Synonymous: | 3-Butyl-2-[[4-[2-(2H-Tetrazol-5-Yl)Phenyl]Phenyl]Methyl]-2,4-Diazaspiro[4.4]Non-3-En-1-One |
CAS: | 138402-11-6 |
Molecular Formula: | C25H28N6O |
Molecular Weight: | 428.53 |
Appearance | White crystalline powderr |
Storage | Cool and airtight storage |
Category | Drugs for treating hypertension |
Irbesartan is an angiotensin II receptor inhibitor. Angiotensin II receptors are divided into AT1 and AT2. Irbesartan can inhibit the conversion of Ang Ⅰ to ang Ⅱ by selectively blocking the AT1 receptor of ANGLI, and can specifically antagonize the angiotensin converting enzyme 1 receptor (AT1). The antagonistic effect of irbesartan on AT1 is 8500 times that of AT2. By selectively blocking the binding of Ang Ⅱ to AT1 receptor, Inhibit vasoconstriction and aldosterone release, and produce antihypertensive effect. This product does not inhibit angiotensin converting enzyme, renin and other hormone receptors, nor does it inhibit ion channels related to blood pressure regulation and sodium balance. Irbesartan can also reduce myocardial electrical remodeling, so as to reduce the mortality of patients with hypertension. It is the most effective drug for the treatment of hypertension and cardiovascular diseases.
Irbesartan was well absorbed after oral administration; Its absolute bioavailability is 60% ~ 80%, and eating will not significantly affect its bioavailability. The peak time of plasma was 1 ~ 1.5 hours and the elimination half-life was 11 ~ 15 hours. Steady state within three days. Irbesartan is metabolized by glucuronidation or oxidation. In vitro studies show that irbesartan is mainly oxidized by cytochrome P450 2C9. This product and its metabolites are excreted through biliary tract and kidney. The plasma protein binding ratio X of irbesartan was about 90%. The pharmacokinetics of irbesartan showed linear and dose correlation in the range of 10-600mg.
The common adverse reactions are headache, dizziness, palpitation, and occasional cough. Generally, they are mild and transient. Most patients can tolerate the continued medication. Urticaria and angioneuroedema are rare. The literature reported that the incidence of adverse reactions of this product was more than 1%, including dyspepsia, heartburn, diarrhea, skeletal muscle pain, fatigue and upper respiratory tract infection, but there was no significant difference compared with the blank control group. The incidence of abdominal pain, anxiety, neuroticism, chest pain, pharyngitis, nausea and vomiting, rash, tachycardia and so on. The incidence of hypotension and orthostatic hypotension was about 0.4%.
It is forbidden for those who are allergic to this product. The 4th to 9th months of pregnancy. lactation.