Generic Name

Azilect

Mechanism

Azilect (rasagiline) is a selective, irreversible monoamine‑oxidase B (MAO‑B) inhibitor.
• It blocks MAO‑B‑mediated catabolism of dopamine in the central nervous system, increasing synaptic dopamine availability.
• By sparing MAO‑A, rasagiline produces minimal dietary tyramine sensitivity.
• Its irreversible inhibition is sustained; dosing once daily suffices despite a short plasma half‑life.

Pharmacokinetics

• Absorption: Rapid oral absorption; peak plasma concentration within ~1 h.
• Distribution: Widely distributed; crosses the blood‑brain barrier.
• Metabolism: Primarily glucuronidated in the liver; minor CYP2D6 oxidation.
• Elimination: Metabolites excreted renally; terminal half‑life ~1 h, but pharmacodynamic effect lasts ~15–20 days.
• Food effect: Minimal; can be taken with or without food.
• Drug interactions:
• May enhance systemic MAO‑A inhibition when combined with serotonergic drugs or tyramine‑rich foods.
• No significant CYP inhibition/induction at therapeutic doses.

Indications

• Parkinson’s disease (PD):
• Adjunct therapy to levodopa for patients over 18 yrs.
• Monotherapy in early PD when levodopa is not indicated.
• Post‑stroke recovery: Off‑label use in some trials to improve motor function.

Contraindications

• Contraindicated in patients taking tyramine‑containing foods or drugs that cause tyramine release (e.g., sympathomimetics).
• Severe hepatic or renal impairment: Use with caution; no established dose adjustment.
• Pregnancy and lactation: Category D; avoid if possible.
• History of psychiatric disorders: May precipitate serotonin syndrome when combined with SSRIs, SNRIs, or MAO‑A inhibitors.
• Hypertension: Monitor blood pressure due to potential sympathetic stimulation.

Dosing

• Starting dose: 1 mg orally once daily (or 0.5 mg after the first week).
• Maintenance dose: 1 mg daily unless intolerable side effects develop.
• Administration: Take with or without food; consistent daily timing.
• Titration: If adverse effects arise (e.g., nausea), consider 0.5 mg step down.

Adverse Effects

• Common (≤10 %):
• Nausea, dyspepsia, dry mouth.
• Restlessness, insomnia.
• Visual disturbances (mydriasis).
• Serious (>1 %):
• Seizures (rare).
• Hypertension spikes.
• Serotonin‑syndrome‑like picture in combination with serotonergic agents.
• Reversible dystonia/hyperkinesia may occur during initiation; usually resolves with dose adjustment.

Monitoring

• Clinical: Motor function scores (UPDRS), non‑motor symptoms, tremor frequency.
• Safety:
• Blood pressure and heart rate at each visit.
• Liver function tests (baseline, every 3 mo).
• Renal panel if chronic kidney disease suspected.
• Drug level monitoring: Not required due to predictable pharmacodynamics.

Clinical Pearls

• Dual‑therapy synergy: Adding Azilect to levodopa/benserazide can delay motor complications for up to 2 years in early PD.
• Tyramine safety: Because rasagiline is a selective MAO‑B inhibitor, patients can safely ingest modest tyramine foods; educate them on avoiding *high‑tyramine* sources (aged cheese, cured meats).
• Dosing nuance: A 0.5 mg taper for the first week can reduce initial nausea without compromising efficacy.
• Seizure risk: Though rare, monitor for nocturnal seizures in patients with a history of epilepsy—consider baseline EEG if clinically indicated.
• Serotonin syndrome checkpoint: Review all concomitant serotonergic meds and educate patients on symptom recognition (agitation, hyperreflexia, diaphoresis).
• Pregnancy caution: If conception is planned, counsel a 2‑week washout period to avoid teratogenic risk.

Key Takeaway:

Azilect is a convenient, once‑daily MAO‑B inhibitor that safely enhances dopaminergic tone in Parkinson’s disease with a favorable safety profile when used with standard precautions.