Most of the same drugs have similar pharmacological effects, but often due to different chemical structures, there are differences in efficacy and many other aspects. In recent years, with the deepening of research, antihypertensive drugs are also gradually optimized, and antihypertensive drugs such as olmesartan ester and epsartan have emerged, providing more effective choices for the clinic.
Olmesartanetil
Olmesartantil, the 7th type 1 receptor antagonist approved by the US FDA for the treatment of hypertension angiotensin II, has unique pharmacokinetic and pharmacodynamic characteristics compared to other drugs. The drug is a precursor drug that is completely deesterified in the gastrointestinal tract into the active metabolite olmesartan to exert a hypotensive effect.
Oral absorption is not affected by food, the half-life in the blood can be as long as 13 hours, hydrolyzed in the digestive tract, and basically not metabolized. About 35% to 50% of the drug is excreted from the urine, and the rest is excreted from the intestine through bile, showing a more balanced dual-channel excretion, suitable for mild to moderate liver and kidney function of poor people to take, and small interaction with other drugs.
In the structure of olmesartan ester, due to the simultaneous possession of carboxyl and hydroxyl groups, it binds to the type 1 receptor (AT1) of angiotensin II, and the affinity for AT1 receptor is 12500 times stronger than that of AT2 receptor. It can control blood pressure for a long time, the ratio of antihypertensive valley peak is satisfactory, and the effect on primary mild to moderate hypertension is good. The latest research shows that olmesartan ester can also reduce lipid peroxidation, anti-arteriosclerosis, and lower blood sugar. It can also inhibit the decline in cognitive function in mice on high-salt and cholesterol diets.
Olmesartantil not only lowers blood pressure, but also provides organ protection and other benefits for patients with heart failure, type 2 diabetes and renal dysfunction. Chinese guidelines for the prevention and treatment of hypertension recommend that olmesartan ester be used in patients with hypertension with type 2 diabetic nephropathy, proteinuria, left ventricular hypertrophy, etc.
Clinical studies have shown that olmesartan 20-40 mg once a day compared with losartan 50-100 mg once a day, both of which can effectively reduce blood pressure, but the results of the trough of systolic and diastolic blood pressure at 4 weeks of treatment suggest that the effective case number and efficiency of the olmesartan group are higher than the losartan group, the onset of action of the olmesartan group is faster than that of the losartan group, and the individual and overall trough/peak ratios of systolic and diastolic blood pressure in the olmesartan group are higher than those in the losartan group.
It can be seen that the antihypertensive effect of olmesartan is better than that of losartan, and this result is also consistent with the results of clinical trials abroad. Comparing the inhibitory effect of angiotensin II on THE1 receptor, olmesartan is 12 times that of losartan, or 2 times that of EXP3174 (the active metabolite of losartan). As a result, olmesartan is more effective and effective than losartan, and lasts longer than 24 hours of blood pressure reduction.
Ipsartan
Epsartan is the latest angiotensin-II receptor antagonist that selectively binds to the AT1 receptor. Oral onset of action in 2-4 hours, maximum effect in 6-8 hours, stable antihypertensive effect at 24h, and antihypertensive effect at 48h. Of these, 33% are excreted by the kidneys and 67% by feces. Elimination half-life 5.1-10.5h. In addition to its common characteristics of sartans, it also affects the efficacy and its negative effect on cardiovascular disease due to its firm binding to the AT1 receptor and the increase in the concentration of AT1 caused by negative feedback.
In healthy volunteers, epsartan is able to antagonize the secretory effects of angiotensin II on blood pressure, renal blood flow, or aldosterone. Blood pressure can be continuously and smoothly controlled for up to 24 hours without the first dose of orthostatic hypotension. Discontinuation of epsartan does not cause a rapid rise in blood pressure. After taking epsartan in patients with high blood pressure, a decrease in blood pressure does not cause a change in heart rate.
Epsartan, which does not affect fasting triglycerides, total cholesterol, or LDL cholesterol levels in patients with hypertension. In addition, it does not affect fasting blood glucose levels and kidney self-regulation mechanisms. It can increase the average effective renal plasma flow in healthy adult men, maintain the level of renal function in patients with primary hypertension and renal insufficiency, and does not reduce the glomerular filtration rate in normal men, hypertensive patients or patients with different degrees of renal insufficiency.
In healthy subjects given a salt-restricted diet, epsartan was shown to promote urinary sodium excretion. Thus, epsartan can be safely used in patients with essential hypertension and patients with varying degrees of renal insufficiency without causing sodium retention or deterioration of renal function. There is no significant effect on the excretion of uric acid in the urine. Does not enhance the effects associated with bradykinin, such as coughing.
Clinical trials have shown a significant reduction in diastolic blood pressure in patients treated with epsartan, with a further antihypertensive range of 1.8 to 6.1 mmHg at each dose compared with placebo. Moreover, at the end of the test, the systolic blood pressure trough decreased, and after subtracting the placebo effect, the reduction of each reagent amount was 0.8 to 10.3 mmHg. In patients with severe hypertension, the systolic blood pressure in the epsartan group was significantly lower than that in the enalapril group.
Epsartan is taken once daily in the morning. For most patients, the maximum antihypertensive effect is generally achieved after 2-3 weeks of treatment. It is more suitable for patients with hypertension with type 2 diabetic nephropathy, proteinuria, left ventricular hypertrophy, etc. It can be taken alone or in combination with other antihypertensive drugs, especially with hydrochlorothiazide and the like. If used in combination with the horizon class, a greater antihypertensive effect can also be obtained. In patients with moderate or severe renal insufficiency (creatinine clearance <60 ml / min), the daily dose should not exceed 600 mg.
In short, drugs are also like mobile phones, computers, cars, there are also updates, can not say that a generation is better than a generation, but each generation has its own unique advantages, the key is to suit their own specific situation. Only by choosing the right antihypertensive drug can you achieve the maximum antihypertensive effect while avoiding side effects.