Product Overview
[Drug Name]
Generic Name: Rabeprazole Sodium Enteric-Coated Capsules
Trade Name: Zino Rabeprazole Sodium Enteric-Coated Capsules 20mg x 7 capsules
[Main Ingredients]
The main ingredient of this product is rabeprazole sodium. Chemical Name: 2-[4-(3-methoxypropoxy)-3-methyl-2-pyridyl]-methyl]sulfinyl]-1H-benzimidazole sodium. Molecular Formula:
C₁₈H₂₀N₃NaO₃₅ Molecular Weight: 38143
[Properties]
This product is an enteric-coated capsule containing off-white or slightly yellow granules or powder.
[Indications/Main Functions]
This product is indicated for: 1. Active duodenal ulcers; 2. Benign active gastric ulcers; 3. Erosive or ulcerative gastroesophageal reflux disease (GERD) with clinical symptoms; 4. In combination with appropriate antibiotics, it can eradicate Helicobacter pylori-positive duodenal ulcers; 5. Maintenance treatment of erosive or ulcerative gastroesophageal reflux disease. The efficacy of treatment beyond 12 months has not been evaluated.
[Specifications]
20mg x 7 tablets (Jinuo)
[Dosage and Administration]
This product should not be chewed or crushed; it should be swallowed whole. 1. Usage in Adults/Elderly Patients A. Active duodenal ulcers and benign active gastric ulcers: 20mg once daily in the morning. Most patients with active duodenal ulcers resolve after 4 weeks of treatment. However, 2% of patients may require 4 more weeks of treatment to achieve resolution. Some patients with duodenal ulcers respond to a therapeutic dose of 10 mg once daily in the morning. Most benign active gastric ulcers resolve after 6 weeks of treatment. However, 9% of patients require an additional 6 weeks of treatment to achieve resolution. B. Patients with erosive or ulcerative gastroesophageal reflux disease (GERD): 20 mg once daily for 4-8 weeks. C. Long-term maintenance therapy for GERD: 12 months of treatment at a maintenance dose of 10 mg or 20 mg once daily. Some patients respond to a maintenance dose of 10 mg daily. D. Curative treatment of Helicobacter pylori: In combination with appropriate antibiotics, it can be used to eradicate Helicobacter pylori-positive duodenal ulcers. This product should be taken in the morning, before meals. Although the timing of administration and food intake do not affect the efficacy of rabeprazole sodium, this route of administration may facilitate treatment. 2. Use in Patients with Hepatic and Renal Insufficiency: No dosage adjustment is required for patients with hepatic and renal insufficiency. However, when using this drug in patients with severe hepatic insufficiency, please refer to the "Adverse Reactions and Precautions" section.
[Adverse Reactions]
1. Uncommon (incidence 0.1-5%): photosensitivity reaction, headache, nausea, vomiting, constipation, diarrhea, rash; erythropenia, leukocytopenia, leukocytosis, eosinophilia, neutrophilia, lymphocytopenia; elevated AI, AST, ALP, GTP, LDH, total bilirubin, total cholesterol, and BUN; proteinuria. 2. Rare (incidence <0.1%): shock, palpitations, bradycardia, lower abdominal pain, dyspepsia, chest pain, myalgia, visual disturbances, insomnia, drowsiness, fatigue, decreased grip strength, limb weakness, dysesthesia, slurred speech, unsteady gait, and hemolytic anemia. In addition, a cirrhotic patient with a history of hepatic encephalopathy abroad experienced confusion, loss of cognitive function, and drowsiness.
[Contraindications]
Rabeprazole sodium is contraindicated in patients with allergies to benzimidazole metabolites, or excipients.
[Drug Interactions]
Rabeprazole is metabolized by the cytochrome P450 (CYP450) enzyme system. Studies in healthy subjects have shown that rabeprazole sodium does not have significant clinical interactions with other drugs metabolized by the CYP450 system. Rabeprazole sodium produces a sustained inhibitory effect on gastric acid secretion. Because rabeprazole sodium decreases acidity, it may interact with drugs whose absorption is dependent on gastric pH. For example, daily administration of ketoconazole and 20 mg of rabeprazole sodium in healthy subjects reduced ketoconazole bioavailability by approximately 30%. Concomitant administration of digoxin increased digoxin's AUC and Cmax by 19% and 29%, respectively. Therefore, patients should be monitored when taking these drugs concurrently with rabeprazole sodium. The mean plasma concentration area under the curve for rabeprazole decreased by 8% and 6% when rabeprazole sodium was taken concurrently with antacids or one hour after antacid administration, respectively.
