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Clinical Pharmacology and Therapeutics May 1985Average steady-state propranolol plasma concentration (Css) were calculated from published steady-state propranolol clearance data for dose rates (Ro) of 40, 80, 160,...
Average steady-state propranolol plasma concentration (Css) were calculated from published steady-state propranolol clearance data for dose rates (Ro) of 40, 80, 160, 240, and 320 mg/ day in divided doses every 6 hours. The Css-Ro data for each of four subjects were fit essentially perfectly by the equation: Css = KmRo/ (Vm-Ro). Very similar Vm and Km values were obtained with the Vmi and Kmi values for four parallel Michaelis-Menten pathways of propranolol metabolism. It is shown by use of the mean Vm and Km values that the propranolol input rate profoundly affects its bioavailability, which is expected for a first-pass drug that follows Michaelis-Menten elimination kinetics after oral dosing. This most likely explains the poor bioavailability of propranolol after a sustained-release formulation. The decreased bioavailability of propranolol when the number of subdivisions of the daily dose is increased is also explained.
Topics: Administration, Oral; Biological Availability; Delayed-Action Preparations; Humans; Kinetics; Male; Mathematics; Propranolol
PubMed: 3987171
DOI: 10.1038/clpt.1985.76 -
Psychological Science Jul 2015Research on emotion and decision making has suggested that arousal mediates risky decisions, but several distinct and often confounded processes drive such choices. We... (Randomized Controlled Trial)
Randomized Controlled Trial
Research on emotion and decision making has suggested that arousal mediates risky decisions, but several distinct and often confounded processes drive such choices. We used econometric modeling to separate and quantify the unique contributions of loss aversion, risk attitudes, and choice consistency to risky decision making. We administered the beta-blocker propranolol in a double-blind, placebo-controlled within-subjects study, targeting the neurohormonal basis of physiological arousal. Matching our intervention's pharmacological specificity with a quantitative model delineating decision-making components allowed us to identify the causal relationships between arousal and decision making that do and do not exist. Propranolol selectively reduced loss aversion in a baseline- and dose-dependent manner (i.e., as a function of initial loss aversion and body mass index), and did not affect risk attitudes or choice consistency. These findings provide evidence for a specific, modulatory, and causal relationship between precise components of emotion and risky decision making.
Topics: Adrenergic beta-Antagonists; Adult; Affect; Arousal; Choice Behavior; Decision Making; Double-Blind Method; Female; Humans; Linear Models; Male; Propranolol; Risk-Taking; Young Adult
PubMed: 26063441
DOI: 10.1177/0956797615582026 -
The New England Journal of Medicine May 1977
Topics: Humans; Propranolol; Thyroid Crisis
PubMed: 850526
DOI: 10.1056/NEJM197705122961916 -
European Journal of Pediatrics Nov 2013Propranolol hydrochloride is a nonselective β-blocker that is used for the treatment of hypertension, arrhythmia, and angina pectoris. In Japan, it was recently... (Clinical Trial)
Clinical Trial Comparative Study
UNLABELLED
Propranolol hydrochloride is a nonselective β-blocker that is used for the treatment of hypertension, arrhythmia, and angina pectoris. In Japan, it was recently approved for the treatment of childhood arrhythmia. It has been observed to produce drastic involution of infantile hemangiomas. The aim of this prospective study was to examine propranolol's superiority to classical therapy with pulsed dye laser and/or cryosurgery in treating proliferating infantile hemangiomas. Fifteen patients between the ages of 1 and 4 months with proliferating infantile hemangiomas received grinded propranolol tablets 2 mg/kg per day divided in three doses. Twelve patients with proliferating infantile hemangiomas receiving pulsed dye laser and/or cryosurgery were enrolled as controls. Baseline electrocardiogram, echocardiogram, and chest x-ray were performed. Monitoring of heart rate, blood pressure, and blood glucose was performed every 2 weeks. Efficacy was assessed by performing blinded volume measurements and taking photographs at every visit. Propranolol induced significantly earlier involution and redness reduction of infantile hemangiomas, compared to pulsed dye laser and cryosurgery. Adverse effects such as hypoglycemia, hypotension, or bradycardia did not occur.
