Kytril

Granisetron
Clinical data


Trade names	Kytril, Sancuso, others
AHFS/Drugs.com	Monograph
MedlinePlus	a601211
Pregnancy category	AU: B1
Routes of administration	by mouth, intravenous, transdermal
ATC code	A04AA02 (WHO)
Legal status
Legal status	AU: S4 (Prescription only) UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Bioavailability	60%
Protein binding	65%
Metabolism	Hepatic
Biological half-life	3–14 hours
Excretion	Renal 11–12%, faecal 38%
Identifiers
IUPAC name 1-Methyl-N-((1R,3r,5S)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl)-1H-indazole-3-carboxamide
CAS Number	109889-09-0^Y
PubChem (CID)	3510
IUPHAR/BPS	2300 [³H]granisetron: 2292
DrugBank	DB00889^Y
ChemSpider	10482033^Y
UNII	WZG3J2MCOL^Y
KEGG	D04370^Y
ChEBI	CHEBI:5537^N
ChEMBL	CHEMBL519643^N
ECHA InfoCard	100.212.327
Chemical and physical data
Formula	C₁₈H₂₄N₄O
Molar mass	312.41 g/mol
3D model (Jmol)	Interactive image
SMILES CN4[C@@H]1CCC[C@H]4C[C@H](C1)NC(=O)c3nn(C)c2ccccc23
InChI InChI=1S/C18H24N4O/c1-21-13-6-5-7-14(21)11-12(10-13)19-18(23)17-15-8-3-4-9-16(15)22(2)20-17/h3-4,8-9,12-14H,5-7,10-11H2,1-2H3,(H,19,23)/t12-,13+,14-^Y Key:MFWNKCLOYSRHCJ-BTTYYORXSA-N^Y
^NY (what is this?)

Granisetron is a serotonin 5-HT₃ receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much effect on vomiting due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors.

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 3M Drug Delivery Systems Division in St. Paul, MN, for ProStrakan, Inc., a pharmaceutical company headquartered in Bedminster, NJ, with global headquarters in Scotland.

Granisetron is metabolized slowly by the liver, giving it a longer than average half-life. 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.

It may be used for chemotherapy-induced nausea and vomiting and appears to work about the same as ondansetron. The most common side-effects of chemotherapy treatment are nausea, vomiting and diarrhea. This is one type of drug that a doctor can prescribe to prevent, lessen, or relieve discomfort.

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