Collection: Comparison and selection of oral hypoglycemic agents, this is very clear!

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Guide: Each type of oral hypoglycemic drugs has its own characteristics. When selecting drugs, it is necessary to fully consider the characteristics of the drugs, and select the drugs according to the specific conditions of the patients.In fact, no drug is the best for all patients, and the best is the best!For a long time, “insulin secretion deficiency” and “insulin resistance” are considered to be the main causes of type 2 diabetes. Traditional oral hypoglycemic drugs are also designed and developed mainly for the above two problems, such as sulfonylureas and glibenclamide.The mechanism of action is to promote insulin secretion, and the mechanism of action of biguanides and thiazolidinediones is to improve insulin resistance.In recent years, with the deepening of the research on the pathogenesis of diabetes, the etiology of type 2 diabetes has developed from the early “duo” to the current “octave”, and some enterogenous hormones (mainly called “incretin” have been discovered.”) and the important role of the kidney in the regulation of blood sugar, many new hypoglycemic drugs have emerged from this, among which the most representative, prospects are generally optimistic when the number “DPP-4 (dipeptidyl peptidase-4Inhibitors” and “SGLT-2 (sodium-glucose cotransporter-2) inhibitors”.Compared with traditional hypoglycemic drugs, these new hypoglycemic drugs not only have good hypoglycemic effect, high safety, but also benefit from other aspects such as weight loss and cardiovascular protection.Below, the author compares the old and new hypoglycemic drugs from the aspects of mechanism of action, advantages, adverse reactions, cost-effectiveness, indications, etc., hoping to help the rational selection of hypoglycemic drugs.1 sulfonylureas These drugs mainly reduce insulin by stimulating islet beta cells to secrete insulin and increase insulin levels in the body.Sulfonylureas are a large family with many members. Currently, glibenclamide, gliclazide, glibenclamide, glipizide, glimepiride, etc. are commonly used in clinical practice. Different sulfonylureas are used.There are some differences in the effects of hypoglycemic effect, duration of action, route of excretion, and risk of hypoglycemia. These points should be fully considered in clinical selection.1. Advantages: 1 significant hypoglycemic effect (effectively reduce fasting and postprandial blood glucose); 2 no adverse effects on cardiovascular; 3 cheap, cost-effective.2. Disadvantages: 1 easy to cause hypoglycemia; 2 can increase weight; 3 a small number of patients will have allergic reactions after medication, such as rash, leukopenia.3. Indications: Suitable for patients with type 2 diabetes (especially non-obese patients) who still retain part of islet function. For patients with type 2 diabetes who cannot tolerate metformin, sulfonylureas may be used as the starting drug.Precautions for use 1) Ineffective for patients with type 1 diabetes, because the islet secretion function of patients with type 1 diabetes has completely failed.2) There may be a primary failure (ineffective at the beginning) or a secondary failure (effective at the beginning, and then gradually decreased until it is ineffective), which is generally considered to be related to the patient’s own islet failure.3) In order to reduce the burden on the kidneys, elderly patients with mild to moderate renal insufficiency should use sulfonylureas (gliclazin), which are mainly excreted via the biliary tract.4) The elderly should not choose a strong, long-acting sulfonylurea (glibenclamide) to avoid the induction of severe hypoglycemia.5) Pregnant women and lactating women are banned.6) Sulfonylureas should not be combined with sulfa antibiotics (such as cotrimoxazole) because they have a synergistic effect and increase the risk of hypoglycemia.2 Glinide is a new generation of non-sulfonylurea insulin secretagogue, which is mainly used to reduce postprandial blood glucose. Representative drugs include repaglinide and nateglinide.1. Advantages: 1 rapid onset, short duration of action, can effectively reduce postprandial hyperglycemia, and is not prone to hypoglycemia before meals; 2 has little effect on body weight; 3 mainly through biliary excretion, renal dysfunction can still beUse; 4 meals immediately, convenient and flexible, patient compliance; 5 when sulfonylureas fail, switching to glinide can still be effective.2. Disadvantages: 1 can cause hypoglycemia, but the incidence is low and the degree is light; 2 the price is high.3. Indications: with sulfonylureas, especially suitable for elderly patients, renal insufficiency and irregular eating disorders in patients with diabetes.Precautions for use 1) Take the medicine and take it before the meal. Do not take the medicine without taking the meal.2) It should not be combined with sulfonylureas.3) Can be combined with other types of oral hypoglycemic drugs and basal insulin.3 Biguanides mainly reduce blood sugar by inhibiting hepatic glycogen output, reducing insulin resistance, promoting glucose uptake and utilization by peripheral tissues, and reducing intestinal absorption of glucose.Biguanides include metformin and phenformin, which have been clinically eliminated because they are prone to lactic acidosis.Metformin is the first choice treatment for type 2 