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

Risk Factor C (Monitor therapy)
CYP1A2 Inducers (Moderate)	May decrease the serum concentration of Riluzole.
Tobacco (Smoked)	May decrease the serum concentration of Riluzole. Hair Removing Hard Beans Wax Painless Beauty Wax Beans For All Skins Wax Beans For Face Body Legs

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.