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Riluzole: Drug information

Riluzole: Drug information
(For additional information see "Riluzole: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Exservan;
  • Rilutek;
  • Tiglutik [DSC]
Brand Names: Canada
  • APO-Riluzole;
  • MYLAN-Riluzole;
  • Rilutek
Pharmacologic Category
  • Glutamate Inhibitor
Dosing: Adult
Amyotrophic lateral sclerosis

Amyotrophic lateral sclerosis: Oral: 50 mg twice daily.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling; use with caution. Avoid use in patients with baseline hepatic transaminases >5 times ULN; discontinue use if evidence of hepatic impairment occurs during treatment.

Dosing: Adjustment for Toxicity: Adult

Pulmonary toxicity: If interstitial lung disease develops, discontinue riluzole immediately.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%:

Gastrointestinal: Nausea (16%), oral hypoesthesia (oral film: 38%)

Hepatic: Increased serum alanine aminotransferase (>ULN: 50%; >3 x ULN: 8%; >5 x ULN: 2%)

Nervous system: Dizziness (females 11%; males: 4%)

Neuromuscular & skeletal: Asthenia (19%)

1% to 10%:

Cardiovascular: Hypertension (5%), peripheral edema (3%), tachycardia (3%)

Dermatologic: Eczema (2%), pruritus (4%)

Gastrointestinal: Abdominal pain (5%), flatulence (3%), oral paresthesia (2%), vomiting (4%), xerostomia (4%)

Genitourinary: Urinary tract infection (3%)

Nervous system: Drowsiness (2%), insomnia (4%), vertigo (2%)

Neuromuscular & skeletal: Arthralgia (4%)

Respiratory: Decreased lung function (10%), increased cough (3%)

Frequency not defined:

Gastrointestinal: Constipation

Hematologic & oncologic: Severe neutropenia

Hepatic: Hepatic injury, increased serum transaminases

Respiratory: Interstitial pulmonary disease (including hypersensitivity pneumonitis)

Postmarketing:

Gastrointestinal: Pancreatitis

Hepatic: Hepatitis (acute), toxic hepatitis (icteric)

Renal: Renal tubular disease

Contraindications

Hypersensitivity to riluzole or any component of the formulation

Canadian labeling: Additional contraindications (not in US labeling): Hepatic disease or baseline serum transaminases >3 times ULN; pregnancy; breast-feeding

Warnings/Precautions

Concerns related to adverse effects:

• CNS depression: May cause dizziness or somnolence, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery, driving).

• Hepatic effects: May cause drug-induced hepatic injury (including fatality); asymptomatic elevations of hepatic transaminases may also occur. Elevations of transaminases may occur within 3 months of use. Use is not recommended in patients who develop hepatic transaminases >5 times the upper limit of normal. Monitor for hepatic injury; discontinue use if evidence of hepatic dysfunction occurs (eg, elevated bilirubin).

• Neutropenia: Severe neutropenia has been reported (ANC <500/mm3) within the first 2 months of therapy. Evaluate patients with febrile illnesses.

• Pulmonary disorders: Interstitial lung disease (ILD), including hypersensitivity pneumonitis, has occurred. Discontinue therapy immediately if ILD occurs.

Disease-related concerns:

• Hepatic impairment: Use with caution in patients with hepatic impairment.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Film, Oral:

Exservan: 50 mg (60 ea) [contains fd&c yellow #6 (sunset yellow)]

Suspension, Oral:

Tiglutik: 50 mg/10 mL (300 mL [DSC]) [contains saccharin sodium]

Tablet, Oral:

Rilutek: 50 mg

Generic: 50 mg

Generic Equivalent Available: US

May be product dependent

Pricing: US

Film (Exservan Oral)

50 mg (per each): $62.86

Tablets (Rilutek Oral)

50 mg (per each): $61.54

Tablets (Riluzole Oral)

50 mg (per each): $19.14 - $37.33

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

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

Tablet, Oral:

Rilutek: 50 mg

Generic: 50 mg

Administration: Adult

Oral:

Film: Administer at least 1 hour before or 2 hours after a meal; only one film should be taken at a time. Place film on tongue and allow to dissolve; do not administer with liquids. As film dissolves, swallow saliva in a normal manner but avoid chewing, spitting, or talking. Do not cut or split film.

