riluzole

Contraindicated in:

Severe hypersensitivity.

Use Cautiously in:

Hepatic impairment;
Japanese patients (may have ↑ risk of adverse reactions);
Female patients (↓ metabolism);
OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypertension, peripheral edema

GI: abdominal pain, nausea, anorexia, diarrhea, dyspepsia, flatulence, HEPATOTOXICITY, ↑liver enzymes, vomiting

Hemat: neutropenia

Metab: weight loss

MS: arthralgia, back pain

Neuro: dizziness, weakness, circumoral paresthesia, headache

Resp: INTERSTITIAL LUNG DISEASE (ILD)

Misc: ANAPHYLAXIS

Interactions ⬆ ⬇

Drug-drug:

Effects may be ↑ by amitriptyline, caffeine, fluoroquinolones, or theophylline.
Effects may be ↓ by cigarette smoke (nicotine), rifampin, or omeprazole.

Drug-Natural Products:

St. John's wort may ↓ levels and effectiveness.

Drug-Food:

Effects may be ↓ by charcoal-broiled foods.
High-fat meals↓ absorption.

Availability ⬆ ⬇

(Generic available)

Oral films (Exservan): 50 mg
Oral suspension (Tiglutik): 50 mg/10 mL
Tablets: 50 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 50 mg every 12 hr.

US Brand Names ⬆ ⬇

Exservan, ~~Rilutek,~~ Tiglutik

Action ⬆ ⬇

Action may be related to:
- Inhibition of glutamate release,
- Inactivation of sodium channels,
- Interference with neurotransmitter binding at receptor sites.

Therapeutic effects:

Extended survival or time to tracheostomy in ALS.

Classifications ⬆ ⬇

Therapeutic Classification: agents for amyotrophic lateral sclerosis

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed (60%) after oral administration.

Distribution: Readily penetrates brain.

Protein Binding: 96%.

Metabolism/Excretion: Highly metabolized by the liver (some metabolites are pharmacologically active); 2% excreted unchanged in urine.

Half-Life: 12 hr (after multiple doses).

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
PO	unknown	unknown	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Instruct patient to take as directed at the same time each day on an empty stomach. Missed doses should be omitted; start again at next scheduled dose. Do not ↑ or double doses. Higher doses do not ↑ effectiveness but do ↑ the incidence of side effects.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially St. John's wort.
May cause drowsiness or dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Advise patient to notify health care professional immediately if signs and symptoms of liver injury (unexplained nausea, vomiting, abdominal pain, fatigue, anorexia, jaundice, dark urine) or interstitial lung disease (dry cough, difficult or labored breathing) occur.
Instruct patient to notify health care professional of any febrile illnesses.
Advise patient to avoid drinking alcohol while taking riluzole.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Indications ⬇

Contraind./Precautions ⬆ ⬇