repaglinide tablets

1. Repaglinide is a short-acting insulin secretagogue; Repaglinide lowers blood sugar levels by promoting the release of insulin from the pancreas. This effect depends on the functional beta cells in the pancreatic islets. 2. Repaglinide binds to receptors on beta cells to close ATP-dependent potassium channels in the beta cell membrane, depolarizes beta cells, opens calcium channels, and increases the influx of calcium. This process induces beta cells to secrete insulin. 3. When patients with type 2 diabetes take repaglinide orally, they experience an insulin secretion response within 30 minutes after a meal. This can cause a decrease in blood sugar during meals. Plasma repaglinide levels drop rapidly, and 4 hours after taking the drug, the drug concentration in the plasma of patients with type 2 diabetes is very low. Studies have shown that taking 0.5-4 mg of repaglinide in type 2 diabetes reduces blood sugar concentration in a dose-dependent manner. 4. Clinical research results show that repaglinide should be taken before meals. This product should usually be taken within 15 minutes before a meal, and the medication time can also be controlled 0-30 minutes before a meal.

The main ingredient of this product is repaglinide. Chemical name: S(+)-2-ethoxy-4[2-[[3-methyl-1-[2-(1-piperidinyl)phenyl]-butyl]amino-2-oxyethyl]benzoic acid.

This product is in the form of tablets.

It is used for patients with type 2 diabetes (non-insulin-dependent) whose high blood sugar cannot be effectively controlled by diet control and exercise. Repaglinide tablets can be used together with metformin. Compared with the use of each alone, the combination of the two has a synergistic effect on controlling blood sugar.

1. Repaglinide tablets should be taken before the main meal (i.e. before meals). The insulin secretion response will occur within 30 minutes of oral administration of this product. Usually, this drug is taken within 15 minutes before meals, and the time of taking the drug can also be controlled within 0-30 minutes before meals. 2. Please take repaglinide tablets as prescribed by your doctor. The dosage varies from person to person and depends on personal blood sugar. The recommended starting dose is 0.5 mg, and it can be adjusted every week or every two weeks if necessary. The recommended starting dose for patients receiving other oral hypoglycemic drugs to switch to repaglinide tablets is 1 mg. 3. The maximum recommended single dose is 4 mg, taken with meals. However, the maximum daily dose should not exceed 16 mg. 4. When patients with type 2 diabetes who usually have good blood sugar control with diet experience temporary control failure, short-term use of repaglinide can effectively control blood sugar. 5. For patients with weakness and malnutrition, the dose should be adjusted with caution. If used in combination with metformin, the dose of repaglinide tablets should be reduced. Although repaglinide is mainly excreted in the bile, it should still be used with caution in patients with renal insufficiency.

Like other oral hypoglycemic drugs, taking repaglinide may cause blood sugar changes, such as hyperglycemia and hypoglycemia. Like every diabetes treatment, the occurrence of these reactions depends on individual factors, such as eating habits, dosage, exercise and stress. The clinical application of repaglinide and other hypoglycemic drugs shows that the following adverse reactions may occur when taking repaglinide: According to the incidence of adverse reactions, they are defined as follows: Rare adverse reactions: incidence 1/10000, 1/1000. Very rare adverse reactions: incidence 1/10000. 1. Immune system disorders Allergic reactions Skin allergic reactions such as itching, redness, and urticaria may occur. Very rarely, extensive allergic reactions or immune reactions such as vasculitis occur. 2. Metabolic and nutritional disorders Hyperglycemia Symptoms of hyperglycemia usually appear gradually and may include nausea, drowsiness, increased urine output, thirst and loss of appetite. Rare adverse reactions: Hypoglycemia Like other hypoglycemic drugs, taking repaglinide may cause hypoglycemia. Symptoms include anxiety, dizziness, sweating, tremor, hunger and inattention. These reactions are usually mild and can be easily corrected by giving carbohydrates. If they are more severe, glucose can be infused with the help of others. Combination with other drugs may increase the risk of hypoglycemia (see [Drug Interactions]). 3. Eye abnormalities Very rare: Visual abnormalities Changes in blood sugar levels are known to cause temporary visual abnormalities, especially when starting treatment with hypoglycemic drugs. These changes are usually transient. 4. Gastrointestinal discomfort Rare: Abdominal pain, nausea Very rare: Diarrhea, vomiting and constipation Gastrointestinal reactions such as abdominal pain, diarrhea, nausea, vomiting and constipation have been reported in clinical trials. Compared with other oral insulin secretion-promoting drugs, the frequency and severity of these symptoms are no different. Based on post-marketing experience, individual reports of hypoglycemic reactions have been received when repaglinide is used in combination with metformin or thiazolidinediones. 5. Skin and subcutaneous tissue abnormalities Rare: Allergic reactions Skin allergic reactions such as itching, rash, and urticaria may occur. Due to the different chemical structures, there is no reason to suspect that cross-allergic reactions with sulfonylurea drugs may occur. Very rarely, extensive allergic reactions or immune reactions such as vasculitis occur. 6. Hepatobiliary disorders Liver dysfunction Very rare reports of severe liver dysfunction: However, the relationship with repaglinide has not been established. 7. Research Very rare: Elevated liver enzymes Individual cases have reported elevated liver enzymes during treatment with repaglinide. Most cases were mild and transient, and very few patients stopped treatment due to elevated liver enzymes.

