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Edited by Yimaitong, please do not reprint without authorization
.
Introduction: How much do you master more than 40 kinds of hypoglycemic drugs? Endocrinologists deal with diabetes and hypoglycemic drugs almost every day, but if asked, how many hypoglycemic drugs are currently on the market in China? Most people may say biguanides, sulfonylureas, thiazolidines.
.
.
Stop, just knowing the categories of drugs and their effects is not enough.
The trend of refined diabetes management requires doctors to master more
.
·Can metformin be used after iodine imaging? ·It is also a sulfonylurea, what are the differences between gliclazide and glibenclamide? ·Which oral hypoglycemic drugs are effective in 15 minutes? ……According to the latest information, this article summarizes the medication information of the five classic oral hypoglycemic drugs
.
Dozens of other hypoglycemic drugs (such as insulin, GLP-1RA, SGLT-2i, DPP-4i, etc.
) will be shared with you in subsequent articles
.
Clinical essentials: 6 principles of drug treatment for type 2 diabetes 1.
If life>
.
Those who are not suitable for metformin can choose α-glycosidase inhibitors or insulin secretagogues
.
2.
If metformin is used alone but the blood sugar still fails to reach the target, dual therapy should be carried out, plus insulin secretagogues, α-glycosidase inhibitors, thiazolidinediones (TZDs), dipeptidyl peptidase-IV (DPP-4) inhibitor, sodium-glucose cotransporter 2 (SGLT2) inhibitor, glucagon-like peptide-1 (GLP-1) receptor agonist, or insulin
.
3.
Triple therapy, the above-mentioned hypoglycemic drugs with different mechanisms can be used in combination with 3 drugs
.
4.
If the triple therapy is still not up to standard for blood sugar control, the treatment plan should be adjusted to multiple insulin therapy (basic insulin plus meals insulin or multiple premixed insulin daily)
.
Insulin secretagogues should be discontinued when using multiple insulin treatments
.
5.
Patients with type 2 diabetes with atherosclerotic cardiovascular disease or high-risk cardiovascular risk, regardless of whether their glycosylated hemoglobin (HbA1c) meets the standard, as long as there is no contraindication, should be added to metformin with atherosclerotic GLP-1RA or SGLT-2i with evidence of benefit in sclerosing cardiovascular disease
.
6.
Patients with type 2 diabetes with chronic kidney disease or heart failure, regardless of whether their HbA1c meets the standard, as long as there is no contraindication, should add SGLT-2i on the basis of metformin; patients with type 2 diabetes with chronic kidney disease, such as Can not use SGLT-2i, consider using GLP-1RA
.
The biguanide hypoglycemic agent Metformin can reduce fasting and postprandial hyperglycemia.
The main mechanism is to inhibit liver gluconeogenesis, reduce liver glucose output, increase the sensitivity of surrounding tissues to insulin, and inhibit the uptake of glucose by intestinal wall cells
.
At the same time, metformin can also inhibit the biosynthesis and storage of cholesterol, and reduce blood triglycerides and total cholesterol levels
.
Because it does not stimulate insulin secretion, it will not cause hypoglycemia when used alone
.
Sulfonylureas Hypoglycemic Drugs Sulfonylureas are insulin secretagogues, which are mainly used to reduce blood sugar by stimulating the secretion of insulin from pancreatic islet β cells.
They are mainly used in collectives with a certain number (about 30%) of functional pancreatic β Cell Diabetes
.
The first generation: tolbutamide and chlorpropamide, due to high liver toxicity and high incidence of hypoglycemia, they are no longer used for the treatment of diabetes; the second generation: glibenclamide, glipizide, and gliclazide Special, gliquidone, etc.
; third generation: glimepiride
.
1.
Glibenclamide The second-generation sulfonylurea drug, taken before meals, has a fast and strong hypoglycemic effect.
It is metabolized by the liver, and low-active metabolites are excreted from the kidneys
.
2.
Glipizide The second-generation sulfonylureas, taken before meals, and effective 30 minutes after oral administration
.
Metabolites are inactive and excreted by the kidneys, excretion is faster, no accumulation, so less cause hypoglycemia
.
3.