CONCLUSION
The dramatic response of infantile hemangiomas to propranolol and few side effects suggest that early treatment of infantile hemangiomas could result in decreased disfigurement. Propranolol should be considered as a first-line treatment of infantile hemangiomas.
Topics: Administration, Oral; Adrenergic beta-Antagonists; Cryosurgery; Drug Administration Schedule; Female; Hemangioma; Humans; Infant; Lasers, Dye; Male; Propranolol; Prospective Studies; Skin Neoplasms; Treatment Outcome
PubMed: 23812512
DOI: 10.1007/s00431-013-2075-7 -
Pharmacological Reports : PR Dec 2015The purpose of the experiment was to assess interactions of dopamine with propranolol as an infiltrative anesthetic.
BACKGROUND
The purpose of the experiment was to assess interactions of dopamine with propranolol as an infiltrative anesthetic.
METHODS
After injecting the rats with four doses of drugs subcutaneously, the cutaneous analgesic effect of propranolol was compared with dopamine through the blockade of cutaneous trunci muscle reflex (CTMR) in response to local skin pinprick. Drug-drug interactions were examined via an isobolographic analysis.
RESULTS
We demonstrated that the action of propranolol and dopamine was dose dependent to skin infiltrative analgesia. On the ED(50) (50% effective dose) basis, the rank of drug potency was propranolol (11.3 [10.6-12.2]μmol) > dopamine (195 [188-205]μmol) (p < 0.001). At the equi-anesthetic doses (ED(25), ED(50), ED(75)), the block duration caused by dopamine was equal to that caused by propranolol. Coadministration of dopamine and propranolol exhibited a synergistic effect on infiltrative cutaneous analgesia.
CONCLUSIONS
The preclinical data showed that dopamine produced a lesser potency but a comparable duration of cutaneous analgesia compared to propranolol. Adding dopamine to propranolol potentiated and prolonged propranolol's cutaneous analgesic effect.
Topics: Analgesia; Anesthesia, Local; Animals; Dopamine; Dose-Response Relationship, Drug; Drug Synergism; Injections, Subcutaneous; Male; Propranolol; Rats; Skin; Time Factors
PubMed: 26481546
DOI: 10.1016/j.pharep.2015.05.016 -
Journal of Chromatography. A Apr 2020In this study a heart-cutting 2D-LC method was successfully developed and optimized in order to discriminate and quantitate (S)-propranolol, (R)-propranolol, and its...
In this study a heart-cutting 2D-LC method was successfully developed and optimized in order to discriminate and quantitate (S)-propranolol, (R)-propranolol, and its hydroxy metabolites, namely the isomeric (S)-4'‑hydroxy propranolol, (R)-4'‑hydroxy propranolol, (S)-5'‑hydroxy propranolol, (R)-5'‑hydroxy propranolol, (S)-7'-hydroxy propranolol, and (R)-7'‑hydroxy propranolol in one chromatographic run. Thereby, experiments investigating chiral discrimination in ring hydroxylation of propranolol were made feasible. Analysis of human urine samples after administration of a single oral dose of 40 mg of propranolol clearly revealed considerable chiral shifts in propranolol and its 4'-, 5'-, and 7'-hydroxy metabolites. Furthermore, the excretion rates of the individual (S)- and (R)-enantiomers were continuously monitored over 24 h post administration. Studies were performed utilizing a 2D-LC system hyphenated to a triple quadrupole mass spectrometer. The chromatographic system was endued with a reversed phase column (phenyl-hexyl) in first dimension and a teicoplanin based chiral column in second dimension. The method was basically validated and successfully evaluated as robust. Calibration was performed achieving accuracy between 80% and 120%. Maximal excretion rates of (S)-propranolol, (R)-propranolol, (S)-4'‑hydroxy propranolol, (R)-4'‑hydroxy propranolol, (S)-5'‑hydroxy propranolol, (R)-5'‑hydroxy propranolol, and (R)-7'‑hydroxy propranolol were 237 ng/min, 281 ng/min, 4 ng/min, 4 ng/min, 1 ng/min, 9 ng/min, and 3 ng/min, respectively.
