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Chemically, trimethobenzamide HCl is N-[p-[2-(dimethylamino)-ethoxy]benzyl]-3,4,5-trimethoxybenzamide hydrochloride. It has a molecular weight of 424.93 and the following structural formula:
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Capsules: Each 100-mg Tigan ® capsule for oral use contains trimethobenzamide hydrochloride equivalent to 100 mg. The capsule has an opaque blue cap marked "Tigan" and an opaque white body marked "M186". Each 250-mg Tigan ® capsule for oral use contains trimethobenzamide hydrochloride equivalent to 250 mg. The capsule has an opaque blue cap marked "Tigan" and an opaque blue body marked "M187".
Inactive Ingredients: FD&C Blue No. 1, FD&C Red No. 3, lactose, magnesium stearate, starch and titanium dioxide.
Suppositories (200 mg): Each suppository contains 200 mg trimethobenzamide hydrochloride and 2% benzocaine in a base compounded with polysorbate 80, white beeswax and propylene glycol monostearate.
Suppositories, Pediatric (100 mg): Each suppository contains 100 mg trimethobenzamide hydrochloride and 2% benzocaine in a base compounded with polysorbate 80, white beeswax and propylene glycol monostearate.
Ampuls: Each 2-mL ampul contains 200 mg trimethobenzamide hydrochloride compounded with 0.2% parabens (methyl and propyl) as preservatives, 1 mg sodium citrate and 0.4 mg citric acid as buffers and pH adjusted to approximately 5.0 with sodium hydroxide.
Multi-Dose Vials: Each mL contains 100 mg trimethobenzamide hydrochloride compounded with 0.45% phenol as preservative, 0.5 mg sodium citrate and 0.2 mg citric acid as buffers and pH adjusted to approximately 5.0 with sodium hydroxide.
The mechanism of action of Tigan ® as determined in animals is obscure, but may be 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.
Tigan ® is indicated for the control of nausea and vomiting.
The injectable form of Tigan ® in children, the suppositories in premature or newborn infants, and use in patients with known hypersensitivity to trimethobenzamide are contraindicated. Since the suppositories contain benzocaine they should not be used in patients known to be sensitive to this or similar local anesthetics.
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Caution should be exercised when administering Tigan ® to children for the treatment of vomiting. Antiemetics are not recommended for treatment of uncomplicated vomiting in children and their use should be limited to prolonged vomiting of known etiology. There are three principal reasons for caution:
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Tigan ® may produce drowsiness. Patients should not operate motor vehicles or other dangerous machinery until their individual responses have been determined. Reye' syndrome has been associated with the use of Tigan ® and other drugs, including antiemetics, although their contribution, if any, to the cause and course of the disease has not been established. This syndrome is characterized by an abrupt onset shortly following a non-specific febrile illness, with persistent, sever vomiting, lethargy, irrational behavior, progressive encephalopathy leading to coma, convulsions and death.
Usage in Pregnancy: Trimethobenzamide hydrochloride was studied in reproduction experiments in rats and rabbits and no teratogenicity was suggested. The only effects observed were an increased percentage of embryonic resorptions or stillborn pups in rats administered 20 mg and 100 mg/kg and increased resorptions in rabbits receiving 100 mg/kg. In each study these adverse effects were attributed to one or two dams. The relevance to humans is not known. Since there is no adequate experience in pregnant or lactating women who have received this drug, safety in pregnancy or in nursing mothers has not been established.
Usage with Alcohol: Concomitant use of alcohol with Tigan ® may result in an adverse drug interaction.
During the course of acute febrile illness, encephalitides, gastroenteritis, dehydration and electrolyte imbalance, especially in children and the elderly or debilitated, CNS reactions such as opisthotonos, convulsions, coma and extrapyramidal symptoms have been reported with and without use of Tigan ® (trimethobenzamide hydrochloride) or other antiemetic agents. In such disorders caution should be exercised in administering Tigan ®, particularly to patients who have recently received other CNS-acting agents (phenothiazines, barbiturates, belladonna derivatives). It is recommended that severe emesis should not be treated with an antiemetic drug alone; where possible the cause of vomiting should be established. Primary emphasis should be directed toward the restoration of body fluids and electrolyte balance, the relief of fever and relief of the causative disease processes. Overhydration should be avoided since it may result in cerebral edema.
The antiemetic effects of Tigan ® may render diagnosis more difficult in such conditions as appendicitis and obscure signs of toxicity due to overdosage of other drugs.
There have been reports of hypersensitivity reactions and Parkinson-like symptoms. There have been instances of hypotension reported following parenteral administration to surgical patients. There have been reports of blood dyscrasias, blurring of vision, coma, convulsions, depression of mood, diarrhea, disorientation, dizziness, drowsiness, headache, jaundice, muscle cramps and opisthotonos. If these occur, the administration of the drug should be discontinued. Allergic-type skin reactions have been observed; therefore, the drug should be discontinued at the first sign of sensitization. While all symptoms will usually disappear spontaneously, symptomatic treatment may be indicated in some cases.
(See and PRECAUTIONS .)
Dosage should be adjusted according to the indication for therapy, severity of symptoms and the repsonse of the patient.
CAPSULES, 250 mg and 100 mg
One 250 mg capsule t.i.d. or q.i.d.
Usual Children's Dosage
30 to 90 lbs: One or two 100 mg capsules t.i.d. or q.i.d.
SUPPOSITORIES, 200 mg (not to be used in premature or newborn infants)
One suppository (200 mg) t.i.d. or q.i.d.
Usual Children's Dosage
Under 30 lbs: One-half suppository (100 mg) t.i.d. or q.i.d.
30 to 90 lbs: One-half to one suppository (100 to 200 mg) t.i.d. or q.i.d.
SUPPOSITORIES, PEDIATRIC, 10 mg (not to be used in premature or newborn infants)
Usual Children's Dosage
Under 30 lbs: One suppository (100 mg) t.i.d. or q.i.d.
30 to 90 lbs: One to two suppositories (100 to 200 mg) t.i.d. or q.i.d.
INJECTABLE, 100 mg (not for use in children)
2 mL (200 mg) t.i.d. or q.i.d. intramuscularly
NOTE: The injectable form is intended for intramuscular administration only; it is not recommended for intravenous use.
Intramuscular administration may cause pain, stinging, burning, redness and swelling at the site of injection. Such effects may be minimized by deep injection into the upper outer quadrant of the gluteal region, and by avoiding the escape of solution along the route.
Rx Only.
Store Tigan® from 15° to 30°C (59° to 86°F).
Capsules, 100 mg trimethobenzamide hydrochloride each, bottles of 100; 250 mg trimethobenzamide hydrochloride each, bottles of 100 and 500
NDC 61570-186-01 100 mg 100's
NDC 61570-187-01 250 mg 100's
NDC 61570-187-05 250 mg 500's
Suppositories, Pediatric, 100 mg, boxes of 10
Suppositories, 200 mg, boxes of 10 and 50
NDC 61570-503-10 100 mg (box of 10)
NDC 61570-504-10 200 mg (box of 10)
NDC 61570-504-50 200 mg (box of 50)
Ampuls, 2 mL, boxes of 10
NDC 61570-540-02 100 mg/mL in 2 mL ampul
Multi-Dose Vials, 20 mL
NDC 61570-541-20 100 mg/mL in 20 mL Multi-Dose Vials
Manufactured by:
King Pharmaceuticals, Inc.
Bristol, TN 37620
Copyright © 3/00 Monarch Pharmaceuticals