Trimethobenzamide (injection)

Trimethobenzamide (injection)
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Turky Alkathery, M.D. [2]

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Overview

Trimethobenzamide (injection) is an antiemetic that is FDA approved for the treatment of postoperative nausea and vomiting and for nausea associated with gastroenteritis. Common adverse reactions include hypotension, anticholinergic adverse reaction and somnolence.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Indications

Trimethobenzamide hydrochloride is indicated for the treatment of postoperative nausea and vomiting and for nausea associated with gastroenteritis.

Dosage

Dosage should be adjusted according to the indication for therapy, severity of symptoms and the response of the patient.

Geriatric Patients Dose adjustments such as reducing the total dose administered at each dosing or increasing the dosing interval should be considered in elderly patients with renal impairment (creatinine clearance ≤ 70 mL/min/1.73m2). Final dose adjustment should be based upon integration of clinical efficacy and safety considerations.

Patients with Renal Impairment In subjects with renal impairment (creatinine clearance ≤ 70 mL/min/1.73m2), dose adjustment such as reducing the total dose administered at each dosing or increasing the dosing interval should be considered.

INJECTABLE, 100 mg/mL (Not for use in pediatric patients)

Usual Adult Dosage 2 mL (200 mg) t.i.d. or q.i.d. intramuscularly. NOTE: The injectable form is intended for intramuscular administration only; it is not recommended for intravenous use.

Intramuscular administration may cause pain, stinging, burning, redness and swelling at the site of injection. Such effects may be minimized by deep injection into the upper outer quadrant of the gluteal region, and by avoiding the escape of solution along the route.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Trimethobenzamide (injection) in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Trimethobenzamide (injection) in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding Trimethobenzamide (injection) FDA-Labeled Indications and Dosage (Pediatric) in the drug label.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Trimethobenzamide (injection) in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Trimethobenzamide (injection) in pediatric patients.

Contraindications

The injectable form of trimethobenzamide hydrochloride is contraindicated in pediatric patients and in patients with known hypersensitivity to trimethobenzamide.

Warnings

Trimethobenzamide hydrochloride may produce drowsiness. Patients should not operate motor vehicles or other dangerous machinery until their individual responses have been determined.

Precautions

During the course of acute febrile illness, encephalitides, gastroenteritis, dehydration and electrolyte imbalance, especially in children and the elderly or debilitated, CNS reactions such as opisthotonos, convulsions, coma and extrapyramidal symptoms have been reported with and without use of trimethobenzamide hydrochloride or other antiemetic agents. In such disorders caution should be exercised in administering trimethobenzamide hydrochloride, particularly to patients who have recently received other CNS-acting agents (phenothiazines, barbiturates, belladonna derivatives). Primary emphasis should be directed toward the restoration of body fluids and electrolyte balance, the relief of fever and relief of the causative disease process. Overhydration should be avoided since it may result in cerebral edema.

The antiemetic effects of trimethobenzamide hydrochloride may render diagnosis more difficult in such conditions as appendicitis and obscure signs of toxicity due to overdosage of other drugs.

Adverse Reactions

Clinical Trials Experience

There have been reports of hypersensitivity reactions and Parkinson-like symptoms. There have been instances of hypotension reported following parenteral administration to surgical patients. There have been reports of blood dyscrasias, blurring of vision, coma, convulsions, depression of mood, diarrhea, disorientation, dizziness, drowsiness, headache, jaundice, muscle cramps and opisthotonos. If these occur, the administration of the drug should be discontinued. Allergic-type skin reactions have been observed; therefore, the drug should be discontinued at the first sign of sensitization. While these symptoms will usually disappear spontaneously, symptomatic treatment may be indicated in some cases.

Postmarketing Experience

There is limited information regarding Trimethobenzamide (injection) Postmarketing Experience in the drug label.

Drug Interactions

There is limited information regarding Trimethobenzamide (injection) Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): Trimethobenzamide hydrochloride was studied in reproduction experiments in rats and rabbits and no teratogenicity was suggested. The only effects observed were an increased percentage of embryonic resorptions or stillborn pups in rats administered 20 mg and 100 mg/kg and increased resorptions in rabbits receiving 100 mg/kg. In each study these adverse effects were attributed to one or two dams. The relevance to humans is not known. Since there is no adequate experience in pregnant or lactating women who have received this drug, safety in pregnancy or in nursing mothers has not been established.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Trimethobenzamide (injection) in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Trimethobenzamide (injection) during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Trimethobenzamide (injection) in women who are nursing.

