The pharmacokinetics of lisinopril in hospitalized patients with congestive heart failure.

Till, Alice E.; Dickstein, Kenneth; Aarsland, Torbjørn; Gómez, Héctor W.; Gregg, H.; Hichens, Martin

doi:10.1111/j.1365-2125.1989.tb05351.x

Cited by 18 publications

(4 citation statements)

References 11 publications

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“…Other studies have also demonstrated significant accumulation of lisinopril in patients with either CHF or chronic renal insufficiency. Both Gautam et al [6] and Till et al [19] reported higher serum levels of lisinopril in patients with CHF than in healthy individuals. In contrast, Johnston & Duffin [20] documented no alterations in lisinopril pharmacokinetics in patients with CHF.…”

Section: Discussionmentioning

confidence: 99%

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Comparison of the pharmacokinetics of fosinoprilat with enalaprilat and lisinopril in patients with congestive heart failure and chronic renal insufficiency

Greenbaum

Zucchelli

Caspi

et al. 2000

Brit J Clinical Pharma

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Aims To compare the serum pharmacokinetics of fosinoprilat with enalaprilat and lisinopril after 1 and 10 days of dosing with fosinopril, enalapril and lisinopril. Methods Patients with congestive heart failure (CHF, NYHA Class II–IV) and chronic renal insufficiency (creatinine clearance ≤30 ml min−1 ) were randomized to receive fosinopril, enalapril or lisinopril in two parallel‐group studies. In the first study 24 patients were treated with 10 mg fosinopril (n=12 patients) or 2.5 mg enalapril (n=12) every morning for 10 consecutive days. In the second study 31 patients were treated with 10 mg fosinopril (n=16 patients) or 5 mg lisinopril (n=15) every morning for 10 consecutive days. Samples of blood were collected for determination of pharmacokinetic parameters. The area under the curve (AUC) between the first and last days of treatment and the accumulation index (AI) were the primary outcome measures. Results All three angiotensin converting enzyme (ACE) inhibitors exhibited a significant increase in AUC between the first and last days of treatment in both studies. The difference between the AI for fosinoprilat (1.41) and enalaprilat (1.96) was statistically significant (95% CI: 1.05, 1.84). Similarly, the difference between the AI for fosinoprilat (1.21) and lisinopril (2.76) was statistically significant (95% CI: 1.85, 2.69). All three ACE inhibitors completely inhibited serum ACE for 24 h. All treatments were well tolerated. Conclusions Fosinoprilat exhibits significantly less accumulation than enalaprilat or lisinopril in patients with CHF and renal insufficiency, most probably because fosinoprilat is eliminated by both the kidney and liver, and increased hepatic elimination can compensate for reduced renal clearance in patients with kidney dysfunction.

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Section: Discussionmentioning

confidence: 99%

“…In one study, the effective half‐life of lisinopril doubled and tripled in patients with mild and severe renal impairment, respectively [22]. These results are not surprising in view of the elimination of lisinopril solely by renal excretion [19, 23].…”

Section: Discussionmentioning

confidence: 99%

Comparison of the pharmacokinetics of fosinoprilat with enalaprilat and lisinopril in patients with congestive heart failure and chronic renal insufficiency

Greenbaum

Zucchelli

Caspi

et al. 2000

Brit J Clinical Pharma

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“…First, the present study focused only on the PK characteristics of lisinopril in adults and children with normal renal function. The impact of renal impairment or disease state such as congestive heart failure on lisinopril's PK warrants further investigation 57 . Second, from a safety perspective, the twofold deviation boundary used for the model verification in young children (age < 6 years) may be too high since this patient population, such as neonates, may have higher levels of renal failure and electrolyte disturbances.…”

Section: Discussionmentioning

confidence: 99%

Physiologically based pharmacokinetic modelling of lisinopril in children: A case story of angiotensin converting enzyme inhibitors

Xie

Bocxlaer

Vermeulen

2020

Brit J Clinical Pharma

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Aims Lisinopril is an angiotensin converting enzyme inhibitor to treat hypertension. It shows complex pharmacokinetics (PK), and its PK behaviour in paediatric populations is not well characterized. The aim of this study was to develop a physiologically based PK (PBPK) model for lisinopril to describe the drug's PK in children. Methods The PBPK model development was performed in a step‐wise manner. An adult model was initially developed to characterize lisinopril's disposition and absorption and verified using literature data. Subsequently, the adult PBPK model was extrapolated to the paediatric population (0.5–18 years old) by accounting for age‐dependent physiological and anatomical changes. Model performance was evaluated by comparing the PK profiles and drug exposures of observed vs predicted data. Results The disposition of lisinopril was well described by a minimal PBPK model—an effective strategy to capture the biphasic elimination of the drug. The absorption of lisinopril was described by the intestinal peptide transporter‐mediated uptake. The adult model adequately described the literature data with predictions within a twofold range of clinical observations. Good model predictivity was also observed in children older than 6 years of age. The model overpredicted the drug exposure in children under 6 years, probably due to not incorporating the actual, unknown ontogeny of the intestinal peptide transporter. Conclusions The PBPK model predicted the PK of lisinopril in adults and children above 6 years of age well. Model refinement in children under 6 years warrants future informative ontogeny data of the intestinal peptide transporter.

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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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The pharmacokinetics of lisinopril in hospitalized patients with congestive heart failure.

Cited by 18 publications

References 11 publications

Comparison of the pharmacokinetics of fosinoprilat with enalaprilat and lisinopril in patients with congestive heart failure and chronic renal insufficiency

Comparison of the pharmacokinetics of fosinoprilat with enalaprilat and lisinopril in patients with congestive heart failure and chronic renal insufficiency

Physiologically based pharmacokinetic modelling of lisinopril in children: A case story of angiotensin converting enzyme inhibitors

ACE Inhibitors

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