Suspension, tablet: Administer orally or through a percutaneous endoscopic gastrostomy (PEG) tube (silicone or polyurethane) at least 1 hour before or 2 hours after a meal. Gently shake suspension for ≥30 seconds prior to administration. If administered via PEG tube, flush tube with 30 mL of water before and after administration.

Use: Labeled Indications

Amyotrophic lateral sclerosis: Treatment of patients with amyotrophic lateral sclerosis (ALS); may extend survival and/or time to tracheostomy

Metabolism/Transport Effects

Substrate of CYP1A2 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Allopurinol: May enhance the adverse/toxic effect of Riluzole. Specifically, the risk of hepatotoxicity may be increased. Management: Consider alternatives to allopurinol in patients receiving treatment with riluzole due to the potential for additive hepatotoxicity. Risk D: Consider therapy modification

CYP1A2 Inducers (Moderate): May decrease the serum concentration of Riluzole. Risk C: Monitor therapy

CYP1A2 Inhibitors (Strong): May increase the serum concentration of Riluzole. Risk C: Monitor therapy

Methyldopa: May enhance the adverse/toxic effect of Riluzole. Specifically, the risk of hepatotoxicity may be increased. Management: Consider alternatives to methyldopa in patients receiving treatment with riluzole due to the potential for additive hepatotoxicity. Risk D: Consider therapy modification

SulfaSALAzine: May enhance the adverse/toxic effect of Riluzole. Specifically, the risk of hepatotoxicity may be increased. Management: Consider alternatives to sulfasalazine in patients receiving treatment with riluzole due to the potential for additive hepatotoxicity. Risk D: Consider therapy modification

Tobacco (Smoked): May decrease the serum concentration of Riluzole. Risk C: Monitor therapy

Food Interactions

A high-fat meal decreases absorption of riluzole (decreasing AUC by 20% and peak blood levels by 45%). Management: Administer at the same time each day, at least 1 hour before or 2 hours after a meal.

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies.

Breastfeeding Considerations

It is not known if riluzole is present in breast milk. According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.

Monitoring Parameters

Serum aminotransferases including ALT (baseline and periodically during therapy); signs and symptoms of hepatic injury (every month for the first 3 months and periodically thereafter).

Mechanism of Action

Mechanism of action is not known. Pharmacologic properties include inhibitory effect on glutamate release, inactivation of voltage-dependent sodium channels; and ability to interfere with intracellular events that follow transmitter binding at excitatory amino acid receptors

Pharmacokinetics (Adult Data Unless Noted)

Absorption:

Suspension: High-fat meal decreases AUC by 9% and peak blood levels by 55%.

Tablets: High-fat meal decreases AUC by 20% and peak blood levels by 45%.

Protein binding, plasma: 96%, primarily to albumin and lipoproteins

Time to peak: Suspension: 0.8 hours

Distribution: Vd: ~3.4 L/kg

Metabolism: Hepatic via CYP1A2 and UGT-HP4

Bioavailability: Oral: Absolute: ~60%

Half-life elimination: 12 hours

Excretion: Urine (90%; 2% as unchanged drug) and feces (5%)

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

Hepatic function impairment: AUC increased by about 1.7- and 3-fold in patients with mild and moderate chronic hepatic insufficiency, respectively. The pharmacokinetics have not been studied in patients with severe hepatic impairment.

Sex: Mean AUC was found to be 45% higher in women compared with men.

Race/ethnicity: Clearance was 50% lower in male Japanese patients than in white patients.

