Dolasetron

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Dolasetron
Systematic (IUPAC) name
(3R)-10-oxo-8-azatricyclo[5.3.1.03,8]undec-5-yl 1H-indole-3-carboxylate
Identifiers
CAS number	115956-12-2
ATC code	A04AA04
PubChem	60654
DrugBank	APRD00518
Chemical data
Formula	C19H20N2O3
Mol. mass	324.374 g/mol
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

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.

[edit] 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

[edit] 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.

[edit] References

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

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