Dolasetron
Dolasetron Uses, Dosage, Side Effects, Food Interaction and all others data.
Dolasetron 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. Dolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist. This drug is not shown to have activity at other known serotonin receptors, and has low affinity for dopamine receptors.
Dolasetron 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. It is structurally and pharmacologically related to other 5-HT3 receptor agonists. The serontonin 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 suggested that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting.
Trade Name | Dolasetron |
Availability | Discontinued |
Generic | Dolasetron |
Dolasetron Other Names | Dolasetron, Dolasétron, Dolasetronum |
Related Drugs | lorazepam, ondansetron, Zofran, dexamethasone, Ativan, metoclopramide, Reglan, amisulpride, droperidol |
Weight | 100mg, 50mg, |
Type | Oral tablet |
Formula | C19H20N2O3 |
Weight | Average: 324.38 Monoisotopic: 324.147392512 |
Protein binding | 69-77% |
Groups | Approved, Investigational |
Therapeutic Class | |
Manufacturer | |
Available Country | United States |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Dolasetron is an antinauseant and antiemetic used in chemotherapy and postoperatively.
For the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy, including initial and repeat courses of chemotherapy. Also used for the prevention of postoperative nausea and vomiting. This drug can be used intravenously for the treatment of postoperative nausea and vomiting.
Dolasetron is also used to associated treatment for these conditions: Chemotherapy-Induced Nausea and Vomiting (CINV), Post Operative Nausea and Vomiting (PONV)
How Dolasetron works
Dolasetron is a selective serotonin 5-HT3 receptor antagonist. In vivo, the drug is rapidly converted into its major active metabolite, hydrodolasetron, which seems to be largely responsible for the drug's pharmacological activity. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
Dolasetron Drug Interaction
Major: meperidine, meperidineMinor: sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprimUnknown: calcium carbonate, calcium carbonate, dexamethasone, dexamethasone, cyclobenzaprine, cyclobenzaprine, heparin, heparin, baclofen, baclofen, naproxen, naproxen, pegfilgrastim, pegfilgrastim, acetaminophen, acetaminophen
Dolasetron Disease Interaction
Volume of Distribution
- 5.8 L/kg [adults]
Elimination Route
Orally-administered dolasetron is well absorbed
Half Life
8.1 hours
Clearance
- Apparent cl=9.4 mL/min/kg [Healthy volunteers with IV treatment dose up to 5 mg/kg]
Elimination Route
Hydrodolasetron is eliminated by multiple routes, including renal excretion and, after metabolism, mainly glucuronidation, and hydroxylation.
Innovators Monograph
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