Names and pronunciation
(ra-sa′ji-leen) Azilect
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Drug reference
(ra-sa′ji-leen) Azilect
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Func. class.: Antiparkinson agent
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Chem. class.: MAOI, type B
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Do not confuse: Azilect/Aricept
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ACTION: Inhibits MAOI type B at recommended doses; may increase DOPamine levels
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USES: Idiopathic Parkinson’s disease monotherapy or with levodopa
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CONTRAINDICATIONS: Breast feeding; hypersensitivity to this product, MAOIs; pheochromocytoma Precautions: Pregnancy, children, psy- chiatric disorders, moderate to severe hepatic disorders
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SIDE EFFECTS Monotherapy CNS: Drowsiness, hallucinations, depres- sion, headache, malaise, paresthesia, ver- tigo, syncope CV: Angina, hypertensive crisis (inges- tion of tyramine products), orthostatic hypotension GI: Nausea, diarrhea, dry mouth, dys pepsia GU: Impotence, decreased libido HEMA: Leukopenia INTEG: Alopecia, skin cancers MISC: Conjunctivitis, fever, flu syndrome, neck pain, allergic reaction, alopecia MS: Arthralgia, arthritis, dyskinesia RESP: Rhinitis
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INTERACTIONS • Do not give with meperidine, other an- algesics because serious reactions (in- cluding coma and death) may occur; do not give with sympathomimetics Increase: levels of rasagiline up to 2-fold—ciprofloxacin, CYP1A2 inhibitors (atazanavir, mexiletine, taurine) • Increased dopaminergic adverse reac- tion risk—levodopa, dopamine agonists Increase: severe CNS toxicity with anti- depressants (tricyclics, SSRIs, SNRIs, mir- tazapine, cyclobenzaprine) Increase: hypertensive crisis—MAOIs Drug/Herb • Do not give with St. John’s wort, yohimbe Drug/Food • Do not give with foods/liquids that have large amounts of tyramine (cured meats, aged cheese) Drug/Lab Test Increase: LFTs Decrease: WBCs
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DOSAGE AND ROUTES Parkinson disease Monotherapy • Adult: PO 1 mg/day Adjunctive therapy • Adult: PO 0.5 mg/day, may increase 1 mg/day; change of levodopa dose for adjunct therapy; reduced levodopa dose may be needed Hepatic dose • Adult: PO 0.5 mg for mild hepatic dis- ease Concomitant ciprofloxacin, other CYP1A2 inhibitors • Adult: PO 0.5 mg; plasma concentra- tions of rasagiline may double
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Available forms: Tabs 0.5, 1 mg
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Administer: • With meals to prevent nausea; continu- ing therapy usually reduces or eliminates nausea; do not give with foods/liquids containing large amounts of tyramine • Reduce dose of carbidopa/levodopa cautiously • Renal failure: in dialysis, increase dose slowly
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Assess: • Parkinson symptoms: tremors, ataxia, muscle weakness and rigidity at baseline, periodically; increased dyskinesia, pos- tural hypotension if used in combination with levodopa • Mental status: hallucinations, confu- sion; notify prescriber • Hypertensive crisis: severe head- ache, blurred vision, seizures, chest pain, difficulty thinking, nausea, vomiting, signs of stroke; any unexplained severe head- ache should be considered to be hyper- tensive crisis • Melanoma: periodic skin exams by a dermatologist for possible skin cancer • Cardiac status: B/P, ECG periodically, orthostatic hypotension during 2 months R of treatment during beginning treatment • Tyramine products: foods, other medications may lead to hypertensive crisis (tachycardia, bradycardia, chest pain, nausea, vomiting, sweating, dilated pupils) • Drowsiness, daytime sleepiness or fall- ing asleep, may need to be discontinued • Serotonin syndrome: agitation, coma, tachycardia, hyperreflexia, nausea, vomit- ing, diarrhea; may be precipitated in those taking SSRIs, SNRIs • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; cautious use in breastfeeding, excretion unknown
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Evaluate: • Therapeutic response: improved symptoms in patients with Parkinson’s disease
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To change positions slowly to prevent orthostatic hypotension • To avoid hazardous activities until stabi- lized on product; that dizziness can occur • To rinse mouth frequently; to use sug- arless gum to alleviate dry mouth • To take as prescribed; not to miss dose or double doses; to take missed dose as soon as remembered if several hours before next dose • To prevent hypertensive crisis by avoid- ing high-tyramine foods (>150 mg), give list to patient, to report signs/symptoms of hypertensive crisis (headache, chest pain, nausea, palpitations, racing heart) • To avoid CNS depressants, alcohol • To notify all providers of product use; to avoid elective surgery, other proce- dures involving CNS depressants • Check skin periodically for possible skin cancer, higher evidence in Parkin- son disease HIGH ALERT
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PHARMACOKINETICS Onset, peak, duration unknown; 35%-40% absorbed; protein binding >88%-94%; metabolized by CYP1A2 in liver; excreted by kidneys <1%, half-life 1.3 hr
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• Adult: PO 1 mg/day Adjunctive therapy
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• Adult: PO 0.5 mg/day, may increase 1 mg/day; change of levodopa dose for adjunct therapy; reduced levodopa dose may be needed Hepatic dose
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• Adult: PO 0.5 mg for mild hepatic dis- ease Concomitant ciprofloxacin, other CYP1A2 inhibitors
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• Adult: PO 0.5 mg; plasma concentra- tions of rasagiline may double
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