CAS Number: 14611-52-0

Eldepryl | 14611-52-0

Eldepryl (generic name selegiline) is a selective, irreversible monoamine oxidase type B (MAO-B) inhibitor primarily used to treat Parkinson’s disease (PD), either as an initial monotherapy to delay the need for levodopa or as an adjunct to levodopa/carbidopa to reduce "off" episodes and improve motor symptoms. By inhibiting MAO-B, it reduces the degradation of dopamine in the brain, thereby increasing dopamine levels. Common side effects include insomnia (avoiding evening doses is advised), nausea, dizziness, and headache; at higher doses, dietary restrictions for tyramine-rich foods are necessary to avoid hypertensive crisis, and drug interactions with SSRIs or meperidine can cause serotonin syndrome. Notably, a 2015 study on rat models of PD found that Eldepryl may exert its therapeutic effects by inhibiting nerve cell autophagy in the substantia nigra, as evidenced by reduced expression of autophagy-related proteins Beclin1 and LC3, suggesting that modulation of autophagic activity could be a novel pathway for PD treatment.

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References

  • Autophagy-related protein expression in the substantia nigra and eldepryl intervention in rat models of Parkinson׳s disease
    It is the basis of the experimental study to establish a reliable Parkinson׳s disease animal models. Rotenone, a natural organic pesticide, easily traverses blood-brain barrier, directly enters dopaminergic neurons, without the help of dopamine transporter (Sherer et al., 2007), induces the loss of dopaminergic neurons, increases oxidation of mitochondrial proteins, and promotes the development of autophagic vesicles (Lin et al., 2014).
    DOI: 10.1016/j.brainres.2015.08.033
  • L-deprenyl (selegiline) added to Sinemet CR in the management of Parkinson's disease patients with motor response fluctuations
    L-deprenyl (Eldepryl) added to Sinemet CR in the treatment regimens of seven patients with Parkinson's disease (PD) and therapeutic response fluctuations (RF) allowed a statistically significant reduction in total daily levodopa intake and an increase in the mean interdose interval. Trends were noted towards a reduction in the number of daily ''off'' periods and an increase in the portion of the waking day spent ''on.'' Three patients suffered an increase in the intensity of their dyskinesias, and discontinued taking deprenyl. Four patients, all of whom reported improved functioning during ''off'' periods, have continued taking the combination. Sinemet CR and deprenyl can safely be used together in patients with advanced PD, and the combination may result in improved control of motor fluctuations in selected patients.
    DOI: 10.1097/00002826-199106000-00005
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