Selegiline, also known as L-deprenyl and sold under the brand names Eldepryl and Emsam among others, is a medication which is used in the treatment of Parkinsons disease and major depressive disorder. It is provided in the form of a capsule or tablet taken by mouth for Parkinsons disease and as a patch applied to skin for depression. Selegiline acts as a monoamine oxidase inhibitor, and increases levels of monoamine neurotransmitters in the brain. At typical clinical doses used for Parkinsons disease, selegiline is a selective and irreversible inhibitor of monoamine oxidase B (MAO-B), increasing levels of dopamine in the brain. In larger doses (more than 20 mg/day), it loses its specificity for MAO-B and also inhibits MAO-A, which increases serotonin and norepinephrine levels in the brain. Medical uses
Parkinsons disease
In its pill form, selegiline is used to treat symptoms of Parkinsons disease. It is most often used as an adjunct to drugs such as levodopa (L-DOPA), although it has been used off-label as a monotherapy. The rationale for adding selegiline to levodopa is to decrease the required dose of levodopa and thus reduce the motor complications of levodopa therapy. Selegiline delays the point when levodopa treatment becomes necessary from about 11 months to about 18 months after diagnosis. There is some evidence that selegiline acts as a neuroprotectant and reduces the rate of disease progression, though this is disputed.Selegiline has also been used off-label as a palliative treatment for dementia in Alzheimers disease.
While the NDA was under review, Somerset was acquired in a joint venture by two generic drug companies, Mylan and Bolan Pharmaceuticals. Selegiline was approved for Parkinsons disease by the FDA in 1989.In the 1990s, J. Alexander Bodkin at McLean Hospital, an affiliate of Harvard Medical School, began a collaboration with Somerset to develop delivery of selegiline via a transdermal patch in order to avoid the well known dietary restrictions of MAO inhibitors. Somerset obtained FDA approval to market the patch in 2006. Society and culture
In E for Ecstasy (a book examining the uses of the street drug ecstasy in the UK) the writer, activist and ecstasy advocate Nicholas Saunders highlighted test results showing that certain consignments of the drug also contained selegiline. Consignments of ecstasy known as "Strawberry" contained what Saunders described as a "potentially dangerous combination of ketamine, ephedrine and selegiline," as did a consignment of "Sitting Duck" Ecstasy tablets.David Pearce wrote The Hedonistic Imperative six weeks after starting taking selegiline.In Gregg Hurwitzs novel Out of the Dark, selegiline (Emsam) and tyramine-containing food were used to assassinate the president of the United States. Veterinary use
In veterinary medicine, selegiline is sold under the brand name Anipryl (manufactured by Zoetis). It is used in dogs to treat canine cognitive dysfunction and, at higher doses, pituitary-dependent hyperadrenocorticism (PDH). Canine cognitive dysfunction is a form of dementia that mimics Alzheimers disease in humans. Geriatric dogs treated with selegiline show improvements in sleeping pattern, reduced incontinence, and increased activity level; most show improvements by one month.