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Trimethobenzamide: Drug information

Trimethobenzamide: Drug information
(For additional information see "Trimethobenzamide: Patient drug information" and see "Trimethobenzamide: Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Tigan
Pharmacologic Category
  • Antiemetic
Dosing: Adult
Nausea/vomiting

Nausea/vomiting: Note: Use the lowest effective dosage based on response and tolerability.

IM: 200 mg 3 or 4 times daily.

Oral: 300 mg 3 or 4 times daily.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

CrCl >70 mL/minute/1.73 m2: There are no dosage adjustments provided in the manufacturer's labeling.

CrCl ≤70 mL/minute/1.73 m2: Reduce the dose or increase the dosing interval and adjust as needed based on patient response; monitor renal function closely.

Dosing: Hepatic Impairment: Adult

Avoid use in patients with hepatic impairment (due to potential risk of hepatotoxicity).

Dosing: Older Adult

Refer to adult dosing; reduce the dose or increase the dosing interval and adjust as needed based on patient response.

Dosing: Pediatric

(For additional information see "Trimethobenzamide: Pediatric drug information")

Note: Use of the oral capsule in pediatric patients is strongly discouraged due to risk of extrapyramidal symptoms (EPS), serious CNS effects, and other adverse reactions. Parenteral formulations are contraindicated in pediatric patients.

Nausea and vomiting, refractory

Nausea and vomiting, refractory: Limited data available: Note: Not recommended for routine use in pediatric patients due to safety concerns (eg, EPS, serious CNS effects); expert recommendations for nausea and vomiting management do not suggest trimethobenzamide as a therapeutic option; use has been replaced by newer agents with greater efficacy and an improved safety profile (Ref).

Children weighing ≥14 kg and Adolescents: Oral: 100 to 200 mg every 6 to 8 hours as needed (Ref). Note: An appropriate dosage form to achieve pediatric doses may not be available in all areas.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

There are no pediatric-specific dosing recommendations; based on experience in adult patients, dosing adjustment suggested.

Dosing: Hepatic Impairment: Pediatric

Avoid use in patients with hepatic impairment (due to potential risk of hepatotoxicity).

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

Frequency not defined.

Cardiovascular: Hypotension (IV administration)

Central nervous system: Coma, depression, disorientation, dizziness, drowsiness, extrapyramidal reaction, headache, opisthotonos, Parkinsonian-like symptoms, seizure

Dermatologic: Allergic skin reaction

Gastrointestinal: Diarrhea

Hematologic & oncologic: Hematologic disease

Hepatic: Jaundice

Hypersensitivity: Hypersensitivity reaction

Local: Burning sensation at injection site, erythema at injection site, pain at injection site, swelling at injection site

Neuromuscular & skeletal: Muscle cramps

Ophthalmic: Blurred vision

Contraindications

Hypersensitivity to trimethobenzamide or any component of the formulation; use in pediatric patients (injection only)

Warnings/Precautions

Concerns related to adverse effects:

• CNS effects: CNS serious adverse effects (eg, coma, mood depression, disorientation, seizure) have been reported. Consider reducing the daily dosage by increasing the dosing interval or discontinuing use if serious CNS reactions occur. May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Recent or concomitant use of other medications causing CNS depression or adverse events may increase the risk of serious CNS reactions.

• Extrapyramidal symptoms: May cause extrapyramidal symptoms (EPS), primarily acute dystonic reactions (ie, sudden onset of muscular spasms usually in the head/neck or opisthotonos); other EPS (akathisia, restlessness, akinesia, other parkinsonian-like symptoms [eg, tremor]), laryngospasm, dysphagia, oculogyric crisis) may also occur. If EPS occurs, reduce the daily dosage by increasing the dosing interval or discontinue therapy, depending on the severity of symptoms. Treat acute dystonic reactions with anticholinergics. Avoid use in patients receiving concomitant therapy (eg, antipsychotics) that cause EPS.

• Hepatotoxicity: Use may potentially cause hepatotoxicity. If hepatic impairment occurs during therapy, discontinue use.

• Skin reactions: Allergic-type skin reactions have been reported with use; discontinue with signs of sensitization.

Disease-related concerns:

• Hepatic impairment: Avoid use in patients with hepatic impairment.

• Renal impairment: Use with caution in patients with renal impairment; clearance is predominantly renal; dosage reduction recommended in patients with CrCl ≤70 mL/minute/1.73 m2.

Special populations:

• Pediatric: Injection is contraindicated in pediatric patients. Oral formulation is not FDA approved for use in pediatrics due to risk of EPS, serious CNS effects, and other potential adverse effects associated with use.

Other warnings/precautions:

• Masking effects: EPS and other CNS effects that may result from use may mask signs of an undiagnosed primary disease (eg, encephalopathy, metabolic imbalance, Reye syndrome). If CNS symptoms occur, evaluate the risks vs. benefits of continuing therapy.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Capsule, Oral, as hydrochloride:

Tigan: 300 mg [DSC]

Generic: 300 mg

Solution, Intramuscular, as hydrochloride:

Tigan: 100 mg/mL (2 mL)

Tigan: 100 mg/mL (20 mL [DSC]) [contains phenol]

Generic Equivalent Available: US

May be product dependent

Pricing: US

Capsules (Trimethobenzamide HCl Oral)

300 mg (per each): $2.08 - $21.60

Solution (Tigan Intramuscular)

100 mg/mL (per mL): $30.12

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

IM: Administer IM only; not recommended for IV use. Inject deep into upper outer quadrant of gluteal muscle.

Administration: Pediatric

Oral: Administer by mouth.