diabetes, which is recommended by major guides at home and abroad.1. Advantages: 1 The effect of hypoglycemic is good, there is no problem of primary or secondary failure; 2 In addition to hypoglycemic, it can also reduce body weight, blood pressure and blood lipids, and has cardiovascular protection; 3 safety is good, aloneApplication does not cause hypoglycemia, metformin is not easy to cause lactic acidosis; 4 low price, high cost performance; 5 recently found: metformin also has anti-cancer, anti-aging and other effects.2. Disadvantages: 1 prone to gastrointestinal reactions; 2 long-term application may affect the absorption of vitamin B12.3. Indications: Applicable to all type 2 diabetic patients without contraindications for oral hypoglycemic agents, especially obese patients with type 2 diabetes.Precautions for use 1) To reduce the irritating effects of the drug on the gastrointestinal tract, it is recommended to take it during or after meals.2) Diabetes patients with heart failure, hypoxia, severe liver and kidney dysfunction are hanged to avoid lactic acidosis.3) Long-term use of metformin can cause a decrease in vitamin B12 levels, and patients are advised to supplement vitamin B12 appropriately.4) Diabetic patients with normal renal function do not need to stop metformin before angiography, but need to stop the drug for 2 to 3 days after using the contrast agent, and continue to use the drug after reviewing normal renal function.5) Pregnant and lactating women are hanged because metformin can be secreted through milk.6) Because biguanide drugs can inhibit the redox ability of mitochondria, metformin is contraindicated in patients with “mitochondrial diabetes”.7) It can be used alone or in combination with other types of oral hypoglycemic agents and insulin.8) The maximum dose of metformin should not exceed 2000 mg / day.4 α-Glycosidase inhibitors These drugs mainly reduce blood sugar (especially postprandial blood glucose) by delaying the absorption of carbohydrates, representing acarbose and voglibose.It is also the only oral hypoglycemic drug currently approved for “pre-diabetes” intervention.1. Advantages: 1 The action site is in the intestinal tract and is hardly absorbed into the blood, so it has no effect on liver and kidney; 2 alone does not cause hypoglycemia; 3 does not increase body weight; 4 has cardiovascular protection.2. Disadvantages: 1 can cause abdominal distension, increased exhaustion, diarrhea and other gastrointestinal reactions; 2 alone can not cause hypoglycemia, but combined with other hypoglycemic agents can cause hypoglycemia.3. Indications: Suitable for diabetic patients with carbohydrates as the main food, postprandial blood glucose rise (including type 1 and type 2), can also be used in “pre-diabetes” patients.Precautions for use 1) The α-glucosidase inhibitor is required to be chewed together with the first meal, and improper administration may affect the therapeutic effect.2) The drug must have a substrate (ie, carbohydrate) to exert hypoglycemic effects.3) Diabetes patients with hernia, intestinal obstruction, gastrointestinal dysfunction, and recent history of abdominal surgery are banned.4) Children, pregnant women and lactating women are prohibited.5) When patients taking α-glucosidase inhibitors have hypoglycemia, they should be corrected immediately by oral or intravenous glucose. Eating starchy foods is often ineffective.Because the drug can inhibit the activity of intestinal alpha-glucosidase, hinder the digestion and absorption of oligosaccharides and polysaccharides.5 Thiazolidinedione insulin sensitizers These drugs mainly exert hypoglycemic effects by enhancing the sensitivity of peripheral tissues such as skeletal muscle, liver and fat to insulin. Representative drugs include rosiglitazone and pioglitazone.It can be used alone or in combination with other oral hypoglycemic agents or insulin.1. Advantages: 1 can significantly reduce insulin resistance, reduce insulin dosage; 2 protect and improve islet β-cell function, delay islet function decline; 3 alone can not cause hypoglycemia.2. Disadvantages: 1 can lead to sodium retention and edema, increase the risk of heart failure; 2 can lead to abnormal liver function; 3 can increase body weight; 4 can cause “dilute anemia” due to water retention; 5 can increase bone loss,Lead to osteoporosis, increase the risk of fracture in postmenopausal women; 6 pioglitazone can also increase the risk of bladder cancer.3. Indications: For patients with type 2 diabetes (especially abdominal obesity) with severe insulin resistance, it can also be used for pre-diabetes intervention.Precautions for use 1) Liver function should be routinely tested before and during drug use, such as when the transaminase (ALT) exceeds the normal high limit by 2.5 times.2) Diabetic patients with cardiac insufficiency and pulmonary edema are banned because they can cause sodium retention and edema.3) Diabetes patients with severe osteoporosis are banned.4) Pregnant and lactating women should avoid taking it.5) Pioglitazone is contraindicated in patients with current bladder cancer or in patients with a history of bladder cancer.6) Taking this medicine is not affected by eating, it can be taken on an empty stomach or at mealtime.7) It takes a slower effect and it takes a few weeks to take effect. Therefore, it is not possible to stop the drug because the short-term effect is not obvious.6 DPP-4 inhibitor