Irbesartan is the first-line antihypertensive drug for essential hypertension, belonging to angiotensin II receptor antagonist, mainly acting on the renin-angiotensin-aldosterone system, by antagonizing the vasoconstriction of angiotensin II, inhibiting the release of aldosterone, reducing water and sodium retention and lowering blood pressure, its antihypertensive effect is slow, but stable and long-lasting, suitable for patients with mild, moderate and severe hypertension, and is the preferred antihypertensive drug for the initiation and maintenance of hypertension. In addition, irbesartan also has a good cardiovascular protective effect, can reverse left ventricular hypertrophy, anti-atherosclerosis, inhibit fibroblast proliferation and atrial fibrillation electrical remodeling, and can improve glucose and lipid metabolism, reduce urine protein excretion, especially suitable for hypertension patients with left ventricular hypertrophy, cardiac insufficiency, atrial fibrillation, coronary heart disease, diabetic nephropathy, microalbuminuria or proteinuria, metabolic syndrome (hyperlipidemia, diabetes, obesity or hyperuricemia). In addition, enalapril, benazepril and other pril antihypertensive drugs can cause adverse reactions such as dry cough and angioedema, and for patients who cannot tolerate it, sartan antihypertensive drugs such as irbesartan can be selected.
You should know that angiotensin II can constrict blood vessels, cause vascular remodeling, lead to vascular endothelial hyperplasia and fibrosis, is a direct inducing factor of atherosclerosis, can cause renal ischemic atrophy, volume reduction, in the long run, and eventually induce glomerulosclerosis, renal interstitial fibrosis, glomerular basement membrane destruction and other chronic kidney disease, and then develop into uremia, which is irreversible for renal damage. It has a kidney-protective effect and is the preferred antihypertensive drug for hypertensive nephropathy.
Irbesartan can dilate renal blood vessels, and the dilation effect on glomerular effluent arterioles is stronger than that on glomerular afferent arterioles, thereby causing a decrease in glomerular filtration pressure, decreased renal function, decreased glomerular filtration rate, and increased serum potassium and serum creatinine, but this is not contrary to the protective effect of the kidneys, when renal ischemia is not severe, irbesartan can protect the kidneys, and when renal ischemia is severe, it will affect renal function, so when using irbesartan, glomerular filtration rate, serum creatinine and serum potassium changes should be closely monitored, If glomerular filtration rate or serum creatinine rises above 30% of the upper limit of normal, the dose should be reduced and monitoring should be continued if serum potassium exceeds 5Elevated glomerular filtration rate or serum creatinine greater than 50% of the upper limit of normal should be discontinued immediately, and irbesartan should be contraindicated in patients with bilateral renal artery stenosis or hyperkalemia.
For patients with grade 2 or higher hypertension with a blood pressure of 160 100 mmHg, 2 antihypertensive drugs should be used initially, and for hypertensive patients with blood pressure higher than 140 90 mmHg, 2 antihypertensive drugs can also be used initially** to achieve blood pressure as soon as possible. The combination of irbesartan and hydrochlorothiazide has a synergistic antihypertensive effect, which can significantly increase the antihypertensive effect and improve the blood pressure compliance rate. In addition, hydrochlorothiazide can activate the sympathetic nervous system and produce an adverse effect on blood pressure, irbesartan can inhibit sympathetic nerve overactivation and counteract this adverse factor, irbesartan can slightly increase blood potassium and antagonize hypokalemia caused by long-term use of hydrochlorothiazide, therefore, irbesartan combined with hydrochlorothiazide is the preferred antihypertensive combination. Nifedipine and amlodipine antihypertensive drugs mainly dilate arteries, and irbesartan can dilate arteries and veins, and the combination of the two can synergistically lower blood pressure and improve blood pressure control rate. Lower extremity edema is common with horizon antihypertensive drugs, and irbesartan can dilate the back capillaries, reduce intracapillary pressure, and reduce or counteract lower extremity edema. Irbesartan can also block adverse reactions such as increased reflex and heart rate caused by dipine antihypertensive drugs, so irbesartan combined with dipine antihypertensive drugs optimizes the combined antihypertensive regimen.
Irbesartan and propranolol, metoprolol, bisoprolol and other -receptor blockers all act on the renin-angiotensin-aldosterone system, and the antihypertensive mechanisms are partially overlapped and cannot significantly increase the antihypertensive effect, so the combination of irbesartan and -receptor blockers is not recommended and can only be used as a secondary combination regimen. In the same way, irbesartan has a similar mechanism of action with enalapril, benazepril, pedocpril and other pril antihypertensive drugs, and the combined use cannot significantly increase the antihypertensive effect, but it can increase the risk of hyperkalemia and has no synergistic effect on the protection of target organs.
In terms of antihypertensive strength, although valsartan and irbesartan have similar chemical structures, irbesartan has unique aromatic groups in the structure, which is more fat-soluble, more tissue-penetrating, and more antagonistic to angiotensin II, so the antihypertensive strength is better than valsartan. In terms of antihypertensive stability, compared with valsartan, irbesartan has a hypotensive effect throughout the drug period, with a higher antihypertensive trough-to-peak ratio, a more stable antihypertensive effect, and less blood pressure fluctuations. In terms of duration of action, compared with valsartan, irbesartan has better lipid solubility and tissue penetration, higher plasma protein binding rate, more extensive distribution in the body, slower dissociation rate after binding to AT1 receptor of angiotensin II, half-life is twice that of valsartan, and the effect is more durable. Therefore, in general, irbesartan is more effective.
The blood pressure of the human body has a law of diurnal changes, generally after getting up at 8 o'clock and 10 o'clock in the morning, the blood pressure rises significantly, showing a peak, and then falls, at 17 o'clock in the afternoon, the blood pressure rises again from the trough to another peak, high blood pressure in the early morning can cause damage to the cardiovascular and cerebrovascular vessels, and it is a high-risk period for myocardial infarction, sudden cardiac death and stroke, so antihypertensive drugs should be taken before the arrival of the peak blood pressure. Irbesartan is a long-acting antihypertensive drug, taken once a day, can control 24 hours of stable blood pressure, it is recommended to take it at 7 o'clock in the morning, when the peak of blood pressure is reached, just play a role in lowering blood pressure, irbesartan is not affected by meals, can be taken before or after meals, therefore, it is recommended to take irbesartan at 7 o'clock in the morning, fix the time of taking the drug, and improve medication compliance.