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Tranylcypromine

Tranylcypromine is an irreversible, nonselective MAOI with an amphetamine-like structure, used for treatment-resistant depression. It is more stimulating than phenelzine, has a higher risk of hypertensive crisis, and is prescribed only by specialists with strict diet and drug counselling.

Classification. Irreversible nonselective MAO-A and MAO-B inhibitor, non-hydrazine.

Mechanism. Permanently inactivates both MAO isoenzymes, raising stores of serotonin, noradrenaline and dopamine. It also has a weak amphetamine-like releasing effect. Enzyme activity returns over about 2 weeks.

Pharmacokinetics. Rapidly absorbed; peak in 1 to 3 hours. Plasma half-life only about 2 hours, but the pharmacodynamic effect lasts about 2 weeks. Metabolised by CYP2A6 and others.

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