RASAGILINE MESYLATE
Clinical safety rating: safe
Animal studies have demonstrated safety
Irreversible monoamine oxidase type B (MAO-B) inhibitor; selectively inhibits MAO-B, reducing oxidative deamination of dopamine, increasing dopaminergic activity.
| Metabolism | Hepatic via CYP1A2; metabolites include N-desmethylrasagiline and p-hydroxyrasagiline. |
| Excretion | Renal excretion of unchanged drug (<1%) and metabolites (~84% as glucuronide and sulfate conjugates of hydroxy-rasagiline). Fecal elimination accounts for <10%. |
| Half-life | Terminal elimination half-life: 1.5–3.5 hours (mean 3 hours) for rasagiline; clinical MAO-B inhibition persists for weeks due to irreversible binding. |
| Protein binding | ~90–95% bound, primarily to albumin. |
| Volume of Distribution | Vd approximately 4.2–5.7 L/kg (mean 5.1 L/kg), indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability ~36% due to first-pass metabolism (CYP1A2). |
| Onset of Action | Oral: 1–2 weeks for maximal MAO-B inhibition; some clinical benefit may be noted within days, but full therapeutic effect requires up to 4 weeks. |
| Duration of Action | MAO-B inhibition lasts 1–2 weeks after discontinuation due to irreversible enzyme inactivation; clinical duration requires daily dosing to sustain inhibition. |
1 mg orally once daily, with or without food.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (GFR ≥30 mL/min). Not recommended in severe renal impairment (GFR <30 mL/min). |
| Liver impairment | Contraindicated in patients with moderate to severe hepatic impairment (Child-Pugh class B or C). Use with caution in mild hepatic impairment (Child-Pugh class A); no specific dose adjustment provided. |
| Pediatric use | Safety and efficacy not established in pediatric patients under 18 years of age. |
| Geriatric use | No specific dose adjustment required; however, elderly patients may be more susceptible to adverse effects such as dizziness and orthostatic hypotension. Monitor closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Other MAOIs and sympathomimetics can cause hypertensive crisis Can cause hypertensive crisis if tyramine-rich foods are consumed.
| Breastfeeding | Excretion in human milk unknown. Not recommended during breastfeeding due to potential for MAO inhibition in infant. |
| Teratogenic Risk | Pregnancy Category C. Animal studies show fetal toxicity at high doses. No adequate human studies; risk cannot be excluded. Use only if benefit outweighs risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Common Effects | Nausea |
| Serious Effects |
["Concomitant use with other MAO inhibitors (e.g., selegiline, linezolid, IV methylene blue)","Concomitant use with pethidine, tramadol, methadone, St. John's wort","Pheochromocytoma history"]
| Precautions | ["May cause hypertensive crisis with ingestion of tyramine-rich foods or sympathomimetic amines","Do not use with other MAO inhibitors","May cause hallucinations, impulse control disorders, serotonin syndrome"] |
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| Monitor for hypertensive crises, serotonin syndrome, and extrapyramidal symptoms. Fetal monitoring for growth and well-being if used. |
| Fertility Effects | No human data. Animal studies show no impairment of fertility at clinically relevant doses. |