Dolasetron

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Bulgaria: Anzemet; Cyprus: Anzemet; France: Anzemet; Germany: Anemet, Anzemet; Greece: Anzemet; Malta: Anzemet.

North America

Canada: Anzemet; USA: Anzemet.

Latin America

Brazil: Anzemet; Mexico: Anzemet.

Drug combinations

Chemistry

Dolasetron Mesylate: C~19~H~20~N~2~O~3~ CH~4~O~3~S H~2~O. Mw: 438.49. (1) 1H-Indole-3-carboxylic acid, octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester, (2α,6α,8α,9aβ)-, monomethanesulfonate; (2) Indole-3-carboxylic acid, ester with (8r)-hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one, monomethanesulfonate. CAS-115956-13-3; CAS-115956-12-2 (dolasetron)(1991).

Pharmacologic Category

Antiemetics; 5-HT~3~ Receptor Antagonists Selective. (ATC-Code: A04AA04).

Mechanism of action

A selective inhibitor of type 3 serotonergic (5-HT~3~) receptors. Blocks serotonin both peripherally (primary site of action) and centrally at the chemoreceptor trigger zone.

Therapeutic use

Used I.V. or orally for the prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy. Dolasetron is also used I.V. or orally for the prevention of postoperative nausea and vomiting and I.V. for the treatment of postoperative nausea and vomiting.

Pregnancy and lactiation implications

Teratogenic effects not observed in animal studies. There are no adequate, well-controlled studies in pregnant women. Caution if the drug is administered during lactation.

Unlabeled use

Contraindications

Hypersensitivity to dolasetron or any component of the formulation.

Warnings and precautions

Sensitivity reactions, including anaphylactic reaction, facial edema and urticaria, reported rarely. Use with caution in patients allergic to other 5-HT~3~ receptor antagonists (cross-reactivity reported). Acute, usually reversible ECG alterations and/or risk of altered cardiac conduction (use with caution in patients at risk of QT prolongation and/or ventricular arrhythmia). Prolongation of PR, QTc, and JT intervals and widening of the QRS complex observed. Should be used with caution in patients who have or may develop prolongation of cardiac conduction intervals, particularly QTc, including those with congenital QT syndrome, those with uncorrected hypokalemia or hypomagnesemia, patients receiving diuretics which may induce electrolyte abnormalities, patients receiving antiarrhythmic agents or other drugs which alter cardiac conduction (e.g. prolong QT interval), and those receiving cumulative high-dose anthracycline therapy. For chemotherapy-related emesis, it should be used on a scheduled basis. The drug is not intended for treatment of nausea and vomiting or for chronic continuous therapy. No dosage adjustment for dolasetron necessary in hepatic or renal impairment, although the apparent plasma clearance of hydrodolasetron is substantially reduced following oral and I.V. dolasetron in severe renal impairment and following I.V. administration of the drug in severe hepatic impairment.

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