|Trade names||Kytril, Sancuso, others|
|by mouth, intravenous, transdermal|
|Elimination half-life||3–14 hours|
|Excretion||Renal 11–12%, faecal 38%|
|Chemical and physical data|
|Molar mass||7002312417000000000♠312.417 g·mol−1|
|3D model (JSmol)|
|NY (what is this?)|
Granisetron is a serotonin 5-HT3 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 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 for ProStrakan.
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 was patented in 1985 and approved for medical use in 1991.
- 1 Medical uses
- 1.1 Chemotherapy
- 1.2 Post operative
- 1.3 Other
- 2 Adverse effects
- 3 Extended release
- 4 References
- 5 Further reading
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.
A number of medications including granisetron appear to be effective in controlling post-operative nausea and vomiting (PONV). It is unclear if it is more or less effective than other agents such as droperidol, metoclopramide, ondansetron or cyclizine.
Its efficacy has also been questioned with a research Dr. Yoshitaka Fujii having 12 published papers on this topic in Canadian Journal of Anesthesia retracted. A further five papers in the same journal on the same drug by Dr Fujii are considered indeterminate.
- Is a possible therapy for nausea and vomiting due to acute or chronic medical illness or acute gastroenteritis
- Treatment of cyclic vomiting syndrome although there are no formal trials to confirm efficacy.
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.
An extended release injectable version of granisetron, known as Sustol is also available in the United States as of 2016. 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.
- "FDA Approves Sancuso, the First and Only Patch for Preventing Nausea and Vomiting in Cancer Patients Undergoing Chemotherapy". PRNewswire. September 12, 2008.
- Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 448. ISBN 9783527607495.
- Billio, A; Morello, E; Clarke, MJ (January 20, 2010). "Serotonin receptor antagonists for highly emetogenic chemotherapy in adults". The Cochrane Database of Systematic Reviews (1): CD006272. doi:10.1002/14651858.CD006272.pub2. PMID 20091591.
- Carlisle, JB; Stevenson, CA (July 19, 2006). "Drugs for preventing postoperative nausea and vomiting". The Cochrane Database of Systematic Reviews (3): CD004125. doi:10.1002/14651858.CD004125.pub2. PMID 16856030.
- Drugs.com Heron Therapeutics Announces FDA Approval of Sustol (granisetron) Extended-Release Injection for the Prevention of Chemotherapy-Induced Nausea and Vomiting
- FDA.gov Sustol Prescribing Information.
- Aapro, M. (2004). "Granisetron: an update on its clinical use in the management of nausea and vomiting". The Oncologist. 9 (6): 673–686. doi:10.1634/theoncologist.9-6-673. ISSN 1083-7159. PMID 15561811.
|5-HT3 serotonin ion|
|5-HT serotonin G-protein|
|H1 antagonists |
Serotonin receptor modulators
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- 1. 成人の化学療法誘発性悪心・嘔吐の予防と治療prevention and treatment of chemotherapy induced nausea and vomiting in adults [show details]…antagonists, including ondansetron, granisetron, and dolasetron, although they have not been reported with transdermal granisetron or extended-release subcutaneous granisetron . ECG interval changes appear …
- 2. 小児における、アデノイド切除同時施行例を含む扁桃摘出に対する麻酔anesthesia for tonsillectomy with or without adenoidectomy in children [show details]…randomized trials of antiemetic therapies found that serotonergic antagonists (eg, ondansetron, granisetron, tropisetron, dolasetron) were efficacious in preventing PONV in children undergoing tonsillectomy…
- 3. 麻酔後回復室（PACU）における心血管の障害cardiovascular problems in the post anesthesia care unit pacu [show details]…for sudden cardiac death with its use. Ondansetron – The serotonin antagonists (ondansetron, granisetron, and, outside the United States, dolasetron, ramosetron, and tropisetron) may prolong the QT interval…
- 4. 制吐剤の特性characteristics of antiemetic drugs [show details]…well . Four 5-HT3 receptor antagonists are currently approved in the United States: ondansetron, granisetron, dolasetron, and palonosetron. Several well-conducted, randomized, comparative trials have failed …
- 5. 術後に生じる悪心と嘔吐postoperative nausea and vomiting [show details]…First-generation serotonin antagonists – The first-generation serotonin antagonists (ie, ondansetron, granisetron, and, outside the United States, dolasetron, ramosetron, and tropisetron) are equally efficacious …
- Development of novel bioadhesive granisetron hydrochloride spanlastic gel and insert for brain targeting and study their effects on rats.
- Abdelmonem R1, El Nabarawi M2, Attia A1.
- Drug delivery.Drug Deliv.2018 Nov;25(1):70-77. doi: 10.1080/10717544.2017.1413447.
- PMID 29228824
- 5-HT3 antagonists decrease discounting rate without affecting sensitivity to reward magnitude in the delay discounting task in mice.
- Mori M1, Tsutsui-Kimura I2,3,4, Mimura M1, Tanaka KF5.
- Psychopharmacology.Psychopharmacology (Berl).2018 Jun 28. doi: 10.1007/s00213-018-4954-0. [Epub ahead of print]
- PMID 29955899
- Retraction notice to Granisetron, droperidol, and metoclopramide for the treatment of established postoperative nausea and vomiting in women undergoing gynecologic surgery: Am J Obstet Gynecol 2000;182:13-16.
- Fujii Y1, Tanaka H1, Somekawa Y1.
- American journal of obstetrics and gynecology.Am J Obstet Gynecol.2018 Jun;218(6):621. doi: 10.1016/j.ajog.2018.04.023.
- PMID 29793574
- 本橋 慎也,堀 雄史,小野 孝明 [他]
- 薬学雑誌 132(5), 675-681, 2012
- NAID 40019312378
- P-0106 FOLFIRI療法施行時の悪心・嘔吐に対するGranisetron 3mgとPalonosetron 0.75mgの制吐効果に関する比較検討(一般演題 ポスター発表,がん薬物療法(副作用対策),Enjoy Pharmacists' Lifestyles)
- 石川 寛,工藤 祐子,木村 仁,加藤 敏明,町田 望,安井 博史
- 日本医療薬学会年会講演要旨集 21, 199, 2011-09-09
- NAID 110008909576
- Granisetron hydrochloride USP is a white to off-white solid that is readily soluble in water and normal saline at 20ºC. Each white to off-white film coated triangular shaped biconvex tablet contains 1.12 mg Granisetron hydrochloride ...
- Granisetron is only found in individuals that have used or taken this drug. It is a serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic and antinauseant for cancer chemotherapy patients. [PubChem]Granisetron ...
- Granisetron 5-HT3 受容体拮抗型制吐剤 ＊ ＊ 5．妊婦、産婦、授乳婦等への投与 ⑴妊娠中の投与に関する安全性は確立していないので、妊 婦又は妊娠している可能性のある婦人には、治療上の有 益性が危険性を上まわると判断される ...