Trimethobenzamide: Drug information

For additional information see "Trimethobenzamide: Patient drug information" and "Trimethobenzamide: Pediatric drug information"

For abbreviations, symbols, and age group definitions 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: Liver 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recommendations for nausea and vomiting management do not suggest trimethobenzamide as a therapeutic option; use has been replaced by newer agents with greater efficacy and an improved safety profile (Ref).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: Liver 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): $36.38

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 deep IM only; not recommended for IV use. Follow institutional policy and procedures (manufacturer's labeling recommends 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 drug interactions program by clicking on the “Launch drug interactions program” link above.

Acrivastine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Agents with Clinically Relevant Anticholinergic Effects: May increase anticholinergic effects of Trimethobenzamide. Risk C: Monitor

Alcohol (Ethyl): May increase CNS depressant effects of Trimethobenzamide. Risk X: Avoid

Alizapride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Amisulpride (Oral): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Articaine: May increase CNS depressant effects of CNS Depressants. Management: Consider reducing the dose of articaine if possible when used in patients who are also receiving CNS depressants. Monitor for excessive CNS depressant effects with any combined use. Risk D: Consider Therapy Modification

Azelastine (Nasal): May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Benperidol: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Blonanserin: CNS Depressants may increase CNS depressant effects of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider Therapy Modification

Brexanolone: CNS Depressants may increase CNS depressant effects of Brexanolone. Risk C: Monitor

Brimonidine (Topical): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Bromopride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Bromperidol: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Buclizine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Buprenorphine: CNS Depressants may increase CNS depressant effects of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. Risk D: Consider Therapy Modification

BusPIRone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Cannabinoid-Containing Products: CNS Depressants may increase CNS depressant effects of Cannabinoid-Containing Products. Risk C: Monitor

Cetirizine (Systemic): May increase CNS depressant effects of CNS Depressants. Management: Consider avoiding this combination if possible. If required, monitor for excessive sedation or CNS depression, limit the dose and duration of combination therapy, and consider CNS depressant dose reductions. Risk D: Consider Therapy Modification

Chloral Hydrate/Chloral Betaine: CNS Depressants may increase CNS depressant effects of Chloral Hydrate/Chloral Betaine. Management: Consider alternatives to the use of chloral hydrate or chloral betaine and additional CNS depressants. If combined, consider a dose reduction of either agent and monitor closely for enhanced CNS depressive effects. Risk D: Consider Therapy Modification

Chlormethiazole: May increase CNS depressant effects of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Risk D: Consider Therapy Modification

Chlorphenesin Carbamate: May increase adverse/toxic effects of CNS Depressants. Risk C: Monitor

CNS Depressants: May increase adverse/toxic effects of CNS Depressants. Risk C: Monitor

Dantrolene: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Daridorexant: May increase CNS depressant effects of CNS Depressants. Management: Dose reduction of daridorexant and/or any other CNS depressant may be necessary. Use of daridorexant with alcohol is not recommended, and the use of daridorexant with any other drug to treat insomnia is not recommended. Risk D: Consider Therapy Modification

DexmedeTOMIDine: CNS Depressants may increase CNS depressant effects of DexmedeTOMIDine. Management: Monitor for increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of either agent to avoid excessive CNS depression. Risk D: Consider Therapy Modification

Difelikefalin: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Difenoxin: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Dihydralazine: CNS Depressants may increase hypotensive effects of Dihydralazine. Risk C: Monitor

Dimethindene (Topical): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Dothiepin: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Doxylamine: CNS Depressants may increase CNS depressant effects of Doxylamine. Risk C: Monitor

DroPERidol: May increase CNS depressant effects of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Risk D: Consider Therapy Modification

Emedastine (Systemic): May increase CNS depressant effects of CNS Depressants. Management: Consider avoiding this combination if possible. If required, monitor for excessive sedation or CNS depression, limit the dose and duration of combination therapy, and consider CNS depressant dose reductions. Risk C: Monitor

Entacapone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Esketamine (Nasal): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Flunarizine: CNS Depressants may increase CNS depressant effects of Flunarizine. Risk X: Avoid

Flunitrazepam: CNS Depressants may increase CNS depressant effects of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Risk D: Consider Therapy Modification

HydrOXYzine: May increase CNS depressant effects of CNS Depressants. Management: Consider a decrease in the CNS depressant dose, as appropriate, when used together with hydroxyzine. Increase monitoring of signs/symptoms of CNS depression in any patient receiving hydroxyzine together with another CNS depressant. Risk D: Consider Therapy Modification

