• Jantzen Dunlap opublikował 1 rok, 3 miesiące temu

    tion). Conclusion This study showed that pharmacist intervention had a considerable positive impact on the cardiologist prescribing pattern of the essential discharge medications for patients with ACS which could improve patient clinical outcomes. © 2020 Published by Elsevier B.V. on behalf of King Saud University.Multidrug resistance (MDR) is the most common problem of inadequate therapeutic response in tumor cells. Many trials has been developed to overcome drug efflux by P-glycoprotein (P-gp). For instance, co-administration of a number of drugs called chemosensitizers or MDR modulators with a chemotherapeutic agent to inhibit drug efflux. But for optimal synergy, the drug and inhibitor combination may need to be temporally colocalized in the tumor cells. In this study, we encapsulated the Ver and Dox in PLGA nanoparticles to inhibit the P-gp drug efflux in breast cancer. Moreover, the effect of either Dox solution (DoxS), Dox nanoparticles (DoxNP), DoxS + VerS, DoxNP + VerS, DoxNP + VerNP or Dox-VerNP was evaluated. It was found that co administration of DoxNP with VerNP (70.76%) showed similar cellular uptake of Dox to Dox/Ver combination solution (70.62%). However it is observed that DoxNP + VerNP has the highest apoptotic activity (early apoptotic 13.52 ± 0.06%, late apoptotic 53.94 ± 0.15%) on human breast adenocarcinoma (MCF 7) cells. Hence, it is suggested that DoxNP + VerNP is a promising administration for tumor therapy. © 2020 Published by Elsevier B.V. on behalf of King Saud University.Objective To assess the safety and effectiveness of dalbavancin compared to standard of care (SOC) in the treatment of osteomyelitis in adults. SKI-606 clinical trial Method A retrospective cohort study of patients with osteomyelitis due to S. aureus treated with dalbavancin was conducted. Patients who received at least 2 doses of dalbavancin for the treatment of osteomyelitis between January 1, 2015 to January 31, 2018 in a single center in Texas, USA were identified and matched in 11 ratio with controls who received SOC. The primary efficacy outcome was the clinical success at the end of treatment. Secondary efficacy outcome was the clinical success continued for at least 3 months after the completion of the antimicrobial therapy. Results During study period, 21 patients received dalbavancin for the treatment of osteomyelitis; however, only 11 patients were eligible for inclusion and matched to 11 others who received SOC. Primary outcome was achieved in all 11 patients who received dalbavancin and all those patients subsequently attained the secondary outcome. In SOC group, primary outcome occurred in 82% (9/11) of patients in which 8 out of 9 patients subsequently achieved the secondary outcome. No adverse reaction noted in either group. Conclusion Dalbavancin appears to be safe and effective for the management of osteomyelitis in adults. Further studies are needed to confirm these findings. © 2020 The Authors.Background In addition to diet restriction and physical activity, diabetes mellitus is managed by the chronic use of medications that require appropriate storage conditions to maintain their stability and effectiveness. However, there is a lack of information regarding patients’ knowledge of medication storage and practices in Saudi Arabia. link2 Therefore, the objective of this study was to determine the diabetics’ knowledge about medication storage requirements and to evaluate the impact of antidiabetic medications storage on the blood glucose levels. Methods This study was a cross-sectional in the form of an interviewer-guided interview using a close-ended questions. The study was conducted among patients diagnosed with diabetes at diabetic clinics of public hospitals and other diabetic specialized clinics in Hail region of Saudi Arabia, over a period of four months between January to April 2019. Results A total of 501 completed questionnaires were returned. Of the respondents, 51.5% were males and 48.5% were females. Of the total participants 52.7% never achieved normal blood glucose range, which was associated with health literacy and medication storage knowledge. Almost half of the participants stored the medication correctly and others have poor knowledge and practice of medication storage, of whom 7.8% always store their medicines in their cars. link3 Conclusion Almost half of the participants lack the knowledge of appropriate storage conditions of diabetes medications, which was shown to have a significant association with blood glucose levels. © 2020 The Authors.Evidence demonstrates that chronic caffeine exposure, primarily through consumption of coffee or tea, leads to increased alertness and anxiety. Preclinical and clinical studies showed that caffeine induced beneficial effects on mood and cognition. Other studies using molecular techniques have reported that caffeine exhibited neuroprotective effects in animal models by protecting dopaminergic neurons. Moreover, caffeine interacts with dopaminergic system, which leads to improvements in neurobehavioral measures in animal models of depression or attention deficit hyperactivity disorder (ADHD). Glutamatergic receptors have been found to be involved on the neurobiological effects of caffeine. Additionally, caffeine has been found to suppress the inhibitory (GABAergic) activity and modulate GABA receptors. Studies have also found that modulating these neurotransmitters leads to neurobehavioral effects. The linkage between the modulatory role of caffeine on neurotransmitters and neurobehavioral effects has not been fully discussed. The purpose of this review is to discuss in detail the role of neurotransmitters in the effects of caffeine on neurobehavioral disorders. © 2020 The Author.Consumption of Cytochrome P450 2D6 (CYP2D6) inhibiting drugs along with tamoxifen treatment results in decrease in plasma concentration of endoxifen, the major active tamoxifen metabolite. Simultaneous use of CYP2D6 inhibitors, such as selective serotonin reuptake inhibitors (SSIs), as well as lesser tamoxifen adherence may negatively impact tamoxifen efficacy in patients with breast cancer. The objective of our study was to assess the co-prescription of CYP2D6 inhibitors and tamoxifen use and also to relate concomitant CYP2D6 inhibitor use and tamoxifen adherence to breast cancer in Riyadh, Saudi Arabia. All patients treated for breast cancer who had at least one tamoxifen prescription in their electronic medical records (EMRs) from June 2015 to June 2017 were included. Patients who had other adjuvant hormonal therapy were excluded from the study. In total, 499 patients (25 males and 474 females) with breast cancer using tamoxifen were included. Our study was purely observational study revealed that prescription of weak inhibitors with tamoxifen increased in the second year as opposed to decrease in the prescription of strong inhibitors. Also, a substantial percentage of patient population were found to be non-adherent to the tamoxifen therapy in this study. © 2020 The Author(s).Simultaneous analysis of 20 marker components (gallic acid, cimifugin, geniposide, paeoniflorin, ferulic acid, nodakenin, narirutin, naringin, neohesperidin, arctiin, baicalin, oxypeucedanin hydrate, wogonoside, baicalein, arctigenin, glycyrrhizin, wogonin, pulegone, decursin, and decursinol angelate) for quality assessment of the traditional herbal formula, Hyeonggaeyeongyo-tang (HYT) was carried out by using high-performance liquid chromatography (HPLC) with photodiode array detection (PDA) and liquid chromatography-mass spectrometry with tandem mass spectrometry (LC-MS/MS). The coefficient of determination showed excellent linearity of more than 0.9999 for all analytes. The recovery of 20 marker components was 93.92 to 102.66% with relative standard deviation (RSD)  less then  3.00% and RSD value of precision was ≤ 3.44%. The amounts of 20 marker components using HPLC-PDA and LC-MS/MS were determined to be 0.18-14.60 and 0.01-1.76 mg/freeze-dried g, respectively. © 2020 The Author(s).Two series of rhodanine-3-acetic and rhodanine-3-propionic acids derivatives having benzylidene and cinnamylidene substituents with additional electron donating and withdrawing groups at the C-5 position, were synthesised. The structures of the obtained derivatives were confirmed by spectroscopic methods and their lipophilicity was screened. The crystal structures were determined for selected compounds. The antibacterial activity of the derivatives was depended on the type of carboxyalkyl group in the N-3 position and on the type of the substituent in the C-5 position. The derivatives of rhodanine-3-propionic acid demonstrated the highest activity against Gram-positive bacteria. However, none of tested derivatives showed activity against Gram-negative bacteria and yeast. We believe that the presence of the N,N-diethylamine group in the aromatic system and the number of carbon atoms in the carboxyalkyl group is more significant for the biological activity than the fact that the benzylidene or cinnamylidene substituent was present at the C-5 position. © 2020 The Author(s).Monoamine oxidase inhibition is an important therapeutic approach for various neurodegenerative disorders. Reversible MAO inhibitors selectively targeting only one isoform possess substantial merit in terms of safety, efficacy, and side effect profile. This study aimed to isolate the secondary metabolites of Zanthoxylum flavum stems and evaluate their recombinant human MAO inhibition, antimicrobial, and antiprotozoal activities. As a result, fourteen compounds were isolated and identified (nine of them were reported from Z. flavum for the first time). Compound 3 (sesamin) exhibited potent selective MAO-B inhibition (IC50 value of 1.45 ± 0.05 µM) which reported herein for the first time. Compound 2 showed selective MAO-A inhibition activity, compound 5 exhibited good trypanocidal activity, and compound 7 displayed moderate antibacterial activity. The promising MAO-B inhibitory activity of sesamin provoked us to further explore the kinetic properties, the binding mode, and the underlying mechanism of MAO-B inhibition by this lignan. This detailed investigation substantiated a reversible binding and mixed MAO-B catalytic function inhibition via sesamin (Ki 0.473 ± 0.076 μM). Selectivity and reversibility of sesamin on MAO-B provide exciting prerequisites for further in vivo investigation to confirm its therapeutic potentiality. © 2020 The Author(s).Thymoquinone is the most biologically active constituent of Nigella sativa (black seed). A monoterpene compound chemically known as 2-methyl-5-isopropyl-1, 4-quinone. In this study, the gender-dependent pharmacokinetic behavior of thymoquinone in rats was investigated. Thymoquinone was administered orally (20 mg/kg) and intravenously (5 mg/kg) to male and female rats and blood samples were collected at specific time points. Plasma concentration-time curves were plotted and pharmacokinetic parameters were determined using the non-compartmental analysis. In addition, simulations of steady state concentrations of thymoquinone in male and female rats were performed using GastroPlus PK software. After oral administration, the maximum plasma concentration (Cmax) of thymoquinone was 4.52 ± 0.092 μg/ml in male rats and 5.22 ± 0.154 μg/ml in female rats (p = 0.002). Similarly, after intravenous administration, the Cmax was 8.36 ± 0.132 μg/ml in males and 9.51 ± 0.158 μg/ml in females (p = 0.550). The area under the plasma concentration-time curve (AUC)0-∞ following oral dosing was 47.

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