
(raz ah’ gah leen)
Azilect
PREGNANCY CATEGORY C
Drug Classes
Antiparkinsonian
MAO type B inhibitor
Therapeutic Actions
Inhibits MAO type B (found mostly in the CNS), leading to increased levels of dopamine at the synapse particularly in areas of the brain responsible for controlling movement and coordination; much less effect in the periphery leads to fewer peripheral adverse effects.
Indications
Treatment of signs and symptoms of idiopathic Parkinson disease as initial mono-therapy and as adjunct therapy with levodopa
Contraindications and Cautions
Contraindicated with known hypersensitivity to any component of the drug; concurrent use of meperdine, tramadol, methadone, propoxyphene, dextromethorphan, sympathomimetic amines, MAOIs, SSRIs, TCAs; elective surgery; pheochromocytomas; diets rich in tyramine; severe hepatic insufficiency.
Use cautiously with mild hepatic insufficiency, pregnancy, lactation, use of other CYP1A2 inhibitors.
Available Forms
Tablets—0.5, 1 mg
Dosages
Adults
Initial monotherapy: 1 mg/day PO.
Adjunct therapy with levodopa: 0.5 mg/day PO; if response is insufficient, may increase to 1 mg/day PO. In some patients, levodopa dose may need to be decreased. Monitor patient response closely.
Patients with hepatic impairment
In mild hepatic impairment, 0.5 mg/day PO; not recommended in moderate to severe hepatic impairment.
Patients taking CYP1A2 inhibitors (such as ciprofloxacin)
0.5 mg/day PO.
Pediatric patients
Safety and efficacy not established.
Pharmacokinetics
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