Felodipine in hypertension

Mace, P. J. E.; Stallard, T. J.; Littler, W. A.

doi:10.1007/bf00613449

Cited by 27 publications

(6 citation statements)

References 21 publications

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“…The reduction of blood pressure induced by acute administration of felodipine, was associated with an increase in HR and indications of increased activity in the sympathetic and renin-angiotensin systems. This is in analogy with previous reports on felodipine (10,11) as well as nifedipine (3,4). The finding of unchanged P-ALD in spite of increased A11 may be explained by an attenuation of the adrenal aldosterone response to angiotensin I1 as previously shown after nifedipine (12).…”

Section: Discussionsupporting

confidence: 92%

Effects of the Calcium Antagonist Felodipine on the Sympathetic and Renin‐Angiotensin‐Aldosterone Systems in Essential Hypertension

Katzman

Hulthén

Hökfelt

1988

Journal of Internal Medicine

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Studies were performed in 10 male patients with untreated essential hypertension, WHO grade I‐II, aged 25–62 years, to explore the acute (single dose) and long‐term (8 weeks) effects of felodipine on sympathetic activity—evaluated by plasma and urinary catecholamines—as related to blood pressure, heart rate and the activity in the renin‐angiotensin‐aldosterone system. The patients were hospitalized for 8 (acute) and 6 (long‐term) days and were maintained on a standardized daily intake of sodium (150 mmol), potassium (75 mmol) and water (2500 ml). Acute felodipine administration (10 mg) significantly reduced blood pressure and increased heart rate. Plasma and urinary noradrenaline, plasma renin activity and angiotensin II increased, whereas plasma and urinary adrenaline, dopamine, aldosterone and plasma vasopressin were unaltered. Long‐term felodipine treatment, 10 mg twice daily, reduced blood pressure to a similar extent as acute felodipine administration, but heart rate was not significantly changed. Plasma noradrenaline 3 and 12 hours after the last dose and urinary noradrenaline were increased, whereas plasma and urinary adrenaline and dopamine were unchanged. Plasma renin activity and angiotensin II were increased 3 hours, but unchanged 12 hours after the last dose. Plasma aldosterone was unchanged but urinary aldosterone increased. Plasma vasopressin was unchanged. The changes in plasma noradrenaline as related to blood pressure, heart rate, plasma renin activity and angiotensin II during long‐term felodipine treatment may reflect decreased cardiac and renal β‐adrenoceptor‐mediated responses. Increased renal clearance of aldosterone could partly explain the unaltered plasma aldosterone level in spite of increased plasma angiotensin II following long‐term felodipine treatment.

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Section: Discussionsupporting

confidence: 92%

Effects of the Calcium Antagonist Felodipine on the Sympathetic and Renin‐Angiotensin‐Aldosterone Systems in Essential Hypertension

Katzman

Hulthén

Hökfelt

1988

Journal of Internal Medicine

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“…Plasma renin activity generally returned to control values during continued treatment, whereas norepinephrine concentrations often remained elevated during study periods of 1-8 weeks (17,20,48,61,66,79,98). However, it should be noted that, except for one study of 2 weeks of treatment with felodipine extended-release tablets, 10 mg once daily, these were studies of the earlier conventional formulation in relatively high doses of 5 or 5-10 mg twice daily.…”

Section: Hormonal Metabolic and Laboratory Variablesmentioning

confidence: 88%

Tolerability and Safety of Felodipine

Elvelin

Kennerfalk

Elmfeldt

1993

Cardiovascular Drug Reviews

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Felodipine (Plendil@/Flodil@/Modip@, Astra) is a highly vascular selective calcium antagonist of the dihydropyridine type. At present, some 300 clinical studies involving more than 8,000 patients have been carried out with felodipine, the majority with hypertension but a substantial number also with other indications, such as angina pectoris and heart failure.In the early clinical studies, felodipine was given as conventional tablets twice daily. However, since 1986, most studies with felodipine have been performed using the extended-release formulation of the drug, which provides smoother plasma concentrations and 24-h blood pressure control with a once-daily dosage (11,37,38). This is the only formulation currently on the market.In controlled clinical trials, felodipine extended release once daily was found to be an effective antihypertensive treatment and reduced the blood pressure to S 9 0 mm Hg, 24 h after the dose, in 50430% of patients (13,22,41,65,82,106). Treatment with felodipine was reported to be more effective than with nifedipine, enalapril, chlorthalidone, or hydrochlorothiazide, but similarly effective to amlodipine, diltiazem, metoprolol, or aten-0101, at the doses studied (22,41,45,65,67,72,82,106,111). The aim of this article is to provide an overview of the experience with felodipine with regard to tolerability profile, effect on quality of life, safety in patients with diseases commonly occurring together with hypertension, effect on hormonal, metabolic, and laboratory variables, and interactions with food and drugs. PHARMACODYNAMIC AND PHARMACOKINETIC PROPERTIESFelodipine is a highly vascular selective dihydropyridine calcium antagonist. It has been shown to be over 100 times more potent in vascular than in cardiac muscle with a selectivity ratio nearly 10 times higher than that for the dihydropyridines nifedipine and amlodipine (73,87). In clinical studies, felodipine has been found to produce significant

