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British Medical Journal Feb 1977
Topics: Female; Humans; Middle Aged; Oxprenolol
PubMed: 843802
DOI: 10.1136/bmj.1.6060.552 -
British Journal of Clinical Pharmacology May 19811 The effects of oxprenolol 80 mg and propranolol 80 mg on resting forearm blood flow (RFBF) and skin temperature were compared in seven normotensive subjects, for 4 h... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
1 The effects of oxprenolol 80 mg and propranolol 80 mg on resting forearm blood flow (RFBF) and skin temperature were compared in seven normotensive subjects, for 4 h after an oral dose. 2 There was a significant fall of RFBF after propranolol (mean +/- s.e. mean 0.74 +/- 0.24 ml 100 g-1 min-1) compared to a smaller non-significant reduction after oxprenolol (0.35 +/- 0.19 ml 100 g-1 min-1). Propranolol produced a greater fall in heart rate than oxprenolol at all times except at 2.5 h. Three subjects experienced falls in skin temperature of over 4 degrees C with propranolol. There were no comparable falls after oxprenolol. 3 The results suggest that at the same dose oxprenolol has less effect on RFBF and skin temperature than propranolol.
Topics: Adult; Blood Pressure; Forearm; Heart Rate; Humans; Oxprenolol; Propranolol; Regional Blood Flow; Skin Temperature; Time Factors
PubMed: 7272160
DOI: 10.1111/j.1365-2125.1981.tb01154.x -
British Medical Journal (Clinical... Mar 1982
Topics: Adult; Aged; Female; Humans; Intestine, Small; Male; Middle Aged; Oxprenolol; Peritoneum; Peritonitis; Propranolol; Radiography; Sclerosis
PubMed: 6802333
DOI: 10.1136/bmj.284.6319.870 -
British Medical Journal (Clinical... Jun 1983One hundred pregnant women with hypertension (defined as diastolic blood pressure at or above 95 mm Hg) were allocated at random to treatment with methyldopa or... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
One hundred pregnant women with hypertension (defined as diastolic blood pressure at or above 95 mm Hg) were allocated at random to treatment with methyldopa or oxprenolol and were compared with nonhypertensive controls matched according to parity and gestation at delivery. The patients were also stratified into those entering the study early (before 32 weeks' gestation) and those entering late (after 32 weeks' gestation). Although there were no differences in diastolic blood pressure between the hypertensive groups before or during treatment, in the early entry group the systolic blood pressure at entry of those allocated to oxprenolol was significantly higher than that of those receiving methyldopa; this difference remained throughout the treatment period. Also in the early entry group further increments of drug treatment were required to control blood pressure of patients receiving oxprenolol than in those receiving methyldopa. The eventual fetal outcome for all patients treated with methyldopa was the same as that for those treated with oxprenolol; birth weight, placental weight, head circumference, and Apgar score were not significantly different and there were no stillbirths in either group.
Topics: Adult; Birth Weight; Clinical Trials as Topic; Female; Gestational Age; Humans; Hypertension; Methyldopa; Oxprenolol; Pregnancy; Pregnancy Complications, Cardiovascular; Random Allocation
PubMed: 6407638
DOI: 10.1136/bmj.286.6382.1927 -
British Medical Journal Jun 1979Fifty-three pregnant women with moderately severe hypertension were randomly allocated to treatment with methyldopa or oxprenolol. There were no significant differences... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
Fifty-three pregnant women with moderately severe hypertension were randomly allocated to treatment with methyldopa or oxprenolol. There were no significant differences between the groups in age, height, weight, parity, or stage of gestation at the start of treatment. The outcome of pregnancy was better in the group treated with oxprenolol, with greater maternal plasma volume expansion and placental and fetal growth. No intrauterine deaths occurred in either group, and antepartum fetal distress, detected by oxytocin challenge testing, was evident in only one patient, who received methyldopa. This infant, and one other in the methyldopa group, died in the neonatal period. No neonatal deaths occurred in the oxprenolol-treated group. Even in this small number of patients these results were considerably better than those in untreated women with hypertension of similar severity. Apgar scores in both groups were equivalent at birth, while blood sugar concentrations were higher in the oxprenolol group. Oxprenolol appears to be safe and effective in controlling hypertension during pregnancy. There was no evidence of harmful effects on the fetus, and oxprenolol may offer a selective advantage over methyldopa for fetal growth and wellbeing in utero.
