Monoamine oxidase inhibitor
group of drugs that have in common the ability to inhibit oxidative deamination of naturally occurring monoamines
Monoamine oxidase inhibitors (MAOIs) are a class of drugs that inhibit one or both monoamine oxidase enzymes: monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B). These enzymes metabolize monoamine neurotransmitters and related amines, including serotonin, norepinephrine, dopamine, epinephrine, tyramine, and several trace amines.
MAOIs include several pharmacologically distinct groups. The classic antidepressant MAOIs (phenelzine, tranylcypromine, and isocarboxazid) are irreversible, non-selective inhibitors of both MAO-A and MAO-B and are used primarily in major depressive disorder, including treatment-resistant depression. Other MAOIs include reversible inhibitors of MAO-A (RIMAs), such as moclobemide, and selective MAO-B inhibitors, such as selegiline, rasagiline, and safinamide, which are used mainly in Parkinson's disease or, in the case of transdermal selegiline, depression.
MAOI selectivity can vary by dose, route, formulation, and systemic exposure. For example, selegiline is relatively selective for MAO-B at lower doses used in Parkinson's disease, but at higher antidepressant doses also inhibits MAO-A and can function clinically as a non-selective MAOI.
The use of classic MAOIs declined for many years, following earlier reports of serious interactions with tyramine-containing foods and some sympathomimetic or serotonergic drugs. Nevertheless, modern reviews and prescribing guides state that classic MAOIs remain a highly effective treatment option for depression, and can be used safely when standard dietary and medication interaction precautions are followed. The dietary risk is considered much lower than in the early decades of MAOI use, as modern food production, hygiene standards, refrigeration, and starter culture methods have greatly reduced tyramine exposure in ordinary diets. The possibility of serious tyramine related hypertensive reactions is therefore described as substantially reduced under modern dietary standards and guidance, although not completely eliminated.
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