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Riluzole
Systematic (IUPAC) name
6-(trifluoromethoxy)benzothiazol-2-amine
Identifiers
CAS number 1744-22-5
ATC code N07XX02
PubChem 5070
DrugBank APRD00145
Chemical data
Formula C8H5F3N2OS 
Mol. mass 234. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug ATC code N07 is a section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Fluorine, fluorum meaning "to flow" is the Chemical element with the symbol F and Atomic number 9 Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the Sulfur or sulphur (ˈsʌlfɚ see spelling below) is the Chemical element that has the Atomic number 16 The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 199 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes  ?

Riluzole is a drug used to treat amyotrophic lateral sclerosis. In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction In Pharmacology and Toxicology, a route Medication, also referred to as medicine, can be loosely defined as any substance intended for use in the diagnosis cure mitigation treatment or prevention of disease Amyotrophic Lateral Sclerosis ( ALS, sometimes called Maladie de Charcot, or in the United States Lou Gehrig's Disease) is a progressive It delays the onset of ventilator-dependence or tracheostomy in selected patients and may increase survival by approximately two months. Tracheotomy and tracheostomy are Surgical procedures on the neck to open a direct airway through an incision in the trachea (the windpipe A patient is any person who receives medical attention care or treatment.

It is marketed by Aventis Pharmaceuticals Inc with the brand name Rilutek. Aventis was a pharmaceutical and lab assay testing company It was formed in 1999 when Rhône-Poulenc S

Contents

Mechanism of action

Riluzole has several actions:

Riluzole preferentially blocks TTX-S sodium channels, which are associated with damaged neurons (Song et al 1997). Sodium (ˈsoʊdiəm is an element which has the symbol Na( Latin natrium, from Arabic natrun) atomic number 11 atomic mass 22 Ion channels are pore-forming Proteins that help establish and control the small Voltage Gradient across the Plasma membrane of all living Calcium (ˈkælsiəm is the Chemical element with the symbol Ca and Atomic number 20 NMDA receptor antagonists are a class of Anesthetics that work to antagonize, or inhibit the action of the N-methyl d-aspartate receptor ( NMDAR Glutamate transporters, also known as VGLUT, are Neurotransmitter transporters that exist in the membranes of Neurons and Glial cells Neurons (ˈnjuːɹɒn also known as neurones and nerve cells) are responsive cells in the Nervous system that process and transmit information This reduces influx of calcium ions and indirectly prevents stimulation of glutamate receptors. An ion is an Atom or Molecule which has lost or gained one or more Valence electrons giving it a positive or negative electrical charge Together with direct glutamate receptor blockade, the effect of the neurotransmitter glutamate on motor neurons is greatly reduced. See Chemical synapse for an introduction to concepts and terminology used in this article Glutamic acid (abbreviated as Glu or E) is one of the 20 Alpha Amino acids It is not among the human Essential amino acids Its

However, the action of Riluzole on Glutamate receptors have been controvertial as no binding of the molecule has been shown on any known receptor (Wokke 1996). In addition as its antiglutamate action is still detectable in the presence of sodium channel blockers, it is also incertain wether it acts via this way. Rather, its potent glutamate uptake activator activity seems to mediate many of its effects (Azbill et al 2000; Dunlop et al 2003).

Studies of efficacy

A Cochrane Library review states a 9% gain in the probability of surviving one year. The Cochrane Library is a collection of databases in medicine and other healthcare specialties provided by the Cochrane Collaboration and other organisations In secondary analyses of survival at separate time points, there was a significant survival advantage with riluzole 100 mg at six, nine, 12 and 15 months, but not at three or 18 months (Miller RG et al 2005). There was a small beneficial effect on both bulbar and limb function, but not on muscle strength. The corticobulbar (or corticonuclear) tract is a White matter pathway connecting the Cerebral cortex to the Brainstem (the term "bulbar" Muscle (from Latin musculus, diminutive of mus "mouse" is contractile tissue of the body and is derived from the There were no data on quality of life, but patients treated with riluzole remained in a more moderately affected health state significantly longer than placebo-treated patients. Quality of life is the degree of well-being felt by an individual or group of people

Clinical use

While riluzole has been proven to slow down ALS, patients do not report any subjective improvement. Approximately 10% of patients experience side effects such as nausea and fatigue which lead them to discontinue treatment. Nausea ( Latin: Nausea, Greek:, " Sea-sickness " also called wamble) is the sensation of unease and discomfort Safety monitoring includes regular liver function tests and people with liver disease such as hepatitis should be monitored especially carefully. Liver function tests (LFTs or LFs which include liver enzymes, are groups of Clinical biochemistry laboratory blood assays designed to give information about the Hepatitis (plural hepatitides) implies injury to the Liver characterized by the presence of Inflammatory cells in the tissue of

In the UK riluzole has been available through the NHS since 1997 at a standard dosage of 50mg twice daily. The National Health Service is the name commonly used to refer to the four Publicly-funded healthcare systems of the United Kingdom collectively or individually (although There has been some evidence to show that higher doses might produce more significant improvements in ALS patients but at £5 a tablet it is at risk of being prohibitively expensive given the modest benefit to patients. One study in the Netherlands found that riluzole is metabolised differently by males and females, and its levels in plasma are decreased in patients who smoke cigarettes (van Kan et al 2005). Blood plasma is the Liquid component of Blood, in which the Blood cells are suspended A cigarette ( French "small Cigar " from cigar + -ette) is a product consumed through Smoking and manufactured

A number of recent case studies have also indicated that riluzole may have clinical use in mood and anxiety disorders. It has been shown to have antidepressant properties in the treatment of refractory depression (Zarate et al 2004) and as an anxiolytic in Obsessive-compulsive disorder (Coric et al 2005) and in GAD (Mathew et al 2005). An antidepressant is a Psychiatric medication used for alleviating major depression or Dysthymia ('milder' depression Major depressive disorder, also known as major depression, unipolar depression, unipolar disorder, clinical depression, or simply depression Obsessive-compulsive disorder (OCD is a Chronic Anxiety disorder most commonly characterized by obsessive Distressing Intrusive thoughts Generalized anxiety disorder ( GAD) is an Anxiety disorder that is characterized by excessive uncontrollable and often irrational worry about everyday things that

References

External links

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