Since Ms. Li was diagnosed with diabetes three years ago, her blood sugar has been poorly controlled for many times, and she finally decided to take rosiglitazone for medication, which was stabilized by insulin injection.
However, in the past six months, Ms. Li has found that her weight is getting heavier and heavier, especially her abdominal waist circumference can be significantly thickened, and she thought that the doctor had told her that some patients with insulin will gain weight, and there is no need to worry too much, Ms. Li did not think much about it.
However, during this time, overweight brought various inconveniences to Ms. Li, especially after falling asleep, it was difficult to breathe, and sometimes she was even awakened, and she had to sit up and slow down for a period of time before she could continue to fall asleep; She couldn't sleep well at night and couldn't concentrate during the day, and Ms. Li became weaker and weaker.
After examination, Ms. Li's blood sugar control was normal, but unfortunately, through echocardiogram and X-ray examination, it was found that Ms. Li's cardiac function ejection fraction was only 32%, the left ventricular systolic function was reduced, and the left ventricular area was enlarged. This is typical of diabetes mellitus with heart failure.
After Ms. Li was admitted to the hospital for treatment for a period of time, the symptoms of chest tightness were relieved, and the doctor changed her daily rosiglitazone to dapagliflozin, and instructed Ms. Li to take the medicine on time every day, monitor her blood sugar regularly, and seek medical attention in time if she has uncomfortable symptoms.
When Ms. Li went to the pharmacy to get the medicine, she found that she had changed the hypoglycemic medication, and she was confused, was it because of rosiglitazone that caused her heart problems, why did the doctor replace the medicine with dapagliflozin? The doctor told Ms. Li that rosiglitazone has great side effects on the heart, which will cause abnormal heart beating, and that she has had heart problems before and is not suitable to continue to take it, and it is better to replace it with dapagliflozin, which is beneficial to the heart.
In this article, we will learn about the drug dapagliflozin.
1. How does dapagliflozin lower blood sugar?
When the blood glucose concentration exceeds the standard, the functions of many organs in the human body must be changed, and corresponding adjustments should be made to actively absorb, decompose and excrete glucose in the blood, and the kidneys, as a component of the urinary system, play a major role in it.
Under normal circumstances, if the concentration of glucose in the proximal urine exceeds the absorption range of the proximal convoluted tubule, the remaining unabsorbed glucose will be excreted with the urine.
However, when the glucose concentration in the blood exceeds the standard for a long time, the proximal tubule will change, and the amount of SGLT-2 on the epithelial cell membrane that helps the reabsorption of heavy glucose in the original urine will increase, so as to avoid "wasting" the glucose in the original urine, so that more glucose and solutes can be absorbed into the blood and reused.
However, the saving of the kidneys will increase the burden on the human body, not only increase the blood sugar concentration, but also lead to excessive absorption of body fluids and sodium ions, increase the difficulty of treatment of diabetes and induce renal hypertension.
Among traditional hypoglycemic drugs, the presence of SGLT-2 was not controlled until dapagliflozin was marketed in 2014. As a sodium-glucose symporter inhibitor, dapagliflozin targets the proximal tubule, which reduces the reabsorption of glucose in the protourine by the renal tubule by inhibiting protein activity, and increases the excretion of sugar in the patient's body, thereby playing a hypoglycemic role, and in the process of glucose being excreted, the absorption of sodium ions is also restricted, and the blood volume entering the circulation is reduced, thereby controlling the stability of blood pressure.
Dapagliflozin, when inhibiting the action of the proximal tubule, leads to the enhancement of the function of the uric acid transporter GLUT9 subtype 2, accelerates the excretion of uric acid, thereby reducing the patient's uric acid level value.
The advantage of dapagliflozin is that it can improve the microcirculation of the kidneys, reduce the level of serum inflammatory factors, reduce the damage caused to the renal tubules and glomeruli, reduce the excretion of urine protein, and have a certain protective effect on the kidneys.
Dapagliflozin can also effectively control weight, its pharmacological effect is not to change the absorption of fat, but to reduce the body's absorption of blood sugar, increase glucose excretion and take away part of the fluid and energy, reduce the probability of edema, thereby reducing body weight, which is the difference between dapagliflozin and metformin.
SGLT-2 inhibitors, including dapagliflozin, are also very cardiovascular friendly, and dapagliflozin can reduce the concentration of sodium and calcium ions in myocardial cells, reduce the burden on blood volume, and reduce the subendocardial blood flow rate, thereby reducing the load on the heart.
Especially in patients with diabetes mellitus and arteriosclerosis, dapagliflozin can reduce the occurrence of adverse cardiovascular events.
In addition to the above pharmacological effects, dapagliflozin can also increase high-density lipoprotein and reduce the concentration of triglycerides and free fatty acids. As early as 2013, the United States Diabetes Association had a study pointing out that researchers followed patients who took dapagliflozin for a long time and found that their blood lipid levels had been restored to a certain extent, so dapagliflozin could effectively improve blood lipids.
Dapagliflozin is powerful, which means that it can be used in the treatment of diabetic patients with other diseases, but this does not mean that the drug is safe and harmless, and can be used at will, and diabetic patients must be cautious in the process of taking it.
2. How to use dapagliflozin correctly in diabetic patients?
Dapagliflozin only needs to be taken once a day, and the best time to take it is in the morning, because it is not affected by food and can be effective before and after meals. The recommended dose of dapagliflozin is 5 mg for the initial dose, which can be increased to 10 mg if subsequent drugs become tolerated.
