Selegiline transdermal patch

The monoamine oxidase inhibitors (MAOIs) phenelzine and tranylcypromine increase the concentrations of NE, 5-HT, and DA within the neuronal synapse through inhibition of the monoamine oxidase (MAO) enzyme system. Both drugs are nonselective inhibitors of MAO-A and MAO-B. Selegiline is available as a transdermal patch for treatment of major depression. It inhibits MAO-A and MAO-B in the brain, but has reduced effects on MAO-A in the gut. 

Selegiline is an irreversible but relatively selective inhibitor of MAO-B. An oral preparation is currently marketed as a treatment for Parkinson s disease. An oral dose produces meaningful inhibition of MAO-B but not MAO-A. The concept behind the transdermal patch is to preferentially deliver more selegiline to the brain than to the liver such that meaningful inhibition of both MAO-A and MAO-B is achieved in the brain but only MAO-B inhibition is achieved in the liver. The... 

NOTE Most of the drugs are hydrochloride salts, but SURMONTIL and LUVOX are maleates CELEXA is a hydrobromide, and remeron is a free-base. Selegiline is approved for early Parkinson s disease, but may have antidepressant effects, especially at daily doses 20 mg, and is under investigation for administration by transdermal patch. 

Early antidepressant medications were called tricyclic antidepressants (TCA), exemplified by dothiepin and amitriptyline. However, there are toxicity issues with these medications. The next generation of antidepressants was the monoamine oxidase inhibitors (MAOIs). As their name implies, they inhibit the monoamine oxidase enzyme thereby inhibiting the oxidation of monoamines such as serotonin that act as neurotransmitters. Examples include selegiline (available in transdermal patch form as Emsam , Somerset... 

Accordingto the FDA-approved prescribing information for the transdermal selegiline patch, patients receiving the 6 mg/24 hour dose are not required to modify their diet. However, patients receiving the 9 or 12 mg/24 hour dose are still required to follow the dietary restrictions similar to the other monoamine oxidase inhibitors (MAOIs). 

MAOIs had been reserved as a last line of treatment, used only when other classes of antidepressant drugs had failed, because of the mentioned potentially lethal dietary and drug interactions. However, in 2006 a patch form of the drug selegiline, called Emsam, was approved for use by the FDA. When applied transdermally the drug does... 

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