Safinamide

What is safinamide used for?

Safinamide is a prescription medicine that is used to treat Parkinson’s disease.

Before taking safinamide, tell your doctor:

• If you are allergic to safinamide; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
• If you have liver disease.
• If you have taken certain drugs for depression or Parkinson’s disease in the last 14 days. This includes isocarboxazid, phenelzine, tranylcypromine, selegiline, or rasagiline. Very high blood pressure may happen.
• If you are taking any of these drugs: Linezolid or methylene blue.
• If you take any drugs (prescription or OTC, natural products, vitamins) that must not be taken with safinamide, like certain drugs that are used for cough or cold, depression or other mood problems, or pain. There are many drugs that must not be taken with safinamide.

This is not a list of all drugs or health problems that interact with safinamide.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take safinamide with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

Description

XADAGO tablets contain safinamide, which is a MAO-B inhibitor, as the mesylate salt. Safinamide mesylate is (S)-2- [[4-[(3-fluorophenyl) methoxy]phenyl]methyl]aminopropanamide methanesulfonate (1:1) and its structural formula is below.

The molecular formula of safinamide mesylate is C 17H 19FN 2O 2∙CH 4O 3S and its molecular weight is 398.45.

Safinamide mesylate is a white to off-white crystalline powder. Safinamide mesylate is freely soluble in water, methanol and dimethyl sulfoxide. Safinamide mesylate 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.

XADAGO is available as 50 mg and 100 mg film-coated tablets for oral administration. Each XADAGO tablet contains 65.88 mg or 131.76 mg of safinamide mesylate, equivalent to 50 mg or 100 mg, respectively, of safinamide free base. The tablets also contain the following inactive ingredients: colloidal silicon dioxide, crospovidone, hypromellose, iron oxide (red), magnesium stearate, microcrystalline cellulose, polyethylene glycol 6000, potassium aluminum silicate, and titanium dioxide.

Mechanism of Action

The precise mechanism by which XADAGO exerts its therapeutic effects in PD is unknown. XADAGO 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.

What are some things I need to know or do while I take safinamide?

• Tell all of your health care providers that you take safinamide. This includes your doctors, nurses, pharmacists, and dentists.
• Avoid driving and doing other tasks or actions that call for you to be alert until you see how safinamide affects you.
• High blood pressure has happened with safinamide. Have your blood pressure checked as you have been told by your doctor.
• Some foods and drinks, like cheese and red wine, may cause sudden, severe high blood pressure when you are taking safinamide. This effect can be deadly. Talk with your doctor about your risk for this effect. Get a list of foods and drinks to avoid. Avoid these foods and drinks for as long as your doctor has told you after safinamide is stopped.
• Some people have fallen asleep during activities like driving, eating, or talking. Some people did not feel sleepy and felt alert right before falling asleep. This has happened up to 1 year after safinamide was started. If you fall asleep during activities, do not drive or do other tasks or actions that call for you to be alert while you take safinamide. Call your doctor right away if this happens or you feel very sleepy.
• Do not stop taking safinamide all of a sudden without calling your doctor. You may have a greater risk of side effects. If you need to stop safinamide, you will want to slowly stop it as ordered by your doctor.
• Talk with your doctor before you drink alcohol or use other drugs and natural products that slow your actions.
• Tell your doctor if you are pregnant, plan on getting pregnant, or are breast-feeding. You will need to talk about the benefits and risks to you and the baby.

How is safinamide best taken?

Use safinamide as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• Take safinamide at the same time of day.
• Take with or without food.
• Keep taking safinamide as you have been told by your doctor or other health care provider, even if you feel well.

What do I do if I miss a dose?

• Skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

What are the side effects of safinamide that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Signs of high blood pressure like very bad headache or dizziness, passing out, or change in eyesight.
• Trouble controlling body movements that is new or worse.
• Hallucinations (seeing or hearing things that are not there).
• Change in how you act.
• Feeling confused.
• Feeling agitated.
• Strong urges that are hard to control (such as eating, gambling, sex, or spending money).
• Change in eyesight.
• Falls.
• A severe and sometimes deadly problem called serotonin syndrome may happen if you take safinamide with certain other drugs. Call your doctor right away if you have agitation; change in balance; confusion; hallucinations; fever; fast or abnormal heartbeat; flushing; muscle twitching or stiffness; seizures; shivering or shaking; sweating a lot; severe diarrhea, upset stomach, or throwing up; or severe headache.

What are some other side effects of safinamide?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Upset stomach.
• Trouble sleeping.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out safinamide?

• Store at room temperature in a dry place. Do not store in a bathroom.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.

Label

PRINCIPAL DISPLAY PANEL – 50 MG TABLET BOTTLE CARTON

• Rx only
  NDC 27505- 110-30
• Xadago ®
  (safinamide) tablets
• 50 mg
• Keep out of reach of children.
• 30 tablets
• US WorldMeds™

PRINCIPAL DISPLAY PANEL – 100 MG TABLET BOTTLE CARTON

• Rx only
  NDC 27505- 111-30
• Xadago ®
  (safinamide) tablets
• 100 mg
• Keep out of reach of children.
• 30 tablets
• US WorldMeds™

SRC: NLM .