Granisetron
429616
217369230
2008-06-05T19:02:11Z
Carlo Banez
5493017
{{drugbox
| IUPAC_name = 1-methyl-''N''-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-<br />indazole-3-carboxamide
| image = grainsetron.png
| image2 = Granisetron_3D.png
| width = 185
| CAS_number = 109889-09-0
| ATC_prefix = A04
| ATC_suffix = AA02
| PubChem = 3510
| DrugBank = APRD01002
| C=18 | H=24 | N=4 | O=1
| molecular_weight = 312.41 g/mol
| bioavailability = 60%
| protein_bound = 65%
| metabolism = Hepatic
| elimination_half-life = 3–14 hours
| excretion = Renal 11–12%, faecal 38%
| pregnancy_category = B1 <small>([[Australia|Au]])</small>,
| legal_status = S4 <small>(Au)</small>, POM <small>([[United Kingdom|UK]])</small>, ℞-only <small>(U.S.)</small>
| routes_of_administration = Oral, intravenous
}}
'''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]]. 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]] around 1988 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]].
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 [[kidney]]s.
==Indications==
* [[Chemotherapy]]-induced nausea and vomiting
** 5-HT<sub>3</sub> receptor antagonists are the primary drugs used to treat and prevent chemotherapy-induced nausea and vomiting. Many times they are given intravenously about 30 minutes before beginning therapy.
* Post-operative and post-radiation nausea and vomiting
* 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.
==Adverse effects==
Granisetron is a well-tolerated drug with few side effects. Headache, dizziness, and constipations 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.
==External links==
*[http://www.kytril.com Kytril Web site]
==References==
* Katzung, Bertram G. <u>Basic and Clinical Pharmacology, 9th ed.</u> (2004). ISBN 0-07-141092-9
{{5-HT3 antagonists}}
[[Category:Antiemetics]]
[[Category:5-HT3 antagonists]]
[[Category:Tropanes]]
[[fr:Granisétron]]
[[hr:Granisetron]]
[[ja:グラニセトロン]]