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Profiles of Drug Substances,... 2017Propranolol is a noncardioselective β-blocker. It is reported to have membrane-stabilizing properties, but it does not own intrinsic sympathomimetic activity....
Propranolol is a noncardioselective β-blocker. It is reported to have membrane-stabilizing properties, but it does not own intrinsic sympathomimetic activity. Propranolol hydrochloride is used to control hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy. It is also used to control symptoms of sympathetic overactivity in the management of hyperthyroidism, anxiety disorders, and tremor. Other indications cover the prophylaxis of migraine and of upper gastrointestinal bleeding in patients with portal hypertension. This study provides a detailed, comprehensive profile of propranolol, including formulas, elemental analysis, and the appearance of the drug. In addition, the synthesis of the drug is described. The chapter covers the physicochemical properties, including X-ray powder diffraction, pK, solubility, melting point, and procedures of analysis (spectroscopic, electrochemical, and chromatographic). In-depth pharmacology is also presented (pharmacological actions, therapeutic dosing, uses, Interactions, and adverse effects and precautions). More than 60 references are given as a proof of the abovementioned studies.
Topics: Adrenergic beta-Antagonists; Drug Stability; Humans; Hypertension; Molecular Structure; Propranolol
PubMed: 28431779
DOI: 10.1016/bs.podrm.2017.02.006 -
JAAPA : Official Journal of the... Jun 2019The worldwide incidence of melanoma has risen rapidly in the past 50 years and is a considerable public health burden in the United States, with significant financial... (Review)
Review
The worldwide incidence of melanoma has risen rapidly in the past 50 years and is a considerable public health burden in the United States, with significant financial implications. Studies have demonstrated the potential anticarcinogenic effects of antihypertensive agents, specifically beta-blockers, in patients with prostate cancer, breast cancer, and lately cutaneous malignant melanoma. This article explores the empirical clinical evidence of propranolol's anticarcinogenic effects on melanoma and the chemoprotective mechanisms of beta-blockers and other agents that have been used to modify melanoma progression.
Topics: Adrenergic beta-Antagonists; Disease Progression; Humans; Melanoma; Neoplasm Recurrence, Local; Propranolol; Skin Neoplasms
PubMed: 31136408
DOI: 10.1097/01.JAA.0000558241.84003.91 -
Annals of Surgery Oct 2023Propranolol, a nonselective beta-receptor blocker, improves outcomes of severely burned patients. While the clinical and physiological benefits of beta-blockade are well... (Randomized Controlled Trial)
Randomized Controlled Trial
OBJECTIVE AND BACKGROUND
Propranolol, a nonselective beta-receptor blocker, improves outcomes of severely burned patients. While the clinical and physiological benefits of beta-blockade are well characterized, the underlying metabolic mechanisms are less well defined. We hypothesized that propranolol improves outcomes after burn injury by profoundly modulating metabolic pathways.
METHODS
In this phase II randomized controlled trial, patients with burns ≥20% of total body surface area were randomly assigned to control or propranolol (dose given to decrease heart rate <100 bpm). Outcomes included clinical markers, inflammatory and lipidomic profiles, untargeted metabolomics, and molecular pathways.
RESULTS
Fifty-two severely burned patients were enrolled in this trial (propranolol, n=23 and controls, n=29). There were no significant differences in demographics or injury severity between groups. Metabolomic pathway analyses of the adipose tissue showed that propranolol substantially alters several essential metabolic pathways involved in energy and nucleotide metabolism, as well as catecholamine degradation ( P <0.05). Lipidomic analysis revealed that propranolol-treated patients had lower levels of proinflammatory palmitic acid ( P <0.05) and saturated fatty acids ( P <0.05) with an increased ratio of polyunsaturated fatty acids ( P <0.05), thus shifting the lipidomic profile towards an anti-inflammatory phenotype after burn ( P <0.05). These metabolic effects were mediated by decreased activation of hormone-sensitive lipase at serine 660 ( P <0.05) and significantly reduced endoplasmic reticulum stress by decreasing phospho-JNK ( P <0.05).