1. It is contraindicated in patients with known allergy to repaglinide or any excipients in this product; 2. It is contraindicated in patients with type 1 diabetes (insulin-dependent, IDDM); 3. It is contraindicated in patients with diabetic ketoacidosis with or without coma; 4. It is contraindicated in pregnant or lactating women; 5. It is contraindicated in children under 8 years old; 6. It is contraindicated in patients with severe renal or hepatic insufficiency; 7. It is contraindicated when combined with CYP3A4 inhibitors or inducers; 8. It is not suitable for patients over 75 years old.

Precautions for children: Not for use in children under 12 years old. Precautions for pregnancy and lactation: Not for use in pregnant and lactating women. Precautions for the elderly: Not for use in patients over 75 years old.

1. Some drugs are known to affect glucose metabolism. Therefore, doctors should consider possible drug interactions. 2. In vitro studies have shown that the metabolism of repaglinide is affected by CYP2C8 and CYP3A4. 3. Clinical study data conducted in healthy volunteers showed that CYP2C8 is the enzyme that plays a major role in the metabolism of repaglinide, while the effect of strong CYP3A4 inhibitors is limited. However, if the effect of CYP2C8 is inhibited, the effect of CYP3A4 will be relatively enhanced. Therefore, the metabolism and clearance of repaglinide may be changed due to the inhibition or induction of cytochrome P450. Therefore, extreme caution should be exercised when using CYP2C8 and CYP3A4 inhibitors simultaneously with repaglinide. 4. A drug interaction study conducted in healthy volunteers showed that the co-administration of the CYP2C8 inhibitor gemfibrozil (twice daily, 600 mg each time) and repaglinide (single dose 0.25 mg) can increase the AUC of repaglinide in the blood of healthy volunteers by 8.1 times, increase Cmax by 24 days, and extend the elimination half-life (t1/2) from 1.3 hours to 3.7 hours. This may lead to an enhanced hypoglycemic effect of repaglinide and a prolonged duration of action. 5. Therefore, gemfibrozil and repaglinide should be avoided in combination. If they must be used together, the patient's blood sugar level should be closely monitored, because the dose of repaglinide may need to be reduced when the two are used together. In the same study, the combination of repaglinide with gemfibrozil and the CYP3A4 inhibitor itraconazole showed a stronger hypoglycemic effect, with the AUC of repaglinide increasing by 19.4 times and the half-life extending from 1.3 hours to 6.1 hours. 6. Trimethoprim (twice daily, 160 mg each time) is a weak CYP2C8 inhibitor. When taken together with repaglinide (single dose 0.25 mg), repaglinide AUC, Cmax and biological half-life can be slightly increased (1.6 times, 1.4 times and 1.2 times, respectively), and there is no significant statistical difference in the increase in blood glucose levels. These data lacking pharmacodynamic results are obtained based on low-dose treatment with repaglinide. Since there is no safety data for the combined use of repaglinide doses higher than 0.25 mg and trimethoprim doses higher than 320 mg, repaglinide and trimethoprim should be avoided in combination. If combined use is necessary, the patient's blood glucose level should be closely monitored and close clinical monitoring should be performed. 