Ixabepilone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Kava Kava: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Ketotifen (Systemic): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Kratom: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Lemborexant: May increase CNS depressant effects of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Risk D: Consider Therapy Modification

Levocetirizine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Levosulpiride: Benzamide Derivatives may increase adverse/toxic effects of Levosulpiride. Risk C: Monitor

Lisuride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Lofepramine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Lofexidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Loxapine: CNS Depressants may increase CNS depressant effects of Loxapine. Management: Consider reducing the dose of CNS depressants administered concomitantly with loxapine due to an increased risk of respiratory depression, sedation, hypotension, and syncope. Risk D: Consider Therapy Modification

Magnesium Sulfate: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Melitracen [INT]: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Mequitazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Metergoline: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Methotrimeprazine: CNS Depressants may increase CNS depressant effects of Methotrimeprazine. Methotrimeprazine may increase CNS depressant effects of CNS Depressants. Management: Reduce the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D: Consider Therapy Modification

Methoxyflurane: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Metoclopramide: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

MetyroSINE: CNS Depressants may increase sedative effects of MetyroSINE. Risk C: Monitor

Minocycline (Systemic): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Moxonidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Nabilone: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Nalfurafine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Noscapine: CNS Depressants may increase adverse/toxic effects of Noscapine. Risk X: Avoid

Olopatadine (Nasal): May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Opicapone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Opioid Agonists: CNS Depressants may increase CNS depressant effects of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider Therapy Modification

Opipramol: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Orphenadrine: CNS Depressants may increase CNS depressant effects of Orphenadrine. Risk X: Avoid

Oxomemazine: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Oxybate Salt Products: CNS Depressants may increase CNS depressant effects of Oxybate Salt Products. Management: Consider alternatives to this combination when possible. If combined, dose reduction or discontinuation of one or more CNS depressants (including the oxybate salt product) should be considered. Interrupt oxybate salt treatment during short-term opioid use Risk D: Consider Therapy Modification

OxyCODONE: CNS Depressants may increase CNS depressant effects of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider Therapy Modification

Paliperidone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Paraldehyde: CNS Depressants may increase CNS depressant effects of Paraldehyde. Risk X: Avoid

Perampanel: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Periciazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Pipamperone: May increase adverse/toxic effects of CNS Depressants. Risk C: Monitor

Piribedil: CNS Depressants may increase CNS depressant effects of Piribedil. Risk C: Monitor

Pizotifen: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Pramipexole: CNS Depressants may increase sedative effects of Pramipexole. Risk C: Monitor

Procarbazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Rilmenidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Ropeginterferon Alfa-2b: CNS Depressants may increase adverse/toxic effects of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider Therapy Modification

ROPINIRole: CNS Depressants may increase sedative effects of ROPINIRole. Risk C: Monitor

Rotigotine: CNS Depressants may increase sedative effects of Rotigotine. Risk C: Monitor

Suvorexant: CNS Depressants may increase CNS depressant effects of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Risk D: Consider Therapy Modification

Thalidomide: CNS Depressants may increase CNS depressant effects of Thalidomide. Risk X: Avoid

Trimeprazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Valerian: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Zolpidem: CNS Depressants may increase CNS depressant effects of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk D: Consider Therapy Modification

Zuranolone: May increase CNS depressant effects of CNS Depressants. Management: Consider alternatives to the use of zuranolone with other CNS depressants or alcohol. If combined, consider a zuranolone dose reduction and monitor patients closely for increased CNS depressant effects. Risk D: Consider Therapy Modification

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

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]
Brunton LL, Hilal-DanDan R, Knollmann BC. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 13th ed. McGraw Hill; 2018.
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]
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]
Managing acute gastroenteritis among children: oral rehydration, maintenance, and nutritional therapy. MMWR Recomm Rep. 2003;52(RR-16):1-16.
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]
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]
Mokha J. Vomiting and nausea. In: Wyllie R, ed. Pediatric Gastrointestinal and Liver Disease. 6th ed. 2021: chap. 8.
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]
Tigan injectable (trimethobenzamide) [prescribing information]. Malvern, PA: Endo USA; August 2024.
Tigan oral (trimethobenzamide) [prescribing information]. New York, NY: Pfizer Inc; March 2017.

Topic 10023 Version 293.0

خرید پکیج

Trimethobenzamide: Drug information