dolasetron

Absorption

Orally-administered dolasetron is well absorbed

Description

Dolasetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT₃ (K_i = 20 nM). It is selective for 5-HT₃ receptors over 5-HT_1A, 5-HT_1B, 5-HT₂, dopamine D₂, α₁-, α₂-, β-adrenergic, M_1-5 muscarinic acetylcholine, and neurokinin-1 (NK₁) receptors (IC₅₀s = >10 μM for all). Dolasetron inhibits 5-HT-induced membrane currents in NG 108-15 cells (IC₅₀ = 3.8 nM). It increases the latency to emesis and reduces the number of vomiting and retching episodes induced by cisplatin in ferrets when administered at doses of 0.5 or 2 mg/kg. Formulations containing dolasetron have been used in the prevention of postoperative or chemotherapy-induced nausea.

Description

Dolasetron, available commercially as Anzement, is an anti-emetic drug that is especially useful to chemotherapy patients. Its mode of action is as a serotonin 5-HT3?receptor antagonist. A new, more scalable synthetic route to dolasteron was featured in a?recent Patent Watch report.

Chemical properties

White Solid

The Uses of dolasetron

Dolasetron is a bridged pseudopelletierine derivative; specific serotonin (5HT3) receptor antagonist.It is used as antiemetic.

The Uses of dolasetron

prevention and treatment of postoperative nausea and vomiting

The Uses of dolasetron

Bridged pseudopelletierine derivative; specific serotonin (5HT3) receptor antagonist. Antiemetic.

Background

Dolasetron is an antinauseant and antiemetic agent indicated for the prevention of nausea and vomiting associated with moderately-emetogenic cancer chemotherapy and for the prevention of postoperative nausea and vomiting. Dolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist. This drug is not shown to have activity at other known serotonin receptors, and has low affinity for dopamine receptors.

Indications

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.

What are the applications of Application

Dolasetron is an antiserotonin compound

Definition

ChEBI: LSM-5418 is an indolyl carboxylic acid.

brand name

Anzemet (Sanofi Aventis.

Pharmacokinetics

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