Granisetron

Clinical data
Trade names	Kytril, Sancuso, others
AHFS/Drugs.com	Monograph
MedlinePlus	a601211
License data	EU EMA: by INN
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 EU: Rx-only[1]
Pharmacokinetic data
Bioavailability	60%
Protein binding	65%
Metabolism	Hepatic
Eliminationhalf-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
PubChemCID	3510
IUPHAR/BPS	2300 [3H]granisetron: 2292
DrugBank	DB00889 Y
ChemSpider	10482033 Y
UNII	WZG3J2MCOL
KEGG	D04370 Y
ChEBI	CHEBI:5537 N
ChEMBL	ChEMBL519643 N
CompTox Dashboard(EPA)	DTXSID0023111
ECHA InfoCard	100.212.327
Chemical and physical data
Formula	C18H24N4O
Molar mass	312.417 g·mol−1
3D model (JSmol)	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?)  (verify)

Granisetron is aserotonin5-HT₃ receptor antagonist used as anantiemetic to treatnausea and vomiting followingchemotherapy and radiotherapy. Its main effect is to reduce the activity of thevagus nerve, which is a nerve that activates the vomiting center in themedulla oblongata. It does not have much effect on vomiting due to motion sickness. This drug does not have any effect ondopamine receptors ormuscarinic receptors.

Granisetron was developed by chemists working at the British drug companyBeechamc. 1985 and is available as a generic. It is produced byRoche Laboratories under the trade name Kytril. The drug was approved in the United Kingdom in 1991 and in United States in 1994 by theFDA.

A granisetrontransdermal patch with the trade name Sancuso was approved by the US FDA on September 12, 2008.^[2] Sancuso is manufactured by 3M Drug Delivery Systems for Kyowa Kirin, Inc.

It was patented in 1985 and approved for medical use in 1991.^[3] Granisetron is a therapeutic alternative on theWorld Health Organization's List of Essential Medicines.^[4]

It may be used forchemotherapy-induced nausea and vomiting and appears to work about the same asondansetron.^[5] 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.^{[citation needed]}

A number of medications including granisetron appear to be effective in controllingpost-operative nausea and vomiting (PONV).^[6] It is unclear if it is more or less effective than other agents such asdroperidol,metoclopramide, orondansetron.^[7]

The granisetron patch (Sancuso) has been studied for use ingastroparesis,^[8] though it is not FDA approved for this indication.^[9]

• Is a possible therapy for nausea and vomiting due to acute or chronic medical illness or acutegastroenteritis^{[citation needed]}
• Treatment ofcyclic vomiting syndrome although there are no formal trials to confirm efficacy.^{[citation needed]}

Granisetron is a well-tolerated drug with few side effects. Headache, dizziness, and constipation are the most commonly reported side effects associated with its use. There have been no significant drug interactions reported with this drug's use. It is broken down by theliver'scytochrome P450 system and it has little effect on the metabolism of other drugs broken down by this system.^{[citation needed]}

An extended release injectable version of granisetron, known as Sustol is also available in the United States as of 2016.^[10] The long acting form is used for the treatment of both acute and delayed CINV in moderately emetogenic chemotherapy and anthrocycline and/or cyclophosphamide (AC) highly emetogenic regimens. In its review, the FDA did not grant the broad HEC label to the drug citing the focus on AC regimens, primarily breast-cancer, and lack of data.^[11]

• Antiemetics
• 5-HT3 antagonists
• Tropanes
• Indazolecarboxamides
• Cancer treatments
• Drugs developed by Hoffmann-La Roche
• Drugs developed by GSK plc
• World Health Organization essential medicines

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