What Is Lafutidine?
Pharmacological studies show that this product is a high-efficiency, long-acting H2 receptor antagonist, which has a significant inhibitory effect on gastric acid secretion, and can inhibit histamine and pentapeptide.
- Drug Name
- Lafutidine Tablets
- Alias
- Nofi, Shunru, Wesda
- Foreign name
- Lafutidine Tablets
- Whether prescription drugs
- prescription
- Main indications
- This product is used for the treatment of chronic gastritis, stomach and duodenal ulcer
- Athletes use with caution
- Use with caution
- Whether to include health insurance
- Incorporate
- Pharmacological studies show that this product is a high-efficiency, long-acting H2 receptor antagonist, which has a significant inhibitory effect on gastric acid secretion, and can inhibit histamine and pentapeptide.
- Vaccine, food, etc. caused gastric acid secretion. This product has gastric mucosal protection and can dose-dependently inhibit the formation of ulcers in various experimental animal ulcer models.
- Promote ulcer healing, relieve symptoms, and prevent recurrence of ulcers.
Lafuridine
- Common name : Lafuridine
- English name : Lafutidine Tablets
- Commodity name : Nofi, Shunru, Wesda
- Drug aliases Storga, Protecadin
- Chemical formula chemical name : Acetamide, 2-[(2-furanyl-methyl) sulfinyl] -N- [4-[[4- (1-piperidinyl-methyl) -2-pyridinyl] oxy] -2-butenyl]-, (Z)-[CAS].
- Indications : This product is used for the treatment of chronic gastritis, gastric and duodenal ulcers.
- Marketed dosage form: tablet
- Specification : 10mg, 5mg
- Dosage: Take 1 tablet once a day.
Lafuridine
- Chemical name: (+/-)-2-[(2-furylmethyl) sulfinyl] -N- [4- [4- (1-piperidylmethyl) -2-pyridyl] oxy- (Z) -2-Butenyl] acetamide
- English name: Lafutidine
- Molecular formula: C22H29N3O4S
- CAS number: 118288-08-7
- Density: 1.252g / cm3
- Vapor pressure: 1.12E-19mmHg at 25 ° C
- Its main intermediate: LFTD-B
- Density: 1.484g / cm3 Molecular formula: C13H11NO6S CAS number: 123855-55-0
- Chemical name: alpha- (2-furanmethylsulfinyl) acetate- (4-nitrophenol) ester
- Categories: Lavidine intermediates, chemical intermediates, pharmaceutical intermediates, esters
Lafuridine
- Suspend sodium hydride in tetrahydrofuran, dropwise add a solution of (Z) -4-tetrahydropyranoxy-2-butenol in tetrahydrofuran at room temperature, stir, and add 2-chloro-4-piperidylmethylpyridine in order And dimethylformamide, the reaction is completed, and treated to obtain (Z) -4-piperidinylmethyl-2- (4-tetrahydropyridyloxy-2-butene-oxy) pyridine. This compound is dissolved in methanol, and under cooling in an ice bath, p-toluenesulfonic acid monohydrate is added, and the reaction is stirred, and treated to obtain (Z) -4- [4- (piperidinylmethyl) pyridine-2-oxy] 2-butenol. This compound and triethylamine were dissolved in toluene, and a toluene solution of methanesulfonyl chloride was added dropwise under cooling in an ice bath, stirred, and treated to obtain a solution. Potassium tert-butoxide was added to a toluene solution of 2-furanmethylsulfinylacetamide, and the solution obtained above was added dropwise to the reaction. After treatment, lafuridine was obtained.
Lafuridine
- Receptor antagonist with unique gastroprotective effect. It can reduce the basal secretion of gastric acid, and inhibit the gastric acid secretion stimulated by histamine, gastrin and urethane. Compared with similar drugs such as cimetidine and famotidine, the blocking effect on H2 receptors is more effective and durable, so it has the advantage of more sustained anti- gastric acid secretion. It is mainly used to treat gastric ulcer, duodenal ulcer and acute or chronic gastritis.
Lafuridine
- When a healthy male volunteer took a single oral lafurotidine 10mg on an empty stomach, Tmax was 0.8 ± 0.1 hours, Cmax was 174 ± 20ng / ml, T1 / 2 was 3.30 ± 0.39 hours, and AUC0-24hr was 793 ± 85ng · hr / ml. . Tmax was significantly prolonged in the fed state, but eating had no effect on Cmax, AUC, and bioavailability. Lafutidine was orally administered at 10 mg on an empty stomach, and the excretion rates of the original drug, metabolites M-4, M-7, and M-9 within 24 hours of administration were 10.9 ± 1.5%, 1.7 ± 0.2%, and 7.5 ± 0.8, respectively. % And 0.3 ± 0.1%, the total excretion rate in human urine is 20% of the dose. In vitro studies, lafuridine is mainly metabolized by cytochrome P450 isoenzymes, the production of metabolites M-4 and M-9 is related to the participation of CYP3A4, and the production of metabolites M-7 is related to the participation of CYP3A4 and CYP2D6. At a concentration of 3 g / ml, the human plasma protein binding rate was 88.0 ± 1.2%.
Lafuridine
- Elderly: For older people, those with normal renal function (average Cr 88.0 ± 9.4ml / min) and those with a tendency to decrease renal function (Cr20-60ml / min, mean 45.2 ± 7.8ml / min) have no change in blood concentration difference.
- Patients on dialysis: Compared with healthy adults, the dialysis patients' blood Cmax increased by 2 times during nondialysis, T1 / 2 increased by about 2 times, and AUC increased by 3 times. Lafuridine was cleared by 7-18% on hemodialysis.
- Children: Pharmacokinetic studies have not been performed.
- Adverse reactions
- According to a report from Japan, in a total of 1,287 studies, the overall incidence of adverse reactions was 2.5% (32 cases). The main adverse reaction was constipation (2 cases), and 22 cases had abnormal laboratory test values.
- (A) possible serious adverse reactions:
- 1. Hepatic impairment: hepatic impairment and jaundice with elevated AST, ALT, -GTP, etc. may occur. Therefore, close observation is needed. Once the above abnormal situation occurs, the drug should be stopped immediately and the corresponding treatment should be given.
- 2. Granulocytopenia, thrombocytopenia: There may be granulocytopenia (early symptoms: sore throat, general burnout, fever, etc.) and thrombocytopenia. Once the above abnormal situation occurs, the drug is immediately discontinued and the corresponding treatment is given.
- (2) Possible serious adverse reactions similar to other H2 receptor blockers:
- The literature reports that H2 receptor blockers may cause shock, allergic-like symptoms, pancytopenia, aplastic anemia, thrombocytopenia, interstitial nephritis, Stevens-Johnson syndrome, toxic epidermal necrosis (Lyell syndrome), Rhabdomyolysis, atrioventricular block, and incomplete contraction.
- (C) other adverse reactions:
- The following adverse reactions may occur. Once the following abnormalities occur, appropriate reductions and withdrawals should be given.
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- * Spasms have been reported with other H2 receptor blockers.