Disease relevance of BOPINDOLOL

• The clinical pharmacology of bopindolol, a new long-acting beta-adrenoceptor antagonist, in hypertension [1].
• In limited trials bopindolol has also successfully reduced symptoms in patients with angina pectoris, anxiety and essential tremor [2].
• Bopindolol in chronic stable angina pectoris: duration and extent of antianginal action [3].
• When bopindolol was administered once daily for 5 days there was a slight increase in the maximum reduction of exercise-induced tachycardia during treatment with 1 mg/day but not with 4 mg/day, which produced a near maximum effect [4].
• Bopindolol, which undergoes extensive hepatic metabolism, was found to accumulate in patients with chronic renal failure but the disposition in patients on regular haemodialysis did not differ significantly from patients with normal renal function [5].

Psychiatry related information on BOPINDOLOL

• Bopindolol satisfactorily modifies not only resting but also exercise BP during isometric and isotonic load, thus reducing BP fluctuation during physical activities of the hypertensive patient [6].

High impact information on BOPINDOLOL

• The initial response (mean +/- SE) to bopindolol was a fall in cardiac output (-12% +/- 2%) and heart rate (-11% +/- 2%) [1].
• In plasma, no unchanged drug, only the hydrolysis product of bopindolol (referred to as bopindolol concentration) was detectable or could be measured up to 24 hr [7].
• Simultaneous modeling of bopindolol kinetics and dynamics [7].
• Bopindolol is a nonselective beta-adrenoceptor antagonist [corrected] with partial agonist activity which is used in the treatment of hypertension [2].
• The effect of renal impairment on the pharmacokinetics and metabolism of bopindolol [5].

Chemical compound and disease context of BOPINDOLOL

• In the present study in healthy volunteers bopindolol was about ten times more potent than pindolol in reducing isoprenaline-induced and exercise-induced tachycardia [4].
• With the exception of the lower incidence of bradycardia, bopindolol is indistinguishable from atenolol in terms of side effects pattern and frequency [8].
• Double-blind comparison of once-daily bopindolol, pindolol and atenolol in essential hypertension [9].
• The aim of this study was to assess the effects of long-term (9-month) treatment with isradipine, alone or combined with bopindolol, on blood pressure, left ventricular hypertrophy (LVH), and diastolic function [10].
• Antipyrine clearance was markedly decreased in patients with cirrhosis, but no correlation was found with the pharmacokinetic parameters of hydrolysed bopindolol [11].

Biological context of BOPINDOLOL

• The influence of bopindolol monotherapy on blood pressure and plasma lipid fractions was investigated in 24 hypertensive patients [12].
• The primary action of bopindolol appeared to be to reduce myocardial oxygen consumption (mainly by its negative chronotropic effect) for up to the 24th hour after oral administration [3].
• The effects of bopindolol, a new beta-adrenoceptor blocker, on the exercise tolerance of 12 in-patients, mean age 57 (5 years), with stable angina pectoris and documented coronary artery disease were evaluated [3].
• During bopindolol-treatment both the slope and the height of the platelet aggregation response curve were moderately decreased at rest before exercise and significantly (p less than 0.05) decreased at rest after exercise [13].
• The time to maximum concentration, maximum concentration and AUC of hydrolyzed bopindolol were similar in the patients and controls [11].

Anatomical context of BOPINDOLOL

• Haemodynamic effects of bopindolol and atenolol in coronary artery disease. A noninvasive study [14].
• We conclude that bopindolol protects the myocardium against ischaemia and that the effect lasts for at least 24 h when therapy is given once daily [15].
• The pKi values of bopindolol and its two metabolites for beta 2-adrenoceptors in the bovine mesenteric artery were 7.70 +/- 0.13, 8.07 +/- 0.13, 8.20 +/- 0.24, respectively, with 20-785 showing the highest values among these drugs [16].
• In contrast, the results from pharmacological assessment for antagonistic potencies, using atria and trachea, showed that bopindolol and its two metabolites did not have significant selectivity on beta 1- and beta 2-adrenoceptors [17].
• These findings suggest that bopindolol had a beneficial effect on beta-adrenoceptors in the membranes of cardiac muscles of SHR, implying that these effects may contribute to lowering hypertension [18].

Associations of BOPINDOLOL with other chemical compounds

• The effects of bopindolol or metoprolol on BP and heart rate were similar: return to normal values was achieved in 70% of patients with either drug [6].
• 8. Blood flow in the brown fat was markedly increased by carvedilol and bopindolol, but not by celiprolol and propranolol [19].
• Thirty-five hypertensive patients with LVH and supine diastolic blood pressures (DBPs) greater than or equal to 100 and less than or equal to 120 mm Hg received increasing doses of isradipine (1.25, 2.5, and 5 mg twice daily); if blood pressure was not controlled, bopindolol (0.5-2 mg once daily) was added to the treatment [10].
• The first study described here was carried out to define the role of a genetic determinant (debrisoquine-type oxidation polymorphism) on plasma concentration of bopindolol and its pharmacological effect [20].
• The generation of singlet molecular oxygen ((1)O(2)) and hydroxyl radicals (HO*) during peroxidation of bopindolol in the presence of Co(II) ions was studied using electron spin resonance (ESR) and spectrophotometry methods [21].

Gene context of BOPINDOLOL

• The platelet count, the plasma levels of 6-oxo-PGF1 alpha, beta-thromboglobulin (beta-TG) and platelet factor 4 (PF4) were not affected by bopindolol [13].
• It is suggested that (+/-)- and (-)-pindolol, mepindolol and bopindolol may be slowly dissociating beta 1-adrenoreceptor antagonists [22].
• Bopindolol caused a significant attenuation of the rise in plasma renin activity produced by passive head-up tilting to 75-85 degrees [23].
• After bopindolol withdrawal there was, in contrast, an overshoot of plasma prolactin and a persistent elevation of plasma potassium and adrenaline post-isoprenaline [24].
• Following bopindolol administration GFR, RPF, and filtration fraction remained stable, in spite of a fall of DBP from 80 +/- 7 to 76 +/- 4 and to 72 +/- 9 mm Hg in normotensives (p less than 0.05) and from 106 +/- 11-96 +/- 10 and to 91 +/- 8 mm Hg in hypertensives (p less than 0.05) on D1 and D21, respectively [25].

Analytical, diagnostic and therapeutic context of BOPINDOLOL

• Plasma concentrations determined using a radio-receptor assay (RRA) and high pressure liquid chromatography (h.p.l.c.) yielded almost identical results, indicating that hydrolysed bopindolol, the major metabolite, is responsible for the pharmacological activity of the drug [26].
• This article describes the development of an analytical procedure and presents a reversed-phase HPLC method with coulometric detection suitable for plasma analyses during pharmacokinetic investigations of bopindolol therapy [27].
• Scintigraphic ventriculography combined with an exercise test was carried out at baseline before treatment with bopindolol, and repeated after 7 and 14 days treatment [15].
• Determination of bopindolol in pharmaceuticals by capillary isotachophoresis [28].
• To determine the optimal antihypertensive dose of bopindolol, we performed a randomized double-blind study in parallel groups [29].

References