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Landiolol is an ultra-short-acting, selective β1-adrenergic receptor blocker that was originally approved in Japan for the treatment of intraoperative tachyarrhythmias. It has gained attention for its use in the management of tachyarrhythmias and perioperative tachycardia, especially atrial fibrillation for both cardiac and non-cardiac surgeries. It can be the ideal agent for heart rate control due to its high β1-selectivity, potent negative chronotropic effect, a limited negative inotropic potential, and an ultrashort elimination half-life (around 4 min); moreover, it may have a potential therapeutic effects for sepsis and pediatric patients. Landiolol seems to be superior to other short-acting and selective beta-blockers such as esmolol. This review aims to provide a comprehensive overview of landiolol, a new ultra-short-acting β1 selective antagonist, including its pharmacology, clinical applications, efficacy, safety profile, and future directions in research and clinical data. [ABSTRACT FROM AUTHOR]

Alarming statistics show that the number of people affected by excessive weight has surpassed 2 billion, representing approximately 30% of the world's population. The aim of this review is to provide a comprehensive overview of one of the most serious public health problems, considering that obesity requires an integrative approach that takes into account its complex etiology, including genetic, environmental, and lifestyle factors. Only an understanding of the connections between the many contributors to obesity and the synergy between treatment interventions can ensure satisfactory outcomes in reducing obesity. Mechanisms such as oxidative stress, chronic inflammation, and dysbiosis play a crucial role in the pathogenesis of obesity and its associated complications. Compounding factors such as the deleterious effects of stress, the novel challenge posed by the obesogenic digital (food) environment, and the stigma associated with obesity should not be overlooked. Preclinical research in animal models has been instrumental in elucidating these mechanisms, and translation into clinical practice has provided promising therapeutic options, including epigenetic approaches, pharmacotherapy, and bariatric surgery. However, more studies are necessary to discover new compounds that target key metabolic pathways, innovative ways to deliver the drugs, the optimal combinations of lifestyle interventions with allopathic treatments, and, last but not least, emerging biological markers for effective monitoring. With each passing day, the obesity crisis tightens its grip, threatening not only individual lives but also burdening healthcare systems and societies at large. It is high time we took action as we confront the urgent imperative to address this escalating global health challenge head-on. [ABSTRACT FROM AUTHOR]

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Acrylamide, a neurotoxic and carcinogenic chemical compound is formed by frying, roasting, grilling or baking carbohydrate-rich foods at temperatures above 120°C. Acrylamide intake is associated with significantly altered levels of total cholesterol, LDL-cholesterol, triglycerides, creatinine, urea and uric acid in the blood. This study investigates the effect of selenium (as sodium selenite and as a dietary supplement - Celnium®) on the evolution of some biochemical parameters, in Wistar rats, which received high doses of acrylamide. The administration of sodium selenite and Celnium® produced an improvement in liver cell integrity (decrease in aspartate aminotransferase (AST) activity and iron blood level), liver activities (decrease in direct bilirubin, total bilirubin, total cholesterol, LDL-cholesterol) and renal function (decrease in creatinine, uric acid and urea levels) in the treated groups as compared to the group which received only acrylamide. [ABSTRACT FROM AUTHOR]

