Rosiglitazone Maleate Tablets

It can play a role in lowering blood sugar by increasing tissue sensitivity to insulin and improving cell utilization of glucose. It can significantly reduce fasting blood sugar and insulin and C-peptide levels, and also has a significant effect on reducing postprandial blood sugar and insulin. It significantly reduces the level of glycosylated hemoglobin (HbAlc). The mechanism of action of this product is related to the specific activation of a nuclear receptor: peroxisome proliferator-activated g-type receptor (PPARg). In humans, PPARg receptors are distributed in some key target tissues of insulin action, such as adipose tissue, skeletal muscle and liver. The function of PPARg nuclear receptor is to regulate the transcription of insulin response genes, and insulin response genes are involved in controlling glucose production, transport and utilization. In addition, PPARg response genes also regulate fatty acid metabolism. In animal models, rosiglitazone can increase the sensitivity of liver, muscle and adipose tissue to insulin. It can be seen that the expression of insulin-mediated glucose transporter GLUT-4 in adipose tissue is increased. The condition for the effectiveness of thiazolidinediones in the treatment of type 2 diabetes is that the patient still has a certain ability to secrete insulin. If insulin is severely deficient, it will not work. Pharmacokinetics: Oral absorption bioavailability is 99%, the plasma peak time is about 1 hour, and the plasma elimination half-life (t1/2) is 3 to 4 hours. Eating has no significant effect on the total absorption of this product, but the peak time is delayed by 2.2 hours and the peak value is reduced by 20%. The average oral distribution volume of this product is 17.6L (30%). 99.8% is bound to plasma proteins, mainly albumin. This product is mainly excreted from the urine in its original form, and the main metabolic pathway is to bind to sulfate or glucuronic acid through N-demethylation and hydroxylation. All circulating metabolites have no insulin sensitizing effect. In vitro tests have confirmed that most of this product is metabolized through the CYP2C8 pathway of the P450 enzyme system, and a small amount is metabolized through the CYP2C9 pathway. After oral or intravenous administration of 14C-labeled rosiglitazone, 64% is excreted through urine and 23% is excreted through feces. Clinical studies have confirmed that the pharmacokinetic parameters of rosiglitazone are not affected by age, race, smoking or drinking.

Chemical name: (±)-5-[[4-[2-(methyl-2-pyridylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione (Z)-2-butenedioate. Molecular formula: C18H19N3O3S·C4H4O4 Molecular weight: 473.52

This product is an orange film-coated special-shaped tablet. After removing the coating, it is white or off-white.

This product is suitable for type 2 diabetes. Taking this product alone, supplemented with diet control and exercise, can control blood sugar in patients with type 2 diabetes. For patients with type 2 diabetes who have poor blood sugar control with diet control and exercise plus this product or with a single antidiabetic drug, this product can be used in combination with metformin or sulfonylurea drugs. For patients who take the maximum recommended dose of metformin or sulfonylurea drugs and have poor blood sugar control, if this product cannot replace the original antidiabetic drug, it needs to be used in combination with it. Dietary control is the first choice for the treatment of type 2 diabetes. Restricting calories, losing weight and increasing exercise can all help improve insulin sensitivity. Therefore, these measures are not only the basic treatment for type 2 diabetes, but also play an important role in effectively maintaining the efficacy of drugs. Before starting to take this product, diseases that affect blood sugar control, such as infection, should be diagnosed and treated.

Oral: When used as a monotherapy or in combination with sulfonylureas or metformin, the initial dose is 4 mg per day, taken as a single dose. After 12 weeks of treatment, if necessary, the dose can be increased to 8 mg per day, taken once or twice a day.

1. This product rarely causes hypoglycemia when used alone (<2%). 2. Effects on the liver: In a comparative trial for the treatment of type 2 diabetes, the incidence of elevated alanine aminotransferase (ALT) levels was 3 times higher than normal. 3. Mild to moderate edema and mild anemia were more common in elderly patients (≥65 years old) than in those under 65 years old. The incidence of edema was 7.5%:3.5%, and that of anemia was 2.5%:1.7%.

It is contraindicated for those who are allergic to this product.

Precautions for children: Existing data are insufficient to recommend the use of this product in children. Precautions for pregnancy and lactation: Pregnancy Drug Safety Classification Catalog Class C Regardless of whether there is drug exposure, all pregnancies have a background risk of birth defects, miscarriage or other adverse outcomes. This risk is higher for hyperglycemic pregnancies, but the risk can be reduced by good metabolic control. Therefore, it is very important for patients with diabetes or a history of gestational diabetes to maintain good metabolic control before and throughout pregnancy. Blood sugar control should be closely monitored for such patients. Experts recommend the use of insulin monotherapy during pregnancy to maintain blood sugar levels as close to normal as possible. It has been reported that this product can pass the human placental barrier and can be measured in fetal tissue. There is not enough data on the use of this product during human pregnancy and lactation. This product should not be used during pregnancy. This product can restore ovulation in premenopausal and anovulatory women with insulin resistance, so it is recommended that patients take contraceptive measures when taking this product. Drug-related components can be detected in the milk of lactating rats, and it is not clear whether rosiglitazone is secreted into human milk. Since many drugs can be secreted into human breast milk, this product should not be used in breastfeeding women. Elderly precautions: Population pharmacokinetic analysis shows that age has no significant effect on the pharmacokinetics of rosiglitazone (see [Clinical Pharmacokinetics] Special Populations), so elderly patients do not need to adjust the dose due to age when taking this product. In clinical controlled trials, no overall differences were observed in the safety and efficacy of the drug between the elderly group (≥65 years old) and the adult group (<65 years old).

1. There is no clinical interaction with nifedipine, oral contraceptives (ethinyl estradiol, norethindrone) and other drugs metabolized by CYP3A4. 2. When used in combination with glibenclamide, metformin or acarbose, it has no effect on the steady-state pharmacokinetics and clinical efficacy of these drugs. 3. It does not affect the metabolism and clinical treatment of digoxin, warfarin, ethanol, ranitidine, etc. in the body. 4. When used in combination with sulfonylureas, it does not significantly increase the frequency of hypoglycemia caused by the latter. 5. When used in combination with metformin, it does not increase the incidence of gastrointestinal reactions of the latter and does not increase plasma lactate concentration.

Sealed, stored in a dry place below 30°C. The validity period is tentatively 2 years.

4mg

36 months