Topics: Adult; Birth Weight; Blood Glucose; Creatinine; Female; Humans; Hypertension; Methyldopa; Oxprenolol; Plasma Volume; Pregnancy; Pregnancy Complications, Cardiovascular; Random Allocation; Uric Acid
PubMed: 466138
DOI: 10.1136/bmj.1.6178.1591 -
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 Medical Journal Jun 1980The effect of once-daily atenolol, sustained-release oxprenolol (a new formulation of oxprenolol presented as a compressed tablet in a waxed matrix), and long-acting... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
The effect of once-daily atenolol, sustained-release oxprenolol (a new formulation of oxprenolol presented as a compressed tablet in a waxed matrix), and long-acting propranolol (a new formulation presented as spheriods in a capsule) was studied in a double-blind crossover trial in 23 carefully selected hypertensive outpatients. After a run-in period with matching placebo each patient received atenolol (100 mg/day), sustained-release oxprenolol (160 mg/day), long-acting propranolol (160 mg/day), and placebo according to a randomised sequence. After four weeks' treatment with sustained-release oxprenolol blood pressure in the two to four hours before the next dose was not significantly lower than after placebo. The effectiveness of atenolol and of the new formulation of propranolol in reducing blood pressure was confirmed. These results suggest that the present formulation of sustained-release oxprenolol should be reconsidered.
Topics: Adult; Atenolol; Clinical Trials as Topic; Delayed-Action Preparations; Double-Blind Method; Female; Humans; Hypertension; Male; Middle Aged; Oxprenolol; Propanolamines; Propranolol; Random Allocation
PubMed: 7000243
DOI: 10.1136/bmj.280.6231.1573 -
The Journal of Biological Chemistry Oct 1983To evaluate serotonin receptor kinetics in skeletal muscle, we synthesized and developed 2-[125I]iodolysergic acid diethylamide [( 125I]iodoLSD) as a high affinity, high...
Serotonergic and adrenergic regulation of skeletal muscle metabolism in the rat. II. The use of [125I]iodolysergic acid diethylamide and [125I]iodopindolol as probes of sarcolemmal receptor function and specificity.
To evaluate serotonin receptor kinetics in skeletal muscle, we synthesized and developed 2-[125I]iodolysergic acid diethylamide [( 125I]iodoLSD) as a high affinity, high specific activity probe of serotonergic receptor function. The kinetics of binding of this probe and the profile of agonist and antagonist displacement have been compared to results obtained using [125I] iodopindolol as a probe for beta-adrenergic receptor binding. [125I]IodoLSD was prepared by chloramine-T iodination and purified by high pressure liquid chromatography. Fluorescence, ultraviolet, and nuclear magnetic resonance spectra as well as mass spectroscopy demonstrate that the iodinated compound is 2-iodoLSD. This probe bound in a concentration-dependent fashion to sarcolemma in a manner consistent with existence of a single population of specific receptors having a Kd of 1.46 nM and an abundancy of 47 fmol/mg of protein. Half-maximal binding of the probe occurred within 1.0 min and equilibrium binding was observed at 8.0 min. The apparent t 1/2 for the probe-receptor complex was 40 s; the Kd calculated from kinetic data was 1.69 nM. The IC50 for displacement of iodoLSD was 330 +/- 185 nM for methysergide, 757 +/- 309 nM for cyproheptadine, and 2,570 +/- 1,390 nM for serotonin. 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. Using [125I]iodopindolol as a receptor probe, we found the order of potency for adrenergic antagonists to be l-propranolol greater than oxprenolol much much greater than practolol. Serotonergic antagonists, although effective in displacing [125I]iodopindolol, did so only at very high concentrations. These results are consistent with the existence of separate and discrete D-serotonergic and beta 2-adrenergic receptors in skeletal muscle and the finding that adrenergic agonists and antagonists may interact with low affinities with the serotonergic receptor, but that serotonergic agonists and antagonists interact poorly, if at all, with the beta 2-adrenergic receptor.
Topics: Animals; Binding, Competitive; Chromatography, High Pressure Liquid; Epinephrine; Female; Iodine Radioisotopes; Kinetics; Lysergic Acid Diethylamide; Muscles; Pindolol; Rats; Receptors, Adrenergic, beta; Receptors, Serotonin; Sarcolemma; Serotonin
PubMed: 6313663
DOI: No ID Found -
British Journal of Clinical Pharmacology Jun 19881. alpha 1-acid glycoprotein (AAG) concentration and molecular heterogeneity, and oxprenolol protein binding were studied in serum of 15 healthy volunteers, 14 patients...
