Substance
ID:545
Names and Identifiers
Brand Name
Ametik hydrochlorideNausetonTebamideTrimazideStemeticTiganBenzacotTribenzagan
Synonyms
Trimethobenzamidum [INN-Latin]Trimetobenzamida [INN-Spanish]Trimethobenzamide HCLTrimethobenzamide hydrochlorideTrimethobenzamide
IUPAC Traditional name
trimethobenzamide
IUPAC name
N-({4-[2-(dimethylamino)ethoxy]phenyl}methyl)-3,4,5-trimethoxybenzamide
Properties
Physical Property
Hydrophobicity(logP)
2.2
Solubility
40 mg/L
Molecule Details
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
Humans and other mammals
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
•
Hurley JD, Eshelman FN: Trimethobenzamide HCl in the treatment of nausea and vomiting associated with antineoplastic chemotherapy. J Clin Pharmacol. 1980 May-Jun;20(5-6 Pt 1):352-6.
[Pubmed]
•
Hurley JD, Eshelman FN: Trimethobenzamide HCl in the treatment of nausea and vomiting associated with antineoplastic chemotherapy. J Clin Pharmacol. 1980 May-Jun;20(5-6 Pt 1):352-6.
[Pubmed]
•
Dundee JW, Halliday F, Nicholl RM, Moore J: Studies of drugs given before anaesthesia. X. Two non-phenothiazine anti-emetics--cyclizine and trimethobenzamide. Br J Anaesth. 1966 Jan;38(1):50-7.
[Pubmed]
External Links
Molecular Spectra
No Data Available
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References
• Hurley JD, Eshelman FN: Trimethobenzamide HCl in the treatment of nausea and vomiting associated with antineoplastic chemotherapy. J Clin Pharmacol. 1980 May-Jun;20(5-6 Pt 1):352-6. Pubmed
• Dundee JW, Halliday F, Nicholl RM, Moore J: Studies of drugs given before anaesthesia. X. Two non-phenothiazine anti-emetics--cyclizine and trimethobenzamide. Br J Anaesth. 1966 Jan;38(1):50-7. Pubmed
• Hurley JD, Eshelman FN: Trimethobenzamide HCl in the treatment of nausea and vomiting associated with antineoplastic chemotherapy. J Clin Pharmacol. 1980 May-Jun;20(5-6 Pt 1):352-6. Pubmed