Granisetron is a

serotonin Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vas ...

5-HT₃ receptor antagonist used as an

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. They may ...

to treat

nausea Nausea is a diffuse sensation of unease and discomfort, sometimes perceived as an urge to vomit. While not painful, it can be a debilitating symptom if prolonged and has been described as placing discomfort on the chest, abdomen, or back of the ...

and vomiting following

chemotherapy Chemotherapy (often abbreviated to chemo and sometimes CTX or CTx) is a type of cancer treatment that uses one or more anti-cancer drugs (chemotherapeutic agents or alkylating agents) as part of a standardized chemotherapy regimen. Chemotherap ...

and radiotherapy. Its main effect is to reduce the activity of the

vagus nerve The vagus nerve, also known as the tenth cranial nerve, cranial nerve X, or simply CN X, is a cranial nerve that interfaces with the parasympathetic control of the heart, lungs, and digestive tract. It comprises two nerves—the left and right ...

, which is a nerve that activates the vomiting center in the

medulla oblongata The medulla oblongata or simply medulla is a long stem-like structure which makes up the lower part of the brainstem. It is anterior and partially inferior to the cerebellum. It is a cone-shaped neuronal mass responsible for autonomic (involun ...

. It does not have much effect on vomiting due to motion sickness. This drug does not have any effect on

dopamine Dopamine (DA, a contraction of 3,4-dihydroxyphenethylamine) is a neuromodulatory molecule that plays several important roles in cells. It is an organic compound, organic chemical of the catecholamine and phenethylamine families. Dopamine const ...

receptors or

muscarinic receptor Muscarinic acetylcholine receptors, or mAChRs, are acetylcholine receptors that form G protein-coupled receptor complexes in the cell membranes of certain neurons and other cells. They play several roles, including acting as the main end-rec ...

s. Granisetron was developed by chemists working at the British drug company

Beecham Beecham is a surname. Notable people with the surname include: * Audrey Beecham (1915–1989), poet and niece of the conductor * Betty Humby Beecham (1908–1958), British pianist and wife of the conductor * Earl Beecham (born 1965), American foo ...

around 1985 and is available as a generic. It is produced by

Roche Laboratories F. Hoffmann-La Roche AG, commonly known as Roche, is a Swiss multinational healthcare company that operates worldwide under two divisions: Pharmaceuticals and Diagnostics. Its holding company, Roche Holding AG, has shares listed on the SIX S ...

under the trade name Kytril. The drug was approved in the United Kingdom in 1991 and in United States in 1994 by the

FDA The United States Food and Drug Administration (FDA or US FDA) is a federal agency of the Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food s ...

. A granisetron

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. An advantage of a transdermal drug delivery route over other types of medicat ...

with the trade name Sancuso was approved by the US FDA on September 12, 2008. Sancuso is manufactured by 3M Drug Delivery Systems for Kyowa Kirin, Inc. It was patented in 1985 and approved for medical use in 1991. It is on the

World Health Organization's List of Essential Medicines The WHO Model List of Essential Medicines (aka Essential Medicines List or EML), published by the World Health Organization (WHO), contains the medications considered to be most effective and safe to meet the most important needs in a health ...

Medical uses

Chemotherapy

It may be used for

-induced nausea and vomiting and appears to work about the same as

ondansetron Ondansetron, sold under the brand name Zofran among others, is a medication used to prevent nausea and vomiting caused by cancer chemotherapy, radiation therapy, or surgery. It is also effective for treating gastroenteritis. It can be given by ...

. 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.

Post operative

A number of medications including granisetron appear to be effective in controlling

post-operative nausea and vomiting Postoperative nausea and vomiting (PONV) is the phenomenon of nausea, vomiting, or retching experienced by a patient in the postanesthesia care unit (PACU) or within 24 hours following a surgical procedure. PONV affects about 10% of the population ...

(PONV). It is unclear if it is more or less effective than other agents such as

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metoclopramide Metoclopramide is a medication used for stomach and esophageal problems. It is commonly used to treat and prevent nausea and vomiting, to help with emptying of the stomach in people with delayed stomach emptying, and to help with gastroesoph ...

, or

Gastroparesis

The granisetron patch (Sancuso) has been studied for use in

gastroparesis Gastroparesis (gastro- from Ancient Greek γαστήρ – gaster, "stomach"; and -paresis, πάρεσις – "partial paralysis"), also called delayed gastric emptying, is a medical disorder consisting of weak muscular contractions (peristalsis) ...

, though it is not FDA approved for this indication.

Other

* Is a possible therapy for nausea and vomiting due to acute or chronic medical illness or acute

gastroenteritis Gastroenteritis, also known as infectious diarrhea and gastro, is an inflammation of the gastrointestinal tract including the stomach and intestine. Symptoms may include diarrhea, vomiting, and abdominal pain. Fever, lack of energy, and dehydra ...

* Treatment of

cyclic vomiting syndrome Cyclic vomiting syndrome (CVS) is a chronic functional condition of unknown pathogenesis. CVS is characterized as recurring episodes lasting a single day to multiple weeks. Each episode is divided into four phases: inter-episodic, prodrome, vom ...

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

liver The liver is a major Organ (anatomy), organ only found in vertebrates which performs many essential biological functions such as detoxification of the organism, and the Protein biosynthesis, synthesis of proteins and biochemicals necessary for ...

cytochrome P450 Cytochromes P450 (CYPs) are a Protein superfamily, superfamily of enzymes containing heme as a cofactor (biochemistry), cofactor that functions as monooxygenases. In mammals, these proteins oxidize steroids, fatty acids, and xenobiotics, and are ...

system and it has little effect on the metabolism of other drugs broken down by this system.

Extended release

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.go
Sustol Prescribing Information