Safinamide

Trade names

• XADAGO

Actions

• Selective monoamine oxidase B inhibitor.
• Inhibits glutamate release.
• Inhibits dopamine and serotonin reuptake.

Route of Administration

Oral

Bioavailability

95%

Plasma protein binding

88-90%

Half-life

20-30 hours

Metabolism

Hepatic

Elimination

Renal 76%, biliary 1.5%

Important side-effects

Exacerbation of hypertension.

Certain foods that contain very high amounts (>150 mg) of tyramine may cause severe hypertension in patients treated with MAO-B inhibitors.

Serotonin syndrome when concomitantly administrated with serotonergic medication (SSRI, SNRI, tricyclic and tetracyclic antidepressants, etc).

Excessive somnolence.

Dyskinesias.

Orthostatic hypotension.

Hallucinations and psychosis.

Impaired impulse control and compulsive behaviors.

Retinal degeneration and loss of photoreceptor cells were observed in rats. Periodically monitor patients for visual changes in patients with a history of retinal/macular degeneration, uveitis, inherited retinal conditions, family history of hereditary retinal disease, albinism, retinitis pigmentosa, or any active retinopathy (e.g., diabetic retinopathy).

Recommended dose

Start with 50 mg once daily.

After two weeks, the dosage may be increased to 100 mg once daily.

Renal impairment

No dose adjustment is necessary.

Hepatic impairment

In patients with moderate hepatic impairment (Child-Pugh B), the maximum recommended dosage of safinamide is 50 mg orally once daily.

Safinamide is contraindicated in patients with severe hepatic impairment (Child-Pugh C)