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Ondansetron, marketed under the brand name Zofran, is a medication used to prevent nausea and vomiting caused by cancer chemotherapy, radiation therapy, or surgery.
Common side effects include diarrhea, constipation, headache, sleepiness, and itchiness.
Ondansetron was first used medically in 1990.
1 Medical uses
1.1 Cancer treatment
1.2 Postoperative
1.3 Pregnancy
1.4 Cyclic vomiting syndrome
1.5 Gastroenteritis
2 Special populations
2.1 Children
2.2 Elderly
2.3 Poor liver function
3 Adverse effects
3.1 QT prolongation
3.2 Overdose
4 Pharmacodynamics
5 History
6 Society and culture
6.1 Publication bias
6.2 Availability
7 Research
7.1 Psychiatric disorders
7.2 Substance use
7.3 Postanesthetic shivering
8 References
9 External links
Medical uses
Although an effective antiemetic agent, the high cost of brand-name ondansetron initially limited its use to controlling postoperative nausea and vomiting and chemotherapy-induced nausea and vomiting.
Cancer treatment
The 5-HT 3 receptor antagonists are the primary drugs used to treat and prevent chemotherapy-induced nausea and vomiting and radiotherapy-induced nausea and vomiting.
A number of medications including ondansetron appear to be effective in controlling postoperative nausea and vomiting. It is more effective than metoclopramide, and less sedating than cyclizine or droperidol.
Ondansetron is used off-label to treat morning sickness and hyperemesis gravidarum of pregnancy. It is typically used after trials of other drugs have failed.
There appears to be a low risk of harm to the baby with use during pregnancy, though there may be an increase in heart problems among the babies.
Ondansetron is in pregnancy category B in the US.
Cyclic vomiting syndrome
Ondansetron is one of several antiemetic agents used during the vomiting phase of cyclic vomiting syndrome.
Trials in emergency department settings support the use of ondansetron to reduce vomiting associated with gastroenteritis and dehydration.
Special populations
Ondansetron has rarely been studied in people under 4 years of age. As such, little data is available to guide dosage recommendations.
It is not necessary to adjust the dosage for people under 75 years of age. The use of ondansetron has not been studied in people older than 75 years of age, and it is not known if dosage should be adjusted for this group.
Poor liver function
The maximum recommended dose for people with severe liver function impairment is 8 mg/day. In these people, ondansetron is cleared from the body at half to one-third the rate as in healthy people. The concentration of ondansetron in body tissues as opposed to plasma is also higher than in healthy people.
Adverse effects
Headache is the most common adverse effect.
Constipation, diarrhea, and dizziness are other commonly reported side effects.
QT prolongation
Use of ondansetron has been associated with prolongation of the QT interval, which can lead to a potentially fatal heart rhythm known as torsades de pointes. Although this may happen in any person with any formulation, the risk is most salient with the injectable (intravenous) form of the drug and increases with dose. The risk is also higher in people taking other medicines that prolong the QT interval, as well as in people with congenital long QT syndrome, congestive heart failure, and/or bradyarrhythmias. As such, single doses of injectable ondansetron should not exceed 16 mg at one time. (Oral dosing recommendations remain intact, including the recommendation of a single 24-mg oral dose when indicated.) Electrolyte imbalances should be corrected before the use of injectable ondansetron. People are cautioned to seek immediate medical care if symptoms such as irregular heartbeat/palpitations, shortness of breath, dizziness, or fainting occur while taking ondansetron.
No specific treatment is available for ondansetron overdose; people are managed with supportive measures. An antidote to ondansetron is not known.
Ondansetron is a highly specific and selective serotonin 5-HT 3 receptor antagonist, with low affinity for dopamine receptors. The 5-HT 3 receptors are present both peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema. Serotonin is released by the enterochromaffin cells of the small intestine in response to chemotherapeutic agents and may stimulate vagal afferents (via 5-HT 3 receptors) to initiate the vomiting reflex. It is thought that ondansetron’s antiemetic action is mediated mostly via antagonism of vagal afferents with a minor contribution from antagonism of central receptors.
A vial of Zofran 4 mg containing ondansetron for intravenous injection
Ondansetron (marketed under the brand name Zofran) was developed in the mid-1980s by GlaxoSmithKline in London. It was granted US patent protection in September 1987,
Society and culture
Publication bias
In 1997, ondansetron was the subject of a meta-analysis case study published in the British Medical Journal. Researchers examined 84 trials, with 11,980 people receiving ondansetron, published between 1991 and September 1996. Intravenous ondansetron 4 mg versus placebo was investigated in 16 reports and three further reports which had been duplicated a total of six times. The number needed to treat (NNT) to prevent vomiting within 24 hours was 9.5, with 95% confidence interval 6.9 to 15, in the 16 nonduplicated reports. In the three duplicated reports, the NNT was significantly lower at 3.9 (3.3 to 4.8). When all 25 reports were combined, the apparent NNT improved to 4.9 (4.4 to 5.6). Inclusion of duplicate reports led to a 23% overestimation of ondansetron’s antiemetic efficacy.
In addition, the authors found the covert duplication of reports on ondansetron was not easy to detect, because of lack of cross-referencing between papers, and reports containing duplicate findings were cited in eight reviews of the drug.
Ondansetron is a generic drug and is available in many countries under many brand names.
Psychiatric disorders
A 2006 double-blind, randomized controlled trial indicated ondansetron may have value in the treatment of schizophrenia, as an adjunct to haloperidol. The study found the combination to significantly improve negative schizophrenia symptoms, and people taking both drugs experienced fewer of the adverse effects commonly associated with haloperidol.
Early studies have also examined ondansetron as a possible treatment for psychosis resulting from advanced Parkinson’s disease. Its apparent benefits despite a lack of any significant antagonistic properties at dopamine receptors or the 5-HT 2A receptor raises interesting questions about the etiology of psychosis.
Substance use
There is tentative evidence that it may be useful in decreasing the desired effects of alcohol.
Postanesthetic shivering
Two small, placebo-controlled trials have been conducted to assess the efficacy of ondansetron for postanesthetic shivering, a common occurrence after surgery. Ondansetron was found to be as effective as pethidine (meperidine, Demerol) when given as a single intravenous dose before anesthesia.

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