Effects of Single and Repeated Doses of the Calcium Antagonist Felodipine on Blood Pressure, Renal Function, Electrolytes and Water Balance, and Renin-Angiotensin-Aldosterone System in Hypertensive Patients

Leonetti, Gastone; Gradnik, R.; Terzoli, L.; Fruscio, M.; Rupoli, L.; Cuspidi, Cesare; Sampieri, Lorena; Zanchetti, Alberto

doi:10.1097/00005344-198611000-00022

Cited by 46 publications

(15 citation statements)

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“…Renal hemodynamic findings after acute felodipine administration are indicative of a direct renal vasodilator action of felodipine. Our results on renal blood flow agree with the reports published by Anderson et al [24,25], Hulthen et al [8] and Leonetti et al [7], The 99mTc-MAG-! clearance value, estimated using Schlegel's [ 15] method for gamma camera, did not differ significant ly acutely and during long-term administration of the drug.…”

Section: Discussionsupporting

confidence: 93%

“…It has also a wide spectrum of effects on the kidney [6]. It has been reported that felodipine reduces the increased renal vascular resistance in hypertensive rats and in patients with hypertension both after acute and chronic treatment [7,8], A decrease in renal vascular resistance, although dependent on the de crease in mean arterial pressure, may be associated with an increase in renal blood flow [9]. The diuretic and natri uretic effects of felodipine were reported to be due to the direct inhibitory effects of compounds on net renal tubu lar water and sodium reabsorption [10][11][12].…”

Section: Introductionmentioning

confidence: 99%

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Scintigraphic Evaluation of the Short- and Long-Term Renal Effects of Oral Felodipine Using Technetium-99m-Mercaptoacetyl Triglycine

Özdemir¹,

Erbaş

Uğur

et al. 1993

Am J Nephrol

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The short- and long-term effect of felodipine on renal perfusion and tubular function was investigated using a new renal tubular imaging agent, ^99mTc-mercaptoacetyl triglycine (^99mTc-MAG3). Twelve patients with essential hypertension (mean age = 49 + 8 years) were studied. Renal scintigraphies with 180 MBq ^99mTc-MAG3 were performed at baseline, at the 2nd hour following oral administration of 5 mg felodipine and 4 weeks later on 5-10 mg daily felodipine therapy. The time-activity curves of each kidney were obtained following background subtraction. The ^99mTc-MAG3 clearance value was measured for each kidney. In addition, perfusion index (PI), reno index, time to maximum, half-maximum and two thirds of maximum activity values of each kidney were calculated. Systolic and diastolic blood pressures were significantly lowered with long-term administration of felodipine (from 159 ± 12/105 ± 5 to 141 ± 11/87 ± 7 mm Hg, p = 0.01 and p = 0.002, respectively). Heart rate did not change significantly. Initially, a decrease in PI indicating an increase in renal blood flow (from 246 ± 96 to 194 ± 54, p= 0.01) was observed, whereas no change was noted during the chronic administration (to 230 ± 69, p = NS). Total clearance of ^99mTc-MAG3 was decreased nonsignificantly following the initial dose of felodipine (from 361 ± 93 to 351 ± 91 ml/ min, p = NS). During long-term therapy, felodipine did not alter the perfusion and tubular function of the kidneys. Our results indicated that felodipine causes a significant increase in renal blood flow initially, even with a nonsignificant change in systemic blood pressure.

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Section: Discussionsupporting

confidence: 93%

Section: Introductionmentioning

confidence: 99%

Scintigraphic Evaluation of the Short- and Long-Term Renal Effects of Oral Felodipine Using Technetium-99m-Mercaptoacetyl Triglycine

Özdemir¹,

Erbaş

Uğur

et al. 1993

Am J Nephrol

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“…The reduction of blood flow to these two beds that occurs when cardiac output is decreased is aimed at preserving flow to vital organs (heart, brainl and, although it is not directly responsible for the symptoms, it can have important effects on the metabolic processes and the water-salt balance. Notwithstanding a failure to increase renal blood flow, we observed a mild natriuretic effect after felodipine, which is in keeping with other studies [23,24,26,27]. This result has been explained by a direct ~ effect of felodipine on tubular sodium reabsorption or by an interference with renin secretion.…”

