β-Adrenergic Receptors and Reflex Tachycardia After Single and Repeated Felodipine Administration in Essential Hypertension

Savonitto, Stefano; Bevilacqua, Maurizio; Chebat, Enrica; Vago, Tarcisio; Bertora, Pierluigi; Baldi, Gabriella; Renesto, E.; Peruzzi, Elena; Sardina, Marco; Norbiato, Guido

doi:10.1097/00005344-199106000-00017

Cited by 9 publications

(1 citation statement)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…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: 99%

Tolerability and Safety of Felodipine

Elvelin

Kennerfalk

Elmfeldt

1993

Cardiovascular Drug Reviews

View full text Add to dashboard Cite

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

show abstract

Section: Hormonal Metabolic and Laboratory Variablesmentioning

confidence: 99%

Tolerability and Safety of Felodipine

Elvelin

Kennerfalk

Elmfeldt

1993

Cardiovascular Drug Reviews

View full text Add to dashboard Cite

show abstract

Efficacy and Safety of Calcium Antagonists as Antianginal Agents

Opie¹

1994

Developments in Cardiovascular Medicine

View full text Add to dashboard Cite

Effect of antihypertensive treatment on the increased β-adrenoceptor density in patients with essential hypertension

Bono

Cases

Calls

et al. 1995

American Journal of Hypertension

View full text Add to dashboard Cite

The effect of different antihypertensive drugs on the increased surface beta 2-adrenoceptor density in essential hypertension was evaluated to elucidate whether the possible effect of the treatment on these receptors was secondary to blood pressure decreases or a specific effect of the drugs. Thirty-nine untreated essential hypertensive patients and 28 normotensive control subjects were studied in basal conditions. Hypertensive patients were randomly assigned to three treatment groups: bisoprolol (10 mg/day, n = 15), enalapril (20 mg/day, n = 12), and verapamil SR (240 mg/day, n = 12), and were studied before and after 1 month of treatment. Plasma catecholamines were determined by a radioenzymatic assay. Surface beta 2-adrenoceptors were measured in intact lymphocytes by radioligand binding assay using the hydrophilic ligand [3H]-CGP12177. beta 2-adrenoceptor density was increased in hypertensive patients (P < .01). After treatment, mean blood pressure decreased similarly in the three groups, while plasma catecholamines showed no significant changes in any group. beta 2-adrenoceptor number decreased only in bisoprolol-treated patients (P < .05). Mean blood pressure decreases correlated with beta 2-adrenoceptor decrements only in bisoprolol-treated patients (r = 0.65, P < .05). beta 2-adrenoceptor density correlated with plasma epinephrine levels in the control group (r = -0.50, P < .01), but not in hypertensive patients before treatment. This correlation was also observed in hypertensive patients treated with bisoprolol (r = -0.52, P < .05), but not in those treated with verapamil or enalapril. Our results suggest that bisoprolol treatment reduces the increased surface beta 2-adrenoceptor density and restores its regulation by epinephrine in essential hypertension.(ABSTRACT TRUNCATED AT 250 WORDS)

show abstract

β-Adrenergic Receptors and Reflex Tachycardia After Single and Repeated Felodipine Administration in Essential Hypertension

Cited by 9 publications

References 0 publications

Tolerability and Safety of Felodipine

Tolerability and Safety of Felodipine

Efficacy and Safety of Calcium Antagonists as Antianginal Agents

Effect of antihypertensive treatment on the increased β-adrenoceptor density in patients with essential hypertension

Contact Info

Product

Resources

About