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Ondansetron
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DRUG INFO
Ondansetron
Drug Name:
Ondansetron
Indication: For treatment of chemotherapy-induced nausea and vomiting
Pharmacology: Ondansetron is an antinauseant and antiemetic agent indicated for the prevention of nausea and vomiting associated with moderately-emetogenic cancer chemotherapy and for the prevention of postoperative nausea and vomiting. Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist, not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors.
Mechanism Of Action: Ondansetron is a selective serotonin 5-HT3 receptor antagonist. The serotonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. It is thought that chemotherapeutic agents produce nausea and vomiting by releasing serotonin from the enterochromaffin cells of the small intestine, and that the released serotonin then activates 5-HT3 receptors located on vagal efferents to initiate the vomiting reflex. Therefore Ondansetron works by blocking the reception of serotonin at these 5-HT3 receptors.
Drug Category: Anti-anxiety Agents; Antipsychotics; Antipruritics; Antiemetics; Serotonin Antagonists; ATC:A04AA01
Brand Names/Synonyms: Zophren; Zofran; Zudan; Zofran ODT
Dosage Forms: TABLET; LIQUID
Absorption: Ondansetron is well absorbed after oral administration and undergoes limited first-pass metabolism.
Interactions: Interactions for Ondansetron:
Ondansetron does not itself appear to induce or inhibit the cytochrome P-450 drug-metabolizing enzyme system of the liver. Because ondansetron is metabolized by hepatic cytochrome P-450 drug-metabolizing enzymes (CYP3A4, CYP2D6, CYP1A2), inducers or inhibitors of these enzymes may change the clearance and, hence, the half-life of ondansetron. On the basis of limited available data, no dosage adjustment is recommended for patients on these drugs.
Phenytoin, Carbamazepine, and Rifampicin: In patients treated with potent inducers of CYP3A4 (i.e., phenytoin, carbamazepine, and rifampicin), the clearance of ondansetron was significantly increased and ondansetron blood concentrations were decreased. However, on the basis of available data, no dosage adjustment for ondansetron is recommended for patients on these drugs.1,3
Tramadol: Although no pharmacokinetic drug interaction between ondansetron and tramadol has been observed, data from 2 small studies indicate that ondansetron may be associated with an increase in patient controlled administration of tramadol.4,5
Chemotherapy: Tumor response to chemotherapy in the P 388 mouse leukemia model is not affected by ondansetron. In humans, carmustine, etoposide, and cisplatin do not affect the pharmacokinetics of ondansetron.
In a crossover study in 76 pediatric patients, I.V. ondansetron did not increase blood levels of high-dose methotrexate.
Chemical IUPAC Name: 9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-1,2,3,9-tetrahydrocarbazol-4-one
Chemical Formula: C18H19N3O
Half Life: 5.7 hours
Drug Type: Approved Drug
# Accession No: APRD00481
CAS Registry Number: 99614-02-5
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Ondansetron News
(When available)
Hana Posts Positive Study Results Jan 9, 2006
MSN Money ...a clinical trial. The study included 32 patients who received either Hana's Zensana drug or GlaxosmithKline's Zofran. Hana said ...
Emend® Approved for Prevention of Moderate Chemotherapy ... Jan 12, 2006
Cancer Consultants (press release), The first 5-HT3-receptor antagonist, Zofran® (ondansetron), was FDA approved in January 1991 and has proved effective in controlling acute CINV (CINV that ...
Hana Biosciences Announces 2006 Corporate Goals; Key 2005 ... Jan 5, 2006
Genetic Engineering News, ...-- Q1 05: Zensana(TM) pilot pharmacokinetic study demonstrated pharmacokinetic profile comparable to oral Zofran(R), with multidose convenience and faster drug ...
Genzyme Names New Head of Product Development for Campath and ... Jan 13, 2006
Financial News USA (press release), Standard therapy was defined as ondansetron, a nausea treatment marketed as Zofran by GlaxoSmithKline PLC, and dexamethasone, a synthetic steroid. ...
Hana Biosciences Announces Positive Results of Initial ... Jan 9, 2006
Genetic Engineering News, ...demonstrated Zensana(TM) (ondansetron oral spray) 8 mg dose is bioequivalent to the current commercially available 8 mg tablet (Zofran(R); GlaxoSmithKline). ...
Pfizer combats fake Viagra with electronic ID tags Jan 6, 2006
AZ Central.com, ...interview. The company will probably test the technology on either one of its HIV medicines or on Zofran, an anti-nausea drug. Purdue ...
End to patents means major headache for drug makers Dec 23, 2005
The Journal News.com, GlaxoSmithKline PLC, based in London with US operations split between Philadelphia and Research Triangle Park, NC, will lose Zofran, its nausea drug for ...
Blockbuster Drugs' Market Share in Danger Dec 21, 2005
PR Newswire (press release), ...by 2008. This year alone at least eight blockbusters, including Allegra, Plavix and Zofran, have had patents expire. These drugs ...
Medical school scandal illustrates nationwide rip-off Dec 25, 2005
NorthJersey.com, Last year, GlaxoSmithKline paid New Jersey's Medicaid program $2.1 million in a scheme to inflate the price of its anti-nausea drugs Zofran and Kytril. ...
Drug makers face headache as patents expire Dec 18, 2005
Austin American-Statesman (subscription), GlaxoSmithKline PLC will lose the patent protection for Zofran, its nausea drug for cancer patients that earned about $1 billion in US sales last year. ...
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