Safinamide is a monoamine oxidase type B (MAO-B) inhibitor indicated as an adjunct therapy to levodopa/carbidopa in patients with Parkinson’s disease who experience “off” episodes. It has not been proven effective as monotherapy for the treatment of Parkinson’s disease.

The exact mechanism by which Safinamide Mesylate works in Parkinson’s disease is not fully understood. Safinamide Mesylate acts by selectively inhibiting monoamine oxidase B (MAO-B), an enzyme responsible for the breakdown of dopamine. By blocking dopamine catabolism, it helps increase dopamine levels in the brain and enhances dopaminergic activity, which contributes to improvement of Parkinson’s disease symptoms.

For Usual Initial Dosage: The recommended starting dosage of Safinamide tablet is 50 mg orally once daily (at the same time of day). If a dose is missed, the next dose should be taken at the same time the next day.

For Maintenance dosage: After 2 weeks, the dose may be increased to 100 mg once daily, based on individual need and tolerability. Safinamide 100 mg should be tapered by decreasing the dose to 50 mg for one week before stopping.

Use in Children: Safety & effectiveness of Safinamide in infants & children have not been established.

Geriatric Use: No overall differences in safety or effectiveness were observed in these patients and younger patients.

Hepatic Impairment: Safinamide plasma concentrations are increased in patients with hepatic impairment.

• Selective Serotonin Reuptake Inhibitors (SSRIs): Patients should be monitored for serotonin syndrome.
• Sympathomimetic medications: Blood pressure should be monitored as hypertension may occur.
• Tyramine-containing foods: May increase the risk of severe hypertension.
• Breast Cancer Resistance Protein (BCRP) substrates: May increase the plasma concentration of BCRP substrate drugs.

Safinamide is contraindicated in patients with:

• Concomitant use of other monoamine oxidase inhibitors or strong MAO inhibitors (such as linezolid)
• Use of opioid drugs (such as tramadol, meperidine and related agents)
• Use of selective norepinephrine reuptake inhibitors, tricyclic/tetracyclic antidepressants, triazolopyridine antidepressants, cyclobenzaprine, methylphenidate, amphetamine and related derivatives, or St. John’s wort
• Concomitant use of dextromethorphan
• History of hypersensitivity to safinamide
• Severe hepatic impairment (Child-Pugh C: 10–15)

The most common adverse effects of Safinamide include dyskinesia, falls, nausea, and insomnia.

Pregnancy Category C. There are no adequate and well-controlled studies of safinamide in pregnant women. Animal studies have shown developmental toxicity, including teratogenic effects, at clinically relevant doses. In rat pups exposed indirectly through breast milk, skin discoloration related to hyperbilirubinemia due to hepatobiliary toxicity was observed. It is not known whether safinamide is excreted in human milk. Because many drugs pass into breast milk and may cause serious adverse effects in nursing infants, a decision should be made whether to discontinue breastfeeding or discontinue the medicine, considering the importance of treatment for the mother.

• May cause or worsen hypertension
• May cause serotonin syndrome when used with MAO inhibitors, antidepressants, or opioid drugs
• May cause sudden sleep episodes during daily activities
• May worsen dyskinesia; reduction of levodopa dose may be required
• May cause hallucinations and psychotic behavior
• May lead to impulse control disorders or compulsive behaviors
• May cause withdrawal-related hyperpyrexia and confusion

There is no human experience regarding overdose with Safinamide. In case of significant overdose, treatment should be discontinued and supportive care should be given as clinically required. Dietary restriction of tyramine may also be necessary for several weeks.

Antiparkinson drugs

Store below 30°C. Protect from light and keep out of the reach of children.