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Description of granisetron hydrochloride: granisetron hydrochloride is the hydrochloride salt of an indazole derivative with antiemetic properties. As a selective serotonin receptor antagonist, granisetron competitively blocks the action of serotonin at 5-hydroxytryptamine3 (5-HT3) receptors, resulting in the suppression of chemotherapy- and radiotherapy-induced nausea and vomiting. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). 09/04/2014
According to http://en.wikipedia.org/wiki/Granisetron, Granisetron was developed by chemists working at the British drug company Beecham around 1988 and is available as a generic. It is produced by Roche Laboratories under the trade name Kytril. The drug was approved in the United Kingdom in 1991 and in United States in 1994 by the FDA. A granisetron transdermal patch with the trade name Sancuso was approved by the US FDA on September 12, 2008. Sancuso is manufactured by ProStrakan, Inc., a pharmaceutical company headquartered in Bedminster, NJ, with global headquarters in Scotland. Granisetron breaks down slowly, staying in the body for a long time. One dose usually lasts 4 to 9 hours and is usually administered once or twice daily. This drug is removed from the body by the liver and kidneys.
KYTRIL Tablets and KYTRIL Oral Solution contain granisetron hydrochloride, an antinauseant and antiemetic agent. Chemically it is endo-N-(9-methyl-9-azabicyclo [3.3.1] non-3-yl)-1-methyl-1H-indazole-3-carboxamide hydrochloride with a molecular weight of 348.9 (312.4 free base). Its empirical formula is C18H24N4O•HCl. Granisetron hydrochloride is a white to off-white solid that is readily soluble in water and normal saline at 20°C.
Tablets for Oral Administration: Each white,
triangular, biconvex, film-coated KYTRIL Tablet contains 1.12 mg
granisetron hydrochloride equivalent to granisetron, 1 mg. Inactive
ingredients are: hydroxypropyl methylcellulose, lactose, magnesium
stearate, microcrystalline cellulose, polyethylene glycol,
polysorbate 80, sodium starch glycolate, and titanium dioxide.
Oral Solution: Each 10 mL of clear, orange-colored, orange-flavored KYTRIL Oral Solution contains 2.24 mg of granisetron hydrochloride equivalent to 2 mg granisetron. Inactive ingredients: citric acid anhydrous, FD&C Yellow No. 6, orange flavor, purified water, sodium benzoate, and sorbitol.
Granisetron is a selective 5-hydroxytryptamine3
(5-HT3) receptor antagonist with little or no affinity for other
serotonin receptors, including 5-HT1; 5-HT1A; 5-HT1B/C; 5-HT2; for
alpha1-, alpha2-, or beta-adrenoreceptors; for dopamine-D2; or for
histamine-H1; benzodiazepine; picrotoxin or opioid receptors. Serotonin
receptors of the 5-HT3 type are located peripherally on vagal nerve
terminals and centrally in the chemoreceptor trigger zone of the area
postrema. During chemotherapy that induces vomiting, mucosal
enterochromaffin cells release serotonin, which stimulates 5-HT3
receptors. This evokes vagal afferent discharge, inducing vomiting.
Animal studies demonstrate that, in binding to 5-HT3 receptors,
granisetron blocks serotonin stimulation and subsequent vomiting after
emetogenic stimuli such as cisplatin. In the ferret animal model, a
single granisetron injection prevented vomiting due to high-dose
cisplatin or arrested vomiting within 5 to 30 seconds. In most human
studies, granisetron has had little effect on blood pressure, heart rate
or ECG. No evidence of an effect on plasma prolactin or aldosterone
concentrations has been found in other studies.
1: Wu SJ, Xiong XZ, Lin YX, Cheng NS. Comparison of
the efficacy of ondansetron and granisetron to prevent postoperative
nausea and vomiting after laparoscopic cholecystectomy: a systematic
review and meta-analysis. Surg Laparosc Endosc Percutan Tech. 2013
Feb;23(1):79-87. doi: 10.1097/SLE.0b013e31827549e8. Review. PubMed PMID:
(Keyword; CAS#; MedKoo Cat#)
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