Xafinact

Safinamide (Safinamide) instructions

Common name: Safinamide

Trade name: Xadago

Full names: Safinamide, Safinamide, Xadago, Safinamide, Equf ina

Indications:

Xadago is indicated for the treatment of adult patients with idiopathic Parkinson's disease (PD) as an add-on therapy to patients with moderate to late-stage fluctuations on stable doses of levodopa (L-dopa), alone or in combination with other PD medicinal products.

Usage and dosage:

Safinamide treatment should start with 50 mg per day. The daily dose may be increased to 100 mg/day based on individual clinical needs.

If a dose is missed, the next dose should be taken at the usual time the next day.

Adverse reactions:

The most common adverse reactions (the incidence rate is calculated using XADAGO 100 mg/day at least 2% greater than placebo) for motor dysfunction, falls, nausea, and insomnia

Contraindications:

XADAGO is contraindicated in the following patients:

1. Concomitant use of:

Other monoamine oxidase inhibitors or other drugs that are strong inhibitors of monoamine oxidase (e.g., linezolid [l inezolid])

Opioids (eg, tramadol, pethidine, and related derivatives); selective norepinephrine reuptake inhibitors; tri- or tetra-cyclic or triazopyridine antidepressants; cyclobenzaprine; phenylpiperidine methyl acetate, amphetamine, and their derivatives; St. John's wort, dextromethorphan

2. History of hypersensitivity to safinamide.

3. Severe liver damage (Child-Pugh C: 10-15)

Notes:

1. May cause or aggravate hypertension

2. When used with MAO inhibitors, antidepressants, or opioids, it may cause serotonin syndrome.

3. Activities during the day may cause you to fall asleep.

4. May cause or worsen motor dysfunction; consider reducing the dose of levodopa

5. May cause hallucinations and psychotic behavior

6. May cause problems with impulse control/compulsive behavior

7. May cause withdrawal symptoms such as hyperthermia and confusion

Storage:

Store at 25°C (77°F); excursions allowed between 15°C and 30°C (59°F and 86°F)

Mechanism of action:

Safinamide works through dopaminergic and non-dopaminergic mechanisms of action. Safinamide is a highly selective and reversible MAO-B inhibitor that causes increased extracellular levels of dopamine in the striatum. Safinamide is associated with state-dependent inhibition of voltage-gated sodium (Na+) channels and modulation of stimulation of glutamate release. The extent to which non-dopaminergic effects contribute to the overall effect has not been determined.

Safety and efficacy:

Two double-blind, placebo-controlled, multi-country, 24-week studies (Study 1 and Study 2) Performed in PD patients who develop "OFF" status while receiving carbidopa/levodopa and other PD drugs (such as dopamine agonists, COMT inhibitors, anticholinergic drugs, and/or amantadine).

In Study 1, patients were randomized to receive safinamide 50 mg once daily or safinamide 100 mg once daily or placebo. The trial results showed that the three groups of patients (placebo VS (Safinamide 50 mg vs. Safinamide 100 mg), the change in mean hours from baseline to treatment period in the "ON" state was -- VS 0.5 VS 0.53. In the "OFF" state, the change in average hours from baseline to treatment period for the three groups of patients (placebo vs. safinamide 50 mg vs. safinamide 100 mg) was - VS -0.55 VS -0.57, change from baseline in UPDRS motor subscale score - VS -1.75 VS -2.48.

In Study 2, patients were randomly divided into two groups. One group of patients received 100 mg of safinamide each time, and the other group of patients received placebo treatment for up to 24 weeks. The results of the trial showed that the two groups of patients (placebo VS For safinamide 100 mg), the change in mean hours from baseline to on-treatment in the "ON" state was -- VS 0.99. In the “OFF” state, three groups of patients (placebo VS Safinamide 100 mg), the change from baseline to mean hours during treatment was - VS -1.06, and the change from baseline in the UPDRS motor subscale score was - VS -1.70.