Safinamide

What is Safinamide?

• It is a MAO-B inhibitor, as the mesylate salt.
• Safinamide mesylate chemical formula: ( S)-2- [[4-[(3-fluorophenyl) methoxy]phenyl]methyl]aminopropanamide methane sulfonate (1:1)
• Molecular formula: C 17H 19FN 2O 2∙CH 4O 3S
• Molecular weight: 398.45.
• It is a white to off-white crystalline powder.
• It is freely soluble in water, methanol and dimethyl sulfoxide.
• It is sparingly soluble in ethanol and is practically insoluble in ethyl acetate.
• In aqueous buffers that span a pH range of 1.2 to 7.5, safinamide mesylate is highly soluble at pH 1.2 and 4.5, but shows low solubility (<0.4 mg/mL) at pH 6.8 and 7.5.

Safinamide

What are the uses of this medicine?

It is indicated as adjunctive treatment to levodopa/carbidopa in patients with Parkinson's disease (PD) experiencing "off" episodes.

How does this medicine work?

Its precise mechanism in Parkinson's disease (PD) is unknown. It is an inhibitor of monoamine oxidase B (MAO-B). Inhibition of MAO-B activity, by blocking the catabolism of dopamine, is thought to result in an increase in dopamine levels and a subsequent increase in dopaminergic activity in the brain.

Who Should Not Use this medicine?

It is contraindicated in patients with:

• Concomitant use of other drugs in the monoamine oxidase inhibitor (MAOI) class or other drugs that are potent inhibitors of monoamine oxidase, including linezolid. The combination may result in increased blood pressure, including hypertensive crisis.
• Concomitant use of opioid drugs (e.g., meperidine and its derivatives, methadone, propoxyphene, or tramadol); serotonin-norepinephrine reuptake inhibitors (SNRIs), tricyclic, tetracyclic, or triazolopyridine antidepressants; cyclobenzaprine; methylphenidate, amphetamine, and their derivatives; or St John's wort. Concomitant use could result in life-threatening serotonin syndrome.
• Concomitant use of dextromethorphan. The combination of MAOIs and dextromethorphan has been reported to cause episodes of psychosis or abnormal behavior.
• A history of a hypersensitivity to safinamide. Reactions have included swelling of the tongue and oral mucosa, and dyspnea.
• Severe hepatic impairment.

What are the brand names and dosage forms of this medicine?

• Brand name: Xadago; NDC codes: 27505-110-14, 27505-110-30, 27505-110-90, 27505-111-14, 27505-111-30, 27505-111-90.
• Dosage form:

1. 50 mg tablets: Orange to copper with metallic gloss, round, biconcave shaped embossed with "50" on one side.
2. 100 mg tablets: Orange to copper with metallic gloss, round, biconcave shaped embossed with "100" on one side.

Is this medicine FDA approved?

It is approved by US FDA on March 21, 2017.

What are the active and inactive ingredients in Safinamide?

• Active ingredient:

1. Safinamide Mesylate

• Inactive ingredients:

1. Microcrystalline Cellulose
2. Crospovidone
3. Magnesium Stearate
4. Silicon Dioxide
5. Hypromellose, Unspecified
6. Polyethylene Glycol 6000
7. Titanium Dioxide
8. Ferric Oxide Red
9. Mica

How should this medicine be used?

• Take XADAGO exactly as your healthcare provider tells you to take it.
• Take XADAGO at the same time each day.
• Take XADAGO with or without food.
• If you miss a dose, take your next dose of XADAGO at the same time the next day.
• Your healthcare provider may need to change the dose of XADAGO until the dose is right for you.
• Do not start or stop taking XADAGO without talking to your healthcare provider first.

What side effects can this medication cause?

• Hypertension
• Serotonin Syndrome
• Falling Asleep During Activities of Daily Living
• Dyskinesia
• Hallucinations / Psychotic Behavior
• Impulse Control / Compulsive Behaviors
• Withdrawal-Emergent Hyperpyrexia and Confusion
• Retinal Pathology

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

Safety and effectiveness in pregnancy have not been established.

Can this medicine be used in children?

Safety and effectiveness in pediatric patients have not been established.

What should I know about storage and disposal of this medication?

Store XADAGO at room temperature, about 68°F to 77°F (20°C to 25°C).

• Dailymed label info on Safinamide
• FDA Safinamide

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