Страна: США
мова: англійська
Джерело: NLM (National Library of Medicine)
dolasetron mesylate (UNII: U3C8E5BWKR) (dolasetron - UNII:82WI2L7Q6E)
sanofi-aventis U.S. LLC
dolasetron mesylate
dolasetron mesylate 12.5 mg in 0.625 mL
PRESCRIPTION DRUG
New Drug Application
ANZEMET- DOLASETRON MESYLATE INJECTION SANOFI-AVENTIS U.S. LLC ---------- ANZEMET INJECTION (DOLASETRON MESYLATE) DESCRIPTION ANZEMET (dolasetron mesylate) is an antinauseant and antiemetic agent. Chemically, dolasetron mesylate is (2α,6α,8α,9aβ)-octahydro-3-oxo-2,6-methano-2_H_-quinolizin-8-yl-1_H_-indole-3-carboxylate monomethanesulfonate, monohydrate. It is a highly specific and selective serotonin subtype 3 (5-HT ) receptor antagonist both in vitro and in vivo. Dolasetron mesylate has the following structural formula: The empirical formula is C H N O • CH SO H • H O, with a molecular weight of 438.50. Approximately 74% of dolasetron mesylate monohydrate is dolasetron base. Dolasetron mesylate monohydrate is a white to off-white powder that is freely soluble in water and propylene glycol, slightly soluble in ethanol, and slightly soluble in normal saline. ANZEMET Injection is a clear, colorless, nonpyrogenic, sterile solution for intravenous administration. Each milliliter of ANZEMET Injection contains 20 mg of dolasetron mesylate and 38.2 mg mannitol, USP, with an acetate buffer in water for injection. The pH of the resulting solution is 3.2 to 3.8. ANZEMET Injection multidose vials contain a clear, colorless, nonpyrogenic, sterile solution for intravenous administration. Each ANZEMET multidose vial contains 25 mL (500 mg) dolasetron mesylate. Each milliliter contains 20 mg dolasetron mesylate, 29 mg mannitol, USP, and 5 mg phenol, USP, with an acetate buffer in water for injection. The pH of the resulting solution is 3.2 to 3.7. CLINICAL PHARMACOLOGY Dolasetron mesylate and its active metabolite, hydrodolasetron (MDL 74,156), are selective serotonin 5-HT receptor antagonists not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. The serotonin 5-HT receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. In healthy volunteers (N=64), dolasetron mesylate in single Прочитайте повний документ