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Trimethobenzamide

Pronunciation

(trye meth oh BEN za mide)

Index Terms

  • Trimethobenzamide HCl
  • Trimethobenzamide Hydrochloride

Dosage Forms

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

Capsule, Oral, as hydrochloride:

Tigan: 300 mg

Generic: 300 mg

Solution, Intramuscular, as hydrochloride:

Tigan: 100 mg/mL (2 mL)

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

Generic: 100 mg/mL (2 mL [DSC], 20 mL [DSC])

Brand Names: U.S.

  • Tigan

Pharmacologic Category

  • Antiemetic

Pharmacology

Acts centrally to inhibit the medullary chemoreceptor trigger zone by blocking emetic impulses to the vomiting center

Metabolism

Via oxidation, forms metabolite trimethobenzamide N-oxide

Excretion

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

Onset of Action

Oral: 10 to 40 minutes; IM: 15 to 35 minutes

Time to Peak

Oral: ~45 minutes; IM: ~30 minutes

Duration of Action

Oral: 3 to 4 hours; IM: 2 to 3 hours

Half-Life Elimination

7 to 9 hours

Use: Labeled Indications

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

Contraindications

Hypersensitivity to trimethobenzamide or any component of the formulation; injection contraindicated in children

Dosing: Adult

Nausea/vomiting:

Oral: 300 mg 3 or 4 times daily

IM: 200 mg 3 or 4 times daily

Dosing: Geriatric

According to the manufacturer, consider dosage reduction or increasing the dosing interval in elderly patients with renal impairment.

Dosing: Renal Impairment

CrCl ≤70 mL/minute/1.73 m2: Although no specific dosage adjustment provided in the manufacturer’s labeling, dosage reduction or increasing the dosing interval is recommended.

Dosing: Hepatic Impairment

No dosage adjustment provided in the manufacturer’s labeling.

Administration

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

Capsule: Administer capsule orally.

Storage

Capsules and injection: Store at room temperature of 25°C (77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F).

Drug Interactions

AbobotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of AbobotulinumtoxinA. Monitor therapy

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

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

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

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

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

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

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

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

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

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Avoid combination

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

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

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

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

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

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

OnabotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of OnabotulinumtoxinA. Monitor therapy

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

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Consider therapy modification

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

RimabotulinumtoxinB: Anticholinergic Agents may enhance the anticholinergic effect of RimabotulinumtoxinB. Monitor therapy

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid using drugs with substantial anticholinergic effects in patients receiving secretin whenever possible. If such agents must be used in combination, monitor closely for a diminished response to secretin. Consider therapy modification

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

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

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

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

Adverse Reactions

Frequency not defined.

Cardiovascular: Hypotension (IV administration)

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

Dermatologic: Allergic-type skin reactions

Gastrointestinal: Diarrhea

Hematologic: Blood dyscrasias

Hepatic: Jaundice

Local: Injection site burning, pain, redness, stinging, or swelling

Neuromuscular & skeletal: Muscle cramps, opisthotonos

Ocular: Blurred vision

Miscellaneous: Hypersensitivity reactions

Warnings/Precautions

Concerns related to adverse effects:

• CNS effects: The risk of CNS adverse effects (eg, coma, EPS, seizure) may be increased in patients with acute febrile illness, dehydration, electrolyte imbalance, encephalitis, and gastroenteritis; use with caution. 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).

• Extrapyramidal symptoms: May cause extrapyramidal symptoms (EPS) which may be confused with CNS symptoms of primary disease responsible for emesis.

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

Disease-related concerns:

• Renal impairment: Trimethobenzamide clearance is predominantly renal; consider dosage reductions in patients with renal impairment.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.

Special populations:

• Pediatric: Use capsule formulation with caution in children; antiemetics are not recommended for uncomplicated vomiting in children, limit antiemetic use to prolonged vomiting of known etiology. Use of injection is contraindicated in children.

Other warnings/precautions:

• Masking effects: May mask toxicity of other drugs or conditions (eg, appendicitis, Reye syndrome, or other encephalopathy) due to antiemetic effects.

Monitoring Parameters

Renal function (at baseline)

Pregnancy Considerations

Teratogenic effects were not observed in animal reproduction studies. Trimethobenzamide has been used to treat nausea and vomiting of pregnancy (ACOG, 2004).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience diarrhea, fatigue, headache, muscle cramps, or injection site pain, edema, or irritation. Have patient report immediately to prescriber severe dizziness, passing out, tremors, difficulty moving, rigidity, abnormal movements, change in balance, severe loss of strength and energy, blurred vision, depression, seizures, confusion, chills, pharyngitis, bruising, bleeding, or jaundice (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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