7. Rifampicin is a strong CYP3A4 inducer and a CYP2C8 inducer, which simultaneously induces and inhibits the metabolism of repaglinide. Rifampicin (600 mg) was used for 7 days of pre-treatment, and then co-administered with repaglinide (single dose 4 mg) on the 7th day. The AUC was reduced by 50% (this is the combined result of induction and inhibition). When repaglinide was taken 24 hours after the last dose of rifampicin, the AUC of repaglinide was reduced by 80% (induction alone). 8. The co-administration of rifampicin and repaglinide may reduce the dosage of repaglinide. The patient's blood sugar level should be closely monitored when starting rifampicin (rapid inhibition), increasing the dose (mixed inhibition and induction), and stopping rifampicin (induction alone), as well as about 1 week after stopping rifampicin, when its induction effect disappears, and the dosage of repaglinide should be adjusted according to the blood sugar level. 9. Clarithromycin is a strong CYP3A4 inhibitor. When taken twice daily at a dose of 250 mg each time together with repaglinide (single dose 0.25 mg), the exposure of repaglinide can be slightly increased (AUC increased by 1.4 times, Cmax increased by 1.7 times), and the average increase in serum insulin AUC increased by 1.5 times (Cmax increased by 1.6 times). Taking ketoconazole (200 mg daily), a strong CYP3A4 inhibitor, while taking repaglinide (single dose 4 mg) can increase the exposure of repaglinide within a certain range (AUC increased by 1.2 times, Cmax increased by 1.6 times), and the change in blood glucose is less than 8%. 10. When repaglinide is used in combination with cimetidine, nifedipine or simvastatin, all CYP3A4 substrates did not significantly change the pharmacokinetic parameters of repaglinide. 11. Drug interaction studies conducted in healthy volunteers found that repaglinide had no effect on the pharmacokinetic properties of digoxin, theophylline and warfarin. Therefore, when used in combination with repaglinide, there is no need to adjust the dose of these drugs. 12. A pharmacokinetic study conducted in healthy volunteers showed that although the combined use of oral contraceptives (ethinyl estradiol/levonorgestrel) shortened the peak time of repaglinide, it did not change the total bioavailability of repaglinide to the relevant clinical range. Repaglinide has no clinically significant effect on the bioavailability of levonorgestrel, but the effect on the bioavailability of ethinyl estradiol cannot be ruled out. 13. The following drugs may enhance and/or prolong the hypoglycemic effect of repaglinide: gemfibrozil, clarithromycin, ketoconazole, itraconazole, trimethoprim, other types of antidiabetic drugs, monoamine oxidase inhibitors (MAOI), non-selective beta-receptor blockers, angiotensin converting enzyme (ACE) inhibitors, alcohol, and anabolic hormones. 14. The following drugs may weaken the hypoglycemic effect of repaglinide: oral contraceptives, rifampicin, phenobarbital and carbamazepine, thiazide drugs, corticosteroids, danazol, thyroid hormones, octreotide and sympathomimetic drugs. Beta-receptor blockers can mask the symptoms of hypoglycemia. When patients receiving repaglinide use or stop using these drugs, the patient's blood sugar should be closely monitored.

Store in a dry place at 15℃-25℃. Store in the original sealed packaging. Keep out of reach of children. Indicate the expiration date on the outer packaging. Do not use after the expiration date.

1mg

60 months.

Jiangsu Hansoh Pharmaceutical Group Co., Ltd.

• Founded in:

  1995-07-26

• Address:

  Lianyungang Economic and Technological Development Zone, Jiangsu Province

• Tax NO.:

  913207006083959289

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  1,000,000,000 Yuan

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