Product Overview
[Drug Name]
Generic Name: Cisapride Tablets
Trade Name: Jingxin Yirui Cisapride Tablets 5mg*10 Tablets
Pinyin Code: Jingxin ZuoRui XiShaBiLiPian 5mg*10 Tablets
[Main Ingredient]
The main ingredient of this product is cisapride. Chemical Name: cis-4-amino-5-chloro-N-[1-[1-[4-fluorophenoxy]propyl]-3-methoxy-4-pyridyl]-2-methoxyaniline. Molecular Formula: C23H29C1FN304
Molecular Weight: 465.95
[Properties]
This product is a white tablet.
[Indications/Main Functions]
A general gastrointestinal prokinetic agent. It is mainly used for functional dyspepsia, upper gastrointestinal discomfort with negative X-ray and endoscopy examinations, with symptoms such as early satiety, fullness after meals, decreased appetite, bloating, excessive belching, lack of appetite, nausea, vomiting or ulcer-like complaints (burning pain in the upper abdomen). It can also be used to treat mild reflux esophagitis.
[Specification]
5mg*10 tablets
[Usage and Dosage]
(1) The maximum daily dose is 30mg (i.e. 6 tablets). (2) Adults: Depending on the severity of the disease, the total daily dose is 15-30mg (i.e. 3-6 tablets), divided into 2-3 doses, 5mg (i.e. 1 tablet) each time (the dose can be doubled). (3) Children weighing 25-50 kg: The maximum dose is 5mg (i.e. 1 tablet), four times a day. It can be taken orally as a tablet or oral suspension. (4) Infants and children weighing less than 25 kg: 0.2mg/kg body weight each time, three to four times a day. The suspension is preferred. (5) It is recommended to avoid taking it with grapefruit juice as much as possible. (6) In case of renal insufficiency, it is recommended to reduce the daily dose by half.
[Adverse Reactions]
1. Occasionally, transient abdominal cramps, abdominal borborygmi and diarrhea may occur, and the dose can be halved; 2. Occasionally, allergies, mild transient headaches or dizziness, and dose-related urinary frequency have been reported; 3. Rare reversible liver function abnormalities, which may or may not be accompanied by cholestasis; 4. Male breast feminization and galactorrhea, the incidence rate in large-scale monitoring studies (<0.1%) did not exceed the common value of the general population, and was reversible after discontinuation of the drug. The causal relationship is not clear; 5. Rare effects on the central nervous system, namely convulsive epilepsy, extrapyramidal reactions and urinary frequency.
[Contraindications]
1. This product is contraindicated in patients with known allergies. 2. Concomitant oral or parenteral use of drugs that are strong inhibitors of the CYP3A4 enzyme is prohibited, including: triazole antifungal drugs; macrolide antibiotics; HIV protease inhibitors; cefazodone. 3. This product is contraindicated in patients with heart disease, arrhythmias, or QT prolongation. It should not be used with drugs that cause QT prolongation. It is also contraindicated in patients with fluid or electrolyte imbalances, especially hypokalemia and hypomagnesemia. It is contraindicated in patients with bradycardia. It is contraindicated in patients with congenital QT prolongation or a family history of congenital long QT syndrome. It is also contraindicated in patients with pulmonary, hepatic, or renal insufficiency. 4. This product is contraindicated in patients with conditions that could increase gastrointestinal motility and cause harm (such as gastrointestinal obstruction). 5. This product is not recommended for premature neonates.
[Drug Interactions]
1. This product is a potent CYP3A4 inhibitor and should not be used concomitantly with drugs that are primarily metabolized by CYP3A4, such as imidazoles and macrolides, to avoid serious adverse reactions. 2. This product may accelerate gastric emptying, reducing the absorption rate of drugs absorbed through the stomach and increasing the absorption rate of drugs absorbed through the intestine.
[Precautions]
1. Use with caution in patients with increased gastrointestinal motility that could cause harm, and in premature infants less than 34 weeks of gestation. 2. In patients with hepatic or renal impairment, it is recommended to halve the initial daily dose. This dose can be adjusted appropriately based on therapeutic efficacy and potential side effects. 3. In the elderly, due to moderately prolonged elimination half-life, steady-state plasma concentrations are generally increased, so the therapeutic dose should be reduced as appropriate. 4. QT-interval prolongation and/or torsade de pointes may occur in patients taking other medications and those with pre-existing cardiovascular disease or underlying arrhythmias. While the relationship between this drug and individual cases of QT prolongation remains unclear, appropriate consideration should be given to patients at risk for QT prolongation, such as those with unadjusted electrolyte (potassium/magnesium) imbalances, congenital QT prolongation, or those taking medications known to prolong the QT interval. 5. Although it has no embryonic developmental effects, primary embryotoxicity, or teratogenicity in animals, its use during pregnancy, especially in the first trimester, should be carefully weighed against its risks. 6. Although the amount excreted in breast milk is minimal, nursing mothers are advised not to use it. 7. It does not affect psychomotor function and does not cause sedation or drowsiness. However, it can accelerate the absorption of central nervous system depressants, such as barbiturates and alcohol, so concomitant use should be used with caution.
[Pediatric Use]
Use with caution in premature infants less than 34 weeks.
[Elderly Use]
In the elderly, due to the moderately prolonged elimination half-life, steady-state plasma concentrations are generally increased, so the therapeutic dose should be reduced.
[Overdose]
The drug should be discontinued promptly and symptomatic and supportive treatment should be given. It is rarely eliminated after blood or peritoneal dialysis. 【Pharmacology and Toxicology】 1. Animals: (1) In isolated organs, this product can prevent gastric relaxation, accelerate gastric motility, and coordinate the movement of the antrum-duodenum, small intestine and large intestine; (2) In dogs, this product can enhance the digestive activity of the antrum-duodenum, coordinate and enhance gastric emptying, increase the motility of the small intestine and large intestine and shorten the time of intestinal movement, but does not affect gastric secretion; (3) The mechanism of action of this product is mainly to promote the physiological release of acetylcholine in the intestinal myenteric plexus; (4) This product does not stimulate muscarinic and nicotinic receptors, nor does it inhibit the activity of acetylcholinesterase; (5) This product is mainly distributed in the stomach and intestinal tissues. 2. Humans: () Gastrointestinal motility effects: Esophagus: This product can enhance esophageal motility and lower esophageal sphincter tension; This product can prevent gastric contents from refluxing into the esophagus and improve esophageal clearance; Stomach: This product can increase gastric and duodenal contractility and coordination between the antrum and duodenum; This product can reduce duodenal-gastric reflux; This product can improve gastric and duodenal emptying; Intestine: This product can enhance intestinal motility and promote transit between the small intestine and the large intestine. (2) Other effects: Since this product lacks cholinergic effects, it does not increase basal and pentagastrin-induced gastric acid secretion; Since this product relatively lacks dopamine antagonist properties, it has little effect on plasma prolactin levels; This product does not affect psychomotor function, blood pressure, respiratory rate, body temperature, body weight and anticoagulant function; The pharmacological effect of this product begins 30 to 60 minutes after oral administration.