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“…1 -2 Venous plasma concentrations of norepinephrine (NE) increase after short-term administration of the drug, 3 " 5 suggesting sympathetic counterregulation to the blood pressure lowering. However, unchanged venous plasma NE has been reported during short-term treatment in patients already treated with diuretics and /J-blockers.…”

mentioning

confidence: 99%

Acute and chronic calcium antagonist treatment elevates sympathetic activity in primary hypertension.

et al. 1994

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Eleven men with mild to moderate primary hypertension were studied at rest and during mental stress before and during intravenous infusion of the calcium antagonist felodipine. Eight of them were restudied during longterm treatment (extended-release felodipine, 10 mg daily). For comparison, 10 normotensive control subjects were studied with the short-term protocol. Heart rate, cardiac output, central cardiovascular pressures, and forearm blood flow were registered. Arterial and venous sampling was performed. Norepinephrine spillovers to arterial plasma and from the forearm were assessed with the use of radiotracer methodology. In the hypertensive patients, felodipine lowered mean arterial blood pressure acutely by 8% (P<.01). Systemic vascular resistance decreased by 22% (P<.001), cardiac output increased by 20% (P<.01), and norepinephrine spillover to arterial plasma increased by 61% (P<.001). Forearm vascular resistance fell by 30% (P<.001), but norepinephrine overflow from the forearm increased by 115% (i><.001). These forearm responses were not seen in normotensive subjects despite F elodipine is a dihydropyridine-type calcium antagonist with high selectivity for resistance vessels. Acute hemodynamic responses of hypertensive humans to felodipine include dose-dependent reductions of systemic vascular resistance (SVR) and forearm vascular resistance (FVR) and reflexogenic elevations of heart rate and cardiac output.1 -2 Venous plasma concentrations of norepinephrine (NE) increase after short-term administration of the drug, 3 " 5 suggesting sympathetic counterregulation to the blood pressure lowering. However, unchanged venous plasma NE has been reported during short-term treatment in patients already treated with diuretics and /J-blockers.6 During long-term treatment with felodipine the tachycardia disappears, 710 probably because of adaptation of the arterial baroreflex, 11 suggesting that sympathetic nerve activity might return to normal levels. Nonetheless, elevated venous plasma NE levels have been reported also during long-term (2 to 8 weeks) treatment. similar systemic responses to felodipine infusion. After 8 weeks of treatment, mean arterial pressure decreased to 15% below baseline (P<.001), cardiac output returned toward pretreatment levels, and systemic vascular resistance remained low. Forearm blood flow returned toward basal levels, but forearm vascular resistance remained lowered. Total body and forearm norepinephrine spillover values were as elevated as in the acute situation. The hemodynamic "defense reaction" and the sympathoadrenal response to mental stress were essentially unaffected by felodipine. Stress-induced small elevations of neuropeptide Y-like immunoreactivity persisted during felodipine. Thus, the vasodilatation induced by felodipine elicits sympathetic counterregulation, which persists in the long term with respect to peripheral and total sympathetic activities, despite resetting of the baroreflex control of heart rate. vasodilator treatment with a dihydropyridine calci...

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Felodipine in hypertension

Cited by 27 publications

References 21 publications

Effects of the Calcium Antagonist Felodipine on the Sympathetic and Renin‐Angiotensin‐Aldosterone Systems in Essential Hypertension

Effects of the Calcium Antagonist Felodipine on the Sympathetic and Renin‐Angiotensin‐Aldosterone Systems in Essential Hypertension

Tolerability and Safety of Felodipine

Acute and chronic calcium antagonist treatment elevates sympathetic activity in primary hypertension.

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