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Metoclopramide Tablets

Function and Efficacy

This product is a dopamine 2 (D2) receptor antagonist, and also has a 5-hydroxytryptamine 4 (5-HT4) receptor agonist effect, and has a mild inhibitory effect on 5-HT3 receptors. It can act on dopamine receptors in the medullary chemo-emetic zone (CTZ) to increase the threshold of CTZ, and has a strong central antiemetic effect. This product can also block hypothalamic dopamine receptors, inhibit prolactin inhibitory factor, and promote the secretion of prolactin, so it has a certain lactation effect. The inhibitory effect on other parts of the central nervous system is relatively small, with a weak sedative effect and less hypnotic effect. The main effect on the gastrointestinal tract is on the upper digestive tract, promoting the movement of the stomach and upper intestinal segments; increasing the tension of the gastrointestinal sphincter in the resting state, increasing the tension and contraction amplitude of the lower esophageal sphincter, increasing the pressure at the lower end of the esophagus, blocking gastroesophageal reflux, strengthening gastric and esophageal peristalsis, and enhancing the ability to clear the contents of the esophagus, promoting gastric emptying; promoting the relaxation of the pylorus, duodenum and upper jejunum, forming functional coordination between the gastric antrum, gastric body and upper small intestine. These effects can also enhance the antiemetic effect of this product. The transmission effect of this product on the small intestine and colon is still uncertain.

Ingredients

The main ingredient of this product is metoclopramide. Its chemical name is N-[(2-diethylamino)ethyl]-4-amino-2-methoxy-5-chloro-benzamide. Molecular formula: C14H22ClN3O2 Molecular weight: 299.8

Name Description Content CAS NO. Manufacturer
4-Amino-5-chloro-N-(2-(diethylamino)ethyl)-2-methoxybenzamideIngredients

This product is a dopamine 2 (D2) receptor antagonist, and also has a 5-hydroxytryptamine 4 (5-HT4) receptor agonist effect, and has a mild inhibitory effect on 5-HT3 receptors. It can act on dopamine receptors in the medullary chemo-emetic zone (CTZ) to increase the threshold of CTZ, and has a strong central antiemetic effect. This product can also block hypothalamic dopamine receptors, inhibit prolactin inhibitory factor, and promote the secretion of prolactin, so it has a certain lactation effect. The inhibitory effect on other parts of the central nervous system is relatively small, with a weak sedative effect and less hypnotic effect. The main effect on the gastrointestinal tract is on the upper digestive tract, promoting the movement of the stomach and upper intestinal segments; increasing the tension of the gastrointestinal sphincter in the resting state, increasing the tension and contraction amplitude of the lower esophageal sphincter, increasing the pressure at the lower end of the esophagus, blocking gastroesophageal reflux, strengthening gastric and esophageal peristalsis, and enhancing the ability to clear the contents of the esophagus, promoting gastric emptying; promoting the relaxation of the pylorus, duodenum and upper jejunum, forming functional coordination between the gastric antrum, gastric body and upper small intestine. These effects can also enhance the antiemetic effect of this product. The transmission effect of this product on the small intestine and colon is still uncertain.

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Appearance

This product is white tablets.

Indication

Antiemetics. Mainly used for ① symptomatic treatment of nausea, vomiting, belching, indigestion, stomach distension, hyperacidity and other symptoms caused by various causes; ② reflux esophagitis, bile reflux gastritis, functional gastric retention, gastroptosis, etc.; ③ delayed emptying of residual stomach, delayed gastric emptying after vagotomy; ④ gastric emptying disorders caused by collagen diseases such as diabetic gastroparesis, uremia, scleroderma, etc.

Usage and Dosage

Oral. Adults: 5-10 mg each time, 3 times a day. For patients with diabetic gastric emptying dysfunction, take 10 mg orally 30 minutes before the onset of symptoms; or take 5-10 mg before meals and before bedtime, 4 times a day. The total dose for adults should not exceed 0.5 mg/kg/day. Children: 5-14 years old, take 2.5-5 mg each time, 3 times a day, 30 minutes before meals, preferably for short-term use. The total dose for children should not exceed 0.1 mg/kg/day.

Adverse Reactions

1. The more common adverse reactions are: drowsiness, irritability, fatigue and weakness; 2. Rare reactions include: breast swelling and pain, nausea, constipation, rash, diarrhea, sleep disorders, dizziness, severe thirst, headache, and irritability; 3. Increased milk production occurs during medication due to the stimulation of prolactin; 4. Long-term use of large doses may block dopamine receptors and make cholinergic receptors relatively hyperactive, leading to extrapyramidal reactions (especially in young people), which may cause muscle tremors, dysphonia, ataxia, etc.

Precautions

1. Contraindicated in the following cases: ① Those who are allergic to procaine or procainamide; ② The frequency and severity of epileptic seizures can be increased by medication; ③ Gastrointestinal bleeding, mechanical intestinal obstruction or perforation can increase gastrointestinal motility and worsen the condition due to medication; ④ Pheochromocytoma can cause hypertensive crisis due to medication; ⑤ It should not be used for breast cancer patients who vomit due to chemotherapy and radiotherapy. 2. Use with caution in the following cases: ① In case of liver failure, the ability to bind to proteins is lost; ② Renal failure, that is, severe chronic renal failure increases the risk of extrapyramidal reactions, and the dosage should be reduced.

Special Population Medication

Precautions for children: Children should not use it for a long time. Precautions for pregnancy and lactation: It has potential teratogenic effects and should not be used by pregnant women; it can be used for short-term lactation in lactating women. Precautions for the elderly: The elderly should not use it for a long time or in large quantities, otherwise they are prone to extrapyramidal symptoms.

Drug Interactions

1. When used with acetaminophen, levodopa, lithium, tetracycline, ampicillin, ethanol and diazepam, gastric emptying is accelerated, which increases the absorption of the latter in the small intestine; 2. When used with ethanol or central nervous system depressants, the sedative effect is enhanced; 3. When used with anticholinergic drugs and anesthetic analgesics, it has an antagonistic effect; 4. When used with antimuscarinic anesthetic sedatives, the motility of metoclopramide on the gastrointestinal tract can be offset; 5. Because it can release catecholamines, hypertensive patients who are using monoamine oxidase inhibitors should be monitored carefully when using it; 6. When used in combination with paracetamol, tetracycline, levodopa, ethanol, and cyclosporine, its absorption in the small intestine can be increased; 7 When used in combination with apomorphine, the latter's central and peripheral effects can be inhibited; 8 When used in combination with cimetidine and slow-dissolving digoxin, the latter's gastrointestinal absorption is reduced, and this effect can be reduced if taken at an interval of 2 hours; this product can also increase the bile excretion of digoxin, thereby changing its blood concentration; 9 When used in combination with drugs that can cause extrapyramidal reactions, such as phenothiazines, the incidence and severity of extrapyramidal reactions can be increased.

Storage

Keep sealed.

Packaging Specification

5mg

Validity Period

36 months

Manufacturer

Shanxi Linfen Jianmin Pharmaceutical Factory Co., Ltd.

  • Founded in:

    1989-07-22
  • Address:

    No. 227, Pingyang North Street, Linfen City
  • Tax NO.:

    91141000113120236A
  • Registered Funds:

    2.83 million yuan
  • Website:

  • Email:

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