Use: Labeled Indications

Nausea/vomiting: Treatment of postoperative nausea and vomiting; treatment of nausea associated with gastroenteritis

Medication Safety Issues
Sound-alike/look-alike issues:

Tigan may be confused with Tiazac, Ticlid

Trimethobenzamide may be confused with metoclopramide, trimethoprim

Pediatric patients: High-risk medication:

KIDs List: Dopamine antagonists, when used in pediatric patients <18 years of age, are identified on the Key Potentially Inappropriate Drugs in Pediatrics (KIDs) list; use should be avoided in infants and used with caution in children and adolescents due to risk of acute dystonia (dyskinesia) (weak recommendation; moderate quality of evidence) (PPA [Meyers 2020]).

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Risk C: Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Alcohol (Ethyl): May enhance the CNS depressant effect of Trimethobenzamide. Risk C: Monitor therapy

Amantadine: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Risk C: Monitor therapy

Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Risk C: Monitor therapy

Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Risk C: Monitor therapy

Chlorprothixene: Anticholinergic Agents may enhance the anticholinergic effect of Chlorprothixene. Risk C: Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Risk X: Avoid combination

CloZAPine: Anticholinergic Agents may enhance the constipating effect of CloZAPine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for signs and symptoms of gastrointestinal hypomotility and consider prophylactic laxative treatment. Risk D: Consider therapy modification

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Risk X: Avoid combination

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Risk C: Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Risk C: Monitor therapy

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Risk X: Avoid combination

Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Risk C: Monitor therapy

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Risk X: Avoid combination

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C: Monitor therapy

Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Risk C: Monitor therapy

Opioid Agonists: Anticholinergic Agents may enhance the adverse/toxic effect of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination. Risk C: Monitor therapy

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Risk X: Avoid combination

Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium citrate. Risk X: Avoid combination

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Risk X: Avoid combination

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Risk C: Monitor therapy

Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Risk X: Avoid combination

Rivastigmine: Anticholinergic Agents may diminish the therapeutic effect of Rivastigmine. Rivastigmine may diminish the therapeutic effect of Anticholinergic Agents. Management: Use of rivastigmine with an anticholinergic agent is not recommended unless clinically necessary. If the combination is necessary, monitor for reduced anticholinergic effects. Risk D: Consider therapy modification

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Risk D: Consider therapy modification

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Risk X: Avoid combination

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Risk C: Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Pregnancy Considerations

Although use for the treatment of nausea and vomiting in pregnancy has been reported (Milkovich 1976; Pretorius 1961), use of other agents is preferred (ACOG 189 2018).

Breastfeeding Considerations

It is not known if trimethobenzamide is present in breast milk. According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should take into account the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.

Monitoring Parameters

Renal function in elderly patients and patients with reduced renal function.

Mechanism of Action

Acts centrally as a dopamine (D2) receptor antagonist at the medullary chemoreceptor trigger zone to block emetic impulses to the vomiting center (Brunton 2018).

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: Oral: 10 to 40 minutes; IM: 15 to 35 minutes

Duration of action: Oral: 3 to 4 hours; IM: 2 to 3 hours

Metabolism: Via oxidation, forms metabolite trimethobenzamide N-oxide

Bioavailability: Oral dose is 100% of IM dose

Half-life elimination: 7 to 9 hours

Time to peak: Oral: ~45 minutes; IM: ~30 minutes

Excretion: Urine (30% to 50%, as unchanged drug)

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (PR) Puerto Rico: Tigan | Trimethobenzamide;
  • (TR) Turkey: Anti vomit | Emedur | Vomitin | Voselmit
  1. American College of Obstetricians and Gynecologists (ACOG) Committee on Practice Bulletins-Obstetrics. ACOG Practice Bulletin No. 189: Nausea and vomiting of pregnancy. Obstet Gynecol. 2018;131(1):e15-e30. doi: 10.1097/AOG.0000000000002456. [PubMed 29266076]
  2. Brunton LL, Hilal-DanDan R, Knollmann BC. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 13th ed. McGraw Hill; 2018.
  3. Gan TJ, Belani KG, Bergese S, et al. Fourth consensus guidelines for the management of postoperative nausea and vomiting. Anesth Analg. 2020;131(2):411-448. doi:10.1213/ANE.0000000000004833 [PubMed 32467512]
  4. Gan TJ, Diemunsch P, Habib AS, et al. Consensus guidelines for the management of postoperative nausea and vomiting. Anesth Analg. 2014;118(1):85-113. [PubMed 24356162]
  5. Managing acute gastroenteritis among children: oral rehydration, maintenance, and nutritional therapy. MMWR Recomm Rep. 2003;52(RR-16):1-16.
  6. Meyers RS, Thackray J, Matson KL, et al. Key Potentially Inappropriate Drugs in Pediatrics: The KIDs List. J Pediatr Pharmacol Ther. 2020;25(3):175-191. [PubMed 32265601]
  7. Milkovich L, van den Berg BJ. An evaluation of the teratogenicity of certain antinauseant drugs. Am J Obstet Gynecol. 1976;125(2):244-248. [PubMed 773181]
  8. Mokha J. Vomiting and nausea. In: Wyllie R, ed. Pediatric Gastrointestinal and Liver Disease. 6th ed. 2021: chap. 8.
  9. Pretorius HM, Quinlan DK. Nausea and vomiting in pregnancy. A report of a new drug trimethobenzamide (Tigan). S Afr Med J. 1961;35:1090. [PubMed 14488683]
  10. Tigan injectable (trimethobenzamide) [prescribing information]. Chestnut Ridge, NY: Par Pharmaceutical; January 2022.
  11. Tigan oral (trimethobenzamide) [prescribing information]. New York, NY: Pfizer Inc; March 2017.
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