B001 Angiotensin II ? receptor (AT1) blockade reduces ventricular arrhythmias in uncomplicated essential hypertensive patients

Crippa, Massimo P.; Damiani, G; Notaristefano, I.; Costa, Renato; Pini, Luigi Alberto; Franchini, D.; Boni, E; Corda, Luciano; Chiari, Égler; Zaninelli, Augusto; Fariello, R

doi:10.1016/s0895-7061(97)90844-x

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“…90 The benefits of ARB therapy of hypertension go beyond the reduction in blood pressure. The additional advantages of ARB therapy include: (1) reduction in left ventricular hypertrophy; 5,22,48,[91][92][93][94][95] (2) improvement in diastolic function; 96 (3) decrease in ventricular arrhythmias; 97 (4) reduction in the abnormal QT dispersion; 98 (5) improvement in endothelial dysfunction; 99 (6) improvement in large artery compliance; 95 (7) reduction in microalbuminuria; 29,35,45,89,100,101 (8) preservation of or improvement in renal function; 36,39,45,[84][85][86][87][88][89] except in patients with severe congestive heart failure or renal artery stenosis; (9) increase in insulin sensitivity; 102,103 and (10) decrease in serum uric acid levels (by only losartan); [104][105][106] hyperuricaemia is associated with increased risk for stroke and heart attack in hypertensive patients. 107 …”

Section: Advantages Of Angiotensin Receptor Blocker Therapy In Hypertmentioning

confidence: 99%

Clinical pharmacokinetics of angiotensin II (AT1) receptor blockers in hypertension

2000

J Hum Hypertens

289

215

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Angiotensin II receptor blockers (ARBs) represent a new class of effective and well tolerated orally active antihypertensive agents. Recent clinical trials have shown the added benefits of ARBs in hypertensive patients (reduction in left ventricular hypertrophy, improvement in diastolic function, decrease in ventricular arrhythmias, reduction in microalbuminuria, and improvement in renal function), and cardioprotective effect in patients with heart failure. Several large long-term studies are in progress to assess the beneficial effects of ARBs on cardiac hypertrophy, renal function, and cardiovascular and cerebrovascular morbidity and mortality in hypertensive patients with or without diabetes mellitus, and the value of these drugs in patients with heart disease and diabetic nephropathy.The ARBs specifically block the interaction of angiotensin II at the AT 1 receptor, thereby relaxing smooth muscle, increasing salt and water excretion, reducing plasma volume, and decreasing cellular hypertrophy. These agents exert their blood pressure-lowering effect mainly by reducing peripheral vascular resistance usually without a rise in heart rate. Most of the commercially available ARBs control blood pressure for 24 h after once daily dosing. Sustained efficacy of blood pressure control, without any evidence of tachyphylaxis, has been demonstrated after long-term administration (3 years) of some of the ARBs. The efficacy of ARBs is similar to that of thiazide diuretics, beta-blockers, angiotensin-converting enzyme inhibitors or calcium channel blockers in patients with similar degree of hypertension. Higher daily doses, dietary salt restriction, and concomitant diuretic or ACE inhibitor administration amplify the antihypertensive effect of ARBs. The ARBs have a low incidence of adverse effects (headache, upper respiratory infection, back pain, muscle cramps, fatigue and dizziness), even in the elderly patients. After the approval of losartan, five other ARBs (candesartan cilexetil, eprosartan, irbesartan, telmisartan, and valsartan) and three combinations with hydrochlorothiazide (irbesartan, losartan and valsartan) have been approved as antihypertensive agents, and some 28 compounds are in various stages of development.The ARBs are non-peptide compounds with varied structures; some (candesartan, losartan, irbesartan, and valsartan) have a common tetrazolo-biphenyl structure. Except for irbesartan, all active ARBs have a carboxylic acid group. Candesartan cilexetil is a prodrug, while losartan has a metabolite (EXP3174) which is more active than the parent drug. No other metabolites of ARBs contribute significantly to the antihypertensive effect.Keywords: angiotensin receptor blockers; candesartan; eprosartan; irbesartan; losartan; telmisartan; valsartan; pharmacokinetics After oral administration, the ARBs are rapidly absorbed (time for peak plasma levels ‫؍‬ 0.5-4 h) but they have a wide range of bioavailability (from a low of 13% for eprosartan to a high of 60-80% for irbesartan); food does not influence the bioavaila...

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Section: Advantages Of Angiotensin Receptor Blocker Therapy In Hypertmentioning

confidence: 99%

Clinical pharmacokinetics of angiotensin II (AT1) receptor blockers in hypertension

2000

J Hum Hypertens

289

215

View full text Add to dashboard Cite

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B001 Angiotensin II ? receptor (AT1) blockade reduces ventricular arrhythmias in uncomplicated essential hypertensive patients

Cited by 1 publication

References 0 publications

Clinical pharmacokinetics of angiotensin II (AT1) receptor blockers in hypertension

Clinical pharmacokinetics of angiotensin II (AT1) receptor blockers in hypertension

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