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Dolasetron
Systematic (IUPAC) name
(3R)-10-oxo-8-azatricyclo[5.3.1.0 3,8]undec-5-yl 1H-indole-3-carboxylate
Identifiers
CAS number 115956-12-2
ATC code A04AA04
PubChem 60654
DrugBank APRD00518
ChemSpider 16736416
Chemical data
Formula C 19H20N2O3  
Mol. mass 324.374 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Protein binding 69 to 77%
Metabolism  ?
Half life 8.1 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat. B (US)
Legal status Rx only
Routes Intravenous, oral
 Yes check.svgY(what is this?)  (verify)

Dolasetron (trade name Anzemet) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much antiemetic effect when symptoms are due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors.

Dolasetron breaks down slowly, staying in the body for a long time. One dose usually lasts 4 to 9 hours and is usually administered once or twice daily. This drug is removed from the body by the liver and kidneys.

Contents

Clinical uses

  • Chemotherapy-induced nausea and vomiting
    • 5-HT3 receptor antagonists are the primary drugs used to treat and prevent chemotherapy-induced nausea and vomiting. Many times they are given intravenously about 30 minutes before beginning therapy.
  • Post-operative and post-radiation nausea and vomiting
  • Is a possible therapy for nausea and vomiting due to acute or chronic medical illness or acute gastroenteritis
  • Unlike most other 5HT3 antagonists, data is lacking for use of dolasetron with aprepitant in chemotherapy-induced nausea and vomiting (CINV).

Adverse effects

Dolasetron is a well-tolerated drug with few side effects. Headache, dizziness, and constipations 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's cytochrome P450 system and it has little effect on the metabolism of other drugs broken down by this system.

See also

  • 5-HT3 receptor antagonist: Drug discovery and development

References

  • Katzung, Bertram G. Basic and Clinical Pharmacology, 9th ed. (2004). ISBN 0-07-141092-9







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