Effect of Ranitidine on the Pharmacokinetics of Orally Administered Eprosartan, an Angiotensin II Antagonist, in Healthy Male Volunteers

Tenero, David M.; Martin, David E.; Ilson, Bernard E.; Boyle, Duane A.; Boike, Steven C.; Carr, Alison; Lundberg, David; Jorkasky, Diane K.

doi:10.1345/aph.17188

Cited by 9 publications

(5 citation statements)

References 9 publications

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“…They were also not affected by concomitant administration of ranitidine (Tenero et al, 1998d). Reciprocally, eprosartan had no effect on single oraldose digoxin pharmacokinetics , steady-state prothrombin time ratios in healthy subjects receiving warfarin (Kazierad et al, 1998), or on 24-hour plasma glucose profiles in patients with diabetes receiving glyburide.…”

Section: G Pharmacokinetic Drug-drug Interactionsmentioning

confidence: 86%

A Systematic Comparison of the Properties of Clinically Used Angiotensin II Type 1 Receptor Antagonists

et al. 2013

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Section: G Pharmacokinetic Drug-drug Interactionsmentioning

confidence: 86%

A Systematic Comparison of the Properties of Clinically Used Angiotensin II Type 1 Receptor Antagonists

et al. 2013

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“…For eprosartan, the C max and AUC increase by 30–50% and by 70–90% in patients with moderate‐to‐severe renal impairment, respectively, and the unbound fraction of the drug increases by 35% and 59% in patients with moderate and severe renal dysfunction, respectively . The AUC for eprosartan (but not the C max ) has also been shown to increase by approximately 40% on average in patients with decreased hepatic function . The pharmacokinetics of irbesartan has been shown to be unaltered in patients with renal impairment or cirrhosis of the liver .…”

Section: Discussionmentioning

confidence: 99%

The Model for End-stage Liver Disease score is potentially a useful predictor of hyperkalemia occurrence among hospitalized angiotensin receptor blocker users

et al. 2014

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“…11 For example, fluconazole 124 or ranitidine 160 do not have a significant effect on the pharmacokinetics of eprosartan.…”

Section: Interactions Of Angiotensin Receptor Blockers With Other Drugsmentioning

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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Effect of Ranitidine on the Pharmacokinetics of Orally Administered Eprosartan, an Angiotensin II Antagonist, in Healthy Male Volunteers

Abstract: Repeated doses of ranitidine did not have a marked effect on the single-dose pharmacokinetics of eprosartan.

Cited by 9 publications

References 9 publications

A Systematic Comparison of the Properties of Clinically Used Angiotensin II Type 1 Receptor Antagonists

A Systematic Comparison of the Properties of Clinically Used Angiotensin II Type 1 Receptor Antagonists

The Model for End-stage Liver Disease score is potentially a useful predictor of hyperkalemia occurrence among hospitalized angiotensin receptor blocker users

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

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