riluzole (Rx)

Brand and Other Names:Rilutek, Tiglutik, more...Exservan
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 50mg

oral suspension

  • 5mg/mL (300-mL multidose bottle)

oral film

  • 50mg

Amyotrophic Lateral Sclerosis

50 mg PO q12hr

Also see Administration

Dosage Modifications

Hepatic impairment

  • Mild or moderate (Child-Pugh A or B): Patients had increases in AUC; thus, may be at increased risk of adverse reactions
  • Severe (Child-Pugh C): Unknown
  • Not recommended for patients with baseline serum aminotransferases (AST/ALTs) >5x ULN or evidence of liver dysfunction (eg, elevated bilirubin)

Dosing Considerations

Measure serum AST/ALTs before and during treatment

Huntington Disease (Orphan)

Orphan indication sponsor

  • Rhone-Poulenc Rorer Pharmaceuticals, Inc; 500 Arcola Road, PO Box 5096; Collegeville, PA 19426-0800

Ataxia (Orphan)

Orphan designation for treatment of spinocelebellar ataxia

Sponsor

  • Biohaven Pharmaceutical Holding Company, Ltd; 234 Church Street, Suite 304; New Haven, Connecticut 06511

Amyotrophic Lateral Sclerosis (Orphan)

Oral suspension (Teglutik [brand name]): Orphan designation for amyotrophic lateral sclerosis (ALS)

Sponsor

  • Italfarmaco SpA; 54 Via dei Lavoratori; Cinisello Balsamo, Italy

Safety and efficacy not established

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Interactions

Interaction Checker

and riluzole

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (2)

              • abametapir

                abametapir will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP1A2 substrates. If not feasible, avoid use of abametapir.

              • givosiran

                givosiran will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP1A2 substrates with givosiran. If unavoidable, decrease the CYP1A2 substrate dosage in accordance with approved product labeling.

              Monitor Closely (11)

              • bupivacaine implant

                riluzole, bupivacaine implant. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Local anesthetics may increase the risk of developing methemoglobinemia when concurrently exposed to drugs that also cause methemoglobinemia.

              • cannabidiol

                cannabidiol, riluzole. affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Owing to the potential for both CYP1A2 induction and inhibition with the coadministration of CYP1A2 substrates and cannabidiol, consider reducing dosage adjustment of CYP1A2 substrates as clinically appropriate.

              • ciprofloxacin

                ciprofloxacin will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

              • dichlorphenamide

                dichlorphenamide and riluzole both decrease serum potassium. Use Caution/Monitor.

              • fexinidazole

                fexinidazole will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

              • fluvoxamine

                fluvoxamine will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

              • isoniazid

                isoniazid will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

              • pefloxacin

                pefloxacin will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

              • rucaparib

                rucaparib will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP1A2 substrates, if clinically indicated.

              • stiripentol

                stiripentol, riluzole. affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP1A2 inhibitor and inducer. Monitor CYP1A2 substrates coadministered with stiripentol for increased or decreased effects. CYP1A2 substrates may require dosage adjustment.

              • teriflunomide

                teriflunomide decreases levels of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

              Minor (26)

              • amobarbital

                amobarbital will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • armodafinil

                armodafinil will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • butabarbital

                butabarbital will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • butalbital

                butalbital will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • carbamazepine

                carbamazepine will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • cigarette smoking

                cigarette smoking will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • cimetidine

                cimetidine will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • erythromycin base

                erythromycin base will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • erythromycin ethylsuccinate

                erythromycin ethylsuccinate will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • erythromycin lactobionate

                erythromycin lactobionate will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • erythromycin stearate

                erythromycin stearate will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • food

                food decreases levels of riluzole by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.

