Riluzole: profile and news

A Twitch of Potential Apr 23, 2006
...implicated a genetic mutation in a small subset of MND patients, and the pharmaceutical company Rhone-Poulenc Rorer launched riluzole (Rilutek), the first ... - TIME

Faust Pharmaceuticals announces Phase IIa results for ALS Apr 26, 2006
...to acquire data on FP0011 patient tolerance and safety, and to check whether it was possible to administer FP0011 in combination with riluzole, currently the ... - PharmaLive.com (press release),

Cutting-Edge Research on Repair of Spinal Cord Injuries Presented ... May 1, 2006
...the authors present several promising medications under investigation for protecting and promoting neurologic function, including riluzole, minocycline, and ... - Genetic Engineering News,

More than 160 Medicines to Treat Rare Diseases Approved in Last ... Apr 20, 2006
For instance, after 126 years, a breakthrough treatment—Rilutek® (riluzole)—was approved for treatment of amyotrophic lateral sclerosis, or ALS, in 1995. ... - PharmaLive.com (press release),

Other information

Indication
For the treatment of amyotrophic lateral sclerosis (ALS, Lou Gehrig's Disease)

Pharmacology
Riluzole, a member of the benzothiazole class, is indicated for the treatment of patients with amyotrophic lateral sclerosis (ALS). Riluzole extends survival and/or time to tracheostomy. It is also neuroprotective in various in vivo experimental models of neuronal injury involving excitotoxic mechanisms. The etiology and pathogenesis of amyotrophic lateral sclerosis (ALS) are not known, although a number of hypotheses have been advanced. One hypothesis is that motor neurons, made vulnerable through either genetic predisposition or environmental factors, are injured by glutamate. In some cases of familial ALS the enzyme superoxide dismutase has been found to be defective.

Mechanism Of Action
The mode of action of Riluzole is unknown. Its pharmacological properties include the following, some of which may be related to its effect: 1) an inhibitory effect on glutamate release, 2) inactivation of voltage-dependent sodium channels, and 3) ability to interfere with intracellular events that follow transmitter binding at excitatory amino acid receptors.

Drug Category
Neuroprotective Agents; Anticonvulsants; Anesthetics; Central Nervous System Agents; ATC:N07XX02

Brand Names/Synonyms
Rilutek; Riluzole; Riluzole Hcl

Dosage Forms
TABLET

Absorption
Not Available

Interactions
Interactions for Riluzole:

There have been no clinical studies designed to evaluate the interaction of riluzole with other drugs.

As with all drugs, the potential for interaction by a variety of mechanisms is a possibility.

Hepatotoxic Drugs: The clinical trials in ALS excluded patients on concomitant medications which were potentially hepatotoxic, (e.g., allopurinol, methyldopa, sulfasalazine). Accordingly, there is no information about the safety of administering RILUTEK in conjunction with such medications. If the practitioner chooses to prescribe such a combination, caution should be exercised.

Drugs Highly Bound To Plasma Proteins: Riluzole is highly bound (96%) to plasma proteins, binding mainly to serum albumin and to lipoproteins. The effect of riluzole (up to 5 mcg/mL) on warfarin (5 mcg/mL) binding did not wshow any displacement of warfarin. Conversely, riluzole binding was unaffected by the addition of warfarin, digoxin, imipramine and quinine at high therapeutic concentrations.

Effect of Other Drugs On Riluzole Metabolism: In vitro studies using human liver microsomal preparations suggest that CYP 1A2 is the principal isozyme involved in the initial oxidative metabolism of riluzole and, therefore, potential interactions may occur when riluzole is given concurrently with agents that affect CYP 1A2 activity. Potential inhibitors of CYP 1A2 (e.g., caffeine, pheriacetin, theophylline, amitriptyline, and quinolones) could decrease the rate of riluzole elimination, while inducers of CYP 1A2( e.g., cigarette smoke, charcoal broiled food, rifampicin, and omeprazole) could increase the rate of riluzole elimination.

Effect of Riluzole On the Metabolism of Other Drugs: CYP 1A2 is the principal isoenzyme involved in the initial oxidative metabolism of riluzole; potential interactions may occur when riluzole is given concurrently with other agents which are also metabolized primarily by CYP 1A2 (e.g., theophylline, caffeine and tacrine). Currently, it is not known whether riluzole has any potential for enzyme induction in humans.

Drug Laboratory Test Interactions: None known

Chemical IUPAC Name
6-(trifluoromethoxy)benzothiazol-2-amine

Chemical Formula
C8H5F3N2OS

Half Life
12 hours

Drug Type
Approved Drug

# Accession No
APRD00145

CAS Registry Number
1744-22-5