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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
Oxprenolol is extensively metabolised in the liver, direct O-glucuronidation being the major metabolic pathway and oxidative reactions minor ones. Oxprenolol is excreted chiefly in the urine (almost exclusively in the form of inactive metabolites).
Miscellaneous Methods of Analysis
Published in Joseph Chamberlain, The Analysis of Drugs in Biological Fluids, 2018
The method has been particularly useful in drug metabolism studies where it is desirable to obtain quantitative values of a particular labeled species from a mixture of radiolabeled drug and metabolites. The great advantage when the method is used in this way is that the only requirement is a liquid scintillation counter, a supply of authentic, crystalline material, and some skill in recrystallization techniques. Usually, the technique would be applied to estimate the parent drug, but it is equally applicable to radiolabeled metabolites as long as authentic crystalline material is available. The technique can be applied simultaneously to the analysis of several compounds as long as adequate methods are available for separation of the components; however, if the amount of sample to be analyzed is not a problem, then it would appear more sensible to carry out separate experiments for each putative analyte. When used in the multiple mode, HPLC is very useful as the separation method, as typified by the determination in biological fluids of |14C|oxprenolol and nine radiolabeled metabolites.1313 The carriers are ideal internal standards and the method was suitable for determining the disposition and metabolism of oxprenolol in a quantitative manner, which had not been possible by any of the previously published methods.
Application of beta-blockers in burn management
Published in Baylor University Medical Center Proceedings, 2022
Jonathan Kopel, Gregory L. Brower, Grant Sorensen, John Griswold
One of the initial observations by Szabó et al10 evaluated the nonselective beta-blocker oxprenolol (Trasicor) in patients with approximately 20% TBSA burns. The study found that patients treated with oxprenolol lost less weight than the untreated control group (5.4%, n = 8 vs 9.2%, n = 15; respectively).10 Another study by Breitenstein et al11 compared the effect of intravenous vs oral beta-blocker administration on resting metabolic rate. In 10 patients with an average burn of 28% TBSA, the decrease in metabolism relative to the baseline resting metabolic rate produced by intravenous (1.55 kcal/min vs 1.44 kcal/min) and oral (1.45 kcal/min vs 1.36 kcal/min) administration of propranolol was similar. The resting energy expenditure was calculated from VO2, VCO2, and the energy equivalent of VO2, corrected for the nonprotein respiratory quotient. The comparable decreases in lipid oxidation indicate that the route of administration does not affect the efficacy of propranolol-mediated reductions in hypermetabolism (i.e., lipid oxidation) in burn patients.
Treatment for beta-blocker poisoning: a systematic review
Published in Clinical Toxicology, 2020
Joe-Anthony Rotella, Shaun L. Greene, Zeff Koutsogiannis, Andis Graudins, Yit Hung Leang, Kelvin Kuan, Helen Baxter, Elyssia Bourke, Anselm Wong
Nine case reports [77–79,97–102] described improvement in blood pressure but were highly variable with regards to timing and duration of effect in addition to being confounded by multiple treatments being utilised concurrently. Timing of administration in relation to effect was often poorly documented. One case report documented an improvement in haemodynamics (40–60 mmHg mean arterial pressure) 2 h after the commencement of a glucagon infusion in addition to dopamine and isoprenaline following an ingestion of 8 g of oxprenolol, but no response to a total of 30 mg IV glucagon boluses [100]. Another case reported improvement in haemodynamics (systolic BP 70–110 mmHg and heart rate 72–96/min) following two intravenous boluses of glucagon 10 mg after an overdose of propranolol 3 g in a 28-year-old male, who was also on an isoprenaline infusion [103]. Adverse effects reported included nausea and vomiting in two instances [79,98].
Beta-blocker carteolol and oxprenolol produce cutaneous analgesia in response to needle pinpricks in the rat
Published in Neurological Research, 2023
In human studies, topical 1% (0.17 mg/kg) and 2% (0.33 mg/kg) carteolol decreased mean pulse rate [28] and suppressed exercise-induced tachycardia [29], respective. Oral administration of oxprenolol (40 mg; 0.67 mg/kg) showed a significant decrease in blood pressure and heart rate in healthy volunteers [30], while oxprenolol (50 mg/kg) taken orally produced a hypotensive effect in spontaneously hypertensive rats [31]. We showed that subcutaneous carteolol (20 mM; 17.54 mg/kg) and oxprenolol (10 mM; 8.05 mg/kg) completely reduced responsiveness to cutaneous stimuli.