Gliquidone The second-generation sulfonylureas, taken before meals, the plasma concentration reaches the peak 2 to 3 hours after oral administration of 30 mg, the plasma half-life is 1.
5 hours, and the effect can last for 2 to 3 hours
.
Most of the metabolites are excreted from the feces via the biliary system
.
4.
Gliclazide The second-generation sulfonylureas, except for the effect of promoting insulin secretion, can also increase glucose uptake, and rarely cause severe hypoglycemia
.
The drug is mainly metabolized by the liver, and the metabolites have no significant hypoglycemic activity, and are mainly eliminated through urine
.
5.
Glimepiride The third-generation sulfonylureas, fasting or meals have no significant effect on drug absorption, and rarely cause severe hypoglycemia
.
Glinide-type hypoglycemic agents Glinide-type hypoglycemic agents are non-sulfonylurea insulin secretagogues, which are suitable for diabetic patients with pancreatic β-cells that still have certain functions, increased postprandial blood sugar, and abnormal glucose tolerance
.
1.
Repaglinide is taken before meals, it has a quick effect after oral administration, and the action time is short.
The plasma concentration of the drug reaches its peak 1 hour after taking the drug, and then drops rapidly, and it is quickly cleared from the blood within 4 to 6 hours
.
Repaglinide and its metabolites are mainly excreted through bile
.
2.
Nateglinide is taken before a meal and takes effect within 15 minutes.
The average peak concentration of the drug usually appears within 1 hour of taking the drug
.
83% of nateglinide and its metabolites are excreted in urine and 10% in feces
.
Alpha-glycosidase inhibitors hypoglycemic agents Alpha-glycosidase inhibitors can reduce postprandial blood glucose levels by delaying the absorption of glucose in the small intestine, with a mild hypoglycemic effect and a long-lasting effect
.
If carbohydrates in the diet account for more than 50% of calories, the effect of reducing blood sugar will be more obvious
.
1.
Acarbose is taken with meals, mainly degraded in the intestine or excreted in feces in its original form, which can reduce postprandial blood sugar, and long-term use can also reduce fasting blood sugar and HbA1c
.
2.
Voglibose is taken before meals, and meals can be taken after taking the medicine
.
It is easily absorbed after oral administration, and the plasma drug concentration reaches its peak time of 2 hours, and it decreases by 50% after 8 hours
.
It is mainly excreted in feces in the form of prototype or intestinal degradation products, and only 1.
7% is excreted in urine
.
3.
The bioavailability of oral administration of 25 mg of miglitol is 100%, and the bioavailability of oral administration of 100 mg of drugs is about 50% to 70%, and the absorption can reach saturation at higher doses
.
Its protein binding rate is less than 4%, and more than 95% is excreted in the urine in its original form
.
Thiazolidinedione hypoglycemic drugs Thiazolidinedione drugs can increase the sensitivity of surrounding tissues to insulin, improve insulin resistance, and improve the function of pancreatic β-cells
.
In addition to lowering blood sugar, it also has the effects of lowering blood pressure, improving lipid metabolism, and anti-oxidation
.
It usually does not cause hypoglycemia when used alone
.
1.
Rosiglitazone can reduce fasting and postprandial blood sugar.
The use of this product to treat type 2 diabetes requires patients to have a certain degree of insulin secretion.
If insulin is severely lacking, taking this product is invalid
.
2.
Pioglitazone The absolute bioavailability of pioglitazone is 99%, and the peak concentration is reached 2 hours after oral administration
.
Food will delay the peak concentration time to 3~4 hours, and the plasma elimination half-life is 3~7 hours
.
Pioglitazone mainly binds to serum albumin, and most of it is excreted into the bile in the form of its original form or metabolites, and is cleared from the feces
.
Reference materials: [1] Chinese Medical Association, Chinese Medical Association Clinical Pharmacy Branch, Chinese Medical Association Journal, etc.
Guidelines for rational use of type 2 diabetes at the grassroots level[J].
Chinese Journal of General Practitioners, 2021, 20(6): 615 -630.
DOI: 10.
3760/cma.
j.
cn114798-20210318-00257.
[2] Liu Jian, Li Yue.
Prescriptions for the treatment of endocrine system diseases[M].
People's Medical Publishing House.