Section: Discussionsupporting

confidence: 92%

Felodipine in severe chronic congestive heart failure: Acute effects on central hemodynamics and regional blood flow distribution

Binetti

Rubino

Varani

et al. 1989

Cardiovasc Drug Ther

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In order to assess the effect of felodipine, a new calcium antagonist with vascular selectivity, on regional blood flow distribution at rest in chronic congestive heart failure, ten patients were studied during an acute test. Right heart catheterization allowed the evaluation of hemodynamic parameters; renal blood flow was calculated using paraamino-hippuric acid clearance; hepatic blood flow measurement was based on indocyanine green clearance; and limb blood flow was assessed with venous occlusion plethysmography. Blood samples were collected for the analysis of plasma catecholamines, renin, and aldosterone. All parameters were recorded in duplicate under basal conditions and after felodipine infusion. The infusion of felodipine induced a significant increase in cardiac index, stroke work index, and limb blood flow. Systemic and pulmonary arterial blood pressure, pulmonary wedge pressure, and systemic resistance underwent a significant decrease. The heart rate, pulmonary resistance, renal blood flow, and hepatic blood flow were not changed. In conclusion, felodipine was of benefit in congestive heart failure at rest in an acute test, acting through a marked decrease in vascular resistance and a consequent improvement in cardiac output and limb blood flow. No changes in renal and hepatic blood flow were observed.

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“…Its ability to decrease vascular resistance has been demonstrated in hypertensive patients (Leonetti et al, 1986;Hedner et al, 1986), as well as in patients with congestive heart failure (Kassis et al, 1987;Dunselman et al, 1987). The absorption and disposition kinetics of felodipine have been described in young healthy subjects (Edgar et al, 1985(Edgar et al, , 1987a, in hypertensive patients of middle age (Edgar et al, 1987b) and in elderly hypertensive patients (Landahl et al, 1988).…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of felodipine after intravenous and chronic oral administration in patients with congestive heart failure.

Dunselman

Edgar

Scaf

et al. 1989

Brit J Clinical Pharma

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1 In a randomized, parallel, double-blind study felodipine was administered to 11 and placebo to 12 patients with congestive heart failure. The kinetics of felodipine were studied after acute intravenous administration and after chronic oral treatment for 8 weeks. The relationship between cardiac output and pharmacokinetics was analyzed. The pharmacokinetic data were compared with data from young healthy individuals and hypertensive patients.2 After oral therapy, significant correlations were found between cardiac output and AUC and systemic bioavailability (F). Furthermore, cardiac output before therapy was also significantly correlated with absorption characteristics. No relationship could be demonstrated between cardiac output and i.v. pharmacokinetics. A comparison of patients with heart failure and young healthy individuals revealed that the AUC was three times higher in heart failure patients, while V55 and the ratio of the AUC of the pyridine metabolite to that of felodipine were similar. Oral clearance was reduced by 50% and the terminal half-life was concomitantly increased. Pharmacokinetic data for felodipine are similar in patients with heart failure to published data from elderly hypertensive patients. 3 An increase in liver blood flow during chronic oral therapy, induced by felodipine itself, appears to explain an increase in bioavailability and thus to higher plasma drug concentrations. Thus, it is advisable to start felodipine treatment at a low dosage in patients with congestive heart failure.

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Effects of Single and Repeated Doses of the Calcium Antagonist Felodipine on Blood Pressure, Renal Function, Electrolytes and Water Balance, and Renin-Angiotensin-Aldosterone System in Hypertensive Patients

Cited by 46 publications

References 0 publications

Scintigraphic Evaluation of the Short- and Long-Term Renal Effects of Oral Felodipine Using Technetium-99m-Mercaptoacetyl Triglycine

Scintigraphic Evaluation of the Short- and Long-Term Renal Effects of Oral Felodipine Using Technetium-99m-Mercaptoacetyl Triglycine

Felodipine in severe chronic congestive heart failure: Acute effects on central hemodynamics and regional blood flow distribution

Pharmacokinetics of felodipine after intravenous and chronic oral administration in patients with congestive heart failure.

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