Rasagiline

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Azilect; Belgium: Azilect; Bulgaria: Azilect; Cyprus: Azilect; Czech Republic: Azilect; Denmark: Azilect; Estonia: Azilect; Finland: Azilect; France: Azilect; Germany: Azilect; Greece: Azilect; Hungary: Azilect; Ireland: Azilect; Italy: Azilect; Latvia: Azilect; Lithuania: Azilect; Luxembourg: Azilect; Malta: Azilect; Netherlands: Azilect; Poland: Azilect; Portugal: Azilect; Romania: Azilect; Slovakia: Azilect; Slovenia: Azilect; Spain: Azilect; Sweden: Azilect; UK: Azilect.

North America

Canada: Azilect; USA: Azilect.

Latin America

Argentina: Elbrux, Rasagilina, Raxac.

Drug combinations

Chemistry

Rasagiline Mesylate: C~12~H~13~N CH~4~O~3~S. Mw: 267.34. (1) 1H-Inden-1-amine, 2,3-dihydro-N-2-propynyl-, (R)-, methanesulfonate; (2)(R)-N-2-Propynyl-1-indanamine methanesulfonate. CAS-161735-79-1; CAS-136236-51-6 (rasagiline)(1995).

Pharmacologic Category

Antidepressants; Monoamine Oxidase Inhibitors. Antiparkinsonian Agents; Monoamine Oxidase B Inhibitors. (ATC-Code: N04BD02).

Mechanism of action

Potent, irreversible, selective inhibitor of brain monoamine oxidase (MAO) type B, which plays a major role in catabolism of dopamine. Inhibition of dopamine depletion in striatal region of brain reduces symptomatic motor deficits of Parkinson’s disease. There is also experimental evidence of rasagiline conferring neuroprotective effects (antioxidant, antiapoptotic), which may delay onset of symptoms and progression of neuronal deterioration.

Therapeutic use

Initial monotherapy or as adjunct to levodopa in treatment of idiopathic Parkinson’s disease.

Pregnancy and lactiation implications

Decreased offspring survival and birth weight in animal studies. There are no adequate, well-controlled studies in pregnant women. Animal studies have shown rasagiline capable of inhibiting prolactin secretion (use with caution in nursing women).

Unlabeled use

Contraindications

Hypersensitivity to rasagiline or any component of the formulation. Concomitant use of amphetamine, tramadol, propoxyphene, methadone, dextromethorphan, St. John’s wort, mirtazapine, cyclobenzaprine, or sympathomimetic amines (e.g. pseudoephedrine, ephedrine). Use of meperidine or other MAOIs within 14 days of rasagiline. Elective surgery requiring general anesthesia, local anesthesia containing sympathomimetic vasoconstrictors. Patients with pheochromocytoma.

Warnings and precautions

Rasagiline may cause hallucinations. Signs of severe CNS toxicity (some fatal), including hyperpyrexia, hyperthermia, rigidity, altered mental status, seizure and coma reported in combination with antidepressants. Risk of melanoma may be increased with rasagiline, although increased risk associated with Parkinson’s disease itself. May cause orthostatic hypotension, particularly in combination with levodopa (use with caution in cerebrovascular disease, cardiovascular disease, hypovolemia, or concurrent medication use which may predispose to hypotension/bradycardia). Use with caution in mild hepatic impairment; avoid with moderate to severe impairment. Use of rasagiline with tricyclic antidepressants and SSRIs also associated with rare reactions and should generally be avoided. Do not use within 5 weeks of fluoxetine discontinuation. Do not initiate tricyclic, SSRI or SNRI therapy within 2 weeks of discontinuing rasagiline. Addition of oral selegiline to levodopa therapy may result in exacerbation of levodopa adverse effects. Due to potential for hemodynamic instability, patients should not undergo elective surgery requiring general anesthesia and should avoid local anesthesia containing sympathomimetic vasoconstrictors within 14 days of discontinuing rasagiline. Use caution with foods high in tyramine content, supplements containing tyrosine, phenylalanine, tryptophan, or caffeine. Hypertensive crisis may occur.

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