Rasagiline
AZILECT
Pronunciation: ra-SA-ji-leen
“Raise a lean Aztec”
Mao Zedong → MAOI
What it isIrreversible MAO-B inhibitor; Parkinson disease.
Why this oneOnce daily with no amphetamine metabolites, unlike selegiline.
What limits itSelectivity is lost at higher doses, so tyramine and serotonergic precautions apply. Modest symptomatic effect.
FDA-approved for
- Parkinson disease (2006)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Parkinson's disease — monotherapy or adjunct without levodopa | Adults | 1 mg QD | 1 mg QD | 1 mg/day |
| Parkinson's disease — adjunct to levodopa | Adults | 0.5 mg QD | 1 mg QD if needed | 1 mg/day |
| With ciprofloxacin/other CYP1A2 inhibitors | Adults | 0.5 mg QD | 0.5 mg QD | 0.5 mg/day |
Renal No adjustment for mild-moderate impairment; not studied in severe
Hepatic Mild impairment: do not exceed 0.5 mg QD; not for use in moderate or severe impairment
Instructions
- Consider reducing levodopa dose when combined
- Allow >=14 days between discontinuing rasagiline and starting contraindicated drugs
Available strengths
- tab 0.5, 1 mg
Contraindications
- Meperidine, tramadol, methadone, propoxyphene — risk of serotonin syndrome
- Other MAO inhibitors, including other selective MAO-B inhibitors
- Dextromethorphan — risk of psychosis/bizarre behavior
- St. John's wort and cyclobenzaprine
Cautions
- Hypertension, including severe hypertensive syndromes
- Serotonin syndrome with antidepressants
- Falling asleep during ADLs, somnolence
- Orthostatic hypotension
- Dyskinesia (may lessen with levodopa reduction)
- Hallucinations / psychotic-like behavior
- Impulse-control/compulsive behaviors
- Withdrawal-emergent hyperpyrexia and confusion
Adverse reactions
- Monotherapy: flu syndrome, arthralgia, depression, dyspepsia
- Adjunct to levodopa: dyskinesia, postural hypotension, weight loss, nausea, falls
Pregnancy No adequate human data; decreased offspring survival/weight in animals
Lactation No human data; may inhibit prolactin secretion
Cost
Generic entry2013
NO BOXED WARNINGS
Principal riskSelectivity lost at higher doses; tyramine precautions
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityOrthostasis, hallucinations, dyskinesia and impulse-control symptoms; abrupt withdrawal can be hazardous.
Serotonin and MAOI
Provisional washout figures
Elevating mechanismMAO-B inhibitor; exposure-dependent MAO-A inhibition
Non-elevating actionNone recorded
Exposure dependenceDose-dependent loss of MAO-B selectivity
Washout AFTER an MAOIDose-dependent days
Evidence confidenceModerate
InterpretationSelective MAO-B inhibition at usual doses; MAO-A relevance emerges if selectivity is lost.
Open Rasagiline in the interactive console ↗
Memory aids: interaction avatars