DPP-4 inhibitor reduces the inactivation of glucagon-like peptide-1 (GLP-1) in vivo by inhibiting dipeptidyl peptidase-4 (DPP-4), making GLP-1When the level is elevated, GLP-1 stimulates islet β cells to secrete insulin and inhibits islet α cells to secrete pancreatic hyperglycemia in a glucose concentration-dependent manner, thereby lowering blood sugar.Currently listed in China are sitagliptin, saxagliptin, alogliptin, vildagliptin, linagliptin and the like.1. Advantages: 1 has a glucose concentration-dependent hypoglycemic effect, so the risk of hypoglycemia is small; 2 does not increase body weight; 3 does not increase the risk of cardiovascular events; 4 no gastrointestinal adverse reactions, patients are well tolerated5 patients with sulfonylurea failure still have significant hypoglycemic effect; 6 only need to take the drug once a day (Note: except for vildagliptin), before and after meals, treatment compliance is high.2. Disadvantages: 1 can cause headache, pharyngitis, upper respiratory tract infection, etc., but the incidence is very low; 2 occasional hypersensitivity reaction, vascular neuroedema, elevated liver enzymes, diarrhea, cough and other adverse reactions; 3 more expensive.3. Indications: Applicable to diabetic patients who still have some islet function, especially elderly diabetic patients whose blood sugar is not too high and they are worried about hypoglycemia.Precautions for use 1) Type 1 diabetes patients, diabetic ketoacidosis patients, children, pregnant and lactating women are prohibited.2) The risk of hypoglycemia alone is small, and combined with other hypoglycemic agents, it increases the risk of hypoglycemia.3) When using this type of drug in diabetic patients with renal insufficiency, care should be taken to reduce the drug dose according to the drug instructions.4) The medication is not affected by the meal. In addition to the sitagliptin twice daily, other DPP-4 inhibitors can be taken once a day.7 SGLT-2 Inhibitors These drugs do not rely on improving insulin secretion or resistance to hypoglycemia, but have a unique approach to reduce renal tubular glucose reabsorption by inhibiting renal tubular sodium-glucose transporter-2 (SGLT-2) activity.Increase urine sugar excretion to lower blood sugar (especially fasting blood sugar).The 2019 ADA guidelines have listed SGLT-2 inhibitors as the preferred hypoglycemic agent for people with diabetes and cardiovascular disease (CKD), and the European Medicines Agency (EMA) has officially approved the drug for the treatment of type 1 diabetes.Its representative drugs are dapagliflozin, cagliflozin, and englitavir.1. Advantages: 1 The indications are wide, whether it can be taken by patients with type 2 or type 1 diabetes; 2 good safety, no risk of hypoglycemia alone; 3 in addition to hypoglycemic, there are weight loss, blood pressure reduction,It can reduce the effects of proteinuria, reduce sodium and water retention, and improve heart failure. It is a “all-rounder” and “cross-border” star in hypoglycemic drugs. It is also the most evidenced oral and protective effect on heart and kidney.Hypoglycemic drugs; 4 The drug is 1 tablet (10 mg) per day, before and after meals, and patient compliance is good.2. Disadvantages: 1 Because the drug causes the concentration of urine sugar to rise, it is easy to cause urinary tract and genital infection; 2 can increase the risk of ketoacidosis, and the blood sugar caused by ketoacidosis is often not too high (<11.1Methyl / L), this is different from the classic ketoacidosis, which is called "normal glycemic ketoacidosis"; 3 individual patients will have an allergic reaction, leading to rash or angioedema; 4SGLT-2 inhibitorIt will increase the risk of fractures, and there is no conclusion yet.3. Indications: Due to its unique hypoglycemic mechanism and cardioprotective effects, SGLT-2 inhibitors are suitable for all types of diabetic patients, especially those with cardiovascular disease.Precautions for use 1) Patients should pay attention to local hygiene of the vulva, drink as much water as possible, and prevent urinary tract infections.2) During the medication, it is not advisable to use a low-sugar ketogenic diet to avoid ketoacidosis.3) Because SGLT-2 inhibitors act on the kidneys, patients with severe renal insufficiency are banned.4) When SGLT-2 inhibitors are combined with sulfonylureas or insulin, it is possible to increase the risk of hypoglycemia, and the latter dose needs to be adjusted as appropriate.. 5) If the patient taking the drug has symptoms such as abdominal pain, nausea, vomiting, fatigue, difficulty breathing, etc., even if the blood sugar is not too high at the time, it is necessary to pay attention to the detection of ketone body and eliminate ketoacidosis.In summary, each type of oral hypoglycemic drugs has its own characteristics, and its hypoglycemic effect, side effects, mode of administration, duration of action, indications and contraindications are all different. When selecting drugs, full consideration should be given to the characteristics of the drugs.According to the specific conditions of the patient (such as blood glucose profile, liver and kidney function, body type, medication compliance, complications, age, etc.) to select the appropriate drug.In fact, no drug is the best for all patients, and the best is the best! , please do not reprint without the authorization of the copyright owner.


The author ouyangshaoxia