Molecule

Drug Groups

approved

Description

Trimethobenzamide is a novel antiemetic which prevents nausea and vomiting in humans. Its actions are unclear but most likely involves the chemoreceptor trigger zone (CTZ). In dogs pretreated with trimethobenzamide HCl, the emetic response to apomorphine is inhibited, while little or no protection is afforded against emesis induced by intragastric copper sulfate.

Indication

For the treatment of postoperative nausea and vomiting and for nausea associated with gastroenteritis.

Pharmacology

Trimethobenzamide is a novel antiemetic which prevents nausea and vomiting in humans. Its actions are unclear but most likely involves the chemoreceptor trigger zone (CTZ). In dogs pretreated with trimethobenzamide HCl, the emetic response to apomorphine is inhibited, while little or no protection is afforded against emesis induced by intragastric copper sulfate.

Toxicity

Oral LD₅₀ in mice is 1600 mg/kg.

Affected Organisms

Biotransformation

Hepatic.

Absorption

The relative bioavailability of the capsule formulation compared to the solution is 100%.

Half Life

The mean elimination half-life of trimethobenzamide is 7 to 9 hours.

Elimination

Between 30 – 50% of a single dose in humans is excreted unchanged in the urine within 48–72 hours.

References

External Links