Disease relevance of Coretal

• The value of low-dose oxprenolol in secondary prevention appears to be confined to patients treated relatively soon after myocardial infarction [1].
• These data show that non-cardioselective agents (propranolol and oxprenolol), cardioselective agents (practolol, metoprolol and tolamolol), as well as drugs with intrinsic sympathomimetic activity (oxprenolol and practolol), were equally effective in the treatment of angina pectoris [2].
• A long-term prevention study with oxprenolol in coronary heart disease [1].
• In 417 patients in whom treatment was started within four months of infarction oxprenolol increased the six-year cumulative survival rate from 77 to 95 per cent (P less than 0.001) [1].
• The tachycardia was abolished by 40 mg of oxprenolol which reduced heart-rates during operations to below those recorded during surgical outpatient clinics [3].

Psychiatry related information on Coretal

• Reaction time of the surgeons was significantly slowed by oxprenolol (P < 0.01) [4].
• Exploratory behavior, which was suppressed by previous exposure to shocks, was not influenced by oxprenolol [5].
• Oxprenolol had no effect on the short term memory test in either high or low anxiety groups in any experimental test situation [6].
• During ambulatory BP monitoring, patients treated with oxprenolol had the lowest level at each level of physical activity and self-reported emotional arousal [7].
• Heart rate reactivity was lowest when patients received oxprenolol, but peripheral resistance during emotional stress was significantly increased [8].

High impact information on Coretal

• In 274 patients with treatment starting between 5 and 12 months of infarction the survival rate was similar in the two groups, but in 412 patients entered between 1 and 7 1/2 years after their first infarction oxprenolol reduced the six-year survival rate from 92 to 79 per cent (P = 0.002) [1].
• Near maximum improvement in exercise tolerance occurred when the acute cumulative oral dose had reached 160 mg for propranolol and oxprenolol, 200 mg for metoprolol and tolamolol and 400 mg for practolol [2].
• Heart-rates of surgeons during operations and other clinical activities and their modification by oxprenolol [3].
• Thrombocytopenia due to slow-release oxprenolol [9].
• Oxprenolol attenuated the renin response in all subjects without completely abolishing it [10].

Chemical compound and disease context of Coretal

• 473 patients with suspected acute myocardial infarction were entered into a randomised, double-blind, placebo-controlled comparison of disopyramide phosphate, 150 mg three times a day, and oxprenolol, 40 mg three times a day [11].
• Propranolol and oxprenolol raised the ventricular fibrillation threshold by 42 and 56%, respectively [12].
• After 6 weeks of treatment with the nonselective beta-adrenergic receptor blocker oxprenolol in 11 subjects with low renin hypertension, blood pressure was reduced and the plasma vasopressin concentration fell from 27.6 +/- 6.4 to 13.5 +/- 4.2 pg/ml (p less than 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)[13]
• The effects of oral oxprenolol (480 mg) and lorazepam (2 mg) on skin conductance, reaction time, critical flicker frequency and self-rating visual analogue scales for anxiety, sedation and concentration were investigated in 6 healthy male volunteers [14].
• The duration of action of pindolol, measured by the reduction in exercise-induced tachycardia, is longer than that of many other beta-adrenoceptor-blocking drugs such as propranolol, alprenolol, and slow-release oxprenolol tested at equipotent beta-adrenoceptor-blocking doses [15].

Biological context of Coretal

• Plasma renin activity and plasma aldosterone, which were suppressed during oxprenolol administration, rose significantly during placebo, coinciding with a significant fall in hematocrit and hemoglobin [16].
• Adrenergic antagonists such as l-propranolol and oxprenolol also displaced [125I]iodoLSD, but did so with IC50 values of 17,800 +/- 5,100 and 23,300 +/- 5,500 nM, respectively [17].
• Both groups were then followed up every two weeks, and increasing doses of hydrochlorothiazide (25 and 50 mg), oxprenolol (160 and 320 mg), and dihydralazine (50 and 100 mg) were added until the diastolic blood pressure was lower than 90 mm Hg [18].
• Stereoselective pharmacokinetics of oxprenolol and its glucuronides in humans [19].
• Oxyprenolol glucuronides in plasma and urine were measured as oxprenolol equivalents after enzymatic hydrolysis [19].

