section name header

Pronunciation

ra-SA-ji-leen

Classifications

Therapeutic Classification: antiparkinson agents

Pharmacologic Classification: monoamine oxidase type b inhibitors

Indications

REMS


Action

  • Irreversibly inactivates monoamine oxidase (MAO) by binding to it at type B (brain sites); inactivation of MAO leads to increased amounts of dopamine available in the CNS.
  • Differs from selegiline by its nonamphetamine characteristics.
Therapeutic effects:
  • Improvement in symptoms of Parkinson's disease, allowing increase in function.

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:

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