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British Medical Journal (Clinical... Oct 1985
Topics: Female; Humans; Hypertension; Oxprenolol; Pregnancy; Pregnancy Complications, Cardiovascular
PubMed: 3931826
DOI: 10.1136/bmj.291.6502.1129 -
British Journal of Clinical Pharmacology Oct 1985Single doses of bucindolol 50, 100 and 200 mg were compared to placebo and single doses of oxprenolol 40, 80 and 160 mg in seven patients with mild hypertension, in a... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
Single doses of bucindolol 50, 100 and 200 mg were compared to placebo and single doses of oxprenolol 40, 80 and 160 mg in seven patients with mild hypertension, in a double-blind randomized study. Both bucindolol and oxprenolol inhibited exercise induced tachycardia. The mean maximum inhibition of exercise heart rate was similar after each dose of both drugs (20%, P less than 0.001). Bucindolol produced a significantly greater reduction in blood pressure than either oxprenolol or placebo. This was most apparent in standing systolic and diastolic and post-exercise systolic blood pressures between 1 and 2 h after dosing and was dose-related. All seven patients experienced adverse effects related to hypotension within the first 2 h after ingestion of bucindolol 200 mg. Plasma concentrations of oxprenolol, bucindolol or 5-hydroxy-bucindolol, sampled 2 h after dosing, could not be related to either the changes in blood pressure or to the occurrence of symptoms. The results emphasise the need for careful dose-finding of new drugs prior to their more widespread evaluation in phase 3 studies.
Topics: Adrenergic beta-Antagonists; Adult; Blood Pressure; Exercise Test; Female; Heart Rate; Humans; Hypertension; Male; Middle Aged; Oxprenolol; Posture; Propanolamines; Time Factors
PubMed: 2866786
DOI: 10.1111/j.1365-2125.1985.tb05083.x -
British Journal of Clinical Pharmacology Oct 1985Six elderly patients with established hypertension and six young healthy subjects were studied after 8 days of treatment with atenolol 50 mg day-1, metoprolol 50 mg... (Comparative Study)
Comparative Study
Six elderly patients with established hypertension and six young healthy subjects were studied after 8 days of treatment with atenolol 50 mg day-1, metoprolol 50 mg day-1, oxprenolol 80 mg day-1 and propranolol 80 mg day-1. The area under the blood concentration-time curve was increased in the elderly group for each drug, but the difference was statistically significant only for atenolol. The lower serum albumin concentrations in the elderly group did not result in a decrease in the percentage of propranolol or oxprenolol bound to serum proteins.
Topics: Adrenergic beta-Antagonists; Adult; Age Factors; Aged; Atenolol; Blood Proteins; Female; Half-Life; Humans; Hypertension; Kinetics; Male; Metoprolol; Oxprenolol; Propranolol; Protein Binding
PubMed: 2866783
DOI: 10.1111/j.1365-2125.1985.tb05072.x -
British Medical Journal (Clinical... Aug 1985One hundred and eighty three hypertensive pregnant women were randomly assigned to antihypertensive treatment with oxprenolol (96 women) or methyldopa (87 women).... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
One hundred and eighty three hypertensive pregnant women were randomly assigned to antihypertensive treatment with oxprenolol (96 women) or methyldopa (87 women). Control of hypertension was equivalent in both treatment groups, and in 64 (35%) cases hydralazine had to be added to the treatment to achieve the therapeutic goal (diastolic blood pressure below 85 mm Hg). Five perinatal deaths occurred, one in the oxprenolol group and four in the methyldopa group. Detailed analysis confirmed a previous report of greater fetal growth in the group treated with oxprenolol; this trend was present regardless of severity of hypertension and parity. With increasing duration of treatment the differences between the two groups diminished, and there was no difference after 10 weeks of treatment, a finding that may explain some of the reported discrepancies among therapeutic studies. As hypertension in pregnancy may pursue an accelerated course, necessitating urgent delivery, and there is no satisfactory method of predicting the duration of treatment in individual patients fetal benefit is most likely to be achieved by treatment with oxprenolol, provided that there is no maternal contraindication to treatment with beta blockers.
Topics: Adult; Birth Weight; Clinical Trials as Topic; Female; Humans; Hydralazine; Hypertension; Infant, Newborn; Male; Methyldopa; Oxprenolol; Pregnancy; Pregnancy Complications, Cardiovascular; Random Allocation
PubMed: 3929874
DOI: 10.1136/bmj.291.6495.563 -
British Journal of Clinical Pharmacology Feb 1985A series of visual analogue scales (VAS) was used to examine the prevalence of side-effects among hypertensive patients taking beta-adrenoceptor blocking drugs. When... (Comparative Study)
Comparative Study
A series of visual analogue scales (VAS) was used to examine the prevalence of side-effects among hypertensive patients taking beta-adrenoceptor blocking drugs. When compared to untreated non-hypertensive control subjects, patients taking beta-adrenoceptor blockers had a greater prevalence of tired legs (P less than 0.001), cold digits (P less than 0.01), insomnia (P less than 0.01) and loss of overall wellbeing (P less than 0.01). Side-effects did not differ significantly between patients taking atenolol (n = 30), oxprenolol (n = 16), propranolol (n = 15) or metoprolol (n = 10). If there is an important difference in the prevalence of side-effects between different beta-adrenoceptor blockers, a much larger study will be needed to demonstrate it.
