View source for Granisetron

{{Short description|Serotonin 5-HT3 antiemetic}}
{{Use mdy dates|date=December 2024}}
{{cs1 config |name-list-style=vanc |display-authors=6}}
{{Infobox drug
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 461123553
| IUPAC_name = 1-Methyl-''N''-((1''R'',3''r'',5''S'')-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl)-1''H''-indazole-3-carboxamide
| image = Granisetron structure.svg
| width = 185
| image2 = Granisetron_3D.png
<!--Clinical data-->
| tradename = Kytril, Sancuso, others
| Drugs.com = {{drugs.com|monograph|granisetron-hydrochloride}}
| MedlinePlus = a601211
| pregnancy_category = 
| pregnancy_AU = B1
| licence_EU = yes
| legal_status =
| legal_AU = S4
| legal_US = Rx-only
| legal_EU = Rx-only
| legal_EU_comment = <ref>{{cite web | title=Sancuso EPAR | website=European Medicines Agency (EMA) | date=April 20, 2012 | url=https://www.ema.europa.eu/en/medicines/human/EPAR/sancuso | access-date=December 3, 2024}}</ref>
| legal_UK = POM
| routes_of_administration = [[Oral administration|By mouth]], [[intravenous]], transdermal
<!--Pharmacokinetic data-->
| bioavailability = 60%
| protein_bound = 65%
| metabolism = Hepatic
| elimination_half-life = 3–14 hours
| excretion = Renal 11–12%, faecal 38%
<!--Identifiers-->
| index_label = 
| index2_label =[<sup>3</sup>H]granisetron
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 109889-09-0
| ATC_prefix = A04
| ATC_suffix = AA02
| PubChem = 3510
| IUPHAR_ligand2 = 2292
| IUPHAR_ligand = 2300
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00889
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 10482033
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = WZG3J2MCOL
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D04370
| ChEBI_Ref = {{ebicite|changed|EBI}}
| ChEBI = 5537
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 519643
<!--Chemical data-->
| C=18 | H=24 | N=4 | O=1
| smiles = CN4[C@@H]1CCC[C@H]4C[C@H](C1)NC(=O)c3nn(C)c2ccccc23
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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-
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = MFWNKCLOYSRHCJ-BTTYYORXSA-N
}}

'''Granisetron''' is a [[serotonin]] [[5-HT3 antagonist|5-HT<sub>3</sub> receptor antagonist]] used as an [[antiemetic]] to treat [[nausea]] and vomiting following [[chemotherapy]] and radiotherapy. 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 receptor]]s.

Granisetron was developed by chemists working at the British drug company [[Beecham (pharmaceutical company)|Beecham]] {{circa|1985}} and is available as a generic. It is produced by [[Hoffmann-La Roche|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 [[Food and Drug Administration|FDA]].

A granisetron [[transdermal patch]] with the trade name Sancuso was approved by the US FDA on September 12, 2008.<ref>{{cite web | publisher = PRNewswire | url = https://www.drugs.com/newdrugs/fda-approves-sancuso-first-only-patch-preventing-nausea-vomiting-cancer-patients-undergoing-1119.html | title = FDA Approves Sancuso, the First and Only Patch for Preventing Nausea and Vomiting in Cancer Patients Undergoing Chemotherapy | date = September 12, 2008}}</ref> Sancuso is manufactured by 3M Drug Delivery Systems for Kyowa Kirin, Inc.

It was patented in 1985 and approved for medical use in 1991.<ref>{{cite book | vauthors = Fischer J, Ganellin CR |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=448 |url=https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA448 |language=en}}</ref> It is on the [[WHO Model List of Essential Medicines|World Health Organization's List of Essential Medicines]].<ref name="WHO22nd">{{cite book | vauthors = ((World Health Organization)) | title = World Health Organization model list of essential medicines: 22nd list (2021) | year = 2021 | hdl = 10665/345533 | author-link = World Health Organization | publisher = World Health Organization | location = Geneva | id = WHO/MHP/HPS/EML/2021.02 | hdl-access=free }}</ref>

==Medical uses==

===Chemotherapy===
It may be used for [[chemotherapy]]-induced nausea and vomiting and appears to work about the same as [[ondansetron]].<ref>{{cite journal | vauthors = Billio A, Morello E, Clarke MJ | veditors = Billio A | title = Serotonin receptor ntagonists for highly emetogenic chemotherapy in adults | journal = The Cochrane Database of Systematic Reviews | issue = 1 | pages = CD006272 | date = January 2010 | pmid = 20091591 | doi = 10.1002/14651858.CD006272.pub2 | hdl = 11379/614814 | hdl-access = free }} {{Retracted|doi=10.1002/14651858.CD006272.pub3|pmid=24323437|http://retractionwatch.com/2010/09/20/progressive-how-the-cochrane-library-handles-updates-in-progress/ ''Retraction Watch''|intentional=yes}}</ref> 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|date= February 2018}}