              • mexiletine

                mexiletine will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • modafinil

                modafinil will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • omeprazole

                omeprazole will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • peginterferon alfa 2a

                peginterferon alfa 2a will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • pentobarbital

                pentobarbital will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • phenobarbital

                phenobarbital will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • pipemidic acid

                pipemidic acid will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • primidone

                primidone will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • rifampin

                rifampin will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • secobarbital

                secobarbital will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • smoking

                smoking will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • tobacco use

                tobacco use will decrease the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • verapamil

                verapamil will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

              • zileuton

                zileuton will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.

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              Adverse Effects

              >10%

              Oral hypoesthesia (29%)

              Asthenia (19%)

              Nausea (16%)

              1-10%

              Decreased lung function (10%)

              Hypertension (5%)

              Abdominal pain (5%)

              Vomiting (4%)

              Arthralgia (4%)

              Dizziness (4%)

              Dry mouth (4%)

              Insomnia (4%)

              Pruritus (4%)

              Tachycardia (3%)

              Flatulence (3%)

              Increased cough (3%)

              Peripheral edema (3%)

              Urinary tract infection (3%)

              Circumoral paresthesia (2%)

              Somnolence (2%)

              Vertigo (2%)

              Eczema (2%)

              Postmarketing Reports

              Acute hepatitis

              Icteric toxic hepatitis

              Renal tubular impairment

              Pancreatitis

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              Warnings

              Contraindications

              Hypersensitivity to drug or any component of the formulation

              Cautions

              Cases of drug-induced liver injury reported; asymptomatic elevations of hepatic transaminases reported, and recurred in some patients upon rechallenging treatment (see Dosage Modifications)

              Case reports of clinical hepatitis reported

              Interstitial lung disease, including hypersensitivity pneumonitis, occurred; discontinue immediately if interstitial lung disease develops

              Neutropenia reported; advise patients to report any febrile illness

              Drug interactions overview

              • Riluzole is a CYP1A substrate
              • CYP1A2 inhibitors
                • In vitro findings suggest coadministration of riluzole with CYP1A2 inhibitors may increase in riluzole exposure
                • Coadministration with strong or moderate CYP1A2 inhibitors (eg, ciprofloxacin, enoxacin, fluvoxamine, methoxsalen, mexiletine, oral contraceptives, thiabendazole, vemurafenib, zileuton) may increase risk of riluzole-associated adverse reactions
              • CYP1A2 inducers
                • In vitro findings suggest coadministration with CYP1A2 inducers may decrease in riluzole exposure, which may result in decreased efficacy
              • Hepatotoxic drugs
                • Clinical trials in ALS patients excluded patients on concomitant medications which were potentially hepatotoxic (eg, allopurinol, methyldopa, sulfasalazine)
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              Pregnancy & Lactation

              Pregnancy

              There are no studies in pregnant women, and case reports have been inadequate to inform of drug-associated risk

              Unknown if risk of major birth defects and miscarriage in patients with amyotrophic lateral sclerosis

              Animal data

              • In studies in which riluzole was orally administered to pregnant animals, developmental toxicity (decreased embryofetal/offspring viability, growth, and functional development) was observed at clinically relevant doses
              • Based on these results, advise women of possible risks to fetus associated with use of riluzole during pregnancy
              • In rats, oral administration of riluzole resulted in decreased fertility indices and increases in embryo lethality

              Lactation

              Unknown if distributed in human breast milk

              Riluzole or its metabolites have been detected in milk of lactating rat

              Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

              Pregnancy Categories

              A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

              B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

              C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

              D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

              X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

              NA: Information not available.

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              Pharmacology

              Mechanism of Action

              Benzothiazole

              Mechanism of action in patients with ALS is unknown

              Absorption

              Bioavailability: ~60%

              Peak plasma time: 0.8 hr

              Food effects

              • Tablet: Decreases AUC by 20% and peak plasma concentration by 45%
              • Suspension: Decreases AUC by 9% and peak plasma concentration by 55%

              Distribution

              Protein binding: 96% (mainly to albumin and lipoproteins)

              Metabolism

              Metabolized by oxidation via CYP1A2

              Direct and sequential glucuronidation: UGT-HP4

              Metabolites: 6 major metabolites, some active

              Elimination

              Half-life: 12 hr

              Accumulation: ~ 2-fold

              Excretion: Feces (5%); urine (90%)

