Product Name

Dolasetron Mesylate

Name: Dolasetron Mesylate - LGM Pharma
SKU: 115956-13-3

CAS Number

115956-13-3

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Product Name:

Dolasetron Mesylate

CAS Number:

115956-13-3

Indication:

For the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy, including initial and repeat courses of chemotherapy. Also used for the prevention of postoperative nausea and vomiting. This drug can be used intravenously for the treatment of postoperative nausea and vomiting.

Mode of Action:

Dolasetron is a selective serotonin 5-HT₃ receptor antagonist. In vivo, the drug is rapidly converted into its major active metabolite, hydrodolasetron, which seems to be largely responsible for the drug’s pharmacological activity. The antiemetic activity of the drug is brought about through the inhibition of 5-HT₃ receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT₃ receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.

Pharmacodynamics:

Dolasetron is a highly specific and selective serotonin 5-HT₃ receptor antagonist, not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. It is structurally and pharmacologically related to other 5-HT₃ receptor agonists. The serontonin 5-HT₃ receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema. It is suggested that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT₃ receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting.

Metabolism:

Hepatic

IUPAC:

1H-Indole-3-carboxylic acid, octahydro-3-oxo-2, 6-methano-2H-quinolizin-8-yl ester, (2alpha, 6alpha, 8alpha, 9abeta)-, monomethanesulfonate

ATC:

A04AA04

DrugBank:

DB00757

Formula:

C19-H20-N2-O3.C-H4-O3-S

Molecular Mass:

420.4836

Synonyms:

Anzemet, Dolasetron mesylate, Indole-3-carboxylic acid, ester with (8R)-hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one, monomethanesulfonate, MDL 73,147EF, MDL 73147EF, UNII-71YF100S3H

SMILES:

CS(=O)(=O)O.c1ccc2c(c1)c(c[nH]2)C(=O)O[C@@H]3C[C@@H]4CC5C[C@H](C3)[N@]4CC5=O

AHFS Code:

56:22.2

InChi:

1S/C19H20N2O3.CH4O3S/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;1-5(2,3)4/h1-4,9,11-14,20H,5-8,10H2;1H3,(H,2,3,4)/t11?,12-,13+,14+;

General Reference:

Balfour JA, Goa KL: Dolasetron. A review of its pharmacology and therapeutic potential in the management of nausea and vomiting induced by chemotherapy, radiotherapy or surgery. Drugs. 1997 Aug;54(2):273-98. Pubmed
Gregory RE, Ettinger DS: 5-HT3 receptor antagonists for the prevention of chemotherapy-induced nausea and vomiting. A comparison of their pharmacology and clinical efficacy. Drugs. 1998 Feb;55(2):173-89. Pubmed
Gan TJ: Selective serotonin 5-HT3 receptor antagonists for postoperative nausea and vomiting: are they all the same? CNS Drugs. 2005;19(3):225-38. Pubmed

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Dolasetron Mesylate

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