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Trimebutine maleate sustained-release tablets instructions

Time:2015/9/30 7:19:44


Please read the instructions carefully and use under the guidance of the physician


[Drug Name]

Generic name: trimebutine maleate sustained-release tablets

English name: Trimebutine Maleate Sustained-release Tablets

Pinyin: Malaisuan Qumeibuting Huanshipian

Ingredient main ingredients trimebutine maleate.

Chemical name: (±) -3,4,5- trimethoxy benzoic acid (2-dimethylamino-2-phenyl) butyl maleate, chemical structural formula:

Formula: C22H29NO5 · C4H4O4

Molecular Weight: 503.55

【Properties】 coated tablets, remove the coating after significant white or white.

Indications (1) Gastrointestinal motility disorder caused by loss of appetite, nausea, vomiting, belching, bloating, abdominal Wong, abdominal pain, diarrhea, constipation. (2) intestinal bowel syndrome.

[Specification] 0.3g

Dosage oral, twice daily, each 0.3g (a).

Adverse reactions occasional thirst, numbness in the mouth, the mouth smell, nausea, vomiting, abdominal pain, bowel, diarrhea, constipation, digestive disorders, and tachycardia, drowsiness, dizziness, drowsiness, fatigue, fever or chills, headache, rash, alanine aminotransferase (ALT), aspartate aminotransferase (AST) increased and so, menstrual disorders, breast tenderness, anxiety, mild hearing loss are rarely reported.

Taboo allergic to the chemicals were banned.

[Note] (1) This product contains lactose, galactose intolerance with lactase deficiency, glucose - galactose malabsorption in patients with genetic diseases can not be used. (2) should be discontinued rash and other reactions observed.

Pregnant women and lactating women drug] is not related test also no reliable references, pregnant women do not recommend taking trimebutine maleate. If found pregnant during medication, you need to consult your doctor and can continue to use.

Pediatric Use is not related test also no reliable references.

[Geriatric medicine] is not related test also no reliable references. Generally weak physiological function in elderly patients using this service should consult a doctor, as appropriate reductions.

Drug interactions (1) tubocurarine: maleic acid Trimebutine will enhance the role of myostatin. (2) procainamide: trimebutine maleate and procainamide combination of sinus node conduction synergistic effect against the vagus, heart rate and electrocardiogram should be monitored. (3) cisapride: trimebutine maleate may occur with cisapride pharmacological antagonism, cisapride weaken the role of the stomach and intestines.

[Drug Overdose when a drug overdose, must consult a doctor, should immediately stop taking and using methods such as gastric lavage to remove unabsorbed drug and symptomatic treatment.

Pharmacology and Toxicology

1. The role of gastrointestinal motility:

(1) regulation of gastric motility: results from the body suggest that the product can make guinea pig stomach antrum amplitude cyclic movement of self-regulation in muscle concentration 10-5g / ml decrease, increase faint irregular movement of frequency and amplitude, it tends to be regular rhythmic contractions. After vagotomy chest anesthetized dogs intravenous administration of the product 1mg / kg, found to inhibit digestive diseases Pylorus hyperkinetic movement muscles, but also can enhance muscle movement hypothyroidism movement.

(2) the impact on the digestive system to promote the movement of: adult jejunum red to the goods 4 ~ 6mg / kg, can induce physiological gastrointestinal promote sports.

(3) on the exhaust protruding stomach function: chronic gastritis oral administration of 200mg, decreased gastric emptying can be improved, the gastric emptying hyperthyroidism can be suppressed.

(4) The regulation of bowel movement: the body from the test results suggest that when the concentration of 10-5g / ml, for hypotonia (low load) of guinea pig colon smooth muscle, increased tension effect; increased tension (high load) The guinea pig colonic smooth muscle, lowering tension, reduce the role of amplitude.

People intravenous injection of this product 50mg, neostigmine may Yang system hyperactivity clear which cause the ileum, the ascending colon, S-shaped colon moves to the load level before.

(5) the lower esophageal sphincter pressure (LESP) of the regulation: anesthetized dogs intravenous administration of the product 0.6mg / kg, can reduce the internal pressure caused by gastrin tetrapeptide, also can cause intestinal secretin pressure drop within the get picked.

(6) the role of gastrointestinal smooth muscle: body from the test results suggest that in the presence of atropine, phentolamine, propranolol and tetrodotoxin, etc., the product of guinea pig stomach muscle remains vestibule of the ring action. After the removal of anesthesia celebrate chest vagus nerve, the product of the digestive tract Dodo still effect. Suggesting that the product has a direct effect on the gastrointestinal smooth muscle.

2. antiemetic effect: the goods on apomorphine-induced vomiting in dogs weak inhibition. Dogs after intravenous injection of 3mg / kg or orally give this product 60mg / kg, copper sulfate can significantly prolong the time required to induce hey spit.

[Toxicology]

Repeat dose toxicity: rat oral administration of trimebutine maleate (at a dose of 400mg / kg or more / day continuous administration of a month or 200mg / kg / day administered continuously for 6 months), appear in the stomach before mucosa keratinocytes hyperthyroidism and excessive tissue is characterized by mucosal changes. Harriers orally administered trimebutine maleate (at a dose of more than 100mg / kg / day administered continuously over a month or 25mg / kg / day administered continuously for 6 months), the emergence of creatinine and urea nitrogen increased, Urine protein, urine sugar positive and tubular epithelial regeneration of the chest changes in renal dysfunction. These changes in the withdrawal of 1 to 2 months after the disappearance, or tends to disappear.

Pharmacokinetics] often release formulation relative bioavailability and bioequivalence studies show the human creature, 18 healthy male volunteers after oral administration of 300mg, peak time (Tmax), peak plasma concentration (Cmax) and T1 / 2 小时 were 0.71 ± 0.15, 239.84 ± 97.88mg / ml and 2.24 ± 0.48 hours. This product is hydrolyzed in vivo to form N demethylation metabolites excreted in the urine.

This product Cmax after administration of sustained-release tablets of the original prescription and the two major metabolites were significantly lower than regular release formulations, Tmax significantly delayed, the volatility factor (DF) was significantly lower than the regular release formulation.

[Storage] stored shading, sealed, dry place.

【Packing】 pharmaceutical packaging aluminum foil, PVC solid medicinal hard film, (1) a pack board, each board 4. (2) a pack board, each board 7.

[Validity] 18 months.

[Executive standard] State Food and Drug Administration National Drug Standards YBH02742012

[Approval No.] H20120072 Zhunzi


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