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rasagiline (Azilect)
Indications:
- Parkinson's disease*
a) may be used as initial therapy
b) may be used in conjunction with Sinemet
- parkinsonism
Contraindications:
1) coadministation of:
- meperidine, tramadol, methadone, propoxyphene, dextromethorphan, mirtazapine, St John's wort, cyclobenzaprine, vasocontrictors, other MAO inhibitors, general anesthesia (at least 2 week washout)
2) does not improve cognitive function in Parkinson's disease [4]
Dosage:
1) 1 mg PO QD for monotherapy
2) start 0.5 mg PO QD for use with Sinemet
Tabs: 0.5 mg, 1 mg
Pharmacokinetics:
- metabolized by cyt P450 1A2
Adverse effects:
1) monotherapy
a) headache
b) arthralgia
c) depression
d) dyspepsia
e) falls
2) use in conjunction with Sinemet
a) dyskinesias
b) accidents
c) GI symptoms
d) headaches
e) weight loss
f) arthralgia
g) orthostasis (most common 1st 2-3 months)
h) hallucinations
3) increased risk for melanoma
Drug interactions:
1) drugs that inhibit cyt P450 1A2 can prolong 1/2life of rasagiline
2) 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
3) concurrent use of other MAO inhibitors increases risk of hypertension
4) 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
Mechanism of action:
1) inhibits monoamine oxidase B
2) may have disease-modifying effects in Parkinson's disease [3]
Interactions
drug interactions
drug adverse effects (more general classes)
General
monoamine oxidase [MAO] inhibitor
pharmacologic agents for treatment of Parkinson's disease
Database Correlations
PUBCHEM correlations
References
- Prescriber's Letter 13(7): 2006
New treatments for Parkinson's Disease (Azilect and Zelapar)
Detail-Document#: 220710
(subscription needed) http://www.prescribersletter.com
- Prescriber's Letter 14(2): 2007
New drugs approved by the FDA in 2006
Detail-Document#: 2302213
(subscription needed) http://www.prescribersletter.com
- Olanow CW et al,
A Double-Blind, Delayed-Start Trial of Rasagiline in
Parkinson's Disease
N Engl J Med 2009, 361:1268
PMID: 19776408
http://content.nejm.org/cgi/content/short/361/13/1268
- 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: 27030249