Topics: Chromatography, Liquid; Humans; Hydroxylation; Mass Spectrometry; Propranolol; Stereoisomerism; Teicoplanin
PubMed: 31911001
DOI: 10.1016/j.chroma.2019.460828 -
Lancet (London, England) May 1977
Topics: Adult; Humans; Hypertension; Male; Penile Induration; Propranolol
PubMed: 68215
DOI: 10.1016/s0140-6736(77)92373-x -
Postgraduate Medical Journal 1976Propranolol is an antihypertensive drug whose mode of action in lowering arterial pressure remains undecided. Animal experiments indicate that an action within the... (Review)
Review
Propranolol is an antihypertensive drug whose mode of action in lowering arterial pressure remains undecided. Animal experiments indicate that an action within the central nervous system (CNS) contributes to the hypotensive effect. Intravenous infusion of propranolol to the conscious rabbit lowers arterial pressure and this is accompanied by a decrease in preganglionic sympathetic nervous activity. This indicates that propranolol decreases sympathetic nervous outflow by a central action and since the dextro isomer of propranolol does not exert such an effect then this action must be related to beta-adrenoceptor blockade.
Topics: Animals; Blood Pressure; Brain Chemistry; Central Nervous System; Humans; Neurons; Propranolol; Rabbits; Sympathetic Nervous System
PubMed: 787951
DOI: No ID Found -
General Hospital Psychiatry 2012Yawning is a frequent behavior with circadian effects. Sometimes, its frequency is very high and it is disturbing. However, there is no evidence-based treatment for...
OBJECTIVE
Yawning is a frequent behavior with circadian effects. Sometimes, its frequency is very high and it is disturbing. However, there is no evidence-based treatment for yawning.
METHOD
This is a case report of a man with severe yawning from about 2 years ago.
RESULTS
Yawning reduced after taking propranolol.
CONCLUSION
Current evidence suggests that propranolol may decrease yawning through its thermoregulation effect. It is worthwhile conducting controlled clinical trials to study whether propranolol is an effective treatment for yawning.
Topics: Humans; Male; Middle Aged; Propranolol; Treatment Outcome; Yawning
PubMed: 22055334
DOI: 10.1016/j.genhosppsych.2011.09.021 -
International Journal of Pharmaceutical... 2012Propranolol hydrochloride is a beta blocker used to treat high blood pressure, abnormal heart rhythms, heart disease, pheochromocytoma, and certain types of tremors....
Propranolol hydrochloride is a beta blocker used to treat high blood pressure, abnormal heart rhythms, heart disease, pheochromocytoma, and certain types of tremors. Propranolol is marketed by Wyeth (now a part of Pfizer) and AstraZeneca under the brand names Inderal, Inderal LA, Avlocardyl, Deralin, Dociton, Inderalici, InnoPran XL, Sumial, Anaprilium, Bedranol SR (Sandoz). It is also available generically from several manufacturers. Propranolol hydrochloride is available as tablet, capsule, and oral liquid dosage forms in several strengths. Some patients are unable to tolerate oral tablets and capsules, challenging compounding pharmacies to seek alternative dosing options; namely oral solutions and suspensions. The objective of this study was to determine the stability of propranolol hydrochloride in SyrSpend SF. The drug was compounded into a 1-mg/mL suspension using SyrSpend SF and subsequently stored in a low-actinic plastic prescription bottle at room temperature conditions. Six samples were assayed at each specific time point extending to 90 days by a stability-indicating high-performance liquid chromatography method. The method was validated for its specificity through forced-degradation studies. Based on the data collected, when protected from light at room temperature, the beyond-use date of propranolol hydrochloride in SyrSpend SF was shown to be at least 90 days.
Topics: Adrenergic beta-Antagonists; Chromatography, High Pressure Liquid; Drug Stability; Propranolol; Suspensions
PubMed: 23259369
DOI: No ID Found