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
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
Riluzole News (When available)
Fighting back against ALSJan 14, 2006 Jerusalem Post, At present, ALS is totally untreatable; there is only one drug - known commercially as Rilutek and generically as riluzole - that has been approved by the US ...
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