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Review
. 2006 May 15;63(10):915-28.
doi: 10.2146/ajhp050395.

Rasagiline: A Second-Generation Monoamine Oxidase type-B Inhibitor for the Treatment of Parkinson's Disease

Affiliations
Review

Rasagiline: A Second-Generation Monoamine Oxidase type-B Inhibitor for the Treatment of Parkinson's Disease

Jack J Chen et al. Am J Health Syst Pharm. .

Abstract

Purpose: The pharmacology, pharmacokinetics, clinical efficacy, and safety of rasagiline are reviewed.

Summary: Rasagiline is a novel, investigational propargylamine that irreversibly and selectively inhibits monoamine oxidase type B (MAO-B). Rasagiline demonstrates complete and selective inhibition of MAO-B and is at least five times more potent than selegiline. Unlike selegiline, which is metabolized to amphetamine derivatives, rasagiline is biotransformed to the nonamphetamine compound aminoindan. Clinical studies have revealed that rasagiline is associated with improved outcomes in patients with early Parkinson's disease (PD) and also reduces "off" time in patients with moderate to advanced PD with motor fluctuations. Rasagiline is rapidly absorbed by the gastrointestinal tract and readily crosses the blood-brain barrier. The optimal therapeutic dosage is 0.5-1 mg administered orally once daily. Rasagiline appears to be well tolerated, although elderly patients may be more prone to treatment-emergent adverse cardiovascular and psychiatric effects. At the recommended therapeutic dosage of up to 1 mg once daily, tyramine restriction is unnecessary. In addition to MAO-B inhibition, rasagiline has demonstrated neuroprotective properties in experimental laboratory models. The mechanisms whereby rasagiline exerts neuroprotective effects are multifactorial and include upregulation of cellular antioxidant activity and antiapoptotic factors.

Conclusion: Rasagiline is an investigational selective and irreversible inhibitor of MAO-B that has demonstrated efficacy and safety for the treatment of PD. Whether rasagiline is associated with clinically significant neuroprotection is the subject of ongoing clinical trials.

Comment in

  • Duplicate publication.
    Ly AV. Ly AV. Am J Health Syst Pharm. 2006 Dec 1;63(23):2310. doi: 10.2146/ajhp060515. Am J Health Syst Pharm. 2006. PMID: 17106001 No abstract available.
  • Duplicate publication.
    Chen JJ. Chen JJ. Am J Health Syst Pharm. 2006 Dec 1;63(23):2310. doi: 10.2146/ajhp060514. Am J Health Syst Pharm. 2006. PMID: 17106002 No abstract available.

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