Trimebutine Maleate Sustained-Release Tablets

There are many kinds of gastrointestinal diseases, both acute and chronic. Most gastrointestinal diseases are caused by irregular diet and overeating. Some gastrointestinal diseases are caused by eating something bad suddenly, which causes gastrointestinal discomfort, such as nausea, vomiting, diarrhea, etc. At this time, you can go to the pharmacy to buy a box of trimebutine maleate sustained-release tablets and take them, which will relieve the symptoms. If the symptoms are severe, it is recommended to go to the hospital for medical treatment. The following is a detailed introduction to trimebutine maleate sustained-release tablets.

[Properties] This product is a film-coated tablet, which appears white or off-white after removing the coating.

[Indications] (1) Loss of appetite, nausea, vomiting, belching, abdominal distension, borborygmus, abdominal pain, diarrhea, constipation, etc. caused by gastrointestinal motility disorders. (2) Irritable bowel syndrome.

[Specification] 0.3g [Usage and Dosage] Oral, twice a day, 0.3g (one tablet) each time.

[Adverse Reactions] Occasionally, there may be thirst, numbness in the mouth, strange taste in the mouth, nausea, vomiting, upper abdominal pain, intestinal rumbling, diarrhea, constipation, digestive disorders and tachycardia, drowsiness, dizziness, lethargy, fatigue, fever or chills, headache, rash, increased alanine aminotransferase (ALT) and aspartate aminotransferase (AST). There are also rare reports of menstrual disorders, breast tenderness, anxiety, and mild deafness.

[Contraindications] It is contraindicated for those who are allergic to this product.

[Precautions] (1) This product contains lactose and should not be used by patients with hereditary diseases such as galactose intolerance, lactase deficiency, glucose-lactose malabsorption, etc.

(2) If reactions such as rash occur, the drug should be discontinued and observation should be conducted.

[Use in pregnant and lactating women] No relevant trials have been conducted and there is no reliable reference literature. It is not recommended for pregnant women to take trimebutine maleate. If you find out you are pregnant while taking the medicine, you need to inform your doctor and consult whether you can continue taking the medicine.

[Use in Children] No relevant trials have been conducted and there are no reliable references.

[Use in the Elderly] No relevant trials have been conducted and there are no reliable references. Elderly patients usually have weaker physiological functions, so they should consult a doctor before taking this product and reduce the dosage as appropriate.

【Drug Interactions】

(1) Tubocurarine: Trimebutine maleate can enhance the effects of tubocurarine.

(2) Procainamide: The combination of trimebutine maleate and procainamide produces a synergistic antivagal effect on sinoatrial node conduction. Heart rate and electrocardiogram should be monitored.

(3) Cisapride: Trimebutine maleate can have a pharmacological antagonistic effect with cisapride, weakening the gastrointestinal motility of cisapride.

[Drug Overdose] In case of drug overdose, you must consult a doctor, stop taking the drug immediately, use gastric lavage or other methods to remove unabsorbed drugs, and perform symptomatic treatment.

【Pharmacology and Toxicology】

1. Effects on digestive tract motility:

(1) Gastric motility regulation: In vitro test results indicate that this product, at a concentration of 10-5 g/ml, can reduce the amplitude of the autonomic movement of the circular muscle of the guinea pig gastric vestibule, increase the frequency and amplitude of irregular weak movements, and make it tend to regular rhythmic contraction. When 1 mg/kg of this drug was given intravenously to anesthetized dogs with thoracic vagus nerve cut, it was found that it could inhibit the movement of hyperkinetic muscles in the pyloric region of the stomach in patients with digestive system diseases, and also enhance the movement of hypokinetic muscles.

(2) Effect on propulsive motility of the digestive system: Intra-jejunal administration of 4-6 mg/kg of this drug to adults can induce physiological propulsive motility of the digestive tract.

(3) Effect on gastric emptying function: Oral administration of 200 mg of this product can improve the weakening of gastric emptying function and inhibit the hyperfunction of gastric emptying function in patients with chronic gastritis.

(4) Regulatory effect on intestinal motility: The results of in vitro experiments indicate that at a concentration of 10-5 g/ml, it has the effect of increasing the tension of guinea pig colon smooth muscle with low tension (low load); it has the effect of reducing the tension and amplitude of guinea pig colon smooth muscle with increased tension (high load). Intravenous injection of 50 mg of this product can inhibit the hypermotility caused by neostigmine and make the ileum, ascending colon and sigmoid colon move to the pre-load level.

(5) Regulation of lower esophageal sphincter pressure (LESP): Intravenous injection of 0.6 mg/kg of this drug in anesthetized dogs can reduce the increase in intraesophageal pressure caused by tetragastrin, and can also restore the decrease in intraesophageal pressure caused by secretin.

(6) Effect on gastrointestinal smooth muscle: In vitro test results indicate that this product still has an effect on the circular muscle of the guinea pig gastric vestibule in the presence of atropine, phentolamine, propranolol and tetrodotoxin. After the vagus nerve is removed during anesthesia, this product still has an effect on gastrointestinal motility. This suggests that this product has a direct effect on the smooth muscle of the digestive tract.

2. Antiemetic effect: This product has a weak inhibitory effect on apomorphine-induced vomiting in dogs. Intravenous injection of 3 mg/kg or oral administration of 60 mg/kg of this product to dogs can significantly prolong the time required for copper sulfate-induced vomiting.