Alpha 1-acid glycoprotein concentration and molecular heterogeneity: relationship to oxprenolol binding in serum from healthy volunteers and patients with lung carcinoma or cirrhosis.
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. 2. The AAG serum concentration was increased to 180.7% in patients with lung cancer and decreased to 73.4% in cirrhotic patients as compared with controls (P less than 0.05). 3. The concanavalin A (conA) dependent heterogeneity of serum AAG was very similar in controls and patients with lung cancer: a ratio of 9/9/2 was obtained for the conA nonreactive, the conA weakly reactive and the conA strongly reactive subfraction respectively; in cirrhotic patients, the ratio shifted to 11/7/1. 4. The heterogeneity in electric charge, demonstrated by isoelectric focusing, was similar in the three groups of subjects: 70-80% of the focussed bands were found in the main three bands. 5. The binding of oxprenolol to serum proteins was increased in lung tumour patients and decreased in liver cirrhotic patients as compared with controls (P less than 0.05). There was no change in binding affinity and oxprenolol binding was significantly correlated to total AAG serum concentration and to the concentration of each of the conA dependent subtypes, in controls as well as in both patients groups.
Topics: Adult; Blood Proteins; Concanavalin A; Electrophoresis; Female; Humans; Immunoelectrophoresis; Isoelectric Focusing; Liver Cirrhosis; Lung Neoplasms; Male; Middle Aged; Orosomucoid; Oxprenolol; Protein Binding
PubMed: 3203044
DOI: 10.1111/j.1365-2125.1988.tb05260.x -
The Journal of Biological Chemistry Oct 1983The biochemical mechanisms of serotonergic and adrenergic action on skeletal muscle cyclic nucleotide, glycogen, and amino acid metabolism have been investigated in...
Adrenergic and serotonergic regulation of skeletal muscle metabolism in rat. I. The effects of adrenergic and serotonergic antagonists on the regulation of muscle amino acid release, glycogenolysis, and cyclic nucleotide levels.
The biochemical mechanisms of serotonergic and adrenergic action on skeletal muscle cyclic nucleotide, glycogen, and amino acid metabolism have been investigated in intact rat epitrochlaris skeletal muscle preparations. Endogenous catecholamine levels in these preparations were 28.6 +/- 2.1 pg/mg of muscle. Release of these catecholamines by tyramine produced a 25% inhibition of alanine and glutamine release. Pretreatment of animals in vivo with 6-hydroxydopamine depleted catecholamine content by 85%. On incubation, preparations from these pretreated animals showed no effect of tyramine on amino acid metabolism. Serotonin (10(-5) M) and epinephrine (10(-5) M) inhibited alanine and glutamine release equally in preparations from 6-hydroxydopamine-pretreated as compared to control rats. Adrenergic antagonists such as dl-propranolol (10(-8)-10(-6) M), oxprenolol (10(-8)-10(-6) M), and practolol (10(-6)-10(-4) M) blocked equally the inhibition of alanine and glutamine release, prevented the stimulations of muscle cAMP levels, phosphosphorylase a formation, and the depletion of muscle glycogen produced by either epinephrine or serotonin. In contrast, serotonergic antagonists such as methysergide (10(-8)-10(-6) M) and cyproheptadine (10(-8)-10(-6) M) blocked the inhibition of alanine and glutamine release, the stimulations of muscle cAMP levels and phosphorylase a formation, and the decreased muscle glycogen content effected by serotonin but not by epinephrine. Incubation of muscles with both epinephrine and serotonin together produced additive stimulation of muscle cAMP levels, but not of the inhibition of alanine and glutamine release. These data indicate that the action of these agonists on skeletal muscle protein and amino acid, glycogen, and cyclic nucleotide metabolism proceeds directly via separate and discrete serotonergic and adrenergic receptor-adenylyl cyclase mechanisms in skeletal muscle.
Topics: Alanine; Amino Acids; Animals; Cyclic AMP; Epinephrine; Glutamine; Glycogen; Kinetics; Muscles; Rats; Receptors, Adrenergic; Receptors, Serotonin; Serotonin; Serotonin Antagonists; Sympatholytics
PubMed: 6313662
DOI: No ID Found