Instructions for use of dipotassium biguanide sustained-release tablets

As people age, their height and physical fitness will become worse. The three highs are the most common diseases among the middle-aged and elderly people. Patients with the three highs must not only control their diet, but also cannot get rid of the root cause, they can only control it. Moreover, sudden onset of high blood pressure will threaten people's life safety. High blood sugar is also very dangerous, which will cause blurred vision and increased urine sugar. Metformin sustained-release tablets can be used to treat hyperglycemia. The following is the instruction manual of dipotassium biguanide sustained-release tablets.

[Ingredients] The main ingredient of this product is metformin hydrochloride, and its chemical name is 1,1-dimethylbiguanide hydrochloride.

【Properties】This product is white or off-white irregular tablets.

【Action Category】

[Pharmacology and Toxicology] Pharmacology: It can promote the binding of insulin to receptors and improve the sensitivity of diabetic patients to insulin, increase the anaerobic glycolysis of sugar in peripheral tissues and promote the utilization of sugar, inhibit fat decomposition, reduce plasma free fatty acid levels, weaken insulin resistance and improve the utilization of glucose, thereby playing the role of lowering blood sugar, lowering blood lipids and inhibiting arteriosclerosis. Toxicology: The oral LD50 of metformin hydrochloride in rats is 1.0g/kg, and the subcutaneous LD50 is 0.3g/kg.

[Pharmacokinetics] After oral administration, it is absorbed through the gastrointestinal tract and its effect lasts for 24 hours. The plasma protein binding rate is less than 5%. It is not metabolized by the liver and is excreted through the kidneys. About 1/3 is excreted in the urine in the form of metabolites of hydroxyphenformin. The relative bioavailability of a single dose of metformin hydrochloride extended-release tablets was 101.7±14.6% compared with that of ordinary tablets. Compared with ordinary tablets, the apparent half-life (T1/2) of sustained-release tablets were 5.78±1.18 and 2.62±0.46h, Tmax were 3.3±0.7 and 2.2±0.3h, Cmax were 1.80±0.37 and 2.49±0.38μg·ml-1, and the mean residence time (MRT) was 8.14±1.31 and 4.69±0.76h. The peak time of metformin hydrochloride sustained-release tablets was delayed, the peak concentration was reduced (P=0.0001), and the (apparent) half-life was prolonged. The relative bioavailability F of metformin hydrochloride sustained-release tablets after multiple doses to steady state was 87.0±8.5%.

[Indications] (1) It can be used for patients with type 2 diabetes (non-insulin-dependent) who are unsatisfactory in controlling their body weight with diet alone, especially those who are obese. It may have the effect of reducing their weight. (2) It is effective for some patients with type 2 diabetes who have poor response to sulfonylureas.

[Usage and Dosage] Oral administration, during or after meals. The initial dosage is usually once a day, 1 tablet (500 mg) at a time, taken with dinner. The dosage is adjusted according to blood sugar and urine sugar. The maximum daily dosage should not exceed 4 tablets (2000 mg). If taking 4 tablets (2000 mg) once a day does not achieve satisfactory therapeutic effect, it can be changed to taking 2 tablets (1000 mg) twice a day.

[Adverse Reactions] 1. Gastrointestinal reactions such as nausea, vomiting, and diarrhea may occur occasionally. 2. Feeling weak, tired, dizzy, or have a rash. 3. Although the incidence of lactic acidosis is very low, it should be paid attention to. 4. It can reduce the intestinal absorption of vitamin B12.

[Contraindications] This product is contraindicated in patients with type 2 diabetes accompanied by ketoacidosis, liver and kidney dysfunction (serum creatinine exceeds 1.5 mg/dl), pulmonary insufficiency, heart failure, acute myocardial infarction, severe infection and trauma, major surgery, and clinical hypotension and hypoxia; patients with a history of lactic acidosis and those who are allergic to this product.

[Precautions] 1. In patients using metformin hydrochloride, lactic acidosis may occur due to accumulation of metformin hydrochloride. This is a rare and serious metabolic complication that can be life-threatening if it occurs. Patients taking this drug should have their renal function monitored and the drug should be administered at the lowest effective dose to significantly reduce the risk of lactic acidosis. 2. This product is not allowed to be chewed orally. It should be swallowed whole and taken during or after meals. 3. When patients need to undergo radiological studies using intravenous iodinated contrast agents, they should temporarily stop taking this product because this may cause acute changes in renal function. 4. When this product is used in combination with sulfonylurea drugs, it may cause hypoglycemia and the patient's blood sugar level should be monitored. 5. The combined use of this product with insulin will enhance the hypoglycemic effect, so the dosage should be adjusted. 6. Blood sugar, glycosylated hemoglobin, urine sugar, and urine ketone bodies should be monitored regularly. 7. Some patients were found to have lower than normal vitamin B12 levels in the absence of clinical symptoms. This may be because metformin hydrochloride interferes with the absorption of vitamin B12, which may lead to anemia. Although the possibility is small, it is still recommended to monitor the patient's blood picture and check blood parameters at least once a year. 8. When this product is taken together with ethanol, it will enhance the effect of metformin hydrochloride on lactic acid metabolism, which can easily lead to lactic acidosis. Therefore, you should try to avoid drinking alcohol when taking this product. 9. If allergic reactions such as rash occur, stop using this product.