Olmesartan and Allisartan are the first-line antihypertensive drugs commonly used in clinical practice, belonging to angiotensin II receptor antagonists, referred to as “sartan” antihypertensive drugs, mainly by selectively antagonizing angiotensin II and its AT1 It is a new generation of “sartan” antihypertensive drugs by binding to the type receptors, thereby blocking the vasoconstriction, water and sodium retention and myocardial remodeling effects of angiotensin II and exerting antihypertensive effects. Compared with other “sartan” antihypertensive drugs, olmesartan and allisartan bind more firmly to the AT1-type receptor of angiotensin II, the binding time is longer, and they can inhibit the activation of AT1-type receptors, and have both It has the characteristics of strong and long-acting antihypertensive. Taking it once a day can achieve stable blood pressure reduction for 24 hours. It usually takes effect within 2 weeks, and the maximum antihypertensive effect can be achieved after 4 weeks.
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In addition to the antihypertensive effect, olmesartan and allisartan can also Effectively antagonizes the damage of angiotensin II to target organs, has 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 It can improve insulin resistance and reduce urinary protein. Long-term use can significantly reduce the risk of cardiovascular and cerebrovascular events such as myocardial infarction and cerebral stroke. It has relatively good curative effect on hypertensive patients with target organ damage such as obesity, diabetes, heart and kidney. It is especially suitable for hypertensive patients with heart failure, myocardial infarction, atrial fibrillation, impaired glucose tolerance or diabetic nephropathy.
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The advantages of Olmesartan are that it can promote the release of nitric oxide, It can expand the lumen of penile blood vessels, increase the blood perfusion of the cavernous body of the penis, and increase the level of androgen, which helps to enhance male erectile function, increase libido, and improve sexual function, especially for male hypertensive patients with sexual dysfunction. In addition, Olmesartan is well tolerated and safe, with few adverse reactions directly related to the drug, common adverse reactions such as dizziness, headache, rhinitis, pharyngitis, flu-like symptoms, back pain, usually mild symptoms, and continuous treatment compliance high. Finally, olmesartan is not metabolized by liver enzymes, and there are few interactions between drugs. Combination medication has better safety. At present, olmesartan has entered the “bulk purchase”, and the price of drugs has generally decreased. However, in 2013, the US FDA issued a warning that olmesartan can cause sprue and should be taken seriously. If severe diarrhea accompanied by weight loss occurs during the medication process, the drug should be stopped immediately and seek medical attention. No other “sartan” class has been found so far. Medications can cause sprue diarrhea.
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Alisartan is the first self-developed “Sartan” in my country Antihypertensive drug is a new compound obtained from losartan after structural modification. After hydrolysis by gastrointestinal esterase, it becomes an active product with antihypertensive effect and target organ protection effect. Its antihypertensive trough-to-peak ratio is More than 60%, the antihypertensive effect is lasting and stable. While reducing blood pressure, allisartan can also inhibit the uric acid transporter in the renal tubules, thereby preventing the reabsorption of uric acid and helping to reduce blood uric acid levels. In addition, allisartan has common adverse reactions such as headache, dizziness, elevated blood lipids, and elevated transaminases, which are generally mild and short-lived, and most of them can be relieved on their own or after symptomatic treatment. Allisartan is mainly metabolized by gastrointestinal esterase, not metabolized by liver drug enzymes, and does not increase the load of liver drug enzymes, thereby reducing the burden on the liver, reducing the interaction with other drugs, and helping to prevent adverse drug reactions.