Riluzole

Glutamate is a major excitatory neurotransmitter in the central nervous system. Theoretically, increased glutamater-gic neurotransmission may lead to excitatory neurotoxicity or excitotoxicity. The only two currently approved neuroprotective agents in the United States, riluzole for ALS and memantine for AD, may act to prevent glutamatergic excitotoxicity. 

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Morrison KE. Therapies in amyotrophic lateral sclerosis - beyond riluzole. Curr Opin Pharmacol 2002 2 302-9. 

Other drugs Acetazolamide, acetosulfone, acetylcysteine, acitretin, allopurinol, aminoglutehimide, benzaflbrate, brompheniramine, calcium dobe-silate, chloropheniramine, chlorpropamide, colchicine, deferiprone, dapsone, flutamide, glibenclamide, hydroxychloroquine, mebhydro-lin, meprobamate, metapyrilene, methazolamide, metochlopramide, prednisone, promethazine, retinoic acid, riluzole, ritodrine, tolbutamide, yohimbine... 

Amyotrophic lateral sclerosis (ALS) is a progressive, usually fatal, neurodegenerative disease caused by the degeneration of motor neurons in the central nervous system. No cure has yet been found for ALS. The U.S. Food and Drug Administration (FDA) has approved riluzole as the first drug treatment for the disease. It delays the onset of ventilator-dependence or tracheostomy in selected patients. A Cochrane review states a 9% gain in the probability of surviving one year (see Miller et ah, 2007). 

In terms of clinical proof of neuroprotective effects in chronic neurodegenerative diseases, so far there are promising clinical results in ATS only with riluzole, and even then, the increase of survival obtained was only modest. The failure of r emacemide in a recent study in Huntington s disease was clearly a big setback. On the other hand, the moderate-affinity NMDA receptor antagonist memantine provides clear symptomatic improvement in dementia in both clinical and preclinical situations, and the precHnical data predict neuroprotective effects, substantiated by numerous animal models. 

Bruno V, Battaglia G, Copani A, et al (2001) Metabotropic glutamate receptor subtypes as targets for neuroprotective drugs. J Cereb Blood FlowMetab 21 1013-1033 Bryson HM, Fulton B, Benfield P (1996) Riluzole—a review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in amyotrophic lateral sclerosis. Drugs 52 549-563... 

Gurney ME, Fleck TJ, Himes CS, Hall ED (1998) Riluzole preserves motor fimction in a transgenic model of familiar amyotrophic lateral sclerosis. Neurology 50 62-67 Haines DR, Gaines SP (1999) N of 1 randomised controlled trials oforal ketamine in patients with chronic pain. Pain 83 283-287... 

Kennel P, Revah F, Bohme GA, et al (2000) Riluzole prolongs survival and delays muscle strength deterioration in mice with progressive motor neuropathy (pmn). J Neurol Sci 180 55-61... 

Wahl F, Renou E, Mary V, Stutzmann JM (1997) Riluzole reduces brain lesions and improves neurological fimction in rats after a traumatic brain injury. Brain Res 756 247-255 WaUstrom E, Diener P, Ljungdahl A, et al (1996) Memantine abrogates nemological deficits, but not CNS inflammation, in lewis rat experimental autoimmime encephalomyelitis. J Neurol Sci 137 89-96... 

Take riluzole at least 1 hr before or 2 hr after a meal and at the same times each day... 

Oral 100 mg tablets 100 mg sustained-release tablets Parenteral 30 mg/mL for IM, IV injection Riluzole (Rilutek)... 

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