Dose-Related Antihypertensive Effects of Irbesartan in Patients With Mild-to-Moderate Hypertension

Pool, James L.

doi:10.1016/s0895-7061(97)00501-3

Cited by 108 publications

(61 citation statements)

References 12 publications

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“…6,10,14,15,27 The drug exhibits nearly linear dose-response (blood pressure lowering) relationship for 50-300 mg dose. 6,10,23,27,32,46 After oral dosing, maximum blood pressure lowering effect occurs at 3-6 h. 6,14,15 Peak efficacy of blood pressure lowering effect is reached in 4 -8 weeks. 6,10,14,15 Irbesartan is effective in hypertensive patients, irrespective of S77 age or gender.…”

Section: Pharmacodynamic Characteristics Of Angiotensin Receptor Blocmentioning

confidence: 99%

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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: Pharmacodynamic Characteristics Of Angiotensin Receptor Blocmentioning

confidence: 99%

“…The ARBs have a low incidence of adverse effects, [2][3][4][5][6][7][8][9][10][11][12][13][14][15][21][22][23][24][25][26][27][28][29][30][31][32][33][34][35][36][37][38][39][40]42,44,[46][47][48][49][50][51][52][53][54][55][56][57][58][59]62,63,[76][77]<...>…”

Section: Adverse Effects Of Angiotensin Receptor Blockersmentioning

confidence: 99%

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

2000

J Hum Hypertens

289

215

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“…Signalling via both receptors has been reported to regulate MMP expression with most studies suggesting ATR1 mediates MMP up-regulation 18) . ATR1 blockade leads to increased levels of AII both in vivo and in culture [25][26][27][28] . The physiological role of ATR2, which has minimal, restricted expression in healthy adults 29) , but is present in atheroma 24) , is only partially understood with suggestions it opposes ATR1 or alternately has a synergistic role with ATR1 blockade 30) .…”

Section: Introductionmentioning

confidence: 99%

Involvement of Angiotensin II Type 1 and 2 Receptors in Gelatinase Regulation in Human Carotid Atheroma <i>in vitro </i>

Clancy

Koblar

Golledge

2016

JAT

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“…Clinical studies of irbesartan/HCTZ suggest that this combination is not only clinically effective, but also has a favourable safety profile, 18 producing significantly greater dose-dependent reductions in blood pressure compared with monotherapy [19][20][21] while attenuating some of the side effects (for example, hypokalaemia) associated with HCTZ. 21 Here, we investigate the efficacy, safety and tolerability of high-dose irbesartan/HCTZ in patients with moderate hypertension, a high proportion of whom were overweight, with dyslipidaemia and/or diabetes.…”

Section: Introductionmentioning

confidence: 99%

A comparison of the efficacy and safety of irbesartan/HCTZ combination therapy with irbesartan and HCTZ monotherapy in the treatment of moderate hypertension

et al. 2007

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This prospective, double-blind, parallel-group study randomized patients with moderate hypertension (seated systolic blood pressure (SeSBP) 160-179 mm Hg when seated diastolic blood pressure (SeDBP) o110 mm Hg; or SeDBP 100-109 mm Hg when SeSBP o180 mm Hg) 3:1:1 to treatment with irbesartan 300 mg/hydrochlorothiazide (HCTZ) 25 mg combination therapy (n ¼ 328), irbesartan 300 mg monotherapy (n ¼ 106) or HCTZ monotherapy 25 mg (n ¼ 104). Treatment was initiated at half dose, with forced titration to full dose after two weeks followed by ten further weeks' treatment. The primary efficacy variable was the mean reduction in SeSBP from baseline to week 8. Baseline characteristics were similar between groups, with mean baseline blood pressure approximately 162/98 mm Hg; the mean age was 55 years. At week 8 there was a reduction in SeSBP of 27.1 mm Hg with irbesartan/HCTZ, compared with 22.1 mm Hg with irbesartan monotherapy (P ¼ 0.0016) and 15.7 mm Hg with HCTZ (Po0.0001). Both the rate of decline and the total degree of decline achieved were greatest with irbesartan/ HCTZ and least with HCTZ. A significantly greater percentage of patients reached a treatment goal of SeSBP o140 mm Hg and SeDBP o90 mm Hg by week 8 with irbesartan/HCTZ (53.4%), compared with irbesartan (40.6%; P ¼ 0.0254) and HCTZ (20.2%; Po0.0001) alone. Treatment was well tolerated in all three-treatment groups with a slight increase in adverse events in the combination therapy group. In conclusion, irbesartan/HCTZ (300/25 mg) is well tolerated and achieves rapid and sustained reductions in both systolic blood pressure and diastolic blood pressure in patients with moderate hypertension.

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Dose-Related Antihypertensive Effects of Irbesartan in Patients With Mild-to-Moderate Hypertension

Cited by 108 publications

References 12 publications

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

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

Involvement of Angiotensin II Type 1 and 2 Receptors in Gelatinase Regulation in Human Carotid Atheroma <i>in vitro </i>

A comparison of the efficacy and safety of irbesartan/HCTZ combination therapy with irbesartan and HCTZ monotherapy in the treatment of moderate hypertension

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