How Riluzole Is A Derivative Of Benzothiazole Essay

2.11.1 Structure: riluzole is a derivative of benzothiazole (Hofmann, 1879), a bicyclic ring compound which comprises a benzene ring fused with five membered ring containing one sulfur and one nitrogen atom. It has the molecular formula C8HÂ ¬F3N2OS with a molecular weight of 234.20. 2.11.2 Properties: Riluzole is white to slight yellow powder soluble in dimethylsulfoxide, dimethylformamide and methanol, freely soluble in dichloromethane, sparingly soluble in 0.1 N HCl and very slightly soluble in water and 0.1 N NaOH. Riluzole is available as a capsule-shaped, white, film-coated tablet for oral administration. Each tablet contains 50 mg of riluzole. It is marketed by Sanofi-Aventis with the brand name Rilutek. 2.11.3 Side-effects or damaging effects Riluzole is a very good neuroprotective drug, but it has some side-effects associated with it that includes nausea, vomiting, anorexia, diarrhea, asthenia, somnolence, vertigo, circumoral paresthesia, abdominal pain and dizziness (Siniscalchi, 1997). Remy et al has reported cases of two patients who have developed acute hepatitis (hepatocellular damage with inflammatory infiltration and microvesicular steatosis without fibrosis) after taking riluzole at the recommended dose (100 mg daily) for 7 and 4 weeks, respectively. In both cases, liver histology showed liver enzymes returned to normal 4 and 8 weeks, respectively, after riluzole withdrawal (Remy, 1999). 2.11.4 Mechanism of actions Riluzole has emerged as a potent