absorbed from the GI tract. Time to peak plasma concentration: Approx 1-3 hr. Metabolism: Undergoes considerable metabolism, including breakdown of the side chain and probably conjugation. Excretion: Via urine, mainly as metabolites. Plasma elimination half-life: Approx 2.5 hr. |
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Chemical Structure
 Source: National Center for Biotechnology Information. PubChem Database. Transamine, CID=19493, https://pubchem.ncbi.nlm.nih.gov/compound/Transamine (accessed on Jan. 23, 2020) |
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Storage
Store between 15-30°C.
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MIMS Class
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ATC Classification
N06AF04 - tranylcypromine ; Belongs to the class of non-selective monoamine oxidase inhibitors. Used in the management of depression.
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References
Anon. Tranylcypromine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 19/02/2016. Buckingham R (ed). Tranylcypromine Sulfate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 19/02/2016. McEvoy GK, Snow EK, Miller J et al (eds). Tranylcypromine Sulfate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 19/02/2016. Tranylcypromine Sulfate Tablet, Film Coated (Actavis Pharma, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 19/02/2016.
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