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

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AR) Argentina: Edilosiv | Rilutek | Teglutik;
  • (AT) Austria: Rilutek | Riluzol Easypharm | Riluzol pmcs | Riluzol stada;
  • (AU) Australia: Apo riluzole | Pharmacor riluzole | Rilutek | Riluzole sandoz | Riluzole winthrop | Teglutik;
  • (BE) Belgium: Rilutek | Riluzol actavis | Teglutik;
  • (BG) Bulgaria: Rilutek;
  • (BR) Brazil: Rilutek | Riluzol | Tekzor;
  • (CH) Switzerland: Rilutek;
  • (CL) Chile: Rizuril | Teglutik;
  • (CN) China: Rilutek;
  • (CO) Colombia: Extensik | Rilutek | Riluzol;
  • (CZ) Czech Republic: Rilutek | Riluzol pmcs | Sclefic;
  • (DE) Germany: Glentek | Rilutek | Riluzol 1 A Pharma | Riluzol actavis | Riluzol AL | Riluzol alkem | Riluzol Beta | Riluzol CT | Riluzol Heumann | Riluzol Hexal | Riluzol Hormosan | Riluzol mylan | Riluzol Neuraxpharm | Riluzol Ratiopharm | Riluzol stada | Riluzol sun | Riluzol Zentiva | Teglutik;
  • (DO) Dominican Republic: Rilutek;
  • (EE) Estonia: Rilutek;
  • (EG) Egypt: Rilutek;
  • (ES) Spain: Rilutek | Riluzol actavis | Riluzol combino pharm | Riluzol genfarma | Riluzol mylan | Riluzol normon | Riluzol pmcs | Riluzol sun | Riluzol Teva | Teglutik;
  • (FI) Finland: Rilutek | Teglutik;
  • (FR) France: Rilutek | Riluzole Actavis | Riluzole Biogaran | Riluzole EG | Riluzole mylan | Riluzole pmcs | Riluzole sandoz | Riluzole Teva | Riluzole Zentiva | Teglutik;
  • (GB) United Kingdom: Rilutek | Riluzole Teva | Teglutik;
  • (GR) Greece: Rilutek | Teglutik;
  • (HK) Hong Kong: Apo riluzole | Rilutek;
  • (HR) Croatia: Alsemol;
  • (HU) Hungary: Fanizan | Rilutek | Sclefic;
  • (IE) Ireland: Rilutek | Teglutik;
  • (IL) Israel: Rilutek;
  • (IN) India: Rilutek;
  • (IT) Italy: Rilutek | Riluzolo | Riluzolo Actavis | Riluzolo Sandoz | Riluzolo Sun | Riluzolo teva | Teglutik;
  • (JP) Japan: Rilutek;
  • (KE) Kenya: Rilutek;
  • (KR) Korea, Republic of: Rilutek | Yooritek;
  • (LB) Lebanon: Rilutek;
  • (LT) Lithuania: Rilutek | Riluzole Zentiva;
  • (LU) Luxembourg: Rilutek;
  • (LV) Latvia: Rilutek;
  • (MX) Mexico: Riluzol;
  • (MY) Malaysia: Rilutek;
  • (NL) Netherlands: Glentek | Rilutek | Riluzol | Riluzol actavis | Riluzol cf | Riluzol mylan | Riluzol pch | Riluzol sandoz | Riluzol sun;
  • (NO) Norway: Rilutek | Riluzol | Teglutik;
  • (NZ) New Zealand: Rilutek;
  • (PE) Peru: Rilutek;
  • (PH) Philippines: Rilutek;
  • (PL) Poland: Rilutek | Riluzol pmcs | Sclefic | Zolerilis;
  • (PR) Puerto Rico: Exservan | Rilutek | Tiglutik;
  • (PT) Portugal: Rilutek | Riluzol | Riluzol actavis | Riluzol combino | Riluzol Generis;
  • (PY) Paraguay: Rilutek;
  • (SA) Saudi Arabia: Rilutek;
  • (SE) Sweden: Glentek | Rilutek | Riluzol abacus medicine | Riluzol actavis | Riluzol pmcs | Riluzol stada | Riluzole 2care4 | Riluzole Teva | Teglutik;
  • (SG) Singapore: Rilutek;
  • (SI) Slovenia: Rilutek | Sclefic | Teglutik;
  • (SK) Slovakia: Rilutek | Riluzol pmcs;
  • (TH) Thailand: Rilutek;
  • (TN) Tunisia: Rilutek | Riluzol pmcs | Riluzole mylan;
  • (TR) Turkey: Rilutek;
  • (TW) Taiwan: Laidec | Rilutek | Ritek;
  • (UA) Ukraine: Borizolum | Rilutek;
  • (UY) Uruguay: Rilutek;
  • (VE) Venezuela, Bolivarian Republic of: Rilutek;
  • (ZA) South Africa: Rilutek
  1. Exservan (riluzole) oral film [prescribing information]. Warren, NJ: Aquestive Therapeutics; July 2022.
  2. Rilutek (riluzole) [prescribing information]. Zug, Switzerland: Covis Pharmaceuticals, Inc; July 2016.
  3. Rilutek (riluzole) [product monograph]. Laval, Quebec, Canada: Sanofi-Aventis; May 2010.
  4. Tiglutik (riluzole) [prescribing information]. Berwyn, PA: ITF Pharma Inc; December 2019.
Topic 9865 Version 220.0

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