riluzole (Rx)

Brand and Other Names:Rilutek, Tiglutik
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 50mg

oral suspension

  • 5mg/mL (300-mL multidose bottle)
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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]) and orally dissolving tablet: 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

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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

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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

            Storage

            Tablets: Store at 20-25°C (68-77°F), excursions permitted to 15-30°C (59-86°F)

            Suspension

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

            FormularyPatient Discounts

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            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.