Phenformin Hydrochloride_Kain Industrial Additives

Phenformin hydrochloride
[Overview] Phenformin hydrochloride is a biguanide hypoglycemic drug. It has a hypoglycemic effect on people with diabetes who have normal or lost pancreatic islet function, but is ineffective on normal people. It is suitable for patients with type 2 diabetes who are not satisfied with simple diet control, especially those who are obese and those with hyperinsulinemia. Phenformin hydrochloride can lower the patient’s blood sugar, and can also reduce weight and hyperinsulinemia. If it is combined with sulfonylurea hypoglycemic drugs, it can produce a synergistic effect, which is better than using it alone. Currently, some countries have banned this drug. Because this drug is effective, cheap and easy to obtain, it is easily incorporated into traditional Chinese medicine anti-diabetic preparations, misleading patients and seriously affecting drug safety.
【Physical and chemical properties】
Appearance and properties: white powder
Density: 1.24 g/cm3
Melting point: 175-178ºC
Boiling point: 413.7ºC at 760 mmHg
Flash point: 204ºC
【Pharmacological effects】
It is a biguanide oral hypoglycemic drug. Its mechanism of hypoglycemic action is mainly to increase the amount of glucose uptake by adipose tissue, but it cannot promote the secretion of insulin and increase the anaerobic glycolysis rate of muscle tissue, thereby improving the utilization of glucose; it also has an antagonistic effect on anti-insulin factors; it can inhibit Hepatic gluconeogenesis reduces the production of glucose; hinders the absorption of glucose in the digestive tract, ultimately reducing blood sugar concentration. In addition, this product can also inhibit the body’s release of glucagon.
【Pharmacokinetics】
It can be rapidly absorbed after oral administration, with a bioavailability of 60%, a plasma protein binding rate of 20%, a drug effect that lasts for 6 to 8 hours, and a half-life of 3 to 5 hours. This product is mainly metabolized in the liver, and about 1/3 will be excreted through the kidneys in the form of metabolites.
【Indications】
It can be used for adults with non-insulin-dependent diabetes and some insulin-dependent diabetes. For some unstable or juvenile diabetes, it can be used in combination with insulin to control blood sugar and reduce the dosage of insulin. It can be used to suppress appetite and inhibit intestinal absorption of glucose to reduce the weight of obese diabetic patients.
【Drug Interaction】
1. It can enhance the anticoagulant effect of anticoagulants (such as warfarin, etc.) and may cause bleeding tendencies.
2. When used together with insulin, the blood sugar-lowering effect will be enhanced. When used together, the dose of insulin should be reduced.
【Adverse reactions】
1. Nausea, vomiting, diarrhea, metallic taste in mouth;
2. There will be symptoms such as fatigue, tiredness, weight loss, dizziness, rash, etc.;
3. It can reduce the intestinal absorption of vitamin B12, reduce hemoglobin, produce megaloblastic anemia, and also cause malabsorption;
4. Lactic acidosis occurs, with clinical manifestations such as vomiting, abdominal pain, hyperventilation, and mental disorder. Increased lactic acid concentration in the blood cannot be explained by uremia, ketoacidosis, or salicylic acidosis.
【Notes】
1. After using this product, the anaerobic glycolysis reaction of glucose in the body increases, and the production of lactic acid increases, which in turn causes severe lactic acidemia, with a mortality rate of 50%.
2. It is contraindicated in patients with congestive heart failure, liver and kidney dysfunction, diabetes complicated by ketoacidosis, and acute infection. Pregnant women should weigh the pros and cons when using this product.
3. If serious gastrointestinal adverse reactions occur, the dosage of this product should be reduced or discontinued.
4. During the treatment process, close observation is required during the first administration to prevent the occurrence of hypoglycemia, coma and acidemia.
5. If you take this product while drinking alcoholic beverages, it may cause acidemia, abdominal pain, and hypothermia.
【Taboo】
1. Type Ⅱ diabetes is accompanied by ketoacidosis, liver and renal insufficiency (serum creatinine exceeds 1.5 mg/dl), heart failure, acute myocardial infarction, severe infection and trauma, major surgery, and clinical hypotension and hypoxia;
2. Diabetes combined with serious chronic complications (such as diabetic nephropathy, diabetic fundus lesions);
3. Patients with vitamin B12, folic acid and iron deficiencies;
4. Patients with severe heart and lung diseases;
5. Alcoholics;
6. People who are known to be allergic to this product;
7． Before intravenous pyelography or arteriography;
8. Patients with poor general condition (such as malnutrition, dehydration).
【Main References】
1. Fang Luqiu et al. Determination of phenformin hydrochloride by flow injection chemiluminescence method using NBS-fluorescein system [J]. Journal of Analytical Testing, 2004, 23(2): 20-22.
2. Li Bing et al. Identification of metformin hydrochloride, phenformin hydrochloride, gliclazide and glibenclamide as ingredients in traditional Chinese medicine hypoglycemic preparations and Western medicines [J]. Journal of Shandong University (Medical Edition), 2006, 44(8): 843-845.
3. https://drugs.medlive.cn/drugref/html/1999.shtml