Riluzole is available by the brand name of Rilutek (marketed by Sanofi Aventis), among others. The exact mechanism of the drug is not known.

Riluzole (Rilutek - Sanofi) Uses:

• Amyotrophic lateral sclerosis:

  • It is used in the treatment of patients with amyotrophic lateral sclerosis (ALS).
  • Riluzole may extend survival and/or the time to tracheostomy

Riluzole (Rilutek) Dose in Adults

Riluzole (Rilutek) Dose in the treatment of Amyotrophic lateral sclerosis (ALS):

• 50 mg orally two times a day.

Riluzole (Rilutek) Dose in Children

Not applicable

Pregnancy Risk Category: D

• Negative events were observed in animal reproduction studies.

Use of iluzole while breastfeeding

• It is unknown if the drug will be excreted into breastmilk.
• Breastfeeding women should not be exposed to the drug.

Riluzole dose in Renal disease:

The manufacturer has not recommended any adjustments in the dose in patients with renal disease.

Riluzole dose in liver disease:

• Although the manufacturer has not made any adjustments to the dosage, you should still use it with caution.
• Patients with higher than five times the normal hepatic enzyme levels at baseline should avoid it.
• If hepatic dysfunction develops during treatment, the treatment must be stopped immediately.

Common Side Effects of Riluzole (Rilutek):

• Gastrointestinal:

  • Nausea

• Neuromuscular & skeletal:

  • Weakness

Less Common Side Effects of Riluzole:

• Cardiovascular:

  • Hypertension
  • Peripheral Edema
  • Tachycardia

• Central Nervous System:

  • Dizziness
  • Drowsiness
  • Vertigo
  • Malaise

• Dermatologic:

  • Pruritus
  • Eczema
  • Exfoliative Dermatitis

• Gastrointestinal:

  • Abdominal Pain
  • Vomiting
  • Flatulence
  • Oral Paresthesia
  • Dental Caries
  • Oral Candidiasis
  • Stomatitis

• Genitourinary:

  • Urinary Tract Infection
  • Dysuria

• Hepatic:

  • Increased Liver Enzymes

• Neuromuscular & Skeletal:

  • Arthralgia
  • Tremor

• Respiratory:

  • Decreased Lung Function
  • Cough

Contraindications to Riluzole (Rilutek):

• Allergy reactions to riluzole and any component of this formulation
• Liver disease and serum transaminases more than 3x the ULN at baseline
• Pregnancy
• Breastfeeding

Warnings and precautions

• Depression in the CNS:

  • It can cause CNS depression, manifested as somnolence or drowsiness.
  • The drug should not be used on patients who are using heavy machinery or have mental alertness.

• Hepatic effects

  • Hepatotoxicity can occur and may prove fatal.
  • During the initial three months of therapy, liver enzymes can be deranged.
  • Patients with liver enzymes greater than 5x the normal upper limit must stop taking the medication.
  • For the first three months, it is important to monitor liver enzymes monthly and then every other month thereafter.
  • If hepatic dysfunction develops, the treatment must be stopped immediately.

• Neutropenia

  • During the first two months of therapy, there may be severe neutropenia (less than 500/mm3).
  • If a patient has a fever or any other symptoms of infection, he/she should be evaluated and monitored regularly.

• Pulmonary disorders

  • ILD (interstitial pulmonary disease) and HSP (hypersensitivity pneumonia) have been reported. 
  • If ILD is suspected, treatment should be stopped immediately.

• Hepatic impairment

  • Patients with liver disease should be cautious.

Riluzole: Drug Interaction

Monitor:

• Liver enzymes before and during the treatment.
• Clinical features of liver injury for the first three months and periodically thereafter.

How to administer Riluzole (Rilutek)?

• Orally, it is best to administer it. 
• It should be taken orally at the same time as a meal, either one hour before or after it.
• Before the suspension is administered, it should be shaken vigorously for at least 30 seconds.

Mechanism of action of Riluzole (Rilutek):

• It is unknown what the drug does. 
• It inhibits excitatory neurotransmitters like glutamate and inactivates voltage-gated sodium channels.
• Interference with intracellular events that occur after the binding of excitatory neurons is also possible.

Absorption:

• Suspension High-fat meals reduce absorption (AUC drops by 9%, peak blood levels by 55%).
• Tablets High-fat meals reduce the absorption of tablets (the AUC is decreased by 20% and peak blood levels are reduced by 45%).

Plasma protein binding96% of the protein is bound to proteins, most notably to albumin and lipoproteins. Time to get there

Peak serum concentration It takes 0.8 hours to suspend.

MetabolismCYP1A2 & UGT-HP4 are the methods by which it is metabolized in the liver

Bioavailability After oral administration: Absolute: 60%

Eliminating half-life: 12 hours

Excretion: Urine (90%, 2% as an unchanged drug) and feces (5%).

International Brands of Riluzole:

• Rilutek
• Tiglutik
• APO-Riluzole
• MYLAN-Riluzole;
• Borizol
• Laidec
• Rilutan
• Rilutek
• Sclefic
• Teglutik
• Xie Yi Li

Riluzole Brand Names in Pakistan:

No Brands Available in Pakistan.