Anatomical context of Coretal

• As in CHO-beta 3 cells, the classical beta 1- and beta 2-antagonists CGP12177, oxprenolol, and pindolol were partial agonists in adipocytes [20].
• This was achieved by determining: 1) the effect of oxprenolol (0.3 mg/kg), a potent beta receptor blocking agent possessing no significant direct membrane effects on the myocardium, on the dose of ouabain necessary to cause VT (i.e., the toxic dose); and 2) whether oxprenolol had antirrhythmic efficacy against preexisting VT [21].
• Our results suggest that enantioselective interactions of the chiral oxprenolol with the chiral lipids of biological membranes can be excluded [22].
• The intrinsic activities of alprenolol, oxprenolol and pindolol (expressed as % of the maximal tissue response to isoprenaline) were significantly higher in the uterus than in the right atrium.(ABSTRACT TRUNCATED AT 250 WORDS)[23]
• 3. Absorption of oxprenolol occurred throughout the GI tract including the colon [24].

Associations of Coretal with other chemical compounds

• Blood pressure fell with both (141.8 +/- 4.8/96.0 +/- 2.3 to 128.0 +/- 5.1/87.2 +/- 1 mm Hg on oxprenolol, p less than 0.01; 150.8 +/- 5.5/98.0 +/- 1.7 to 129.9 +/- 5.5/86.8 +/- 3.4 mm Hg on propranolol, p less than 0.01) [25].
• A dose of atenolol was established on the basis of morning mean systolic blood pressure (mean of 5 readings) in 27 long-standing hypertensive patients previously controlled on one of three nonselective beta-blockers: propranolol, oxprenolol, or pindolol [26].
• The flatter dose-response curve of pindolol for exercise heart rate (EHR) has been reported from practolol and oxprenolol, which also exert partial agonist activity [27].
• Six healthy subjects were given a 0.5 mg subcutaneous dose of terbutaline on two occasions: 1 hour after oral administration of a placebo and 1 hour after 80 mg oxprenolol orally [28].
• With thiazide dosage constant throughout, maximal dose titration to 386. +/- 52.1 (SEM) mg/day of oxprenolol and 360.0 +/- 45.4 mg/day of propranolol was achieved over the first 5 wk [25].

Gene context of Coretal

• In vivo, the administration of oxprenolol, a beta-receptor antagonist, significantly reduced serum IL-10 levels 90 min after LPS challenge [29].
• The beta 1- and beta 2-adrenoceptor stimulatory effects of alprenolol, oxprenolol and pindolol: a study in the isolated right atrium and uterus of the rat [23].
• This inhibition was effectively reversed by the beta 2-antagonist oxprenolol, indicating that the inhibition was mediated through the beta 2-adrenergic receptor [30].
• In vivo treatment of rats with beta-diethylaminoethyl-diphenylpropylacetate hydrochloride (SKF 525A), an inhibitor of hepatic monooxygenases, decreases the serum binding of oxprenolol and propranolol, which bind mainly to alpha 1-acid glycoprotein, but not that of phenytoin, which is bound to albumin [31].
• 1. alpha 1-acid glycoprotein (AAG) concentration and molecular heterogeneity, and oxprenolol protein binding were studied in serum of 15 healthy volunteers, 14 patients with lung carcinoma and 17 patients with liver cirrhosis [32].

Analytical, diagnostic and therapeutic context of Coretal

• Oxprenolol enantiomers in plasma and urine were determined by an enantiospecific HPLC method [19].
• Determination of oxprenolol in plasma by column liquid chromatography [33].
• The systemic availability of oxprenolol after colonic and oral administration has been compared in a crossover study involving six healthy male volunteers [34].
• A new osmotic drug delivery system (Oros) has been evaluated in multiple-dose studies in young healthy volunteers as a sustained-release vehicle for once-daily administration of oxprenolol [35].
• The plasma concentration-time profiles of oxprenolol were determined over 32 h using gas liquid chromatography after the initial dose and following seven doses [36].

References