Brands, Medical Use, Clinical Data
- Neuroprotective Agents
- Antiparkinson Agents
- Central Nervous System Agents
Brands / Synonyms
Apo-Selegiline; Carbex; Eldepryl; Gen-Selegiline; Jumex; L-Deprenalin; Novo-Selegiline; Nu-Selegiline; Sd Deprenyl; Selegeline Hcl; Selegilina [Inn-Spanish]; Selegiline; Selegiline Hcl; Selegiline-5; Selegilinum [Inn-Latin]
For the adjunct treatment for Parkinson's disease.
Dopamine is an essential chemical that occurs in many parts of the body. It is the premature degradation of dopamine that results in the symptoms of Parkinson's disease. Monoamine oxidase (MAO) is an enzyme which accelerates the breakdown of dopamine. Selegiline can prolong the effects of dopamine in the brain by preventing its breakdown through seletively blocking MAO. It also may prevent the removal of dopamine between nerve endings and enhance release of dopamine from nerve cells.
Mechanism of Action
Although the mechanisms for selegiline's beneficial action in the treatment of Parkinson's disease are not fully understood, the inhibition of monoamine oxidase type B (MAO B) is thought to be of primary importance. MAO B is involved in the oxidative deamination of dopamine in the brain. Selegiline is best known as an irreversible inhibitor of MAO. MAO's activity is inhibited when selegiline binds to the isoalloxazine flavin adenine dinucleotide (FAD) at its active center. In addition, there is evidence that selegiline may increase dopaminergic activity through other mechanisms.
Rapidly absorbed from the gastrointestinal tract.
LD50=63 mg/kg (rats, IV)
Biotrnasformation / Drug Metabolism
ELDEPRYL is contraindicated in patients with a known hypersensitivity to this drug.
ELDEPRYL is contraindicated for use with meperidine (DEMEROL & other trade names). This contraindication is
often extended to other opioids.
The occurrence of stupor, muscular rigidity, severe agitation, and elevated temperature has been reported in some
patients receiving the combination of selegiline and meperidine. Symptoms usually resolve over days when the
combination is discontinued. This is typical of the interaction of meperidine and MAOIs. Other serious reactions
(including severe agitation, hallucinations, and death) have been reported in patients receiving this combination.
Severe toxicity has also been reported in patients receiving the combination of tricyclic antidepressants and
ELDEPRYL and selective serotonin reuptake inhibitors and ELDEPRYL. One case of hypertensive crisis has been reported
in a patient taking the recommended doses of selegiline and a sympathomimetic medication (ephedrine).