This article is from "Nankai Sun Pharmacist", which is used for medical science popularization for reference. Olmesartan and alisartan are commonly used first-line antihypertensive drugs in clinical practice, belonging to angiotensin II receptor antagonists, referred to as "sartan" antihypertensive drugs, mainly by selectively antagonizing angiotensin II and its AT1 receptor binding, thereby blocking angiotensin II vasoconstriction, water and sodium retention and myocardial remodeling, and exerting antihypertensive effects, which are a new generation of "sartan" antihypertensive drugs. Compared with other "sartan" antihypertensive drugs, olmesartan and alisartan bind more firmly to the AT1 receptor of angiotensin II, bind for a longer time, and can inhibit the activation of AT1 receptor, which has the characteristics of both strong and long-term antihypertensive drugs, taken once a day, can achieve 24 hours of stable blood pressure reduction, generally takes effect within 2 weeks, and can achieve the maximum antihypertensive effect after 4 weeks.
In addition to antihypertensive effects, olmesartan and alisartan can also effectively antagonize angiotensin II damage to target organs, and have clear cardiovascular protective effects, such as anti-atherosclerosis, reverse left ventricular hypertrophy, protect vascular endothelial cells, inhibit fibroblast proliferation and atrial fibrillation electrical remodeling, and can improve insulin resistance, reduce urine protein, long-term use can significantly reduce the risk of cardiovascular and cerebrovascular events such as myocardial infarction and stroke, and have a positive effect on obesity, diabetes, heart, Patients with hypertension with damage to target organs such as the kidneys have relatively good efficacy, especially for hypertensive patients with heart failure, myocardial infarction, atrial fibrillation, impaired glucose tolerance or diabetic nephropathy.
The advantages of olmesartan are that it can promote the release of nitric oxide, dilate the lumen of blood vessels, increase the perfusion of cavernous blood flow, and can increase androgen levels, which helps to enhance male erectile function, increase libido, and improve sexual function, especially for male hypertension patients with sexual dysfunction. In addition, olmesartan is well tolerated and safe, and there are few adverse reactions directly related to the drug, such as dizziness, headache, rhinitis, pharyngitis, flu-like symptoms, back pain, etc., which are usually mild and have high persistence. Finally, olmesartan does not undergo liver enzyme metabolism, there are fewer drug-drug interactions, and the combination of drugs has a better safety. However, in 2013, the US FDA issued a warning that olmesartan can cause sprue, which should be paid attention to, and if severe diarrhea with weight loss occurs during the medication, the drug should be stopped immediately and sought medical attention.
Alisartan is China's first self-developed "sartan" class antihypertensive drug, is a new compound obtained by losartan after structural modification, through the hydrolysis of gastrointestinal esterase into an active product with antihypertensive effect and target organ protection, its antihypertensive trough-to-peak ratio is greater than 60%, antihypertensive effect is long-lasting and stable, while lowering blood pressure, alisartan can also inhibit uric acid transporters in the renal tubules, thereby preventing the reabsorption of uric acid, helping to reduce blood uric acid levels. In addition, alisartan is associated with headache, dizziness, elevated blood lipids, elevated aminotransferases and other adverse reactions, which are generally mild and transient, and most of them can be relieved spontaneously or after symptomatic treatment. Alisartan is mainly metabolized by gastrointestinal esterases, and is not metabolized by liver enzymes, and does not increase the burden of liver enzymes, thereby reducing the burden on the liver, reducing interactions with other drugs, and helping to prevent adverse drug reactions.