CONCLUSION
Propranolol's ability to mitigate pathophysiological changes to essential metabolic pathways results in significantly improved stress responses.
Topics: Humans; Propranolol; Adrenergic beta-Antagonists; Burns; Metabolomics; Adipose Tissue
PubMed: 37389480
DOI: 10.1097/SLA.0000000000005973 -
Postgraduate Medical Journal 1976In the withdrawal phase of chronic alcoholism, hyperkinetic circulation, characterized by increased cardiac output, is the rule. Even in alcoholics who have been sober... (Review)
Review
In the withdrawal phase of chronic alcoholism, hyperkinetic circulation, characterized by increased cardiac output, is the rule. Even in alcoholics who have been sober for a long time, increased cardiac output is very common and these changes are similar to those seen in some patients with labile hypertension. This could be caused by psychic tension. In the withdrawal phase propranolol was found to normalize the circulation and to reverse the decreased peripheral vascular resistance. We observed that the patients seemed to be calm after 40 mg of propranolol by mouth. In a double blind study of propranolol and placebo this effect was confirmed and in another study 120 mg of propranolol a day was compared to 30 mg of diazepam a day (double-blind, crossover). Using different psychological methods all significant differences are in favour of propranolol. The findings are in agreement with other reports. It is our clinical impression that propranolol is a useful drug for psychic tension symptoms in chronic alcoholism. Very few side effects have been found.
Topics: Alcoholism; Cardiac Output; Humans; Propranolol; Stress, Psychological; Substance Withdrawal Syndrome
PubMed: 787956
DOI: No ID Found -
Biomedical Chromatography : BMC Jan 2019Propranolol, a β-adrenergic receptor antagonist, is a chiral compound that is marketed as a racemate, but only the (S)-(-)-enantiomer is responsible for the... (Review)
Review
Propranolol, a β-adrenergic receptor antagonist, is a chiral compound that is marketed as a racemate, but only the (S)-(-)-enantiomer is responsible for the β-adrenoceptor blocking activity. Different chromatographic methods have been applied for separation and determination of enantiomers of (RS)-propranolol. In this article a review is presented on different liquid chromatographic methods used for enantioseparation of (RS)-propranolol, using both HPLC and TLC. In addition, some aspects of enantioseparation under achiral phases of liquid chromatography have been briefly mentioned.
Topics: Chromatography, High Pressure Liquid; Chromatography, Thin Layer; Ketoprofen; Levofloxacin; Propranolol; Stereoisomerism
PubMed: 30121955
DOI: 10.1002/bmc.4370 -
Journal of Clinical Pharmacology 1977
Topics: Adrenergic beta-Antagonists; Cardiac Output; Humans; Hypertension; Propranolol; Renin
PubMed: 13091
DOI: 10.1002/j.1552-4604.1977.tb04594.x -
Pediatric Cardiology Aug 2023
Topics: Humans; Propranolol; Hypoglycemia; Insulin; Blood Glucose
PubMed: 37204487
DOI: 10.1007/s00246-023-03181-2 -
Journal of Psychiatry & Neuroscience :... Jul 2013Considering the pivotal role of negative emotional experiences in the development and persistence of mental disorders, interfering with the consolidation/reconsolidation... (Meta-Analysis)
Meta-Analysis Review
BACKGROUND
Considering the pivotal role of negative emotional experiences in the development and persistence of mental disorders, interfering with the consolidation/reconsolidation of such experiences would open the door to a novel treatment approach in psychiatry. We conducted a meta-analysis on the experimental evidence regarding the capacity of the ß-blocker propranolol to block the consolidation/reconsolidation of emotional memories in healthy adults.
