Moclobemide, a reversible inhibitor of monoamine oxidase-A, is now the main representative of the third generation of monoamine oxidase inhibitors. In this review, pharmacodynamics and pharmacokinetic data on moclobemide are presented. Moclobemide has been extensively evaluated clinically and showed efficacy in major unipolar and bipolar depression, dysthymia, depression in neurological disorders, social phobia, and panic disorder. Tolerability of moclobemide is good and its side effects are mild. The drug does not produce sexual dysfunctions and exerts favorable effects on cognitive functions. The data on moclobemide interactions show that the drug can be safely combined with most antipsychotic, antidepressant, and anxiolytic drugs as well as with most drugs used in somatic illnesses. Due to short elimination half-life and reversibility of monoamine oxidase-A inhibition, a change to an alternative antidepressant can be done within 24 hours of stopping moclobemide, and moclobemide can be introduced within several days after discontinuation of previous antidepressant.