D039 Safety of eprosartan in elderly patients with hypertension

Harland, Daniel R

doi:10.1016/s0895-7061(97)90998-5

Cited by 6 publications

(5 citation statements)

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“…[2][3][4][5][6][7][8][9][10][11][12][13][14][15]21,25,29,35,43,60 The ARBs are effective and relatively safe in the elderly hypertensives, [2][3][4][5][6][7][8][9][10][11][12][13][14][15]42,52,63 and in patients with isolated systolic hypertension. 76 The antihypertensive efficacy of ARBs is enhanced when combined with diuretics, ACE inhibitors, calcium channel blockers, betablockers, or alpha-blockers.…”

Section: Angiotensin Receptor Blockers As Antihypertensive Drugsmentioning

confidence: 99%

“…[36][37][38]42,47,48,50 Age or gender have no effect on blood pressure response to ARBs. [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.…”

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%

“…29,42,52,63 The adverse effect profile is often similar to that of placebo. Some of the adverse effects include, headache, dizziness, non-specific pain, upper respiratory tract infection, viral infection, asthenia/fatigue, sinusitis, and diarrhoea.…”

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

276

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: Angiotensin Receptor Blockers As Antihypertensive Drugsmentioning

confidence: 99%

Section: Advantages Of Angiotensin Receptor Blocker Therapy In Hypertmentioning

confidence: 99%

Section: Adverse Effects Of Angiotensin Receptor Blockersmentioning

confidence: 99%

Section: Adverse Effects Of Angiotensin Receptor Blockersmentioning

confidence: 99%

See 2 more Smart Citations

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

2000

J Hum Hypertens

276

215

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“…16 In addition, an exaggerated hypotensive response as might be expected in the elderly (dizziness, fatigue, injury, postural hypotension, hypotension, syncope) did not occur more frequently in patients over 65 years. 16 These findings were supported by data from a subgroup analysis of a 26-week study in which eprosartan 400-600 mg daily in two divided doses produced a significantly lower incidence of cough than enalapril 5-20 mg once/day. 17 The incidence of adverse experiences overall was comparable between the groups and did not vary with age (Table 2).…”

Section: Relation Between Adverse Events and Agementioning

confidence: 78%

Safety and Tolerability of Eprosartan

Gavras

1999

Pharmacotherapy

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The safety and tolerability of eprosartan were extensively assessed in 17 phase IIb-III studies that included 2709 patients with hypertension. The frequency of adverse events observed with eprosartan was similar to that seen with placebo. Neither the number nor the severity of these effects increased with prolonged therapy, and their frequency was not affected by increased eprosartan dosage or dosing frequency. The drug is equally well tolerated by women and men, by younger (< 65 yrs) and older (> or = 65 yrs) individuals, and by persons of all races. There are no known drug interactions, and eprosartan is well tolerated when given in combination with other frequently prescribed antihypertensive agents, without an increase in adverse events beyond those expected of baseline antihypertensive therapy.

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Potential of the angiotensin II receptor 1 blocker eprosartan in the management of patients with hypertension or heart failure

Hollenberg

2001

Current Science Inc

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When angiotensin-converting enzyme (ACE) inhibition first became available to block the renin system, few could have predicted the evolution that would occur in this field. The advent of angiotensin II receptor 1 (AT(1)) blockers has created new opportunities. These agents, including eprosartan, are extraordinarily well tolerated, not only when compared with antihypertensive agents but also in comparison with the ACE inhibitors, which are rather well tolerated. The AT(1) blocker class is growing rapidly, at least in part because many believe that these drugs will share with the ACE inhibitors the special ability to reduce morbidity and mortality. Does eprosartan have a special role within this class? Eprosartan differs structurally from the other AT(1) blockers in that it is not a biphenyl tetrazole. It differs functionally in vitro in being a pure competitive antagonist, as opposed to the nonequilibrium, insurmountable characteristics of the other blockers. This feature may prove to be useful for titration in the fragile patient. The reduction in catecholamine release induced by eprosartan that has been observed in animal models may account for some special examples of increased efficacy. One such example pertains to the difference in the dose-response relationship for the action of eprosartan on the renal blood supply in comparison with other AT(1) blockers. Eprosartan doses well below those required for control of blood pressure have a pronounced effect on the kidney. If research already under way supports these early suggestions, then eprosartan will be an important addition to our therapeutic armamentarium.

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D039 Safety of eprosartan in elderly patients with hypertension

Cited by 6 publications

References 0 publications

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

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

Safety and Tolerability of Eprosartan

Potential of the angiotensin II receptor 1 blocker eprosartan in the management of patients with hypertension or heart failure

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