METHODS
Selected studies consisted of randomized, double-blind experiments assessing long-term memory for emotional material in healthy adults and involved at least 1 propranolol and 1 placebo condition. We searched PsycInfo, PubMed, Web of Science, Cochrane Central, PILOTS, Google Scholar and clinicaltrials.org for eligible studies from the period 1995-2012. Ten consolidation (n = 259) and 8 reconsolidation (n = 308) experiments met the inclusion criteria. We calculated effect sizes (Hedges g) using a random effects model.
RESULTS
Compared with placebo, propranolol given before memory consolidation reduced subsequent recall for negatively valenced stories, pictures and word lists (Hedges g = 0.44, 95% confidence interval [CI] 0.14-0.74). Propranolol before reconsolidation also reduced subsequent recall for negatively valenced emotional words and the expression of cue-elicited fear responses (Hedges g = 0.56, 95% CI 0.13-1.00).
LIMITATIONS
Limitations include the moderate number of studies examining the influence of propranolol on emotional memory consolidation and reconsolidation in healthy adults and the fact that most samples consisted entirely of young adults, which may limit the ecological validity of results.
CONCLUSION
Propranolol shows promise in reducing subsequent memory for new or recalled emotional material in healthy adults. However, future studies will need to investigate whether more powerful idiosyncratic emotional memories can also be weakened and whether this weakening can bring about long-lasting symptomatic relief in clinical populations, such as patients with posttraumatic stress or other event-related disorders.
Topics: Adult; Dose-Response Relationship, Drug; Emotions; Female; Humans; Male; Memory, Long-Term; Mental Recall; Middle Aged; Propranolol; Retention, Psychology; Sex Characteristics
PubMed: 23182304
DOI: 10.1503/jpn.120111 -
Postgraduate Medical Journal 1976The pharmacokinetics of propranolol vary according to the route and duration of administration. After i.v. administration, the decline in drug concentrations is biphasic... (Review)
Review
The pharmacokinetics of propranolol vary according to the route and duration of administration. After i.v. administration, the decline in drug concentrations is biphasic and the drug is cleared very efficiently by the liver, so that its elimination is dependent largely on liver blood flow. Although the drug is some 90-95% bound to plasma, hepatic removal is so avid that both bound and free forms are extracted. Consequently, hepatic elimination is unaffected by drug binding in blood, In contrast, the distribution of drug into the tissues is reduced by plasma binding, so that drug half-life (T 1/2), which varies from 11/2-3 hours among individuals is more prolonged in people with relatively low plasma binding. Recent evidence shows that at all times after i.v. administration the beta-blocking effects of propranolol are related to its plasma concentrations according to the receptor theory. In addition individual differences in the response due to a given total concentration are largely due to variations in plasma binding, the drug's effects being a function of free (unbound) drug in plasma water. After the administration of single oral doses, hepatic extraction remains high and much of the dose is eliminated from hepatic portal blood during transfer from the gut, so that little drug reaches the systemic circulation. In addition, significant amounts of an active metabolite, 4-OH propranolol, are produced so that 2 hours after dosing, propranolol appears more potent that its plasma levels would suggest. With continued administration, the avid removal process becomes saturated, extraction ratio falls and propranolol accumulates some 2-fold. Drug T 1/2 is prolonged to 3-6 hours under these conditions, the ratio of propranolol to its active metabolite increases so that most of its effects can be attributed to the parent drug. Perhaps the most important kinetic fact to emerge is the 20-fold variation in plasma levels found after chronic administration of the same oral dose to different patients. This accounts for most of the individual variation in dosage requirements. Concerning propranolol withdrawal, there is no evidence that the effects of the drug last longer than appropriate for its T 1/2, so that larger doses last longer. Nonetheless, 24-48 hours is more that sufficient for the effects of the drug to dissipate. In view of the rebound angina, arrhythmias and infarction that may occur, abrupt withdrawal should be avoided if possible.
Topics: Biological Availability; Dose-Response Relationship, Drug; Half-Life; Humans; Kinetics; Liver; Propranolol
PubMed: 787953
DOI: No ID Found -
Lancet (London, England) Apr 1967
Topics: Humans; Propranolol
PubMed: 4164409
DOI: No ID Found