The aim of this experiment was to study the apidiet influence of hepatopathy induced by acrylamide, in rats. The objectives were to assess the following parameters: cholesterol and triglycerides, V-LDL, HDL, in terms of chronic hepatic injury induced by acrylamide, in rats. In order to reduce factors that precipitate the progression of hepatic lesions, we administered apitherapic products. Material and methods: Substances: apitherapic products - Apiregya, ApiImunomod, ApiImunostim get from „Stupina SRL‟ (office and laboratories in the Balanesti parish, Gorj county, Romania, phone 0253.270.221). Animals were manipulated under general anesthesia with Thiopental. The levels of investigated parameters were measured using an automatic analyzer (Aeroset, Abbott) and commercial kits (Abbott, USA). A number of 60 white rats Wistar race was used, divided equally in six lots: the control lot - standard nourishment (lot I), apidiet control lot (lot II), apidiet and royal jelly (RJ) control lot (lot III), acryl amide lot (lot IV), apidiet and acrylamide lot (lot V), acry amide, apidiet, and RJ lot (lot VI). After that, a number of 30 subjects were kept for study and research. Animals were kept in normal conditions for light, with access to water and food. Toxic hepatopathy was experimentally induced by acryl amide administered by intra-gastric gavage (hydrous solution, 50 mg/kg). Results and discussions: Apidiet + RJ administration (lot III) was efficient to keep the level of total cholesterol within normal limits. Apidiet + RJ administration in rats with previous acryl amide intoxication was efficient to hold the level of triglycerides within normal limits. No statistically significant differences between the studied lots were registered. This fact demonstrated the efficacy of apidiet+RJ administration in lot with previous acryl amide intra-gastric gavage, in order to maintain VLDL level. The increase of HDL cholesterol level certified benefic effect of apidiet + RJ nourishment after a previous intoxication with acryl amide. Conclusions: Authors recommend apitherapy with Apiregya, ApiImunostim, and ApiImunomod in hepatic affections due to toxic nutrition, in order to normalize the lipid profile. [ABSTRACT FROM AUTHOR]

Unlabelled: Ochratoxin A (OTA) is a toxic secondary metabolite of fungi belonging to the Aspergillus and Penicillium genera, its presence in human blood being the primary indicator of exposure., Aim: In the present study we determined OTA in 38 blood samples collected from healthy Romanian subjects of both genders., Material and Methods: The OTA was determined through the direct, competitive, solid-phase immunoenzymatic method; the minimum quantification limit for determining OTA in serum samples was 0.0289 ng/mL., Results: The positive sample percentage was 100%. OTA concentrations varied between < 0.04 ng/mL and 1 ng/mL. There were no significant differences between OTA concentrations in men versus women (0.24 +/- 0.20 ng/mL versus 0.17 +/- 0.15 ng/mL, p = 0.3527)., Conclusions: The analyzed blood samples exhibit a very high degree of exposure to OTA, but in only approximately 10% of the subjects exceeded 0.5 ng/mL, considered the threshold for OTA-induced renal pathology.

Unlabelled: Acrylamide (AA), obtained for the first time by Moureu in Germany in 1893, is presently used as polyacrylamide in water treatment and wastewater treatment, paper and pulp processing, mineral processing, crude-oil production processes. Acrylamide is a chemical product formed when frying, roasting, grilling or baking carbohydrate-rich foods at temperatures above 120 degrees C. Acrylamide is thus found in a number of foods, such as bread, crisps, French fries and coffee. Tobacco smoking also generates substantial amounts of acrylamide. Acrylamide administration is associated with significant increase of oxidative stress parameters; acrylamide caused disturbances in the oxidative status and enzyme activities and the effect was pronounced with the high doses., Material and Methods: This study investigates the effect of selenium (as sodium selenite and as a selenium dietary supplements--Celnium) on the oxidative stress in Wistar rats which received high doses of acrylamide., Results: The administration of sodium selenite and selenium dietary supplements (Celnium) significantly increased GSH and GPx levels and decreased MDA compared to group which received only acrylamide., Conclusions: Our results show that sodium selenite and selenium dietary supplements (Celnium) can partially prevent the biochemical changes in the liver of the rats which received high doses of acrylamide.

Food-drug interactions are increasingly recognized as important clinical events which may change significantly the bioavailability of oral administrated drugs. Grapefruit juice (GFJ) demonstrated multiple interactions with drugs leading to loss of the therapeutic effects or increased side-effects. GFJ decreases pre-systemic metabolism through a) competitive or mechanism-based inhibition of gut wall CYP3A4 isoenzymes and b) P-glycoprotein (P-gp), c) multidrug resistance protein-2 (MRP2) or d) organic anion-transporting polypeptide (OATP) inhibition. Although, GFJ presents high amounts of flavonoids (e.g. naringin, naringenin), furanocoumarins (e.g. 6',7'-dihydroxybergamottin, bergamottin) are the main chemicals involved in the pharmacokinetic interactions. As compounds of GFJ show additive or synergistic effects, all the major furanocoumarins are necessary for the maximal inhibitory effect. Also, related citrus fruits (sweeties, pummelo and sour orange) or various plants containing furanocoumarins may present pharmacological interactions, yet to be discovered.

