Monoamine oxidase inhibitors (MAOIs) were the first class of antidepressants, but current use of these agents is primarily limited to treating atypical and refractory cases of depression (Table 179-1).1 Newer antidepressants have a more favorable side effect profile, less overdose toxicity, and no dietary restrictions. The declining popularity of oral MAOIs for the treatment of depression is partially offset by increasing use of agents in this class for the treatment of Parkinson's disease.2 In addition, a transdermal method of selegiline administration is approved for use in major depression and appears to avoid some of the worrisome aspects associated with traditional oral therapy.3,4,5
TABLE 179-1U.S. Food and Drug Administration Approved Monoamine Oxidase Inhibitors |Favorite Table|Download (.pdf) TABLE 179-1 U.S. Food and Drug Administration Approved Monoamine Oxidase Inhibitors
|Agent ||Indication ||Formulation ||Average Daily Therapeutic Dose ||Maximum Daily Therapeutic Dose ||Selectivity |
|Isocarboxazid ||Major depression ||10-milligram tablet ||10–40 milligrams ||60 milligrams ||Nonselective |
|Phenelzine ||Major depression ||15-milligram tablet ||45–75 milligrams ||90 milligrams ||Nonselective |
|Tranylcypromine ||Major depression ||10-milligram tablet ||20–40 milligrams ||60 milligrams ||Nonselective |
|Selegiline ||Major depression ||6 milligrams, 9 milligrams, and 12 milligrams per 24-h patch ||6 milligrams per 24-h patch ||12 milligrams per 24-h patch ||Nonselective (as a skin-patch formulation) |
|Rasagiline ||Parkinson's disease ||0.5- and 1.0-milligram tablets ||0.5–1.0 milligram ||1 milligram ||MAO-B |
|Selegiline ||Parkinson's disease ||5-milligram tablet ||10 milligrams ||10 milligrams ||MAO-B (as an oral formulation) |
|1.25-milligram oral disintegrating tablet ||1.25 milligrams ||2.5 milligrams ||MAO-B (as an oral formulation) |
|Moclobemide* ||Major depression, social anxiety ||150- and 300-milligram tablets ||300 milligrams ||600 milligrams ||MAO-A |
Safety and effectiveness of MAOIs in children have not been established, and the four agents used for treatment of depression have the identical U.S. Food and Drug Administration–mandated black box warning stating that patients <24 years old may have increased suicidal thinking and behavior while taking any type of antidepressant medication.
MAOIs are associated with tyramine reactions, serotonin syndrome, and medication incompatibilities that are unique to this class of antidepressants. Overdoses of MAOIs are considered life-threatening emergencies, and even one pill could potentially kill a toddler. The onset of clinical toxicity is often delayed to between 6 and 24 hours after ingestion, which can lead to misdiagnosis and mismanagement.
MAOI antidepressants with improved safety and tolerability, such as moclobemide, are available in Canada, Australia, and Europe, but not the United States. St. John's wort (Hypericum perforatum) contains many active ingredients, some of which have the ability to inhibit monoamine oxidase and block serotonin reuptake.6 St. John's wort is considered generally safe when taken at recommended dosages, but even modest monoamine oxidase inhibition may become clinically significant in overdose, may contribute to serotonin syndrome, or may participate in a drug–drug interaction.
Some medications have monoamine oxidase inhibition as an unrelated pharmacologic action, such ...