rasagiline (Azilect)
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Indications
- Parkinson's disease*
- may be used as initial therapy
- may be used in conjunction with Sinemet
- parkinsonism
Contraindications
- coadministation of:
- meperidine, tramadol, methadone, propoxyphene, dextromethorphan, mirtazapine, St John's wort, cyclobenzaprine, vasocontrictors, other MAO inhibitors, general anesthesia (at least 2 week washout)
- does not improve cognitive function in Parkinson's disease[4]
Dosage
Tabs: 0.5 mg, 1 mg
Pharmacokinetics
Adverse effects
- monotherapy
- use in conjunction with Sinemet
- dyskinesias
- accidents
- GI symptoms
- headaches
- weight loss
- arthralgia
- orthostasis (most common 1st 2-3 months)
- hallucinations
- increased risk for melanoma
- drug adverse effects of MAO inhibitors
- drug adverse effects of antidepressants
- drug adverse effects of psychotropic agents
Drug interactions
- drugs that inhibit cyt P450 1A2 can prolong 1/2life of rasagiline
- use with SSRI, SNRI, tricyclic antidepressants, meperidine may result in CNS toxicity, autonomic instability, hypertension, hypertherma, death
- use 2 week washout period
- use 5 week washout period after stopping fluoxetine
- concurrent use of other MAO inhibitors increases risk of hypertension
- meperidine, tramadol, methadone, propoxyphene, dextromethorphan, mirtazapine, St John's wort, cyclobenzaprine, vasocontrictors, other MAO inhibitors, general anesthesia Interactions:
- tyramine-containing foods may increase risk of hypertensive crisis
- drug interaction(s) of antidepressant in combination with GLP1-agonist
- drug interaction(s) of benzodiazepines with antidepressants
- drug interaction(s) of antidepressants with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists with MAO inhibitors
- drug interaction(s) of NSAIDs with antidepressants
- drug interaction(s) of antidepressant with opiates
- drug interaction(s) of MAO inhibitor with caffeine
Mechanism of action
- inhibits monoamine oxidase B
- may have disease-modifying effects in Parkinson's disease[3]
More general terms
References
- ↑ Prescriber's Letter 13(7): 2006 New treatments for Parkinson's Disease (Azilect and Zelapar) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220710&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Prescriber's Letter 14(2): 2007 New drugs approved by the FDA in 2006 Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=2302213&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 3.0 3.1 Olanow CW et al, A Double-Blind, Delayed-Start Trial of Rasagiline in Parkinson's Disease N Engl J Med 2009, 361:1268 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/19776408 <Internet> http://content.nejm.org/cgi/content/short/361/13/1268
- ↑ 4.0 4.1 Weintraub D, Hauser RA, Elm JJ et al Rasagiline for mild cognitive impairment in Parkinson's disease: A placebo-controlled trial. Mov Disord. 2016 May;31(5):709-14. Epub 2016 Mar 31. PMID: https://www.ncbi.nlm.nih.gov/pubmed/27030249