Topics: Adrenergic beta-Antagonists; Atenolol; Humans; Metoprolol; Oxprenolol; Propranolol; Surveys and Questionnaires
PubMed: 2859044
DOI: 10.1111/j.1365-2125.1985.tb02639.x -
British Journal of Clinical Pharmacology 1985The performance of oxprenolol and metoprolol Oros systems has been evaluated in the dog. One study compared in vivo and in vitro release from both systems over 2-14 h.... (Comparative Study)
Comparative Study
Evaluation of oxprenolol and metoprolol Oros systems in the dog: comparison of in vivo and in vitro drug release, and of drug absorption from duodenal and colonic infusion sites.
The performance of oxprenolol and metoprolol Oros systems has been evaluated in the dog. One study compared in vivo and in vitro release from both systems over 2-14 h. The other compared the systemic availabilities of both drugs after 3 h infusion at a constant rate into the cephalic and hepatic portal veins, and into the lumen of the duodenum and colon. In the in vivo release studies, Oros systems were recovered throughout the gut from the stomach to the colon. The amounts of drug remaining in the systems corresponded closely to those measured in a parallel in vitro release experiment. In vitro testing is thus a reliable indicator of in vivo system performance. In the absorption studies, both metoprolol and oxprenolol were shown to be subject to substantial first-pass metabolism. Additionally, for metoprolol the data indicated a significant loss during transport from the gut lumen into the portal circulation. For both drugs the availability from the colon was equal to that from the duodenum. These results provide some justification for the development of oral dosage forms with extended durations of release even for drugs which undergo significant first-pass metabolism.
Topics: Animals; Colon; Delayed-Action Preparations; Dogs; Duodenum; Female; Intestinal Absorption; Kinetics; Male; Metoprolol; Oxprenolol
PubMed: 4005134
DOI: 10.1111/j.1365-2125.1985.tb02748.x -
British Journal of Clinical Pharmacology 1985The essential features and mode of action of oral osmotic drug delivery systems (Oros) for metoprolol fumarate and oxprenolol succinate are described. Critical aspects...
The essential features and mode of action of oral osmotic drug delivery systems (Oros) for metoprolol fumarate and oxprenolol succinate are described. Critical aspects in the development of systems for once-daily administration of both drugs are discussed, and methods for evaluating in vitro release characteristics are presented. In vitro testing confirmed that drug delivery corresponded closely to the theoretical release behaviour predicted from the physicochemical and membrane permeability characteristics for both oxprenolol and metoprolol systems. In vitro release rates were also shown to be unaffected by pH, in vitro test procedures, dissolution media and long-term storage at different temperatures.
Topics: Delayed-Action Preparations; Drug Compounding; Drug Stability; Humans; Hydrogen-Ion Concentration; Kinetics; Metoprolol; Models, Theoretical; Osmosis; Oxprenolol; Solubility
PubMed: 4005132
DOI: 10.1111/j.1365-2125.1985.tb02745.x -
British Journal of Clinical Pharmacology 1985
Topics: Animals; Delayed-Action Preparations; Humans; Metoprolol; Oxprenolol
PubMed: 4005131
DOI: No ID Found -
British Journal of Clinical Pharmacology 1985Nineteen patients receiving oxprenolol slow-release (SR) 160 mg (three patients) or 320 mg (16 patients) once daily for mild to moderate hypertension were treated with...
Nineteen patients receiving oxprenolol slow-release (SR) 160 mg (three patients) or 320 mg (16 patients) once daily for mild to moderate hypertension were treated with oxprenolol Oros 16/260 once daily for 3 weeks following a 2 week placebo wash-out period. Repeated dosing with both Oros and SR oxprenolol preparations, in comparison with placebo, significantly reduced supine systolic and diastolic blood pressures, and pulse rate at 24 h after dosing. Single Oros doses also significantly reduced pulse rate and diastolic, but not systolic, blood pressure at 24 h. The reduction in supine systolic blood pressure was greater during repeated dosing with oxprenolol SR than after a single dose of the Oros preparation. Control of supine diastolic blood pressure (less than or equal to 90 mm Hg) at 24 h after dosing was achieved in 13 out of 18 patients with oxprenolol SR (two out of three patients given 160 mg, and 11 out of 15 given 320 mg). Similar control was achieved in 11 out of 18 patients after a single dose of oxprenolol Oros, and in 13 out of 17 patients treated for 3 weeks. The mean percentage reduction in exercise heart rate (EHR) compared to placebo, at 24 h after dosing, was 16% following Oros treatment for 3 weeks, and 12% following SR administration. After a single dose of oxprenolol Oros EHR, was reduced by 9% at 24 h compared to placebo. At 3 weeks the Oros formulation was significantly better than the SR tablet at reducing EHR. Oxprenolol Oros 16/260 was effective over 24 h and well tolerated.(ABSTRACT TRUNCATED AT 250 WORDS)
Topics: Adult; Aged; Blood Pressure; Delayed-Action Preparations; Female; Heart Rate; Humans; Hypertension; Male; Middle Aged; Oxprenolol; Physical Exertion
PubMed: 4005124
DOI: 10.1111/j.1365-2125.1985.tb02764.x -
British Journal of Clinical Pharmacology 1985Transit times for oxprenolol and metoprolol Oros drug delivery systems through the gastrointestinal tract have been measured in 35 individuals in six separate studies. A...
Transit times for oxprenolol and metoprolol Oros drug delivery systems through the gastrointestinal tract have been measured in 35 individuals in six separate studies. A total of 45 systems were recovered in a median time of 27.4 h; individual transit times varied from 5.1 to 58.3 h. The residual amount of drug in recovered systems was inversely related to transit time and corresponded closely with the amount estimated from in vitro dissolution profiles.
Topics: Delayed-Action Preparations; Digestive System; Humans; Metoprolol; Oxprenolol
PubMed: 4005123
DOI: 10.1111/j.1365-2125.1985.tb02763.x