Effect of Hydrochlorothiazide on the Pharmacokinetics and Pharmacodynamics of the Angiotensin II Blocker Irbesartan

Marino, Maria; Langenbacher, Kathleen M.; Ford, Neville F.; Beierle, Floyd A.; Raymond, Ralph; Shamblen, E. Cooper; Lasseter, Kenneth C.

doi:10.2165/00044011-199714050-00007

Cited by 24 publications

(19 citation statements)

References 18 publications

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“…Administration of hydrochlorothiazide to hypertensive patients 14,15,128 or nifedipine to normal volunteers 14,15,161 has no effect on the pharmacokinetics of irbesartan. Irbesartan does not alter the pharmacodynamics or pharmacokinetics of warfarin, 14,15,162 or digoxin.…”

Section: Interactions Of Angiotensin Receptor Blockers With Other Drugsmentioning

confidence: 97%

“…6,14,15,32,126,127 Peak plasma levels of irbesartan are achieved at 1.3-3 h after oral dosing. 6,32,41,61,110,[126][127][128][129] Irbesartan displays linear doserelated pharmacokinetics over the dose range of 50-600 mg. 6,14,15,110 The drug is 90% bound, mainly to albumin (binding to alpha 1-acid glycoprotein = 22%). 6,14,15 Steady-state plasma levels are reached in 3 days after daily dosing, and no clinically important accumulation (Ͻ20%) occurs (Table 6b).…”

Section: Adverse Effects Of Angiotensin Receptor Blockersmentioning

confidence: 99%

“…(11-18 h). 6,14,15,32,41,61,110,[126][127][128] The hepatic extraction ratio of irbesartan is low (0.2), 126 and the drug is partially metabolised (6% of the dose) by oxidation (by cytochrome CYP2C9) and glucuronidation to form eight inactive metabolites. 14,15,130 The metabolites account for only 9% of the circulating drug, 5-10% in urine and 6% in faeces.…”

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

285

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: Interactions Of Angiotensin Receptor Blockers With Other Drugsmentioning

confidence: 97%

Section: Adverse Effects Of Angiotensin Receptor Blockersmentioning

confidence: 99%

Section: Adverse Effects Of Angiotensin Receptor Blockersmentioning

confidence: 99%

See 1 more Smart Citation

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

2000

J Hum Hypertens

285

215

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“…The oral absorption of irbesartan is rapid and complete with an average absolute bioavailability of 60 -80%. It is prescribed alone or in combination with hydrochlorothiazide for the treatment of moderate to severe hypertension (Marino, et al, 1997).…”

Section: Introductionmentioning

confidence: 99%

Adsorptive Stripping Voltammetric Determination of Irbesartan in Bulk and Pharmaceutical Products

Habib

Weshahy

Toubar³

et al. 2008

Pharm Chem J

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Adsorptive stripping Voltammetric determination of irbesartan using a hanging mercury drop electrode (HMDE) is described. The method is based on adsorptive accumulation of the species at the HMDE, followed by a first-harmonic alternating current (AC) stripping sweep at pH 6. The behavior of the adsorptive stripping response was studied under various experimental conditions, e.g., type of supporting electrolyte, pH, accumulation time, scan rate, and mode of sweep. In Britton-Robinson buffer solution, a quasi-reversible reduction process involving transfer of two electrons and two protons takes place. The response was linear over the concentration range of 0.16 -1.60 mg/ml with regression coefficient 0.997 and detection limit 0.11 mg/ml. The average of determinations of the cited compound in oral dosages with its standard deviation was 99.39 ± 4.33 %.The result obtained by the proposed method was compared with that obtained by the uv-spectrophotometric technique. Furthermore, the proposed method was also successfully applied as a stability-indicating method.

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“…AIIRAs are generally well tolerated (4,24,29). In a recent pooled analysis of data from placebo-controlled trials, the safety and tolerability profile of irbesartan was similar to that of placebo (62).…”

Section: Introductionmentioning

confidence: 99%

A Review of the New Angiotensin II‐Receptor Antagonist Irbesartan

Powell

Reeves

Marino

et al. 1998

Cardiovascular Drug Reviews

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Effect of Hydrochlorothiazide on the Pharmacokinetics and Pharmacodynamics of the Angiotensin II Blocker Irbesartan

Cited by 24 publications

References 18 publications

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

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

Adsorptive Stripping Voltammetric Determination of Irbesartan in Bulk and Pharmaceutical Products

A Review of the New Angiotensin II‐Receptor Antagonist Irbesartan

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