Pays: États-Unis
Langue: anglais
Source: NLM (National Library of Medicine)
DOLASETRON MESYLATE (UNII: U3C8E5BWKR) (DOLASETRON - UNII:82WI2L7Q6E)
Validus Pharmaceuticals LLC
DOLASETRON MESYLATE
DOLASETRON MESYLATE 50 mg
ORAL
PRESCRIPTION DRUG
ANZEMET Tablets are indicated for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy, including initial and repeat courses in adults and children 2 years and older. ANZEMET Tablets are contraindicated in patients known to have hypersensitivity to the drug.
Store at 68° to 77°F (20° to 25°C) [See USP Controlled Room Temperature]. Protect from light.
New Drug Application
ANZEMET- DOLASETRON MESYLATE TABLET, FILM COATED VALIDUS PHARMACEUTICALS LLC ---------- ANZEMET ANZEMET TABLETS (DOLASETRON MESYLATE, USP) RX ONLY DESCRIPTION ANZEMET (dolasetron mesylate, USP) is an antinauseant and antiemetic agent. Chemically, dolasetron mesylate is (2α,6α,8α,9aß)-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. Each ANZEMET Tablet for oral administration contains dolasetron mesylate (as the monohydrate) and also contains the inactive ingredients: croscarmellose sodium, hypromellose, lactose, magnesium stearate, polyethylene glycol, polysorbate 80, pregelatinized starch, synthetic red iron oxide, and titanium dioxide. 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. It is thought that chemotherapeutic agents produce nausea and vomiting by releasing serotonin from the enterochromaffin cells of the small intestine, and that the released serotonin then activates 5-HT receptors located on vagal efferents to initiate the vomiting reflex. ® 3 19 20 2 3 3 3 2 3 3 3 In healthy volunteers (N=64), dolasetron mesylate in single intravenous doses up to 5 mg/kg Lire le document complet