Riluzole

• ALS (Amyotrophic Lateral Sclerosis) Symptoms, Causes, Life Expectancy

Riluzole is a prescription medication used to slow the progress of Lou Gehrig's disease, known medically as amyotrophic lateral sclerosis (ALS). It is a disease of the central nervous system that affects the ability of a person to move certain muscles. Riluzole is not a cure, but may delay the need for a breathing tube (tracheostomy).

Riluzole belongs to a group of drugs called NMDA receptor antagonists. It works by decreasing glutamate, a natural substance in the body that can damage nerve cells. 

This medication comes in tablet form. It is usually taken twice a day, every 12 hours, on an empty stomach.

Common side effects of riluzole are weakness, nausea, and headache.

Riluzole is a prescription medication used to slow the progress of amyotrophic lateral sclerosis (ALS or Lou Gehrig's disease).

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• amitriptyline (Elavil)
• caffeine-containing products
• ciprofloxacin (Cipro)
• ofloxacin (Floxin)
• omeprazole (Prilosec)
• rifampin (Rifadin)
• theophylline (Theo-Dur)
• vitamins

This is not a complete list of riluzole drug interactions. Ask your doctor or pharmacist for more information.

Avoid coffee, tea, cola, or other products that contain caffeine. Caffeine may cause too much riluzole to build up in your body.

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Stop using riluzole and call your doctor at once if you have:

• sudden chest pain or discomfort, wheezing, dry cough or hack, feeling short of breath;

• cough with mucus, stabbing chest pain;

• low white blood cells--fever, swollen gums, painful mouth sores, pain when swallowing, cold or flu symptoms; or

• liver problems--nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).

Common side effects may include:

• dizziness, spinning sensation;

• weakness, drowsiness;

• stomach pain, nausea, vomiting, loss of appetite;

• diarrhea; or

• numbness or tingling around your mouth.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

An antiglutamate agent that acts in the CNS;1 2 3 4 5 6 7 10 11 12 13 a synthetic aryl-substituted benzothiazolamine.1 2 3 4 5 6 7 8 9

Appears to be metabolized principally by CYP1A2; pharmacokinetic interactions with substrates of CYP1A2 are likely.8 CYP2D6, 2C19, 3A4, and 2E1 not significantly involved in metabolism.a

Not known whether riluzole has potential for enzyme induction in humans.8

Protein-bound Drugs

Potential pharmacokinetic interactions (displacement of riluzole or other protein-bound drugs).8

Drugs Affecting Hepatic Microsomal Enzymes

Inhibitors of CYP1A2: potential pharmacokinetic interaction (decreased rate of riluzole elimination).8

Inducers of CYP1A2: potential pharmacokinetic interaction (increased rate of riluzole elimination).8

Specific Drugs and Food

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

• Take on an empty stomach. Take 1 hour before or 2 hours after meals.
• Take riluzole at the same time of day.
• To gain the most benefit, do not miss doses.
• Keep taking this medicine 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?

• Take a missed dose as soon as you think about it, on an empty stomach.
• If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

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 or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Signs of infection like fever, chills, very bad sore throat, ear or sinus pain, cough, more sputum or change in color of sputum, pain with passing urine, mouth sores, or wound that will not heal.
• Signs of high blood pressure like very bad headache or dizziness, passing out, or change in eyesight.
• A fast heartbeat.
• Swelling in the arms or legs.
• Lung problems have happened with riluzole. Call your doctor right away if you have lung or breathing problems like trouble breathing, shortness of breath, or a cough that is new or worse.
• Very bad and sometimes deadly liver problems have happened with this medicine. Call your doctor right away if you have signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.

• If your symptoms or health problems do not get better or if they become worse, call your doctor.
• Do not share your drugs with others and do not take anyone else's drugs.
• Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
• Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
• Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about riluzole, please talk with your doctor, nurse, pharmacist, or other health care provider.
• 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.

This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about riluzole. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using riluzole.

Review Date: October 4, 2017

Riluzole is a member of the benzothiazole class. The chemical designation for Riluzole is 2-amino-6-(trifluoromethoxy) benzothiazole. Its molecular formula is C8H5F3N2OS, and its molecular weight is 234.2. The chemical structure is:

Riluzole is a white to slightly yellow powder that is very soluble in dimethylformamide, dimethylsulfoxide, and methanol; freely soluble in dichloromethane; sparingly soluble in 0.1 N HCl; and very slightly soluble in water and in 0.1 N NaOH.

Each film-coated tablet for oral use contains 50 mg of Riluzole, USP and the following inactive ingredients: anhydrous dibasic calcium phosphate, colloidal silicon dioxide, croscarmellose sodium, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol 400, povidone, talc and titanium dioxide.

NDC 62756-538-83
Riluzole Tablets, USP
50 mg
Rx only
30 TABLETS
SUN PHARMA

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Rilutek: 50 mg

Generic: 50 mg

Smoking: Clearance was 20% greater in smokers compared to nonsmokers.

50 mg orally every 12 hours.

No increased benefit can be expected from higher daily doses, but adverse events are increased.

Riluzole tablets should be taken at least an hour before, or two hours after, a meal to avoid a food-related decrease in bioavailability.

The manufacturer states that riluzole therapy should not be started in patients presenting with elevated baseline liver function tests (i.e. alanine aminotransferase, aspartate aminotransferase, gamma-glutamate transferase and/or bilirubin).

Riluzole is extensively metabolized in the liver. Riluzole should be prescribed cautiously to patients with a current or past history of liver disease. Clinical trials that have been published excluded patients with liver disease, hence there is no information for dosage adjustments in these patients.

If a patient is currently taking riluzole and develops ALT values less than 5 times the upper limit of normal, therapy may be continued with caution. There is no clinical experience with patients whose ALT has exceeded 5 times the upper limit of normal. The risk-to-benefit ratio of continued riluzole therapy should be considered by the clinician, patient and/or caregiver(s). If riluzole therapy is to continue, the manufacturer recommends weekly monitoring of complete liver function. Therapy should be discontinued if the ALT rises above 10 times the upper limit of normal.

Rechallenge in patients who have previously discontinued riluzole due to elevations of ALT has not been done.