Trimethobenzamide

The mechanism of action of trimethobenzamide 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.

• Trimethobenzamide hydrochloride capsules is indicated in adults for the treatment of postoperative nausea and vomiting and for nausea associated with gastroenteritis. Limitation of Use: Trimethobenzamide hydrochloride capsules is not recommended for use in pediatric patients due to the risk of extrapyramidal signs and symptoms and other serious central nervous system (CNS) effects, and the risk of exacerbation of the underlying disease in pediatric patients with Reye's syndrome or other hepatic impairment.ICD-10: R11.2

• Trimethobenzamide hydrochloride capsules are contraindicated in patients with known hypersensitivity to trimethobenzamide [see Adverse Reactions ( 6 )] .contraindicated

• The recommended adult dosage is 300 mg orally three or four times daily. ( 2.1 ) • Geriatric patients and/or patients with renal impairment (creatinine clearance 70 mL/min/1.73m2 or less): Reduce the daily dosage by increasing the dosing interval; monitor renal function. ( 2.2 , 8.5 , 8.6 ) • Select the lowest effective daily dosage and adjust as needed based upon therapeutic response and tolerability. ( 2.1 , 2.2 ) 2.1 Recommended Adult Dosage The recommended adult dosage is 300 mg orally three or four times daily. Select the lowest effective daily dosage and adjust as needed based upon therapeutic response and tolerability. 2.2 Dosage Adjustment for Geriatric Patients and/or Patients with Renal Impairment In geriatric patients and/or in patients with renal impairment (creatinine clearance 70 mL/min/1.73m2 or less), reduce the daily dosage of trimethobenzamide hydrochloride capsules by increasing the dosing interval and adjust as needed based upon therapeutic response and tolerability. Monitor renal function [see Use in Specific Populations ( 8.5 , 8.6 )] .

Acute Dystonic Reactions and Other Extrapyramidal Symptoms (EPS) : Depending on the severity of symptoms, reduce the dosage or discontinue the drug. Treat acute dystonic reactions with anticholinergics. Avoid trimethobenzamide hydrochloride capsules in patients receiving other drugs that are likely to cause EPS. ( 5.1 , 7.2 ) Masking of Other Serious Disorders : EPS and other CNS symptoms in patients treated with trimethobenzamide hydrochloride capsules may be confused with CNS signs of undiagnosed primary disease (e.g., encephalopathy, metabolic imbalance, Reye's Syndrome). If CNS symptoms occur, evaluate the risks and benefits of continuing trimethobenzamide hydrochloride capsules. ( 5.2 , 7.2 ) Other CNS Reactions : Coma, depression of mood, disorientation, and seizures have been reported. The recent use of other drugs that cause CNS depression or EPS symptoms may also increase the risk; consider reducing the dosage or discontinuing the drug. ( 5.3 , 7.1 , 7.2 ) Hepatotoxicity : Avoid use in patients whose signs and symptoms suggest the presence of hepatic impairment. Discontinue trimethobenzamide hydrochloride capsules in patients who develop impaired liver function while on treatment. ( 5.4 , 8.7 ) Effects on the Ability to Drive or Operate Machinery : Mental and/or physical abilities may be impaired. Concomitant use of other drugs that cause CNS depression or EPS symptoms may increase this effect; either trimethobenzamide hydrochloride capsules or the other interacting drug should be chosen, depending on the importance of the drug to the patient.

The following adverse reactions from voluntary reports or clinical studies have been reported with trimethobenzamide. Because many of these reactions were reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Nervous system disorders: Parkinson-like symptoms, coma, convulsions, opisthotonos, dizziness, drowsiness, headache, [see Warnings and Precautions ( 5.1 , 5.2 , 5.3 )] Psychiatric disorders: disorientation, depression of mood Eye disorders: blurred vision Hematologic disorders: blood dyscrasias Hepatobiliary disorders: jaundice [see Warnings and Precautions ( 5.4 )] Immune system disorders: hypersensitivity, including angioedema and allergic-type skin reactions Gastrointestinal disorders: diarrhea Musculoskeletal disorders: muscle cramps Adverse reactions include hypersensitivity reactions and Parkinson-like symptoms; blood dyscrasias, blurring of vision, coma, convulsions, depression of mood, diarrhea, disorientation, dizziness, drowsiness, headache, jaundice, muscle cramps, and opisthotonos. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Lupin Pharmaceuticals, Inc. at 1-866-403-7592 or FDA at 1-800-FDA-1088 or WWW.FDA.GOV/MEDWATCH .

8.1 Pregnancy Risk Summary The limited available data with trimethobenzamide in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriage. No adverse developmental effect was observed in animal reproduction studies with administration of trimethobenzamide hydrochloride during organogenesis in pregnant rats at doses 0.16 and 0.8 times the recommended human dose (RHD) and in pregnant rabbits at doses 1.6 times the RHD [see Data ]. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data Reproduction studies with trimethobenzamide hydrochloride were conducted in rats and rabbits following administration of trimethobenzamide hydrochloride during organogenesis and no adverse developmental effect was observed in either species.

