nateglinide tablets

Nateglinide is an amino acid derivative and an oral antidiabetic drug used to treat patients with type 2 diabetes. The action of nateglinide depends on the function of pancreatic beta cells. Nateglinide binds to the ATP-sensitive K channel receptor on the beta cell membrane and closes it, causing cell depolarization, calcium channel opening, calcium influx, stimulating insulin secretion, and lowering blood sugar. The insulin secretion-promoting effect of nateglinide depends on the glucose level. When the glucose level is low, the insulin secretion is weakened. Nateglinide has a high degree of tissue selectivity and has a low affinity for cardiac muscle and skeletal muscle.

The main ingredient of this product is nateglinide. Chemical name: N-(trans-4-isopropylcyclohexyl-1-formyl)-D-phenylalanine

This product is white or off-white tablets.

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

The usual dose of this product is 120 mg before meals. It can be used alone or in combination with metformin. The dose should be adjusted according to the results of regular HbA1c tests. Because the main therapeutic effect of nateglinide is to reduce blood sugar during meals (which is an important component of HbA1c), the therapeutic effect of nateglinide can also be monitored by blood sugar 1-2 hours after meals. In clinical trials, nateglinide is usually taken before the main meals, namely breakfast, lunch and dinner. For patients whose HbA1c levels are close to the treatment target at the beginning of treatment (i.e. HbA1c < 7.5%), it can be used alone or in combination with metformin. Take 60 mg of nateglinide before meals and adjust the dose according to the effect of treatment. Dosage for patients with liver damage: The drug dose does not need to be adjusted for patients with mild to moderate liver disease. In patients with type 2 diabetes with mild to moderate hepatic insufficiency, the bioavailability and half-life of nateglinide are not different from those of healthy people to a clinically significant degree. The use of nateglinide in patients with severe liver disease has not been studied, so patients with severe liver disease should use nateglinide with caution. Dosage for patients with renal impairment: No dose adjustment is required for patients with renal impairment. In diabetic patients with moderate to severe renal insufficiency (creatinine clearance 15-50ml/min/1.73m2) and patients requiring dialysis, the bioavailability and half-life of nateglinide compared with healthy subjects do not differ to a clinically significant degree.

Hypoglycemia: As with other antidiabetic drugs, symptoms of hypoglycemia can be observed after taking nateglinide. These symptoms include sweating, shivering, dizziness, increased appetite, palpitations, nausea, fatigue and weakness. These symptoms are generally mild and easy to deal with, and carbohydrates can be consumed if necessary. Clinical research reports show that the proportion of patients with symptoms of hypoglycemia and confirmed blood sugar reduction (blood sugar 3.3mmol/L) is 2.4%. Liver function: Very few patients have increased liver enzymes, which are mild and transient and rarely lead to discontinuation of medication. Allergies: There are very few reports of allergic reactions such as rash, itching and urticaria. Other reactions: Other adverse events found in clinical trials, including gastrointestinal reactions (abdominal pain, indigestion, diarrhea), headaches, and some clinical symptoms that may be associated with diabetic patients (such as respiratory tract infections), occurred at similar rates in the nateglinide treatment group and the placebo treatment group.

Nateglinide is contraindicated in the following patients: 1. Allergic to the active ingredients of the drug or any excipients; 2. Patients with type 1 diabetes (insulin-dependent diabetes); 3. Patients with diabetic ketoacidosis; 4. Pregnant and lactating patients (see: Use of drugs in pregnant and lactating women); 5. Use with caution in patients with severe infection, before and after surgery, or with severe trauma.

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.

Data from in vivo and in vitro studies indicate that nateglinide is metabolized primarily by the cytochrome P450 enzyme CYP2C9 (70%) and partially by CYP3A4 (30%). Nateglinide can inhibit the in vitro metabolism of tolbutamide (a substrate of CYP2C9). In vitro studies have shown that the drug has no inhibitory effect on the metabolic reaction of CYP3A4. These findings suggest that the potential for clinically significant pharmacokinetic interactions between the 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 (a substrate of CYP2C9), troglitazone (a CYP3A4 inducer), and digoxin. Therefore, no dose adjustment is required for nateglinide, digoxin, warfarin, or diclofenac when used together. Similarly, there are no clinically significant pharmacokinetic interactions between nateglinide and other oral antidiabetic drugs, such as metformin or glyburide. When co-administered with sulfinpyrazone (a highly potent and selective CYP2C9 inhibitor), a modest increase in the AUC of nateglinide (28%) was observed in healthy subjects, whereas the mean Cmax and elimination half-life did not change. A prolonged duration of action and the risk of hypoglycemia cannot be excluded when nateglinide is co-administered with CYP2C9 inhibitors. Nateglinide is highly bound to serum proteins (98%), mainly 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, acetylsalicylic acid, tolbutamide and metformin. Similarly, nateglinide had no effect on the serum protein binding of propranolol, glyburide, nicardipine, warfarin, phenytoin, 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 enhanced by certain drugs, including nonsteroidal anti-inflammatory drugs, salicylates, monoamine oxidase inhibitors and non-selective beta-adrenergic blockers. 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 observed for changes in blood sugar when adding or stopping the above drugs.

Sealed, store below 30℃.

60mg

60 months.

Anhui Guozheng Pharmaceutical Co., Ltd.

• Founded in:

  1999-01-16

• Address:

  No. 6, Xiyou Road, Yanhe Community, Changqing Street, Baohe District, Hefei City

• Tax NO.:

  91340100711742115T

• Registered Funds:

  53.5 million yuan

• Email:

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