The so-called best drugs are safe, effective and cheap, which are the three basic criteria for judging the therapeutic status of a drug. At present, clinical antidiabetic drugs can be divided into 9 categories, including: 3 categories of injectable drugs: – insulin class, pramlintide, exenatide; 6 categories of oral drugs: sulfonylureas (such as glibenclamide, glipizide, glimepiride), biguanides (such as metformin), glitazones (such as rosiglitazone, pioglitazone), glinides (such as repaglinide, nateglinide), alpha-glucosidase inhibitors (such as acarbose Six types of oral drugs are the main types of treatment for type 2 diabetes. In recent years, the relevant U.S. agencies have organized relevant experts to conduct a comprehensive evaluation of oral antidiabetic drugs and released a new study in February 2009, the conclusions of which are of great help to domestic clinical use.
The conclusions of the study.
1. the efficacy of the new drugs is not better. Gliadinones, glinides, alpha-glucosidase inhibitors and dipeptidyl peptidase 4 inhibitors are four types of drugs that have been listed in recent years. Compared with the old varieties of sulfonylureas and metformin, their hypoglycemic effects are not superior, such as acarbose, miglitol, nateglinide and sitagliptin, which lower HbAlc (glycosylated hemoglobin) worse than sulfonylureas and metformin.
2. The safety of the new drugs is not better. All oral antidiabetic drugs may cause adverse reactions to a lesser or greater extent, and the safety of newly marketed drugs is not more assured than older varieties such as sulfonylureas and metformin.
3, metformin is the preferred variety of oral diabetes drugs. The role of this product to reduce HbAlc is no less than or better than each of the other varieties, generally do not increase weight and can reduce LDL and triglycerides, for no obvious kidney, liver or heart disease of diabetic patients is the safest drug.
4, the combination of two drugs to reduce the HbAlc better. When a drug alone is not effective in controlling blood sugar, should promptly consider the combination of drugs, but the incidence of adverse reactions may also increase, if the application of the combination, the drug dose can be reduced accordingly, adverse reactions can also be reduced.
5. The cost of new drugs is more expensive. Compared with the old varieties such as glibenclamide, glipizide, glimepiride, metformin, the price of newly listed drugs is often several times to dozens of times higher. In addition, old varieties such as glibenclamide, glipizide and metformin have been included in the national essential drugs catalog (the part equipped for use in primary health care institutions).
It is worth emphasizing that when oral medications cannot effectively control the condition, insulin or other injectable preparations should be considered.
At present, there are four major categories of oral hypoglycemic drugs used to treat diabetes in China.
1, insulin stimulants (Sulphonyl-ureas, SU). The main oral hypoglycemic drugs are sulfonylureas, such as methylsulfonylurea (D860), chlorosulfonylurea, euglycemia, pyrimethoprim, methylsulfonylurea (DAMAC), ketorol, glucophage, and regeneron, such as nandrolone.
2.Insulin sensitizers. They are mainly biguanides, such as glucagon, metformin, gevalt, lycopodium, meticam, diosgenin, etc.; and thiazolidinediones, such as troglitazone, pioglitazone, rosiglitazone (vindia), etc.
3. α-glucosidase inhibitors. Such as bai sugar apple.
4.Chinese patent medicines. Single medicine such as Huanglian, bitter melon; compound such as hypoglycemic A tablets, mulberry granules, etc.
Insulin stimulants.
Sulfonylurea hypoglycemic agents.
Sulfonylureas hypoglycemic agents are the most widely used oral hypoglycemic agents at home and abroad. Its main mechanism of action is to directly stimulate the secretion of insulin by pancreatic β-cells, which also has extra-pancreatic effects and increases insulin sensitivity, so as to achieve hypoglycemic effects. Currently, sulfonylureas are classified into the 1st, 2nd and 3rd generation according to the order of their discovery, with the 1st generation including tosylurea and chlorosulfonylurea. The second generation was used in clinical practice in the 1960s and included gliphenylurea (eugenol), glipizide (mepiquat), gliclazide (damacell), and gliquidone (glucophage). Third generation glimepiride.
Indications: Since the main mechanism of action of sulfonylurea hypoglycemic agents is to stimulate insulin secretion, they are suitable for patients with type 2 diabetes mellitus who still have some pancreatic islet function and are still not satisfactorily controlled by diet therapy.
