Generic
Safinamide Mesylate
2 brands available in the market
At a glance
Safinamide is an MAO-B inhibitor used as adjunctive therapy to levodopa/carbidopa for the treatment of off episodes in Parkinson's disease. It increases dopamine levels in the brain by blocking dopamine catabolism.
Description
Safinamide is a monoamine oxidase type B (MAO-B) inhibitor. It inhibits MAO-B activity, preventing dopamine catabolism, leading to increased dopamine levels and enhanced dopaminergic activity in the brain, which improves motor symptoms in Parkinson's disease.
Indications
- Off episodes in Parkinson's disease (adjunctive to levodopa/carbidopa)
Therapeutic class
Antiparkinson Drugs
Pharmacological class
MAO-B Inhibitor
Pharmacology
Safinamide inhibits MAO-B enzyme, preventing dopamine breakdown, which increases dopamine levels in the brain and enhances dopaminergic activity. It helps improve motor symptoms such as tremors, rigidity, and movement difficulties in Parkinson's disease.
Mechanism of action
Inhibits MAO-B enzyme to prevent dopamine breakdown and increase brain dopamine.
Dosage
Adult Dose (Oral):
- Starting: 50 mg once daily (at the same time each day)
- Maintenance: Increase to 100 mg once daily after 2 weeks (based on tolerability)
- Discontinuation: Taper 100 mg dose to 50 mg for one week before stopping
Administration
- Take orally with or without food
- Take at the same time each day
Missed dose
If you miss a dose, take the next dose at the same time the next day; do not double the dose.
Side effects
Common Side Effects:
- Dyskinesia
- Fall
- Nausea
- Insomnia
Precautions & warnings
- Risk of serotonin syndrome (with SSRIs, SNRIs, tricyclic antidepressants)
- May cause or exacerbate hypertension
- May cause falling asleep during daily activities
- May cause hallucinations and psychotic behavior
- May cause impulse control/compulsive behaviors
- Abrupt discontinuation may cause withdrawal hyperpyrexia and confusion
Contraindications
- Concomitant use with other MAO inhibitors or potent MAO inhibitors (linezolid)
- Opioid drugs (tramadol, meperidine)
- SNRIs, tri- or tetracyclic or triazolopyridine antidepressants
- Cyclobenzaprine, methylphenidate, amphetamines
- St. John's wort
- Dextromethorphan
- Severe hepatic impairment (Child-Pugh C)
- Hypersensitivity to safinamide
Drug interactions
- SSRIs: Monitor for serotonin syndrome
- Sympathomimetics: Monitor for hypertension
- Tyramine: Risk of severe hypertension
- BCRP substrates: Potential increase in plasma concentration
Food interactions
Caution is advised when consuming alcohol with Safinamide; consult your doctor.
Use in pregnancy
Use in Pregnancy: No adequate controlled studies; animal studies show adverse effects; use only if clearly needed; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unknown if excreted in human milk; decide whether to discontinue nursing or the drug; consult your doctor.
Pediatric use
Safety and efficacy not established in children
Geriatric use
No overall differences in safety or effectiveness observed in elderly vs. younger patients
Renal / hepatic impairment
Renal Impairment: Caution required in renal impairment; dose adjustment may be needed; consult your doctor.
Hepatic Impairment: Plasma concentrations increased in hepatic impairment; contraindicated in severe hepatic impairment (Child-Pugh C); consult your doctor.
Overdose effects
No human overdose experience; in severe overdose, discontinue treatment and provide supportive care; dietary tyramine restriction for several weeks.
Storage conditions
Store below 30°C, protected from light; keep out of reach of children.
Chemical structure
Safinamide Mesylate