[Precautions]
1. The possibility of cancer should be ruled out before initiating treatment with this drug. Although no significant drug-related safety issues were observed in age- and sex-matched studies comparing patients with mild to moderate hepatic impairment with healthy controls, physicians recommend that patients with severe hepatic impairment exercise particular caution when initially using this drug. 2. While taking this drug, regular blood tests and blood chemistry tests (such as liver enzyme tests) should be performed. Abnormalities should be detected, and treatment should be discontinued and prompt. 3. Use with caution in patients with impaired liver function.
[Pediatric Use]
Currently, there are no safety and efficacy data for this drug in children.
[Elderly Use]
Clinical studies have shown no differences in efficacy or safety between patients over 65 years of age and younger patients, but greater sensitivity in some elderly patients cannot be ruled out. Because this drug is primarily metabolized in the liver, and elderly patients often have impaired liver function, adverse reactions may occur. Therefore, if adverse reactions to the digestive system occur (see "Adverse Reactions"), use with caution and discontinue the medication if necessary.
[Overdose]
There is no known specific antidote. In the event of an overdose, appropriate supportive care should be implemented based on the patient's clinical symptoms and signs.
[Pharmacology and Toxicology]
Pharmacological Action: Rabeprazole is a benzimidazole compound and a second-generation proton pump inhibitor. It blocks the final step of gastric acid secretion by specifically inhibiting the H+-K+ ATPase system in gastric parietal cells. This effect is dose-dependent and can inhibit both basal and stimulated gastric acid secretion. This product does not antagonize cholinergic and histamine H2 receptors. Toxicological Studies: Genotoxicity: This product tested positive in the Salmonella typhimurium reverse mutation (Ames) test, the Chinese hamster ovary gene mutation test, and the mouse lymphoma cell gene mutation test; its demethylated metabolite also tested positive in these tests. Results were negative in the in vitro hamster lung cell chromosome aberration test, the mouse micronucleus test, and the in vivo and in vitro liver unscheduled DNA synthesis (UDS) test. Reproductive toxicity: In rats, intravenous administration of rabeprazole at a concentration of 50 mg/g/day (plasma AUC approximately 13 times that of the dose at which patients receive the recommended clinical dose) and intravenous administration of 50 mg/g/day (plasma AUC approximately 8 times that of the dose at which patients receive the recommended clinical dose) showed no significant changes in fertility or reproductive behavior, and no harm was observed in the fetuses. Adequate and well-controlled clinical studies involving pregnant women are lacking. Because animal reproductive toxicity does not always predict drug effects in humans, this product should be used during pregnancy only when clearly indicated. Oral administration of rabeprazole (400 mg/g/day) to rats during late pregnancy and lactation resulted in decreased weight gain. Because many drugs are excreted in breast milk and may have toxic side effects in nursing infants, the importance of the drug to the mother should be considered when deciding whether to discontinue breastfeeding or discontinue the drug during this period. Carcinogenicity: In an 88/104-week study in CD-1 mice, oral administration of rabeprazole at doses up to 100 mg/kg/day did not demonstrate an increase in tumor incidence, a blood concentration 1.6 times the recommended dose in patients. A 104-week carcinogenicity study in SD rats was conducted, with males receiving oral doses of 5, 15, 30, and 60 mg/kg/day, and females receiving 5, 15, 30, 60, and 120 mg/kg/day. Both males and females developed gastrointestinal chromoblastic cell (LC) hyperplasia at all doses, and females developed benign gastrointestinal chromoblastic cell (ELC) tumors at all doses. No drug-related tumors were observed in males, even at the highest dose (a blood concentration equivalent to 0.2 times the recommended clinical dose).