Unlabelled: Since 1989, grapefruit juice is reported to modify, with clinical implications, the pharmacokinetic of a series of drugs such as calcium channel blockers that are dihydropyridine derivates and/or some HMGCoA reductase inhibitors. All these drugs are metabolized to a large extent by the most abundant human isoform of cytochrome P450, CYP3A4. Grapefruit inhibits the cytochrome P450 3A4 enzyme system responsible for the oxidative metabolism of many orally administered drugs. The most important compounds of GFJ considered to be involved in the pharmacokinetic interaction are flavonoids (naringin, naringenin, narirutin, quercetin, kaempferol, hesperidin, neohesperidin, didymin, and poncirin), furanocoumarins (6',7'-dihydroxy-bergamottin, bergamottin, bergamottin-6',7'-epoxide, bergapten, epoxy-bergamottin) and sesquiterpens (noot-katone)., Material and Method: The experimental researches had as object the comparative study of total content of flavonoidic compounds, like naringin in different fruit juices: citric fruit (white, pink and red grapefruit), apples, pears--industrial or laboratory prepared juices (by squeezing). They praised a different content in flavonoidic compounds for citric and for the rest of analyzed fruits., Results: For grapefruit juices the concentrations in flavonoidic compounds are higher in total fruit juice: 143.86 mg/100 mL in red, 131.47 mg/100 mL in pink and 84.21 mg/100 mL in white grapefruit juice. In juice prepared from fruit pulp, the concentrations were 81.92 mg/100 mL, 108.23 mg/100 mL and 65.76 mg/100 mL, respectively. The content in naringin, the most important flavanone in citrus fruit, varied between 1.98 and 51.2 mg/100 mL juice.

In spite of known health benefits of grapefruit juice, its consumption in combination with drugs requires caution. The drugs most susceptible to pharmacokinetic interactions with clinical significance are those with narrow therapeutic index and low bioavailability due to important first-pass metabolism. Most vulnerable populations are elderly, cirrhotics, subjects with genetic polymorphisms and individuals taking other CYP3A4 inhibitors. The major drug classes that have been reported to present interactions with grapefruit juice are antiallergics, antibiotics, antimalaria drugs, anxiolytics, calcium channel blockers, HIV protease inhibitors, HMG-CoA reductase inhibitors; the degree of pharmacokinetic interaction varies among the compounds of the same class.

Unlabelled: A new simple, sensitive and selective liquid chromatography coupled with mass spectrometry (LC/MS) method for quantification of dydrogesterone in human plasma was validated., Material and Method: The analytes was eluted in 1.3 minutes on a reversed phase column (Zorbax SB-C18, 100 mm x 3.0 mm I.D., 3.5 microm) under isocratic conditions using a mobile phase of a 20 : 80 (v/v) mixture of ammonium acetate 1 mM and acetonitrile. The flow rate was 1 mL/min at the column temperature of 35 degrees C. The detection of the analyte was in MS/ MS mode using an atmospheric pressure chemical ionization source (APCI+, m/z 313 > m/z 295). The sample preparation was very simple and rapid and consisted in plasma protein precipitation from 0.2 mL plasma using 0.6 mL methanol., Results: Calibration curves were generated over the range of 5-150 ng/mL with values for coefficient of determination greater than 0.997 and by using a weighted (1/y) linear regression. The values of precision and accuracy were less than 12.5% and 7.5%, respectively, both for within- and between-run analysis. The mean recovery of the analyte was 99.8%. This is the first reported method for analysis dydrogesterone in human plasma that uses protein precipitation as sample processing procedure. The validated LC/MS method could be applied for determination of dydrogesterone in human plasma for therapeutic drug monitoring in gynecological disorders.