Phenelzine (sold as Nardil®) is a monoamine oxidase inhibitor (MAOI) used as an antidepressant drug.
Mode of action
Phenelzine is a derivative of
hydrazine, which is
phenylethylamine-like
moiety and similar to normal
substrates of
MAO. When MAO tries to oxidize phenelzine, this hydrazine-moiety binds covalently to the enzyme, thus inactivating it irreversibly. Phenelzine is a non-selective MAO-inhibitor, it inhibits both MAO-A and MAO-B. Furthermore, primarily through its primary metabolite, PEH (phenylethylidenehydrazine), phenelzine elevates levels of GABA in the caudate-putamen and nucleus accumbens. This may contribute to its anxiolytic properties and superior efficiacy in treating severe anxiety.
Pharmacokinetics
Phenelzine is administered orally as phenelzine
sulphate and it is rapidly absorbed form the gastro-intestinal tract. Although phenelzine has a fairly short half-life, its effect lasts for several weeks, until new functional MAO-enzymes have been produced by the body. Phenelzine is acetylated in the liver and its metabolites are excreted in the urine.
More on
[ Phenelzine ]
Antidepressants :: Drugs and Medications
Phenelzine - FamilyDoctor.org - Information for Consumers in English and Spanish.