Patients should observe their blood sugar changes and make records, communicate with their doctors in a timely manner, effectively adjust the dosage, do not increase or decrease the dosage by themselves, and do not blindly follow the dosage of others. Because each person's condition is different, the clinical symptoms and treatment methods of diabetes are also different, and the doctor will give personalized medication according to the patient's actual condition and examination data, and do not decide the dosage of medication by himself.
During the medication, patients should closely monitor their blood sugar and blood pressure changes to determine whether the drug is working.
Dapagliflozin alone rarely lowers blood sugar and blood pressure too much, but when combined with other drugs, hypoglycemia and hypotension may occur. Patients should observe the changes in their own values to avoid the risk of hypoglycemia and hypotension.
Before taking dapagliflozin, it is best for patients to have an assessment of renal function and volume status, and for glomerular filtration rate of more than 45 eGFR (mL/min), it is possible to take it normally, but if the glomerular filtration rate is low, it is best to switch to other types of hypoglycemic drugs. The glomerular filtration rate is low, there may be physiological or pathological damage to renal function, dapagliflozin cannot guide the proximal tubule to exert its drug effect normally, and excessive accumulation of dagliflozin will also increase nephrotoxicity and aggravate renal dysfunction.
In addition, although dapagliflozin has a certain effect of protecting the kidneys, when the patient's blood volume decreases, the kidney is underperfused, and the kidney will be "backstabbed", and in severe cases, there will be acute kidney injury such as decreased urine output and edema of the lower limbs, which must be paid enough attention.
If there is an abnormality, it is necessary to be alert to the presence of leukocytes or bacteria in the urine, which may be a urinary tract infection, because dapagliflozin promotes the excretion of urine containing too much glucose, which is easy to cause the growth of bacteria and microorganisms, and induces urinary tract infections such as urethritis and cystitis.
For diabetic patients, it is very dangerous to cause bacterial infection, because the diabetic patient's own immunity is weakened, and the number of white blood cells may be lower than the normal range, which causes the infection in this case, and it is not easy to recover.
For patients with current urinary tract infection and reproductive system infection, severe renal function abnormality, and bladder cancer, it is necessary to suspend the use of dapagliflozin and consider whether to take it after the inflammation is cured.
During the period of taking the drug, patients should not only pay attention to the changes in their urine, but also pay attention to personal hygiene, keep the lower body clean and dry, and change clothes frequently to reduce the chance of infection.
Dapagliflozin can only be used for the treatment of type 2 diabetes, and for type 1 diabetes and ketoacidosis caused by diabetes, dapagliflozin cannot be taken.
Dapagliflozin in the hypoglycemic at the same time, there may be insufficient absorption of glucose in the body, and then cause the consumption of fat to increase, fat metabolism and decomposition in the human body to produce ketone bodies, resulting in the accumulation of ketone bodies in the body, severe cases will aggravate ketoacidosis, if ketoacidosis occurs during the medication, the patient should stop the drug in time, increase the amount of water intake, through insulin injection, etc., to avoid the deterioration of the condition.
Dapagliflozin is used in the metabolism of glucose with a large amount of liquid solvent, this process will cause increased water loss, this is a normal process, do not hold urine, normal excretion.
Some sensitive patients may even experience symptoms of dehydration, so keep drinking more than 1500 ml of water per day, and stop the drug immediately if there is excessive fluid loss.
Drugs have their indications and suitable populations, dapagliflozin is no exception, the above is the guide on the correct use of dapagliflozin, in addition, pay attention to these aspects in the process of taking dapagliflozin.
After taking the drug, it is not necessarily guaranteed that the blood sugar will be maintained in the normal range, the patient still needs to make adjustments from the diet, do not take the diet with high sugar and high oil food, mainly light, the drug and food work together to control blood sugar and return to normal.
In the process of taking, try not to use urine glucose test to detect blood sugar, so the particularity of the drug is to excrete excess glucose through urine to control the stability of blood sugar, so the urine glucose test often shows false positives, or by detecting the concentration of glucose in the blood, it is more appropriate.
Within 2 weeks of taking dapagliflozin, some patients will have urticaria-like symptoms such as itchy skin, and most of the cases are mild, but if a similar situation occurs at the first dose, it is recommended that patients switch to non-SGLT-2i hypoglycemic drugs.
Although the safety of dapagliflozin is high, for pregnant and lactating women, there is still a risk of affecting the child when taking dapagliflozin, so do not take it during these special periods. The safety and efficacy of dapagliflozin cannot be guaranteed in adolescents under 18 years of age and is therefore not recommended.
Dapagliflozin, as a relatively new hypoglycemic drug, has a wider range of applications and great advantages than other hypoglycemic oral drugs. However, patients should still consult professionals before taking the drug, only patients who meet the scope of drug use can take it, pay attention to their own blood sugar, blood pressure, kidney function and other physiological changes during the taking process, especially for patients who take it for the first time, do not listen to biased beliefs, think that dapagliflozin is effective and buy it by yourself, maybe it is not within the scope of medication.
bibliography
1. "The hypoglycemic drug dapagliflozin has 6 advantages, but 6 should be paid attention to when taking it for a long time", Chinese Hospital Drug Evaluation and Analysis, 2021.12.16
2. "Rational Use of Dapagliflozin", Lilac Garden Medication Guide, 2023.6.16