Granisetron
Encyclopedia
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 ProStrakan, Inc., a pharmaceutical company headquartered in Bedminster, NJ, with global headquarters in Scotland.
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.
's cytochrome P450 system and it has little effect on the metabolism of other drugs broken down by this system.
Serotonin
Serotonin or 5-hydroxytryptamine is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and in the central nervous system of animals including humans...
5-HT3 receptor antagonist
5-HT3 antagonist
The 5-HT3 antagonists are a class of medications that act as receptor antagonists at the 5-HT3 receptor, a subtype of serotonin receptor found in terminals of the vagus nerve and in certain areas of the brain....
used as an antiemetic
Antiemetic
An antiemetic is a drug that is effective against vomiting and nausea. Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer....
to treat nausea
Nausea
Nausea , is a sensation of unease and discomfort in the upper stomach with an involuntary urge to vomit. It often, but not always, precedes vomiting...
and vomiting
Vomiting
Vomiting is the forceful expulsion of the contents of one's stomach through the mouth and sometimes the nose...
following chemotherapy
Chemotherapy
Chemotherapy is the treatment of cancer with an antineoplastic drug or with a combination of such drugs into a standardized treatment regimen....
. Its main effect is to reduce the activity of the vagus nerve
Vagus nerve
The vagus nerve , also called pneumogastric nerve or cranial nerve X, is the tenth of twelve paired cranial nerves...
, which is a nerve that activates the vomiting center in the medulla oblongata
Medulla oblongata
The medulla oblongata is the lower half of the brainstem. In discussions of neurology and similar contexts where no ambiguity will result, it is often referred to as simply the medulla...
. It does not have much effect on vomiting due to motion sickness. This drug does not have any effect on dopamine
Dopamine
Dopamine is a catecholamine neurotransmitter present in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this substituted phenethylamine functions as a neurotransmitter, activating the five known types of dopamine receptors—D1, D2, D3, D4, and D5—and their...
receptors or muscarinic receptors.
Granisetron was developed by chemists working at the British drug company Beecham
Beecham (pharmaceutical company)
Beecham was a British pharmaceutical company. It was once a constituent of the FTSE 100 Index. Beecham, after having merged with SmithKline Beckman, merged with GlaxoWellcome to become GlaxoSmithKline .-History:...
around 1988 and is available as a generic. It is produced by Roche Laboratories
Hoffmann-La Roche
F. Hoffmann-La Roche Ltd. is a Swiss global health-care company that operates worldwide under two divisions: Pharmaceuticals and Diagnostics. Its holding company, Roche Holding AG, has shares listed on the SIX Swiss Exchange....
under the trade name Kytril. The drug was approved in the United Kingdom
United Kingdom
The United Kingdom of Great Britain and Northern IrelandIn the United Kingdom and Dependencies, other languages have been officially recognised as legitimate autochthonous languages under the European Charter for Regional or Minority Languages...
in 1991 and in United States
United States
The United States of America is a federal constitutional republic comprising fifty states and a federal district...
in 1994 by the FDA
Food and Drug Administration
The Food and Drug Administration is an agency of the United States Department of Health and Human Services, one of the United States federal executive departments...
.
A granisetron transdermal patch
Transdermal patch
A transdermal patch is a medicated adhesive patch that is placed on the skin to deliver a specific dose of medication through the skin and into the bloodstream. Often, this promotes healing to an injured area of the body. An advantage of a transdermal drug delivery route over other types of...
with the trade name Sancuso was approved by the US FDA on September 12, 2008. Sancuso is manufactured by ProStrakan, Inc., a pharmaceutical company headquartered in Bedminster, NJ, with global headquarters in Scotland.
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
Liver
The liver is a vital organ present in vertebrates and some other animals. It has a wide range of functions, including detoxification, protein synthesis, and production of biochemicals necessary for digestion...
and kidney
Kidney
The kidneys, organs with several functions, serve essential regulatory roles in most animals, including vertebrates and some invertebrates. They are essential in the urinary system and also serve homeostatic functions such as the regulation of electrolytes, maintenance of acid–base balance, and...
s.
Indications
- ChemotherapyChemotherapyChemotherapy is the treatment of cancer with an antineoplastic drug or with a combination of such drugs into a standardized treatment regimen....
-induced nausea and vomiting- 5-HT3 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 gastroenteritisGastroenteritisGastroenteritis is marked by severe inflammation of the gastrointestinal tract involving both the stomach and small intestine resulting in acute diarrhea and vomiting. It can be transferred by contact with contaminated food and water...
- Treatment of Cyclic vomiting syndromeCyclic vomiting syndromeCyclic vomiting syndrome or cyclical vomiting syndrome is a condition whose symptoms are recurring attacks of intense nausea, vomiting and sometimes abdominal pain and/or headaches or migraines...
although there are no formal trials to confirm efficacy.
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 liverLiver
The liver is a vital organ present in vertebrates and some other animals. It has a wide range of functions, including detoxification, protein synthesis, and production of biochemicals necessary for digestion...
's cytochrome P450 system and it has little effect on the metabolism of other drugs broken down by this system.
External links
See also
- 5-HT3 receptor antagonist: Drug discovery and development