Patent of pyrazolic acid

Drug name: Gliclazide English name: gliclazide Chinese alias: Dymecon, metsulfuron-methyl bicyclol, gliclazide, Youdaling, ractopamine, metsulfuron-methyl drug category: pancreatic hormone and other drugs affecting blood sugar English alias: Diamicron, Dramion, Nordialex Specification: tablets, 80mg each.

Edit the pharmacodynamics and pharmacokinetics of this paragraph.

Promoting islet B cells to secrete insulin, provided that islet B cells have certain functions of synthesizing and secreting insulin; By increasing the insulin level in portal vein or directly acting on the liver, glycogen decomposition and gluconeogenesis in the liver are inhibited, and the production and output of glucose in the liver are reduced; It may also increase the sensitivity of extrapancreatic tissue to insulin and the utilization of sugar (probably mainly through post-receptor action). So the overall effect is to reduce fasting blood glucose and postprandial blood glucose. It is absorbed quickly, and the blood concentration reaches the peak 2-6 hours after oral administration, and the duration can reach 24 hours. T 1/2 is 10 ~ 12 hours, which is mainly inactivated by liver metabolism and can be excreted by 98% the next day. The oral absorption of this product is rapid, the peak time of plasma concentration is 2 ~ 4 hours, the binding rate of plasma protein is 85% ~ 87%, the duration of action is 2 ~ 4 hours, and the serum half-reduction period is 10 ~ 12 hours. Most of this product is metabolized into inactive metabolites by the liver in vivo. After administration, 59% was excreted in urine within 1 day, a small amount was excreted in feces, and 95% was excreted in kidney within 5 days.

Pharmacological effects of editing this paragraph

This product is a second-generation sulfonylurea oral hypoglycemic agent, which has hypoglycemic effect on both normal people and diabetic patients. Its hypoglycemic intensity is between metsulfuron and glibenclamide. This product mainly acts directly on the pancreas, promoting the transport of Ca++ to islet β cells and stimulating insulin secretion. At the same time, it can also improve the metabolism of glucose in surrounding tissues, thus reducing blood sugar. ?

In addition, this product can inhibit the release of arachidonic acid from phospholipids in platelets, thus reducing the synthesis of thromboxane (TXA3), inhibiting various coagulation factors (such as ⅴ, ⅷ,), improving the level of plasminogen activator and promoting fibrinolysis. Animal experiments have also found that this product can reduce the levels of plasma cholesterol, triglycerides and fatty acids.

Edit this instruction

It is suitable for mild and moderate non-insulin-dependent diabetes mellitus with unsatisfactory effect of simple diet control. The patient's islet B cells have certain β cells secreting insulin.

Yes, there are no serious complications. It is mainly used for mild and moderate diabetes with ineffective diet control and no ketosis tendency in adulthood. It can also improve the fundus lesions and metabolic and vascular dysfunction of diabetic patients. For patients who cannot be controlled by single use, it can be combined with biguanide oral hypoglycemic agents and insulin to treat insulin-dependent diabetes, which can reduce the dosage of insulin.

Edit this paragraph of adverse reactions and treatment.

Occasionally mild nausea, vomiting, epigastric pain, constipation, diarrhea, erythema, urticaria, thrombocytopenia, granulocytopenia, anemia and so on. , mostly Gretchett.

The number disappeared after stopping the drug. Severe liver and renal insufficiency is prohibited. It is forbidden for those who are allergic to sulfonylureas. Patients with type II diabetes should be treated with insulin under stress such as infection, trauma and operation, as well as ketoacidosis and non-ketotic hyperosmolar diabetes coma. Not suitable for patients with type I diabetes. When combined with non-steroidal anti-inflammatory drugs (especially salicylates), sulfonamides, dicoumarin anticoagulants, monoamine oxidase inhibitors, receptor blockers, benzodiazepines, tetracycline, chloramphenicol, dicyclofibrate, ethanol and other drugs, the dosage should be reduced to avoid hypoglycemia. When combined with anticoagulant drugs, we should often do related coagulation tests. When the dosage of the drug is too large, eating too little or exercising vigorously, attention should be paid to prevent hypoglycemia.

Edit this paragraph about drug interaction.

Combined with thiazide diuretics, adrenocortical hormones and estrogen preparations may weaken the hypoglycemic effect of this product. Chloramphenicol, dicoumarin, ethanol

Paterson, oxybutazone, clofibrate and sulfadiazine pyrazole can inhibit the metabolism of this product, enhance the hypoglycemic effect, and may even cause hypoglycemia reaction. Aspirin, phenylbutazone and sulfadiazine can compete with this product to combine with plasma protein, thus enhancing the hypoglycemic effect of this product. When combined with non-steroidal anti-inflammatory drugs (especially salicylates), sulfonamides, coumarin anticoagulants, monoamine oxidase inhibitors, B receptor blockers, benzodiazepines, tetracycline, chloramphenicol, dicyclofibrate, ethanol and other drugs, the dosage should be reduced.

Edit the usage and dosage of this paragraph.

Take 80mg orally at the beginning, once before breakfast or before breakfast and lunch, or 40mg three times a day, before meals, and measure ethanol every day after 7 days if necessary.

Increase 80mg. Generally, the daily dose is 80 ~ 240 mg, and the maximum daily dose is not more than 320mg. Preparation and specifications: gliclazide tablets 80 mg. Oral administration, 80mg once, twice a day at first, for 2-3 weeks, and then increase or decrease the dose according to the condition, with the daily dose range of 80-240mg. Can change the blood picture. Check the blood picture regularly during medication. Juvenile diabetes, diabetic ketosis, diabetic coma, etc. Everyone needs insulin injection, and this product cannot be used alone. After oral administration, the dosage is 160mg per day, generally 80 ~ 160 mg per day at first, and then it can be increased to 240 ~ 320 mg per day according to the illness, and taken twice or three times. If the insulin is replaced by this product, if the original dose is relatively large (about 20 ~ 30IU), the insulin will be halved at 1 day, and this product will be added, and then gradually reduced according to the condition. Blood sugar and urine sugar should be checked regularly during medication, so as to adjust the treatment plan.

Edit the function and purpose of this paragraph.

The second generation of oral sulfonylgiles hypoglycemic agents reached the peak 2-6 hours after oral administration, and the t 1/2 was about 10- 12 hours, which was mainly excreted by the kidney. It has hypoglycemic effect on adult diabetic patients, can reduce platelet adhesion, reduce plasma specific viscosity, reduce ADP-induced platelet aggregation and improve nail fold microcirculation. blood platelet

In addition, the experiment proves that this product can reduce the accumulation of cholesterol and the plasma concentrations of glycerol triphosphate and fatty acids in aorta. Therefore, the combination of the two can not only treat diabetic metabolic disorder, but also prevent vascular diseases and improve retinopathy and renal function. Can be used for adult diabetes, diabetes with obesity or vascular diseases.

Notes for editing this paragraph

1. Pregnant women are prohibited. 2. During taking this medicine, you should always check the blood picture of Gliclazide.

3. Use with caution in patients with renal insufficiency. 4. Juvenile diabetes, diabetic ketosis, diabetic coma, etc. Everyone needs insulin injection, and this product cannot be used alone.