Candesartan Cilexetil: Comparison of once-daily versus twice-daily administration for systemic hypertension

Zuschke, C A; Keys, Iris; Munger, Mark A.; Carr, Albert A.; Marinides, George N.; Flanagan, Terry L.; Cushing, Daniel; Hayes, Jodi L.; Michelson, Eric L.

doi:10.1016/s0149-2918(00)88302-2

Cited by 11 publications

(12 citation statements)

References 9 publications

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“…12,14 The trough/peak ratios of blood pressure are in the range of 0.7-1.0. 12,30,49,62 The antihypertensive effect is well maintained for 24 h after 8-16 mg daily dose of candesartan cilexetil; 12,14,15,20,31,53,62 peak efficacy of antihypertensive effect is reached in 4 -6 weeks of daily dosing. 12,14,15 The basic structure of eprosartan is different from other ARBs (Figure 1).…”

Section: Pharmacodynamic Characteristics Of Angiotensin Receptor Blocmentioning

confidence: 97%

“…[2][3][4][5][6][7][8][9][10][11][12][13][14][15]19,21,24,25,[31][32][33][36][37][38][39][40]42,44,47,50,54,56,[58][59][60]62 Sustained efficacy has been shown with long-term therapy with ARBs, with no tachyphylaxis. [36][37][38]42,47,48,50 Age or gender have no effect on blood pressure response to ARBs.…”

Section: Advantages Of Angiotensin Receptor Blocker Therapy In Hypertmentioning

confidence: 99%

“…[2][3][4][5][6][7][8][9][10][11][12][13][14][15]42,52,63 The ARBs do not alter the circadian rhythm of blood pressure. 24,31,34,40,53,62 Therapy with the ARBs does not cause first dose (excessive) hypotension or significant orthostatic hypotension. [2][3][4][5][6][7][8][9][10][11][12][13][14][15]27,49,50,59,60 Cessation of treatment with ARBs causes no rebound hypertension.…”

Section: Advantages Of Angiotensin Receptor Blocker Therapy In Hypertmentioning

confidence: 99%

“…Treatment with the ARBs does not result in clinically significant alterations in laboratory measurements of serum chemistry, haematology and urinalysis. [2][3][4][5][6][7][8][9][10][11][12][13][14][15]19,23,39,44,50,59,62,81 The ARBs do not impair glucose or lipid metabolism. [2][3][4][5][6][7][8][9][10][11][12][13][14][15]19,[81][82][83] These drugs have no adverse effect on renal function.…”

Section: Advantages Of Angiotensin Receptor Blocker Therapy In Hypertmentioning

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%

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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: 97%

Section: Advantages Of Angiotensin Receptor Blocker Therapy In Hypertmentioning

confidence: 99%

Section: Advantages Of Angiotensin Receptor Blocker Therapy In Hypertmentioning

confidence: 99%

Section: Advantages Of Angiotensin Receptor Blocker Therapy In Hypertmentioning

confidence: 99%

Section: Adverse Effects Of Angiotensin Receptor Blockersmentioning

confidence: 99%

See 3 more Smart Citations

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

2000

J Hum Hypertens

289

215

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Blood pressure lowering efficacy of angiotensin receptor blockers for primary hypertension

Heran

Wong

Heran

et al. 2008

Cochrane Database of Systematic Reviews

103

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The evidence from this review suggests that there are no clinically meaningful BP lowering differences between available ARBs. The BP lowering effect of ARBs is modest and similar to ACE inhibitors as a class; the magnitude of average trough BP lowering for ARBs at maximum recommended doses and above is -8/-5 mmHg. Furthermore, 60 to 70% of this trough BP lowering effect occurs with recommended starting doses. The review did not provide a good estimate of the incidence of harms associated with ARBs because of the short duration of the trials and the lack of reporting of adverse effects in many of the trials.

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Efficacy of angiotensin II receptor antagonists in preventing headache: a systematic overview and meta-analysis

Etminan

Levine

Tomlinson

et al. 2002

The American Journal of Medicine

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Candesartan Cilexetil: Comparison of once-daily versus twice-daily administration for systemic hypertension

Cited by 11 publications

References 9 publications

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

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

Blood pressure lowering efficacy of angiotensin receptor blockers for primary hypertension

Efficacy of angiotensin II receptor antagonists in preventing headache: a systematic overview and meta-analysis

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