The pharmacokinetics of quinapril and quinaprilat in patients with congestive heart failure.

Begg, EJ; Robson, RA; Ikram, Hamid; Richards, A. Mark; Bammert-Adams, J. A.; Olson, SC; Posvar, EL; Reece, P. A.; Sedman, AJ

doi:10.1111/j.1365-2125.1994.tb04280.x

Cited by 10 publications

(2 citation statements)

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“…Quinapril HCl, 2-(2-{[1-(ethoxycarbonyl)-3-phenyl-propyl]amino}-1-oxopropyl)-1, 2, 3, 4-tetra hydro-3-isoquinoline carboxylic acid mono hydrochloric acid, is a potent orally active non-sulfhydryl non-peptidic angiotensin converting enzyme (ACE) inhibitor. It is de-esterified in vivo to the active di-acid metabolite quinaprilat (Begg et al, 1994). The full activity of quinapril depends on conversion to the active metabolite quinaprilat (Squire et al, 1994).…”

Section: Introductionmentioning

confidence: 99%

Determination of quinapril and quinaprilat in human plasma by ultraperformance liquid chromatography–electrospray ionization mass spectrometry

Dasandi¹,

Shah²,

Shivprakash³

2008

Biomedical Chromatography

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A novel, specific and sensitive ultraperformance liquid chromatography tandem mass spectrometry (UPLC-MS/ MS) method was developed for the simultaneous determination of quinapril and its active metabolite quinaprilat in human plasma. The method involves a simple, one-step extraction procedure coupled with an Acquity UPLC TM BEH C 18 column (100 × 2.1 mm, i.d., 1.7 mm) with isocratic elution at a flow-rate of 0.2 mL/min and lisinopril as the internal standard. Detection was performed on a triple-quadrupole tandem mass spectrometer in multiple reaction monitoring mode via electrospray ionization. Using 250 mL plasma, the methods were validated over the concentration range 5.010-500.374 ng/mL for quinapril and 10.012-1000 ng/mL for quinaprilat, with a lower limit of quantification of 5.010 ng/mL for quinapril and 10.012 ng/mL for quinaprilat. The intra-and inter-day precision and accuracy were within 10.0%. The recovery was 85.8, 62.6 and 61.3% for quinapril, quinaprilat and lisinopril, respectively. Total run time was 3.0 min only.

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Section: Introductionmentioning

confidence: 99%

Determination of quinapril and quinaprilat in human plasma by ultraperformance liquid chromatography–electrospray ionization mass spectrometry

Dasandi¹,

Shah²,

Shivprakash³

2008

Biomedical Chromatography

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“…The kinetics of several ACE inhibitors, including lisinopril, perindopril and ramipril, are altered by HF,[59,1 I I-I 13, [138][139][140][141][142][143] and dosage reduction is recommended during initiation of therapy, based on the initial BP response.l 143 ] However, there are other ACE inhibitors, such as cilazapril, that do not require dosage adjustment, even though chronic administration leads to accumulation of the drug in patients with HF.l140]…”

Section: Changes Affecting Pharmacokineticsmentioning

confidence: 99%

ACE Inhibitors

Israili

Hall²

1995

Drugs & Aging

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High blood pressure (BP) in the elderly must not be ignored as a normal consequence of aging. The criteria for the diagnosis of hypertension and the necessity to treat it are the same in elderly and younger patients. The aim of treatment of elderly hypertensive patients is to decrease BP safely and to reduce risk factors associated with cerebrovascular, cardiovascular and renal morbidity and mortality. The treatment of elderly hypertensive patients should be adjusted according to the needs of the individual, based upon age, race, severity of hypertension, co-existing medical problems, other cardiovascular risk factors, target-organ damage, risk-benefit considerations and costs. In addition to the elevated BP, other cardiovascular risk factors include smoking, glucose intolerance, hyperinsulinaemia, dyslipidaemia, hypercreatininaemia, peripheral vascular disease, left ventricular hypertrophy, and microalbuminuria (or albuminuria). Thus, the choice of initial antihypertensive therapy in elderly hypertensive patients should be based not only on the expected response, but also on the effects of therapy on lipid, potassium, glucose and uric acid levels, and left ventricular anatomy and function. Co-existing medical conditions (such as asthma, diabetes mellitus, heart failure, renal failure, gout, coronary artery disease, hyperlipidaemia and peripheral vascular disease) are major determinants for the selection of antihypertensive medications. With previous therapies (diuretics, beta-blockers, etc.), good BP control in the elderly was associated with clear and statistically significant reductions in stroke-related morbidity and mortality, but the overall effects on cardiovascular and renal complications of hypertension was either more variable or less obvious. Angiotensin converting enzyme (ACE) inhibitors are not only efficacious antihypertensive agents in the elderly, but also appear promising in counteracting some of the cardiovascular and renal consequences of hypertension. They are well tolerated and have a relatively low incidence of adverse effects. ACE inhibitors possess ancillary characteristics that are potentially beneficial for many elderly patients, including reduction of left ventricular mass, lack of metabolic and lipid disturbances, no adverse CNS effects, no risk of induction of heart failure, and a low risk of orthostatic hypotension. Since ACE inhibitors may improve perfusion to the heart, kidney and brain, they are well worth considering for the treatment of elderly patients with hypertensive target organ damage, especially in patients with heart failure, and diabetic patients with early nephropathy.

