Apo-ondansetron - General Information
A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.
Pharmacology of Apo-ondansetron
Apo-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. Apo-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.
Apo-ondansetron for patients
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.
Ondansetron injection and Ondansetron injection premixed are contraindicated for patients known to have hypersensitivity to the drug.
Additional information about Apo-ondansetron
Apo-ondansetron Indication: For treatment of chemotherapy-induced nausea and vomiting
Mechanism Of Action: Apo-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 Apo-ondansetron works by blocking the reception of serotonin at these 5-HT3 receptors.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Ondansetron
Synonyms: Not Available
Drug Category: Anti-anxiety Agents; Antipsychotics; Antipruritics; Antiemetics; Serotonin Antagonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Ondansetron: Zofran; Zofran ODT; Zophren; Zudan; PMS-ondansetron; Ratio-ondansetron; Sandoz ondansetron; PHL-ondansetron; Novo-ondansetron; Apo-ondansetron;
Absorption: Ondansetron is well absorbed after oral administration and undergoes limited first-pass metabolism.
Toxicity (Overdose): Low blood pressure and fainting, sudden blindness, severe constipation
Protein Binding: 70%-76% (Plasma protein binding)
Half Life: 5.7 hours
Dosage Forms of Apo-ondansetron: Solution Intravenous
Chemical IUPAC Name: 9-methyl-3-[(2-methylimidazol-1-yl)methyl]-2,3-dihydro-1H-carbazol-4-one
Chemical Formula: C18H19N3O
Ondansetron on Wikipedia: http://en.wikipedia.org/wiki/Ondansetron
Organisms Affected: Humans and other mammals