===Post operative===
A number of medications including granisetron appear to be effective in controlling [[post-operative nausea and vomiting]] (PONV).<ref name="Ngo2019">{{cite journal | vauthors = Ngo AL, Orhurhu V, Urits I, Delfin EO, Sharma M, Jones MR, Viswanath O, Urman RD | title = Extended release granisetron: Review of pharmacologic considerations and clinical role in the perioperative setting | journal = Saudi Journal of Anaesthesia | volume = 13 | issue = 3 | pages = 231–236 | date = July 2019 | pmid = 31333369 | pmc = 6625288 | doi = 10.4103/sja.SJA_817_18 | doi-access = free }}</ref> It is unclear if it is more or less effective than other agents such as [[droperidol]], [[metoclopramide]], or [[ondansetron]].<ref name=Carl2006>{{cite journal | vauthors = Carlisle JB, Stevenson CA | title = Drugs for preventing postoperative nausea and vomiting | journal = The Cochrane Database of Systematic Reviews | volume = 2006 | issue = 3 | pages = CD004125 | date = July 2006 | pmid = 16856030 | pmc = 6463839 | doi = 10.1002/14651858.CD004125.pub2 | veditors = Carlisle J }} {{Retracted|doi=10.1002/14651858.CD004125.pub3|pmid=28715610|intentional=yes}}</ref>

=== Gastroparesis ===
The granisetron patch (Sancuso) has been studied for use in [[gastroparesis]],<ref name=":0">{{cite journal | vauthors = Midani D, Parkman HP | title = Granisetron Transdermal System for Treatment of Symptoms of Gastroparesis: A Prescription Registry Study | journal = Journal of Neurogastroenterology and Motility | volume = 22 | issue = 4 | pages = 650–655 | date = October 2016 | pmid = 27400689 | pmc = 5056574 | doi = 10.5056/jnm15203 }}</ref> though it is not FDA approved for this indication.<ref>{{cite web |url= https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022198s003lbl.pdf |archive-url= https://web.archive.org/web/20170210215454/http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022198s003lbl.pdf |url-status= dead |archive-date= February 10, 2017 |title=Sancuso Full Prescribing Information |date=September 2015 |website=U.S. Food and Drug Administration |access-date=November 29, 2019}}</ref>

===Other===
* Is a possible therapy for nausea and vomiting due to acute or chronic medical illness or acute [[gastroenteritis]]{{Citation needed|date= February 2018}}
* Treatment of [[cyclic vomiting syndrome]] although there are no formal trials to confirm efficacy.{{Citation needed|date= February 2018}}

==Adverse effects==
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 the [[liver]]'s [[cytochrome P450]] system and it has little effect on the metabolism of other drugs broken down by this system.{{Citation needed|date= February 2018}}

==Extended release==

An extended release injectable version of granisetron, known as Sustol is also available in the United States as of 2016.<ref>Drugs.com [https://www.drugs.com/newdrugs/heron-therapeutics-announces-fda-approval-sustol-granisetron-extended-release-prevention-4420.html Heron Therapeutics Announces FDA Approval of Sustol (granisetron) Extended-Release Injection for the Prevention of Chemotherapy-Induced Nausea and Vomiting]</ref> 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.<ref>FDA.gov [https://web.archive.org/web/20160910031135/http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022445s000lbl.pdf Sustol Prescribing Information].</ref>

== References ==
{{reflist}}

== Further reading ==
{{refbegin}}
* {{cite journal | vauthors = Aapro M | title = Granisetron: an update on its clinical use in the management of nausea and vomiting | journal = The Oncologist | volume = 9 | issue = 6 | pages = 673–86 | year = 2004 | pmid = 15561811 | doi = 10.1634/theoncologist.9-6-673 }}
{{refend}}

{{Antiemetics}}
{{Serotonergics}}
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[[Category:Antiemetics]]
[[Category:5-HT3 antagonists]]
[[Category:Tropanes]]
[[Category:Indazolecarboxamides]]
[[Category:Cancer treatments]]
[[Category:Drugs developed by Hoffmann-La Roche]]
[[Category:Drugs developed by GSK plc]]
[[Category:World Health Organization essential medicines]]