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Clinical Pharmacokinetics of Drugs in Patients with Heart Failure: An Update (Part 2, Drugs Administered Orally)

2014

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The purpose of the present review article is to update the information regarding pharmacokinetics of drugs in patients with heart failure that has accumulated since the last review article published in 1988 in Clinical Pharmacokinetics. Since this last review, our understanding of the pathophysiology of heart failure has changed from the cardio-renal model to the neuro-humoral model, and the pharmacologic approach to treatment of heart failure has been shifted from inotropic agents to those acting on the renin-angiotensin-aldosterone system. The pharmacologic agents now used for heart failure include many important classes of drugs, such as ACE inhibitors, angiotensin receptor blockers (antagonists) (ARBs), and mineralocorticoid receptor antagonists. In Part 1 of this review, we summarized the pharmacokinetic properties of relevant drugs administered intravenously. In Part 2, the present article, we describe pharmacokinetics of drugs following oral administration. For this purpose we conducted a systematic search of literature using MEDLINE, EMBASE, and Japan Centra Revuo Medicina (in Japanese). We retrieved a total of 110 relevant publications for 49 drugs and updated the information for ten drugs and provided new information for 31 drugs. We recognized that the pharmacokinetic data were obtained primarily from stable heart failure patients with moderate severity [New York Heart Association (NYHA) class II or III]. In addition, most patients were classified as heart failure with reduced ejection fraction. Furthermore, because most of the studies retrieved had no comparative groups of healthy subjects or patients without heart failure, historical controls from previous studies were used for comparisons. In Part 2, we also discuss the pharmacokinetics of active metabolites as well as parent drugs, because many drugs given by oral administration for the treatment of heart failure are prodrugs (e.g., ACE inhibitors and ARBs). The pharmacokinetic changes of drugs in patients with heart failure are discussed in the light of a physiologically based pharmacokinetic model. In addition, we discuss the effects of intestinal tissue heart failure-associated edema on drug absorption as it relates to the biopharmaceutical classification system, particularly for drugs demonstrating reduced systemic exposure as measured by the area under the plasma concentration-time curve after oral administration (AUCpo) in patients with heart failure as compared with healthy subjects. After review of the available data, it was seen that among patients with asymptomatic or compensated chronic heart failure there seemed to be no or minimal alterations in the maximum concentration (C max) and AUCpo of the included drugs, unless there was concurrent liver and/or renal dysfunction. In contrast, the AUCpo of at least 14 drugs (captopril, cilazaprilat, enalapril/enalaprilat, perindopril, carvedilol, candesartan, pilsicainide, felodipine, furosemide, enoximone, milrinone, flosequinan, molsidomine, and ibopamine) were suspected or documented to increa...

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The pharmacokinetics of quinapril and quinaprilat in patients with congestive heart failure.

Cited by 10 publications

References 10 publications

Determination of quinapril and quinaprilat in human plasma by ultraperformance liquid chromatography–electrospray ionization mass spectrometry

Determination of quinapril and quinaprilat in human plasma by ultraperformance liquid chromatography–electrospray ionization mass spectrometry

ACE Inhibitors

Clinical Pharmacokinetics of Drugs in Patients with Heart Failure: An Update (Part 2, Drugs Administered Orally)

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