              Pharmacogenomics

              Patients of Japanese descent are more likely to have higher riluzole concentrations

              In pharmacokinetic analyses, clearance was 50% lower in Japanese males compared with Caucasians, after normalizing for body weight

              Mean AUC ~45% higher in females compared with males

              Clearance in tobacco smokers is 20% greater than nonsmokers

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              Administration

              Oral Administration

              Administer at 1 hr before or 2 hr after a meal

              Suspension: Gently shake bottle at least 30 sec prior to administration

              Oral film

              • Instruct patients and/or caregivers to read the “Instruction for Use” carefully for complete directions on how to properly dose and administer oral films
              • Apply on top of the tongue where it adheres and dissolves
              • Do not cut or split the film
              • Do not administer with liquids
              • As film dissolves, swallow saliva in a normal manner, but refrain from chewing, spitting or talking
              • Take only 1 oral film at a time

              Storage

              Tablets and oral films: Store at 20-25ºC (68-77ºF), excursions permitted to 15-30ºC (59-86ºF)

              Suspension

              • Store at 20-25ºC (68-77ºF), excursions permitted to 15-30ºC (59-86ºF)
              • Protect from bright light, do not freeze
              • Discard after 15 days of initially opening of the bottle
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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              riluzole oral
              -
              50 mg tablet
              riluzole oral
              -
              50 mg tablet
              riluzole oral
              -
              50 mg tablet
              riluzole oral
              -
              50 mg tablet
              Rilutek oral
              -
              50 mg tablet

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              Patient Education
              riluzole oral

              RILUZOLE FILM - ORAL

              (RIL-ue-zole)

              COMMON BRAND NAME(S): Exservan

              USES: This medication is used to treat a certain type of nerve disease called amyotrophic lateral sclerosis (ALS, also commonly called Lou Gehrig's disease). Riluzole helps to slow down the worsening of this disease and prolong survival.

              HOW TO USE: Read the Instructions for Use if available from your pharmacist before you start taking riluzole and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth on an empty stomach (at least 1 hour before or 2 hours after a meal) as directed by your doctor, usually twice daily.With dry hands, open the foil pouch just before use and place the medication on top of the tongue and let it dissolve. Do not cut the film. Do not chew, spit, talk, or drink any liquids while the medication is dissolving. Swallow saliva normally as the medication is dissolving.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of side effects will increase.Tell your doctor if your condition gets worse.

              SIDE EFFECTS: Dizziness, drowsiness, nausea, vomiting, or numbness/tingling around the mouth may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: fast heartbeat, signs of liver disease (nausea/vomiting that doesn't stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine), signs of infection (such as sore throat that doesn't go away, fever), signs of lung problems (such as shortness of breath, cough).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

              PRECAUTIONS: Before taking riluzole, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease.This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding.

              DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (such as prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.

              OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: mental/mood changes (such as confusion, memory loss), severe drowsiness.

              NOTES: Do not share this medication with others.Lab and/or medical tests (such as liver function tests) should be done before you start taking this medication and while you are taking it. Keep all medical and lab appointments. Consult your doctor for more details.

              MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

              STORAGE: Store at room temperature away from light and moisture. Keep the medication in the pouch until ready to use. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

              Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

              IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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              Formulary

              FormularyPatient Discounts

              Adding plans allows you to compare formulary status to other drugs in the same class.

              To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

              Adding plans allows you to:

              • View the formulary and any restrictions for each plan.
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              • Compare formulary status to other drugs in the same class.
              • Access your plan list on any device – mobile or desktop.

              The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

              Tier Description
              1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
              2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
              3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
              4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              NC NOT COVERED – Drugs that are not covered by the plan.
              Code Definition
              PA Prior Authorization
              Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
              QL Quantity Limits
              Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
              ST Step Therapy
              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
              OR Other Restrictions
              Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.