Metabolism

Absorption The pharmacokinetics of trimethobenzamide in healthy adult subjects were compared when trimethobenzamide hydrochloride capsules was administered as a 300 mg oral capsule or a 200 mg (100 mg/mL) intramuscular injection. The time to reach maximum plasma concentration (Tmax) was about 30 minutes after intramuscular injection compared to about 45 minutes after oral capsule administration.

• Jul 12, 1974NDANDA017530Ph Health
• Aug 20, 2003ANDAANDA076546Lupin
• Nov 21, 2023ANDAANDA205950Heritage Pharma Avet

1. 1Nausea33223%
2. 2Somnolence22816%
3. 3Dizziness16612%
4. 4Vomiting1329.3%
5. 5Yawning1218.6%
6. 6Drug Ineffective1027.2%
7. 7Blood Pressure Decreased1017.1%
8. 8Fatigue906.4%
9. 9Fall785.5%
10. 10Blood Pressure Increased684.8%
11. 11Feeling Abnormal664.7%
12. 12Drug Hypersensitivity624.4%
13. 13Asthenia594.2%
14. 14Hyperhidrosis553.9%
15. 15Pain553.9%

The 9 most recently updated of 9 ClinicalTrials.gov registrations naming Trimethobenzamide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Sixth Generation High-sensitivity Cardiac Troponin T for the Early Rule Out of Myocardial Infarction: a Controlled Before and After Study
  Not yet recruiting · Interventional · 19,500 enrolled · University of Edinburgh
  NCT07636642updated 2026-06-09
• A Study to Investigate the Safety, Tolerability, and Pharmacokinetics of PF-06649751 in Subjects With Idiopathic Parkinson's Disease
  Completed · Phase 1 · Interventional · 18 enrolled · Pfizer
  NCT02373072updated 2023-09-22
• Apokyn for Motor IMProvement of Morning AKinesia Trial (AM IMPAKT)
  Completed · Phase 4 · Interventional · 127 enrolled · MDD US Operations, LLC a subsidiary of Supernus Pharmaceuticals
  NCT01770145updated 2023-08-14
• TICON-Day 3, Time Lapse Versus Conventional Method in Day 3 Embryo Culture and Assessment
  Terminated · Phase 4 · Interventional · 408 enrolled · Merck KGaA, Darmstadt, Germany
  NCT03164551updated 2020-12-02
• To Evaluate the Efficacy and Safety of Aspherical Soft Contact Lens in Myopia Control
  Completed · Interventional · 72 enrolled · APP Vision Care Inc.
  NCT04238897updated 2020-01-23
• PET Scanning of Adults With Attention Deficit Hyperactivity Disorder (ADHD)
  Completed · Observational · 16 enrolled · National Institute of Mental Health (NIMH)
  NCT00397748updated 2019-12-16
• Safety/Efficacy of Tigan® to Control Nausea/Vomiting Experienced During Apokyn® Initiation and Treatment
  Completed · Phase 4 · Interventional · 117 enrolled · Ipsen
  NCT00489255updated 2019-01-30
• Corneal Staining Associated With Daily Disposable Beauty Contact Lenses
  Terminated · Interventional · 35 enrolled · Johnson & Johnson Vision Care, Inc.
  NCT01882465updated 2018-06-19
• A Study to Investigate the Safety, Tolerability, and Pharmacokinetics of PF-06649751 Co-administered With Trimethobenzamide Hydrochloride in Healthy Subjects
  Completed · Phase 1 · Interventional · 9 enrolled · Pfizer
  NCT02262767updated 2015-01-14

Frequently asked questions

How does Trimethobenzamide work?

The mechanism of action of trimethobenzamide 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.

What is Trimethobenzamide used for?

According to FDA labeling, Trimethobenzamide carries indications including: Trimethobenzamide hydrochloride capsules is indicated in adults for the treatment of postoperative nausea and vomiting and for nausea associated with gastroenteritis. Limitation of Use: Trimethobenzamide hydrochloride capsules is not recommended for use in pediatric patients due to the risk of extrapyramidal signs and symptoms and other serious central nervous system (CNS) effects, and the risk of exacerbation of the underlying disease in pediatric patients with Reye's syndrome or other hepatic impairment.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Trimethobenzamide?

Trimethobenzamide is classified as Aminoalkyl ethers, Antiemetic, Physiochemical Activity, Decreased Central Nervous System Acetylcholine Activity, Emesis Suppression.

What are the brand names for Trimethobenzamide?

Trimethobenzamide is marketed under brand names including Tigan.

What are the contraindications for Trimethobenzamide?

Trimethobenzamide labeling lists contraindications including: Trimethobenzamide hydrochloride capsules are contraindicated in patients with known hypersensitivity to trimethobenzamide [see Adverse Reactions ( 6 )] .. Always consult the full prescribing information and a clinician.