Clinical Pharmacology of Rasagiline: A Novel, Second‐Generation Propargylamine for the Treatment of Parkinson Disease

@article{Chen2005ClinicalPO,
  title={Clinical Pharmacology of Rasagiline: A Novel, Second‐Generation Propargylamine for the Treatment of Parkinson Disease},
  author={Jack J. Chen and David M. Swope},
  journal={The Journal of Clinical Pharmacology},
  year={2005},
  volume={45}
}
Rasagiline is a novel second‐generation propargylamine that irreversibly and selectively inhibits monoamine oxidase type B (MAO‐B). For the management of Parkinson disease (PD), rasagiline is efficacious across the span of PD stages ranging from monotherapy in early disease to adjunctive treatment in patients with advancing disease and motor fluctuations. Rasagiline completely and selectively inhibits MAO‐B with a potency 5 to 10 times greater than selegiline. Unlike the prototype… 
Rasagiline: A second-generation monoamine oxidase type-B inhibitor for the treatment of Parkinson's disease.
  • Jack J. Chen, A. Ly
  • Medicine
    American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists
  • 2006
TLDR
Rasagiline is an investigational selective and irreversible inhibitor of MAO-B that has demonstrated efficacy and safety for the treatment of PD and whether rasagILine is associated with clinically significant neuroprotection is the subject of ongoing clinical trials.
Rasagiline in treatment of Parkinson’s disease
TLDR
Analysis of delayed-start clinical trial suggests the potential for disease modification, and further trials are examining this effect of rasagiline as an adjunct to levodopa.
Pharmacology of Rasagiline, a New MAO-B Inhibitor Drug for the Treatment of Parkinson’s Disease with Neuroprotective Potential
  • J. Finberg
  • Medicine
    Rambam Maimonides medical journal
  • 2010
TLDR
Rasagiline possesses neuroprotective properties in a variety of primary neuronal preparations and neuron-like cell lines, which is not due to MAO inhibition, and is an effective inhibitor of the plasma membrane dopamine transporter (DAT).
Rasagiline: A novel anti-Parkinsonian monoamine oxidase-B inhibitor with neuroprotective activity
TLDR
It is demonstrated that the major metabolite of rasagiline, 1-(R)-aminoindan has antioxidant and neuroprotective capabilities and thus, may contribute to the overt activity of its parent compound, rasgiline.
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TLDR
Preliminary results maintain some possible advantage to earlier initiation of the 1 mg/day dose of Rasagiline and the clinical significance of the difference detected remains a consideration.
Pharmacokinetic/pharmacodynamic evaluation of rasagiline mesylate for Parkinson’s disease
  • T. Müller
  • Medicine
    Expert opinion on drug metabolism & toxicology
  • 2014
TLDR
This so-called evidence based research suggests that rasagiline is an alternative to the catechol-O-methyltransferase-inhibitor entacapone, in the treatment of wearing-off phenomena.
Rasagiline: A Review of Its Use in the Treatment of Idiopathic Parkinson’s Disease
TLDR
In randomized, controlled trials, oral rasagiline 1 mg once daily was superior to placebo in the symptomatic treatment of early Parkinson’s disease, both as monotherapy or as an adjunct to dopamine agonists.
Comprehensive review of rasagiline, a second-generation monoamine oxidase inhibitor, for the treatment of Parkinson's disease.
TLDR
Rasagiline was effective both as monotherapy in early PD and as adjunctive treatment in patients with advancing PD and motor fluctuations and has the potential to augment the vasopressor effects of diet-derived tyramine (ie, the "cheese reaction").
Monoamine Oxidase‐B Inhibition in the Treatment of Parkinson's Disease
TLDR
Experimental data suggest that MAO-B inhibitors may be neuroprotective through MAO‐B inhibition and other mechanisms that have yet to be clearly defined, making them an option either as monotherapy in early Parkinson's disease or as adjunctive therapy in patients treated with levodopa who are experiencing motor complications.
Safety of rasagiline for the treatment of Parkinson's disease
TLDR
Rasagiline is effective and well tolerated in PD as monotherapy or in combination with levodopa, and the risk of serotonin toxicity with serotoninergic antidepressants remains insufficiently characterized, while current available data in small groups of subjects suggest a low risk.
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