Dolasetron
2643313
215567209
2008-05-28T19:45:31Z
ChemNerd
2246483
Quick-adding category "Indoles" (using [[WP:HOTCAT|HotCat]])
{{drugbox
| IUPAC_name = (3''R'')-10-oxo-8-azatricyclo[5.3.1.0<sup>3,8</sup>]undec-5-yl 1''H''-indole-3-carboxylate
| image = Dolasetron.svg
| image2 = Dolasetron_3D.png
| CAS_number = 115956-12-2
| ATC_prefix = A04
| ATC_suffix = AA04
| ATC_supplemental =
| PubChem = 60654
| DrugBank = APRD00518
| C = 19 | H = 20 | N = 2 | O = 3
| molecular_weight = 324.374 g/mol
| bioavailability =
| protein_bound = 69 to 77%
| metabolism =
| elimination_half-life = 8.1 hours
| pregnancy_category = B (US)
| legal_status = Rx only
| routes_of_administration = Intravenous, oral
}}
'''Dolasetron''' (trade name '''Anzemet''') is a [[serotonin]] [[5-HT3 antagonist|5-HT<sub>3</sub> 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 [[kidney]]s.
==Clinical uses==
* [[Chemotherapy]]-induced nausea and vomiting
** 5-HT<sub>3</sub> receptor antagonists are the primary drugs used to treat and prevent chemotherapy-induced nausea and vomiting. Many times they are given [[Intravenous therapy|intravenous]]ly about 30 minutes before beginning therapy.
* [[Postoperative nausea and vomiting|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]]
==Adverse effects==
Dolasetron is a well-tolerated drug with few [[adverse drug reaction|side effect]]s. 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 oxidase|cytochrome P450]] system and it has little effect on the metabolism of other drugs broken down by this system.
==References==
* Katzung, Bertram G. ''Basic and Clinical Pharmacology'', 9th ed. (2004). ISBN 0-07-141092-9
{{5-HT3 antagonists}}
[[Category:Antiemetics]]
[[Category:5-HT3 antagonists]]
[[Category:Prodrugs]]
[[Category:Indoles]]