section name header

Pronunciation

ra-SA-ji-leen

Classifications

Therapeutic Classification: antiparkinson agents

Pharmacologic Classification: monoamine oxidase type b inhibitors

Indications

REMS

Action

Therapeutic Effects:

Pharmacokinetics

Absorption: 36% absorbed following oral administration.

Distribution: Extensively distributed to tissues; readily crosses the blood-brain barrier.

Metabolism/Excretion: Extensively metabolized by the liver primarily by the CYP1A2 isoenzyme to an inactive metabolite; <1% excreted in urine.

Half-life: 1.3 hr; does not correlate with duration of MAO-B inhibition.

Time/Action Profile

ROUTEONSETPEAKDURATION
POrapid1 hr40 days*

*Recovery of MAO-B function.

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: orthostatic hypotension (may levodopa-induced hypotension), BP, chest pain, syncope.

Derm: melanoma risk, alopecia, ecchymosis, rash.

EENT: conjunctivitis, rhinitis.

GI: weight, anorexia, dizziness, dyspepsia, gastroenteritis, vomiting.

GU: libido, albuminuria.

Hemat: leukopenia.

MS: arthralgia, arthritis, neck pain.

Neuro: depression, dizziness, drowsiness, dyskinesia (may levodopa-induced dyskinesia), hallucinations, impulse control disorders (gambling, sexual), malaise, paresthesia, sleep driving, vertigo.

Resp: asthma.
Misc: fever, flu-like syndrome.

Interactions

Drug-Drug:

Drug-Natural Products:

Drug-Food:

Route/Dosage

Hepatic Impairment

Availability

(Generic available)

Assessment

Lab Test Considerations: Toxicity and Overdose:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Azilect