Also Known As: Selegiline, Atapryl, L-deprenyl, Eldepryl, Emsam, Zelapar, Deprenyl
Selegiline (L-deprenyl, Eldepryl, Emsam, Zelapar) is a drug used for the treatment of early-stage Parkinson's disease, depression and senile dementia. In normal clinical doses it is a selective irreversible MAO-B inhibitor, however in larger doses it loses its specificity and also inhibits MAO-A. Dietary restrictions are common for MAOI treatments, but special dietary restrictions for lower doses have been found to be unnecessary, and dietary restrictions appear to be unnecessary at standard doses when selegiline is taken as Emsam, the transdermal patch form, as no adverse events due to diet have ever been reported with Emsam. The drug was discovered by Jozsef Knoll et al. in Hungary. Selegiline belongs to a class of drugs called phenethylamines. Selegiline is a methamphetamine derivative with a propargyl group attached to the nitrogen atom.
The main use of selegiline is in the treatment of Parkinson's disease. It can be used on its own or in a combination with another agent, most often L-DOPA. For the newly diagnosed Parkinson's patients, some claim that selegiline slows the progression of the disease, although this claim has not been widely accepted and the methodology has been rejected by the Food and Drug Administration (FDA). It delays the time point when the L-DOPA (levodopa) treatment becomes necessary from 10-12 to 18 months, which is beneficial despite not being definitive evidence of neuroprotection. The idea behind adding selegiline to levodopa is to decrease the dose of levodopa and thus reduce the motor complications of levodopa therapy. Comparisons of patients on levodopa + placebo vs levodopa + selegiline showed that selegiline allowed reduction of the levodopa dose by about 40%. Selegiline + levodopa also extended the time until the levodopa dose had to be increased from 2.6 to 4.9 years. As a result there were fewer motor complications in selegiline groups. In one trial, selegiline + levodopa completely halted the progress of Parkinson's disease over 14 months, while in the placebo + levodopa group the deterioration of the patients' condition continued. However, the interpretation of this trial as proving neuroprotective action of selegiline has been questioned.
As of February 28, 2006, selegiline has also been approved by the FDA to treat major depression using a transdermal patch (Emsam Patch). Selegiline (brand name Anipryl) is also used (at extremely high dosages relative to humans) in veterinary medicine to treat the symptoms of Cushing's disease and cognitive dysfunction (Canine Cognitive Dysfunction) in dogs. As of June 26, 2006, a selegiline transdermal patch is being tested for its effectiveness in treating ADHD.
Several clinical studies are currently underway to evaluate selegiline's effectiveness in helping people stop smoking tobacco or cannabis.