Trimethobenzamide

Pronunciation

(trye meth oh BEN za mide)

U.S. Brand Names

Tigan®

Synonyms

Trimethobenzamide Hydrochloride

Generic Available

Yes: Injection

Canadian Brand Names

Tigan®

Use

Treatment of nausea and vomiting

Pregnancy Risk Factor

Lactation

Excretion in breast milk unknown

Contraindications

Hypersensitivity to trimethobenzamide, benzocaine (or similar local anesthetics), or any component of the formulation; injection contraindicated in children; suppositories contraindicated in premature infants or neonates

Warnings/Precautions

May mask emesis due to Reye's syndrome or mimic CNS effects of Reye's syndrome in patients with emesis of other etiologies; use in patients with acute vomiting should be avoided. May cause drowsiness; patient should avoid tasks requiring alertness (eg, driving, operating machinery). May cause extrapyramidal symptoms (EPS) which may be confused with CNS symptoms of primary disease responsible for emesis.

Adverse Reactions

Frequency not defined.

Cardiovascular: Hypotension

Central nervous system: Coma, depression, disorientation, dizziness, drowsiness, EPS, headache, opisthotonos, Parkinson-like syndrome, seizure

Hematologic: Blood dyscrasias

Hepatic: Jaundice

Neuromuscular & skeletal: Muscle cramps

Ocular: Blurred vision

Miscellaneous: Hypersensitivity reactions

Overdosage/Toxicology

Symptoms of overdose include hypotension, seizures, CNS depression, cardiac arrhythmias, disorientation, and confusion. Treatment is symptom-directed and supportive.

Ethanol/Nutrition/Herb Interactions

Ethanol: Concomitant use should be avoided.

Stability

Store capsules, injection solution, and suppositories at room temperature.

Mechanism of Action

Acts centrally to inhibit the medullary chemoreceptor trigger zone

Pharmacodynamics/Kinetics

Onset of action: Antiemetic: Oral: 10-40 minutes; I.M.: 15-35 minutes

Duration: 3-4 hours

Absorption: Rectal: ~60%

Bioavailability: Oral: 100%

Half-life elimination: 7-9 hours

Time to peak: Oral: 45 minutes; I.M.: 30 minutes

Excretion: Urine (30% to 50%)

Dosage

Rectal use is contraindicated in neonates and premature infants

Children:

<14 kg: Oral, rectal: 100 mg 3-4 times/day

14-40 kg: Oral, rectal: 100-200 mg 3-4 times/day

Adults:

Oral: 250-300 mg 3-4 times/day

I.M., rectal: 200 mg 3-4 times/day

Administration

Administer I.M. only; inject deep into upper outer quadrant of gluteal muscle

Patient Education

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. Take as directed before meals; do not increase dose and do not discontinue without consulting prescriber. May cause drowsiness or blurred vision (use caution when driving or engaging in tasks that require alertness until response to drug is known) or diarrhea (buttermilk or yogurt may help). Report chest pain or palpitations, persistent dizziness or blurred vision, or CNS changes (disorientation, depression, confusion). Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

Drowsiness is common; may cause dizziness; may rarely cause depression

Mental Health: Effects on Psychiatric Treatment

Concurrent use with psychotropics may produce additive sedation

Oncology: Emetic Potential

Very low (<10%)

Oncology: Vesicant

Dosage Forms

[DSC] = Discontinued product

Capsule, as hydrochloride: 300 mg

Tigan®: 300 mg

Injection, solution, as hydrochloride: 100 mg/mL (2 mL)

Tigan®: 100 mg/mL (2 mL, 20 mL)

Suppository, rectal, as hydrochloride (Tigan®): 100 mg [DSC], 200 mg [contains benzocaine]

References

Ginsburg CM and Clahsen J, "Evaluation of Trimethobenzamide Hydrochloride (Tigan®) Suppositories for Treatment of Nausea and Vomiting in Children," J Pediatr , 1980, 96(4):767-9.

Hurley JD and Eshelman FN, "Trimethobenzamide HCl in the Treatment of Nausea and Vomiting Associated With Antineoplastic Chemotherapy," J Clin Pharmacol , 1980, 20(5-6 Pt1):352-6.

Kaan SK and Eshelman FN, "The Antiemetic Effects of Trimethobenzamide During Chemotherapy: A Controlled Study," Curr Ther Res , 1979, 26:210-3.

International Brand Names

Ametik® (TR); Anti-Vomit® (TR); Emedur® (TR); Emetol® (TR); Tigan® (CA); Vomet® (TR); Vomitin® (TR)

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