Pediatric Use

There is no FDA guidance on the use of Trimethobenzamide (injection) in pediatric settings.

Geriatic Use

Clinical studies of trimethobenzamide hydrochloride did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger patients. Although there are studies reported in the literature that include elderly patients >65 years old with younger patients, it is not known if there are differences in efficacy or safety parameters for elderly and non-elderly patients treated with trimethobenzamide. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function.

Gender

There is no FDA guidance on the use of Trimethobenzamide (injection) with respect to specific gender populations.

Race

There is no FDA guidance on the use of Trimethobenzamide (injection) with respect to specific racial populations.

Renal Impairment

A substantial route of elimination of unchanged trimethobenzamide is via the kidney. Dosage adjustment should be considered in patients with reduced renal function including some elderly patients.

Hepatic Impairment

There is no FDA guidance on the use of Trimethobenzamide (injection) in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Trimethobenzamide (injection) in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Trimethobenzamide (injection) in patients who are immunocompromised.

Administration and Monitoring

Administration

There is limited information regarding Trimethobenzamide (injection) Administration in the drug label.

Monitoring

There is limited information regarding Trimethobenzamide (injection) Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Trimethobenzamide (injection) and IV administrations.

Overdosage

There is limited information regarding Trimethobenzamide (injection) overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.

Pharmacology

Trimethobenzamide (injection)
Systematic (IUPAC) name
N-{[4-(2-dimethylaminoethoxy)phenyl]methyl}- 3,4,5-trimethoxy-benzamide
Identifiers
CAS number	138-56-7
ATC code	R06AA10
PubChem	5577
DrugBank	DB00662
Chemical data
Formula	Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox
Mol. mass	388.458 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	60-100%
Metabolism	?
Half life	7 to 9 hours (mean)
Excretion	urine (30-50%), faeces
Therapeutic considerations
Pregnancy cat.	C(US)
Legal status	[[Prescription drug|Template:Unicode-only]](US)
Routes	Oral, rectal, intramuscular

Mechanism of Action

The mechanism of action of trimethobenzamide hydrochloride as determined in animals is obscure, but may involve the chemoreceptor trigger zone (CTZ), an area in the medulla oblongata through which emetic impulses are conveyed to the vomiting center; direct impulses to the vomiting center apparently are not similarly inhibited. 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.

Structure

There is limited information regarding Trimethobenzamide (injection) Structure in the drug label.

Pharmacodynamics

There is limited information regarding Trimethobenzamide (injection) Pharmacodynamics in the drug label.

Pharmacokinetics

The pharmacokinetics of trimethobenzamide have been studied in healthy adult subjects. Following administration of 200 mg (100 mg/mL) trimethobenzamide hydrochloride IM injection, the time to reach maximum plasma concentration (Tmax) was about half an hour, about 15 minutes longer for trimethobenzamide hydrochloride 300 mg oral capsule than an IM injection. A single dose of trimethobenzamide hydrochloride 300 mg oral capsule provided a plasma concentration profile of trimethobenzamide similar to trimethobenzamide hydrochloride 200 mg IM. The relative bioavailability of the capsule formulation compared to the solution is 100%. The mean elimination half-life of trimethobenzamide is 7 to 9 hours. Between 30 – 50% of a single dose in humans is excreted unchanged in the urine within 48 – 72 hours. The metabolic disposition of trimethobenzamide in humans is not known. Specifically, it is not known if active metabolites are generated in humans.

Nonclinical Toxicology

There is limited information regarding Trimethobenzamide (injection) Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Trimethobenzamide (injection) Clinical Studies in the drug label.

How Supplied

Single Dose Vials, 2 mL, trays of 25 NDC 42023-143-25 100 mg/mL in 2 mL Single Dose Vials Multi-Dose Vials, 20 mL NDC 42023-142-01 100 mg/mL in 20 mL Multi-Dose Vials

Storage

Store between 20° to 25°C (68° to 77°F). (See USP Controlled Room Temperature.)

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Trimethobenzamide (injection) Patient Counseling Information in the drug label.

Precautions with Alcohol

Concomitant use of alcohol with trimethobenzamide hydrochloride may result in an adverse drug interaction.

Brand Names

There is limited information regarding Trimethobenzamide (injection) Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Trimethobenzamide (injection) Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.