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Selegiline

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Selegiline (l-deprenyl, Eldepryl® or Anipryl® [veterinary]) is a drug used for the treatment of early-stage Parkinson's disease and senile dementia. In normal clinical doses it is a selective MAO-B inhibitor, however in very large doses (>25 mg in a typical adult) it loses its specificity and also inhibits MAO-A. Since it is selective for MAO-B, no special dietary restrictions are needed as with other MAOI drugs. The drug was researched by Joseph Knoll.

Uses

It is sometimes used off-label to treat narcolepsy and as a nootropic, as well as for its purported life-extending effects. It is also reported to positively affect libido, particularly in older males. As of February 28, 2006, Selegiline has also been approved by the Food and Drug Administration (FDA) to treat major depression using a transdermal patch (Emsam Patch). Selegiline is also used (at extremely high dosages relative to humans) in veterinary medicine to treat the symptoms of Cushing's disease and so-called "cognitive dysfunction" in dogs. As of June 26, 2006, a Selegiline transdermal patch is being tested for its effectiveness in treating ADHD (Source:Pharma.org).

Mechanism of Action

Selegiline raises dopamine and phenylethylamine levels in the CNS without directly affecting serotonin or norepinephrine. It does so because of its mentioned selectivity versus MAO-B. Selegiline can indirectly raise norepinephrine because dopamine can be catabolized within the brain to norepinephrine, although the extent of this is variable. Selegiline is partly metabolized to an inactive stereoisomer of methamphetamine in vivo in levels that, even if active, most likely are far too low to have any significant effect. However, due to this selegiline can cause false positives for amphetamine/methamphetamine on drug tests.

Legal Issues

Possibly due to the structural similarity to illegal stimulants, selegiline has been classified as a controlled substance in Japan and thus can only be obtained with a prescription or special government license.

External links


Monoamine oxidase inhibitors (MAOI):

Reversible Inhibitor of Monoamine oxidase A (RIMA):

Dopamine Reuptake Inhibitor (DARI):

Norepinephrine-dopamine reuptake inhibitors:

Norepinephrine Reuptake Inhibitor (NRI) or (NARI):

Serotonin-Norepinephrine Reuptake Inhibitor (SNRI):

Selective Serotonin Reuptake Inhibitor (SSRI):

Selective Serotonin Reuptake Enhancer (SSRE):

Tricyclic antidepressants (TCA):

Tetracyclic antidepressants:

Noradrenergic and Specific Serotonergic Antidepressant (NaSSA):

 


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