Dolasetron

Dolasetron
Clinical data
AHFS/Drugs.com	Monograph
MedlinePlus	a601001
Pregnancy; category	B (US);
Routes of; administration	Intravenous, by mouth
ATC code	A04AA04 (WHO) ;
Legal status
Legal status	In general: ℞ (Prescription only);
Pharmacokinetic data
Protein binding	69 to 77%
Elimination half-life	8.1 hours
Identifiers
	IUPAC name (3R)-10-oxo-8-azatricyclo[5.3.1.03,8]undec-5-yl 1H-indole-3-carboxylate;
CAS Number	115956-12-2 ;
PubChem CID	60654;
DrugBank	DB00757 ;
ChemSpider	16736416 ;
UNII	82WI2L7Q6E;
KEGG	D07867 ;
ChEMBL	ChEMBL1201240 ;
CompTox Dashboard (EPA)	DTXSID4048276 ;
ECHA InfoCard	100.130.141
Chemical and physical data
Formula	C19H20N2O3
Molar mass	324.380 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES [H]C35C[C@@]4([H])CC(OC(=O)c1c[nH]c2ccccc12)C[C@@]([H])(C3)N4CC5=O;
	InChI InChI=1S/C19H20N2O3/c22-18-10-21-12-5-11(18)6-13(21)8-14(7-12)24-19(23)16-9-20-17-4-2-1-3-15(16)17/h1-4,9,11-14,20H,5-8,10H2/t11-,12+,13-,14- ; Key:UKTAZPQNNNJVKR-YXSUXZIUSA-N ;
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Dolasetron (trade name Anzemet) is a serotonin 5-HT₃ receptor antagonist used to treat nausea and vomiting following chemotherapy.^[1] 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 is usually administered once or twice daily and lasts 4 to 9 hours. This drug is removed from the body by the liver and kidneys.

It was patented in 1986 and approved for medical use in 2002.^[2] It is on the World Health Organization's List of Essential Medicines.^[3]

^ Long-term Use of Ondansetron, Dolasetron and Granisetron for the Prevention of Nausea and Vomiting: A Review of the Clinical Effectiveness and Safety [Internet]. CADTH Rapid Response Reports. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health. April 2014. PMID 25610941.
^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 448. ISBN 9783527607495.
^ World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.

[1] Long-term Use of Ondansetron, Dolasetron and Granisetron for the Prevention of Nausea and Vomiting: A Review of the Clinical Effectiveness and Safety [Internet]. CADTH Rapid Response Reports. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health. April 2014. PMID 25610941.

[2] Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 448. ISBN 9783527607495.

[WHO22nd-3] World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.

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