Approved on.
Date of revision:
Mosapride Citrate Tablets Instructions
Please read the instructions carefully and use under the guidance of your physician
[Drug Name].
Generic Name: Mosapride Citrate Tablets
Trade Name: Fastidious
English Name: Mosapride Citrate Tablets
Hanyu Pinyin: Juyuansuan Moshabili Pian
[Ingredients
The main ingredient of this product is mosapride citrate.
Chemical name: 4-Amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morpholinyl]methyl]benzamide citrate dihydrate.
Chemical structure formula.
Molecular formula: C21H25ClFN3O3-C6H8 O7-2H2O
Molecular weight: 650.05
[Properties
This product is a white film-coated tablet, which appears white after removing the coating.
[Indications].
This product is used to improve gastrointestinal symptoms caused by reduced gastrointestinal motility (e.g., functional dyspepsia, chronic gastritis), including heartburn, belching, nausea, vomiting, early satiety, epigastric distention, and epigastric pain.
[Specifications
5mg(based on C21H25ClFN3O) sub>3-C6H8O7count)
[dosage
The usual dosage for adults is 5 mg (1 tablet) 3 times a day, taken orally before or after meals.
[Adverse Reactions
Foreign clinical trials with the same species998cases in which there were 40 cases (4.0%) ) experienced adverse reactions. The main ones were diarrhea and loose stools (1.8%), thirst(0.5%), malaise (0.3%), etc. Of the 792patients who took this product30 cases (3.8%1.1%), elevated triglycerides () and elevated triglycerides (1.0%),AST(GOT), ALT(GPT),ALPandγ-GTP were elevated (each 0.4%), etc. (when approved)
Survey on the post-marketing use of the same species abroad Post-marketing use survey: 3014patients in the special survey (long-term use survey) were74 cases (2.5%) span>) experienced adverse reactions. The main ones were diarrhea and loose stools (0.8%), abdominal pain (0.4%), thirst(0.3%)etc. (at the end of the re-examination)
1.Serious adverse reactions: fulminant hepatitis, hepatic dysfunction, jaundice (all less than 0.1%)
Due to the possibility of fulminant hepatitis withAST (GOT), , ALT(GPT),γ-GTPand other significant elevations in severe liver dysfunction and jaundice, and there have been cases of death, therefore, patients should be closely observed and if abnormalities are detected, the medication should be stopped immediately and appropriate measures should be taken.
2.Other adverse reactions
Categories0.1%～2%<0.1%frequency unknownAllergies Oedema, urticariaRashBloodEosinophiliaLeukopenia Digestive Systemdiarrhea and loose stools, thirst, abdominal pain, emetics and vomitingAbnormal taste, bloatingIntraoral numbness (including tongue, lips, etc.) . LiverALT(GPT)ElevatedAST(GOT),ALP “font-family:Arial”>,γ-GTP, elevated bilirubin Cardiovascular Heart palpitations Psychoneurology Vertigo, dizziness, headache OtherTiredness, elevated triglycerides. Tremor [Taboo
It is contraindicated for those who are allergic to any of the ingredients in this product.
[Precautions
1. Important Basic Precautions
(1) After a period of continuous use of this product (usually 2 weeks), the improvement of digestive symptoms should be evaluated to study the need for continued dosing.
(2) Due to the possibility of fulminant hepatitis, severe liver dysfunction and jaundice, this product should not be taken blindly for a long period of time. At the same time, patients should be closely observed during the administration of this product, and if abnormalities are detected, the medication should be stopped immediately and proper disposition should be taken. In addition, patients should be instructed to stop taking the drug and contact their doctor if they experience symptoms such as discomfort, loss of appetite, yellow urine and yellowing of the bulbar conjunctiva when taking this product.
2.
Patients should remove the product from the PTP sheet before taking it (it has been reported that patients have accidentally ingested the PTP sheet and the sharp, hard, sharp corners pierced the esophageal mucosa and even perforated it, causing serious complications such as mediastinitis).
