Dolasetron
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Dolasetron
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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. weight | 324.374 g/mol |
Pharmacokinetic data | |
Bioavailability | ? |
Protein binding | 69 to 77% |
Metabolism | ? |
Half life | 8.1 hours |
Excretion | ? |
Therapeutic considerations | |
Pregnancy cat. |
? |
Legal status | |
Routes | ? |
Dolasetron (trade name Anzamet®) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Its main affect 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