nateglinide tablets

Pharmacological action Nateglinide is an amino acid derivative and an oral antidiabetic drug. It is used to treat patients with type 2 diabetes. The action of nateglinide depends on the binding and closing of the ATP-sensitive K particle channel receptor on the pancreatic β cell membrane, which depolarizes the cell, opens the calcium channel, and causes calcium influx, thereby stimulating insulin secretion and lowering blood sugar levels. The insulin secretion-promoting effect of nateglinide depends on the blood glucose level. When the glucose level is low, the insulin secretion-promoting effect is weakened. Nateglinide has a certain tissue selectivity and has a low affinity for myocardial and skeletal muscles. Toxicological studies Genetic toxicity: This product did not show mutagenic effects in the Ames test, mouse lymphoma test, Chinese hamster lung cell chromosome aberration test, and mouse in vivo micronucleus test. Reproductive toxicity: When the dose of rats reached 600 mg/kg (about 16 times the exposure of patients taking it orally before meals, 3 times a day, and the therapeutic dose of 120 mg), there was no effect on fertility. When the dose of rats reached 1000 mg/kg (same as above, about 60 times the exposure in clinical treatment), no teratogenic effect was observed. When rabbits were given a dose of 500 mg/kg (same as above, about 40 times the exposure during clinical treatment), it had an adverse effect on embryonic development, and the incidence of gallbladder hypoplasia or small gallbladder increased. There is currently no sufficient and strictly controlled clinical research data for pregnant women, so this product should not be used during pregnancy. Nateglinide can be secreted through rat milk, and its AUCO-48h ratio in milk and plasma is 1:4. Rats were given nateglinide 1000 mg/kg (same as above, about 60 times the exposure during clinical treatment), and their offspring were lighter in weight. It is not yet known whether nateglinide is excreted in human milk, because many drugs can be excreted from human milk, so nateglinide should not be used in lactating women. Carcinogenicity: When SD rats and B6C3F1 mice were orally administered this product for 2 consecutive years, at doses of 900 mg/kg/H (the AUC exposure was 30 times and 40 times the human clinical therapeutic dose in male and female animals, respectively) and 400 mg/kg/H (the AUC exposure was 10 times and 30 times the human clinical therapeutic dose in male and female animals, respectively), no carcinogenicity was shown.

The main ingredient of this product is nateglinide, and its chemical name is: N-(trans-4-isopropylcyclohexanecarbonyl)-D-phenylalanine.

This product is white or off-white tablets

It is suitable for patients with type 2 diabetes who cannot effectively control hyperglycemia with diet control and exercise. It can also be used in patients with type 2 diabetes who cannot effectively control hyperglycemia with metformin. It is used in combination with metformin, but it cannot replace metformin. Nateglinide is not suitable for patients with type 2 diabetes who are not ideal for sulfonylurea hypoglycemic treatment.

Oral administration. Usually adults take 60-120 mg (2-4 tablets) three times a day, within 1-15 minutes before meals. It is recommended to start with a small dose and adjust the dose according to the results of regular HbAlc or blood sugar tests 1-2 hours after meals.

1. Hypoglycemia: Like other antidiabetic drugs, symptoms of hypoglycemia can be observed after taking nateglinide, including sweating, shivering, dizziness, loss of appetite, palpitations, nausea, fatigue and weakness. These symptoms are generally mild and easy to deal with. If necessary, carbohydrates can be eaten. Clinical research reports show symptoms of hypoglycemia and confirm that blood sugar is lowered (reports of allergic reactions such as blood sugar urticaria; 4. Other reactions: including gastrointestinal reactions (abdominal pain, indigestion, diarrhea), headache, mild edema, and increased lactic acid, pyruvic acid, uric acid, and serum potassium.

Nateglinide is contraindicated in the following patients: 1. Allergic to the active ingredients of the drug or any excipients; 2. Type 2 diabetes (insulin-dependent diabetes); 3. Diabetic ketoacidosis.

Precautions for children: The safety and efficacy of nateglinide in pediatric patients have not been evaluated. Therefore, nateglinide is not recommended for use in children. Precautions for pregnancy and lactation: Nateglinide has no teratogenic effects on mice and rabbits. There is no experience of pregnant women taking this drug, so the safety of nateglinide during human pregnancy cannot be estimated. Like other oral antidiabetic drugs, nateglinide is not recommended for use during pregnancy. Nateglinide can be excreted from mouse milk after oral administration. Although it is not clear whether nateglinide can be excreted from human milk, the possibility of hypoglycemia in breastfed infants exists. Therefore, nateglinide should not be used in lactating women. Precautions for the elderly: No differences in drug safety and efficacy were observed between elderly patients and the general population. In addition, age does not affect the pharmacokinetic characteristics of nateglinide. Therefore, there is no need to adjust the dose for elderly patients.

In vitro studies have shown that nateglinide is mainly metabolized by the cytochrome P450 enzyme CYP2C9 (70%) and partially by CYP3A4 (30%). In vitro experiments have shown that it can inhibit the metabolism of mesitylbutazone, based on which it is judged that nateglinide is a potential inhibitor of CYP2C9 in vivo. In vitro experiments have shown that the drug has no inhibitory effect on the metabolic reaction of CYP3A4. In summary, these findings indicate that the potential for clinically significant pharmacokinetic interactions between this drug and other drugs is low. Nateglinide has no effect on the pharmacokinetic characteristics of the following drugs: warfarin (a substrate of CYP3A4 and CYP2C9), diclofenac sodium (a substrate of CYP2C9), troglitazone (a CYP3A4 inducer), and digoxin. Therefore, no dose adjustment is required for nateglinide, digoxin, warfarin, or diclofenac sodium when used together. Similarly, there is no clinically significant pharmacokinetic interaction between nateglinide and other oral antidiabetic drugs, such as metformin or glyburide. Nateglinide is highly bound to serum proteins (98%), primarily to albumin. In vitro displacement studies with highly protein-bound drugs have shown that they have no effect on the protein binding of nateglinide. These drugs are: furosemide, propranolol, captopril, nicardipine, pravastatin, glyburide, warfarin, phenytoin sodium acetylsalicylic acid, tolbutamide, and metformin. Similarly, nateglinide has no effect on the serum protein binding of propranolol, glyburide, nicardipine, warfarin, phenytoin sodium, acetylsalicylic acid, and tolbutamide. Physicians should consider the interaction of some drugs that affect glucose metabolism with nateglinide: The hypoglycemic effect of oral antidiabetic drugs can be potentiated by certain drugs, including nonsteroidal anti-inflammatory drugs, salicylates, monoamine oxidase inhibitors, and non-selective beta-adrenergic blocking agents. The hypoglycemic effect of oral antidiabetic drugs can be weakened by certain drugs, including thiazides, cortisone, thyroid preparations and sympathomimetics. Patients receiving nateglinide should be closely monitored for changes in blood sugar when adding or stopping the above drugs.

Keep away from light and store in sealed container.

90mg

60 months.

YANGTZE River Pharmaceutical Group Nanjing Pharmaceutical. Co., Ltd.

• Founded in:

  2001-01-16

• Address:

  No. 9 Xianlin Avenue, Qixia District, Nanjing

• Tax NO.:

  91320192726063334T

• Registered Funds:

  50 million yuan

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