Beijing, 2019.
.
Introduction: How much do you master more than 40 kinds of hypoglycemic drugs? Endocrinologists deal with diabetes and hypoglycemic drugs almost every day, but if asked, how many hypoglycemic drugs are currently on the market in China? Most people may say biguanides, sulfonylureas, thiazolidines.
.
.
Stop, just knowing the categories of drugs and their effects is not enough.
The trend of refined diabetes management requires doctors to master more
.
·Can metformin be used after iodine imaging? ·It is also a sulfonylurea, what are the differences between gliclazide and glibenclamide? ·Which oral hypoglycemic drugs are effective in 15 minutes? ……According to the latest information, this article summarizes the medication information of the five classic oral hypoglycemic drugs
.
Dozens of other hypoglycemic drugs (such as insulin, GLP-1RA, SGLT-2i, DPP-4i, etc.
) will be shared with you in subsequent articles
.
Clinical essentials: 6 principles of drug treatment for type 2 diabetes 1.
If life>
.
Those who are not suitable for metformin can choose α-glycosidase inhibitors or insulin secretagogues
.
2.
If metformin is used alone but the blood sugar still fails to reach the target, dual therapy should be carried out, plus insulin secretagogues, α-glycosidase inhibitors, thiazolidinediones (TZDs), dipeptidyl peptidase-IV (DPP-4) inhibitor, sodium-glucose cotransporter 2 (SGLT2) inhibitor, glucagon-like peptide-1 (GLP-1) receptor agonist, or insulin
.
3.
Triple therapy, the above-mentioned hypoglycemic drugs with different mechanisms can be used in combination with 3 drugs
.
4.
If the triple therapy is still not up to standard for blood sugar control, the treatment plan should be adjusted to multiple insulin therapy (basic insulin plus meals insulin or multiple premixed insulin daily)
.
Insulin secretagogues should be discontinued when using multiple insulin treatments
.
5.
Patients with type 2 diabetes with atherosclerotic cardiovascular disease or high-risk cardiovascular risk, regardless of whether their glycosylated hemoglobin (HbA1c) meets the standard, as long as there is no contraindication, should be added to metformin with atherosclerotic GLP-1RA or SGLT-2i with evidence of benefit in sclerosing cardiovascular disease
.
6.
Patients with type 2 diabetes with chronic kidney disease or heart failure, regardless of whether their HbA1c meets the standard, as long as there is no contraindication, should add SGLT-2i on the basis of metformin; patients with type 2 diabetes with chronic kidney disease, such as Can not use SGLT-2i, consider using GLP-1RA
.
The biguanide hypoglycemic agent Metformin can reduce fasting and postprandial hyperglycemia.
The main mechanism is to inhibit liver gluconeogenesis, reduce liver glucose output, increase the sensitivity of surrounding tissues to insulin, and inhibit the uptake of glucose by intestinal wall cells
.
At the same time, metformin can also inhibit the biosynthesis and storage of cholesterol, and reduce blood triglycerides and total cholesterol levels
.
Because it does not stimulate insulin secretion, it will not cause hypoglycemia when used alone
.
Sulfonylureas Hypoglycemic Drugs Sulfonylureas are insulin secretagogues, which are mainly used to reduce blood sugar by stimulating the secretion of insulin from pancreatic islet β cells.
They are mainly used in collectives with a certain number (about 30%) of functional pancreatic β Cell Diabetes
.
The first generation: tolbutamide and chlorpropamide, due to high liver toxicity and high incidence of hypoglycemia, they are no longer used for the treatment of diabetes; the second generation: glibenclamide, glipizide, and gliclazide Special, gliquidone, etc.
; third generation: glimepiride
.
1.
Glibenclamide The second-generation sulfonylurea drug, taken before meals, has a fast and strong hypoglycemic effect.
It is metabolized by the liver, and low-active metabolites are excreted from the kidneys
.
2.
Glipizide The second-generation sulfonylureas, taken before meals, and effective 30 minutes after oral administration
.
Metabolites are inactive and excreted by the kidneys, excretion is faster, no accumulation, so less cause hypoglycemia
.
3.
