Effects of tibalosine, a new α-adrenoceptor antagonist, in essential hypertension
| Autor: | Paul Lijnen, Jan A. Staessen, R Grauwels, Robert Fagard, Antoon Amery, L J Verschueren |
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| Rok vydání: | 1983 |
| Předmět: |
Adult
Blood Glucose Male medicine.medical_specialty Metabolic Clearance Rate Posture Renal function Hematocrit Essential hypertension Plasma renin activity Propanolamines chemistry.chemical_compound Double-Blind Method Internal medicine Renin Renin–angiotensin system Humans Medicine Pharmacology (medical) Adrenergic alpha-Antagonists Pharmacology Clinical Trials as Topic Aldosterone medicine.diagnostic_test business.industry Angiotensin II Sodium Hemodynamics Blood Pressure Determination Middle Aged medicine.disease Blood pressure Endocrinology chemistry Creatinine Hypertension Female Angiotensin I business |
| Zdroj: | Clinical Pharmacology and Therapeutics. 33:556-564 |
| ISSN: | 1532-6535 0009-9236 |
| DOI: | 10.1038/clpt.1983.76 |
| Popis: | Tibalosine is a phenylethylamine derivative known to lower arterial pressure in hypertensive animal models. In a double-blind cross-over study, 12 patients with essential hypertension, on a constant sodium intake, received placebo and tibalosine, 150 mg daily. Standing (-5.5/-6.0 mm Hg) and supine (-8.5/-7.5 mm Hg) blood pressure and standing (-7.0 bmp) and supine (-7.5 bpm) pulse rate were reduced by tibalosine. Plasma renin activity (-0.41 ng/ml/hr) and plasma angiotensin 1 (-47 pg/ml) and angiotensin II (-3.0 pg/ml) levels decreased. There were no significant changes observed in plasma aldosterone or in the urinary excretion of aldosterone, kallikrein, or prostaglandin E2, F2 alpha, and F alpha metabolites. During tibalosine treatment, creatinine clearance decreased by 20 ml/min and serum creatinine rose by 0.04 mg/100 ml. The increase in serum sodium by 0.05 mmol/l was not accompanied by significant changes in body weight. There were small, but significant reductions in hemoglobin (-0.4 gm/100 ml), hematocrit (-1.5%), and erythrocyte count (-0.15 X 10(6) cells/mm3) during tibalosine intake, while blood glucose rose by 4.0 mg/100 ml. Apart from a slight tranquilizing effect in two anxious patients, no obvious sedation was observed. Subjective complaints were as frequent during placebo as during active treatment periods. |
| Databáze: | OpenAIRE |
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