(1) Patients with non-insulin-dependent diabetes mellitus (type 2) starting in middle age or above, who have failed to satisfactorily control hyperglycemia with once diet therapy and exercise therapy. About 20-30% of patients between the ages of 20 and 40 years can be treated with sulfonylureas for the first few years without the need for insulin therapy.
(2) Patients with type 2 diabetes starting at the age of 40 or above, with fasting blood glucose >11.1mmol/L, with a disease duration of 5 years or less, who have never been treated with insulin, and who are of normal weight or obese, may also choose sulfonylureas or combine them with biguanides.
(3) Some patients with slow onset type 1 diabetes have not yet completely lost their pancreatic islet B cells in the early stage, and these drugs also have a partial therapeutic effect, but in order to protect the function of the remaining pancreatic islet B cells, they should be switched to insulin or combined with insulin as early as possible.
(4) In recent years, the trial and insulin combination therapy can enhance the efficacy. It is believed that for type 2 diabetic patients, sulfonylurea hypoglycemic drugs can be added to insulin therapy after secondary failure, without stopping the use of sulfonylurea hypoglycemic drugs.
Contraindications.
The following diabetic patients are not suitable for taking sulfonylurea hypoglycemic drugs.
1, where pediatric diabetic patients or insulin-dependent (type 1) diabetic patients, should not apply sulfonylureas.
2, diabetic ketosis, especially with metabolic acidosis or ketoacidosis, or hyperosmolar coma is prohibited.
3.Severe infections, high fever, surgery, pregnancy, childbirth, and various acute and chronic complications of the heart, kidney, liver and brain are contraindicated.
4, jaundice, hematopoietic system inhibition, leukocyte deficiency and allergic or toxic reactions to sulfonylureas are prohibited.
5. Patients who can be controlled by diet or who must lose weight should be treated with a combination of diet and exercise therapy, which should be tried only when hyperglycemia is not controlled, but diet and exercise must still be the mainstay, supplemented by drugs.
Diabetic patients with the following conditions should be especially cautious and preferably do not use sulfonylurea hypoglycemic drugs.
Diabetic patients with liver and kidney dysfunction should use them with caution because sulfonylureas need to be inactivated by the liver, i.e., metabolized by the liver into metabolites with no hypoglycemic effect before they can be excreted from the body. When there is liver dysfunction, such as cirrhosis, the liver’s ability to inactivate these drugs decreases, and they cannot be metabolized in time, so serious and persistent hypoglycemia can easily occur, and when liver function is seriously damaged, the liver’s ability to produce glucose decreases, which may induce hypoglycemia or increase the severity of hypoglycemia, so it should be used constantly for those with liver dysfunction.
Sulfonylureas can make weight gain and biguanides can make weight loss. It is generally advocated that the combined medication should be used early and the dose used should be small, and then the dose should be adjusted gradually according to the blood sugar situation until the effect of satisfactory blood sugar control is obtained. For those who do not have satisfactory effect with biphasic drugs alone, sulforaphane can be added, and vice versa, for those who have primary or secondary failure of sulforaphane, biphasic drugs can also be added.
BIGUIDIN hypoglycemic drugs and sulfonylurea hypoglycemic drugs in combination must pay attention to what kinds of drugs can be used and what kinds of people can not use, especially to pay special attention to liver and kidney function.
Biguanides can also be used in combination with insulin. Whether type 1 or type 2 diabetes is being treated with insulin, patients who want to reduce the amount of insulin or enhance the efficacy of insulin can take additional biguanide hypoglycemic drugs. However, it should be noted that patients with type 1 diabetes who are not treated with insulin cannot be treated with biguanides alone, because these drugs must have insulin in the body in order to play a role in lowering blood sugar.
Sulfonylurea hypoglycemic drugs toxic side effects.
The toxic side effects of sulfonylureas are generally very small, but hypoglycemia is likely to occur with improper use of the drug. Common side effects include.
1. Gastrointestinal reactions. Loss of appetite, nausea, vomiting, diarrhea and abdominal pain, etc., which can subside after the drug dosage is reduced.
2, skin reactions. Such as skin itching, erythema, urticaria, measles-like rash or maculopapular rash, etc., can gradually subside after reducing the amount of the drug, if persistently does not subside, should stop using. Occasionally, serious exfoliative dermatitis is seen, and the use of such drugs should be stopped immediately.
3. Blood system reaction. There are leukopenia, granulocyte deficiency, thrombocytopenia, hemolytic anemia, regenerative dysplasia.