Gliquidone The second-generation sulfonylureas, taken before meals, the plasma concentration reaches the peak 2 to 3 hours after oral administration of 30 mg, the plasma half-life is 1.
5 hours, and the effect can last for 2 to 3 hours
.
Most of the metabolites are excreted from the feces via the biliary system
.
4.
Gliclazide The second-generation sulfonylureas, except for the effect of promoting insulin secretion, can also increase glucose uptake, and rarely cause severe hypoglycemia
.
The drug is mainly metabolized by the liver, and the metabolites have no significant hypoglycemic activity, and are mainly eliminated through urine
.
5.
Glimepiride The third-generation sulfonylureas, fasting or meals have no significant effect on drug absorption, and rarely cause severe hypoglycemia
.
Glinide-type hypoglycemic agents Glinide-type hypoglycemic agents are non-sulfonylurea insulin secretagogues, which are suitable for diabetic patients with pancreatic β-cells that still have certain functions, increased postprandial blood sugar, and abnormal glucose tolerance
.
1.
Repaglinide is taken before meals, it has a quick effect after oral administration, and the action time is short.
The plasma concentration of the drug reaches its peak 1 hour after taking the drug, and then drops rapidly, and it is quickly cleared from the blood within 4 to 6 hours
.
Repaglinide and its metabolites are mainly excreted through bile
.
2.
Nateglinide is taken before a meal and takes effect within 15 minutes.
The average peak concentration of the drug usually appears within 1 hour of taking the drug
.
83% of nateglinide and its metabolites are excreted in urine and 10% in feces
.
Alpha-glycosidase inhibitors hypoglycemic agents Alpha-glycosidase inhibitors can reduce postprandial blood glucose levels by delaying the absorption of glucose in the small intestine, with a mild hypoglycemic effect and a long-lasting effect
.
If carbohydrates in the diet account for more than 50% of calories, the effect of reducing blood sugar will be more obvious
.
1.
Acarbose is taken with meals, mainly degraded in the intestine or excreted in feces in its original form, which can reduce postprandial blood sugar, and long-term use can also reduce fasting blood sugar and HbA1c
.
2.
Voglibose is taken before meals, and meals can be taken after taking the medicine
.
It is easily absorbed after oral administration, and the plasma drug concentration reaches its peak time of 2 hours, and it decreases by 50% after 8 hours
.
It is mainly excreted in feces in the form of prototype or intestinal degradation products, and only 1.
7% is excreted in urine
.
3.
The bioavailability of oral administration of 25 mg of miglitol is 100%, and the bioavailability of oral administration of 100 mg of drugs is about 50% to 70%, and the absorption can reach saturation at higher doses
.
Its protein binding rate is less than 4%, and more than 95% is excreted in the urine in its original form
.
Thiazolidinedione hypoglycemic drugs Thiazolidinedione drugs can increase the sensitivity of surrounding tissues to insulin, improve insulin resistance, and improve the function of pancreatic β-cells
.
In addition to lowering blood sugar, it also has the effects of lowering blood pressure, improving lipid metabolism, and anti-oxidation
.
It usually does not cause hypoglycemia when used alone
.
1.
Rosiglitazone can reduce fasting and postprandial blood sugar.
The use of this product to treat type 2 diabetes requires patients to have a certain degree of insulin secretion.
If insulin is severely lacking, taking this product is invalid
.
2.
Pioglitazone The absolute bioavailability of pioglitazone is 99%, and the peak concentration is reached 2 hours after oral administration
.
Food will delay the peak concentration time to 3~4 hours, and the plasma elimination half-life is 3~7 hours
.
Pioglitazone mainly binds to serum albumin, and most of it is excreted into the bile in the form of its original form or metabolites, and is cleared from the feces
.
Reference materials: [1] Chinese Medical Association, Chinese Medical Association Clinical Pharmacy Branch, Chinese Medical Association Journal, etc.
Guidelines for rational use of type 2 diabetes at the grassroots level[J].
Chinese Journal of General Practitioners, 2021, 20(6): 615 -630.
DOI: 10.
3760/cma.
j.
cn114798-20210318-00257.
[2] Liu Jian, Li Yue.
Prescriptions for the treatment of endocrine system diseases[M].
People's Medical Publishing House.
Beijing, 2019.