[For pregnant and lactating women
1. Pregnant women and women at risk of pregnancy should use this product only if the therapeutic benefit outweighs the risk (the safety of this product in pregnant women has not been confirmed).
2. Women who are breastfeeding should avoid this product and discontinue breastfeeding if they do need to take it [mosapride has been found to be secreted from breast milk in animal studies (rats)].
[Pediatric Use
This trial was not performed and no reliable references are available.
[Geriatric Use
Generally, it should be used with caution in elderly patients due to the decreased physiological functions of the liver and kidneys in the elderly. The dose should be reduced (e.g., 7.5 mg daily) and appropriate measures taken when adverse reactions occur.
[Drug Interactions
Cautions for combined use
Medication NameClinical symptoms and measuresMechanisms of action and risk factorsAnticholinergics
(e.g., atropine sulfate, scopolamine butylbromide, etc.)can diminish the effect of this product, so it should be used at separate intervals when combined with anticholinergics. The GI-promoting effect of this drug depends on the excitation of cholinergic nerves, so Combination with anticholinergics inhibits the effect of this drug. When 15 mg of this drug was administered daily along with 1200 mg of erythromycin, the maximum blood concentration of this drug increased from 42.1 ng/mL compared to that of this drug alone increased to 65.7 ng/mL, half-life increased from 1.6 hours to 2.4 hours, and AUC 0-4 increased from 62 ng-hr/mL to 114 ng-hr/mL (healthy adults).
[Drug overdose].
This trial was not performed and no reliable references are available.
[Pharmacology and Toxicology
Pharmacological effects: This product is selective5-hydroxytryptamine4(5-HT4) receptor agonist, by excitating the 5-HT4receptors of the gastrointestinal cholinergic interneurons and the intermuscular plexus, promotes acetylcholine release, thus enhancing the movement of the digestive tract (stomach and small intestine). Studies have shown that this product has the ability to promote gastric and duodenal motility and accelerate gastric emptying. Studies in rats have shown that its facilitation of gastric emptying is diminished by repeated administration for one week.
Toxicological effects. Long-term in rodents (rat104weeks, mouse92weeks) in dosing studies at doses of30-100 mg/kg day (equivalent to 100-300of the clinically recommended dose). family:Arial”>fold), the incidence of hepatocellular adenoma and thyroid cell adenoma was increased.
[Pharmacokinetics
1.
Results of single dose of 5 mg on an empty stomach in 5 healthy adults
Tmax(h)Cmax ( ng/mL)T1/2(h)0.8±0.1※30.7±2.72.0±0.2※mean±standard deviation
2. Plasma protein binding ratio
99.0% (human serum 1µg/mL, in vitro ultrafiltration or equilibrium dialysis)
3. Major Metabolites and Metabolic Pathways
Main metabolite: des-4-fluorouracil.
Metabolic pathway: Mainly metabolized by the liver to des-4-fluorouracil, then by oxidation at the 5-position of the paraoxohexane ring and hydroxylation at the 3-position of the benzene ring.
4. Excretion pathway and excretion rate
Pathways of excretion: urine, feces.
Excretion rate: urinary excretion rate 48 hours after dosing: 0.1% in prodrug form. The major metabolite (des-4-fluorouracil) was 7.0% (5 mg in a single dose on an empty stomach in a healthy adult).
5. Metabolic enzymes
Cytochrome P-450 isoforms: mainly CYP3A4.
[Storage] Sealed and stored at room temperature.
[Package] Aluminum-plastic package, 24 tablets/box, 36 tablets/box, 48 tablets/box.
[Expiration date] 24 months
[Executive Standard
[Approval number] State Drug Administration H19990317
[Drug Listing Permit Holder
Name
Name: Lunanbetter Pharmaceutical Co.
Registered Address. Hongqi Road, Linyi City, Shandong Province209No.
[Drug Manufacturer
Company Name: Lunan Ltd
Production Address. Yinqishan Road, Linyi City, Shandong Province243No.
Postal Code:276006
Phone Number:0539-8336336(Sales Department) 0539-8336169(Quality Control Department)
Fax Number:0539-8336338
Net
Address: www.LUNAN.com.cn