With the development and progress of society, the progress of population aging and obesity trends has continued to intensify. html type 12 diabetes has become one of the major diseases that affect human health problems around the world. According to incomplete statistics, the number of patients with diabetes worldwide exceeds 300 million, and this number is expected to increase to 592 million by 2035.
For such a high incidence of disease, it is particularly critical whether the blood sugar control level is ideal. At present, most patients still have poor blood sugar control levels, especially for patients with a long course of disease, a combination of multiple chronic complications and comorbidities, patients' blood sugar control faces huge challenges due to the large types of medications and poor compliance.
Therefore, many scientists are committed to breaking through the pathogenesis mechanism to find new targets and researching antidiabetic drugs that can benefit patients from many aspects. sodium-glucose cotransporter inhibitors, such as canagliflozin, dapagliflozin, empagliflozin, etc., referred to as "liflozin" category, is a newly developed target therapeutic drug in recent years.
1, "Liefen" type of sugar-lowering mechanism
Under normal circumstances, healthy adults have 160 to 180 g of glucose filtered through the glomerular every day, more than 99% of glucose is reabsorbed by renal tubular , and 1% of glucose is excreted from the body in the form of urine.
. After the glomerulus of diabetic patients are filtered every day, the reabsorbing of about 280g of glucose is about 280g. Studies have found that this is due to the upregulation of the expression of sodium-glucose cotransporter in diabetic patients, and the sugar absorption capacity is increased. This change ultimately increases the ability of the renal tubules to reabsorb glucose, and the renal glucose threshold increases, causing more glucose to enter the blood circulation and further increase blood sugar.
"Lieflozin" class is a sodium-glucose cotransporter inhibitor. The glucose filtered by the renal tubular lumen is mainly reabsorbed by sodium-glucose cotransporter expressed in the proximal renal tubules. The "leflozin" class reduces the renal reabsorption of filtered glucose by the kidneys, lowers the renal glucose threshold, and increases the excretion of urine sugar , thereby reducing blood sugar. Moreover, this hypoglycemic effect does not depend on the secretion and function of insulin .
2, "Lieflozin" indications
combined with metformin: When metformin alone is not controlled properly, it can be used in combination with metformin to improve blood sugar control in adult patients with type 2 diabetes in combination with diet and exercise.
is combined with metformin and sulfonylurea (gliXX) drugs: When the blood sugar control of metformin and sulfonylurea is poor, it can be used in combination with metformin and sulfonylurea drugs to improve blood sugar control in adult patients with type 2 diabetes in combination with diet and exercise.
is not recommended for the treatment of type 1 diabetes patients or diabetic ketoacidosis (patients).
3, "Liefen" type lowering effect
, in terms of lowering glycemic, "Liefen" type single-drug treatment can reduce glycated hemoglobin (HbAlc) by 0.37% to 1.16%, and the patient's fasting blood sugar level has a significant decrease in the blood sugar after meals. Glycoated hemoglobin tests can usually reflect the patient's blood sugar control situation in the past 8 to 12 weeks.
4, "Liefen" class has the effect of lowering glycemic
on cardiovascular protection
At present, multiple clinical trials have confirmed that "Liefen" class has a certain protective effect on cardiovascular.
protective effect on the kidney
Because the "liflozin" type mainly exerts its role in the regulation of blood sugar homeostasis through the kidneys, its impact and safety on the kidneys have attracted much attention. Diabetic nephropathy Early kidney enlargement, glomerular hypertrophy, ultrafiltration , kidney function is damaged, further developing proteinuria. Studies have shown that "leflozin" can alleviate glomerular filtration and tubular hypertrophy in type 2 diabetes, and reduce tubular toxicity.
antihypertensive effect
A clinical study involving 16 countries and 311 centers confirmed that the "leflozin" class has a significant antihypertensive effect. Compared with diastolic blood pressure , the improvement of systolic blood pressure is more obvious, which can reduce systolic blood pressure by an average of 11.9 mmHg. When combined with other conventional antihypertensive drugs, it can achieve a more satisfactory antihypertensive effect.
Currently, some scholars believe that the blood pressure reduction mechanism of "liflozin" type should be related to the permeable diuretic caused by its sugar discharge. Some scholars also believe that its antihypertensive effect is related to the inhibitory effect of the renin-angiotensin-aldosterone system when promoting urine excretion. The effect of
on body weight
At present, many studies have confirmed that the "liflozin" category has a certain regulatory effect on patients' weight. The weight loss mechanism is related to the "leflozin" type that increases glucose excretion through the kidneys, promotes the decomposition of glycogen in the body, and maintains the body's energy negative balance overall, thereby controlling the patient's weight. Effects of
on blood lipid and blood uric acid
"liflozin" also has an intervention effect in blood lipid management. Clinical studies have confirmed that sodium-glucose cotransporter also has an inhibitory effect on lipid metabolism.
This type of drug can slightly increase low-density lipoprotein (LDL) cholesterol and high-density lipoprotein (HDL) cholesterol. These elevations are caused by the inhibition of sodium-glucose cotransporter, resulting in enhanced oxidation of hepatic fatty acids. Mild increase in
LDL cholesterol did not affect the benefits of the "leflozin" category confirmed in clinical trials to reduce overall cardiovascular death.
For patients with type 2 diabetes and hyperuricemia, long-term hyperuricemia may lead to increased systemic oxidative stress in patients, damage the systemic vascular endothelial cells function, release a large number of inflammatory factors, thereby causing vascular smooth muscle proliferation, and thus aggravate the formation of atherosclerosis.
, and "lifen" can increase uric acid excretion and indirectly reduce blood uric acid levels in the body. The mechanism may be related to the activation of transporters such as uric acid-related glucose transporter 9. A decrease in blood uric acid from baseline was also observed in the study.
To sum up, whether used alone or in combination with other hypoglycemic drugs, the "lifen" type of hypoglycemic drugs have good efficacy and safety in blood sugar control in patients with type 2 diabetes. It can also bring benefits such as weight loss, lipid regulation, lowering blood pressure, lowering uric acid, and cardiovascular and renal protection effects, etc., such as lowering glycemic benefits.
