RESUMEN
Background Dietary supplements are used for a variety of reasons, some of which are for medical conditions, to compensate for dietary insufficiency, to improve physical performance, and to boost immunity. Generally, individuals who visit sports facilities seek different benefits; it could be for health and well-being, to achieve the desired body shape, for enjoyment purposes, or as a way to socialize. To help achieve some of these goals, dietary supplements can be taken. Aims This study is designed to assess the prevalence and awareness of dietary supplement use among Saudi women who frequent fitness centers in Riyadh, Saudi Arabia. Methods A cross-sectional study was conducted in November 2021 among Saudi women who visited gyms in Riyadh, Saudi Arabia. The sample consisted of 355 participants, all of whom were women from Saudi Arabia. The statistical analysis was done using IBM Statistical Package for Social Sciences (SPSS), Version 21.0 (Armonk, NY: IBM Corp.). Necessary statistical tests such as the chi-square, the t-test, and other appropriate tests were used. A p-value of less than 0.05 has been adopted for statistical significance. Results The majority of the 355 female participants consumed dietary supplements (68.7%). The most commonly used supplements were vitamins (82.8%), amino acids and proteins (30.3%), minerals (22.1%), and fatty acids (3.3%). In the study group, 53.3% of those who were using or used supplements had previous knowledge; 13.1% were up-to-date; and 33.6% weren't. No relationship was found between supplement use and educational level, weight, body mass index (BMI), or marital status. Conclusion Dietary supplement use is common among women who visited gyms in Saudi Arabia. Vitamins were the most commonly used supplements, which suggests that users were more concerned about general health and diet deficiencies than anything else. The participants use dietary supplements cautiously; the majority consume dietary supplements under a doctor's prescription and after reading the leaflets.
RESUMEN
BACKGROUND: Metabolic syndrome (MetS) exacerbates susceptibility to inhalation exposures such as particulate air pollution, however, the mechanisms responsible remain unelucidated. Previously, we determined a MetS mouse model exhibited exacerbated pulmonary inflammation 24 h following AgNP exposure compared to a healthy mouse model. This enhanced response corresponded with reduction of distinct resolution mediators. We hypothesized silver nanoparticle (AgNP) exposure in MetS results in sustained pulmonary inflammation. Further, we hypothesized treatment with resolvin D1 (RvD1) will reduce exacerbations in AgNP-induced inflammation due to MetS. RESULTS: To evaluate these hypotheses, healthy and MetS mouse models were exposed to vehicle (control) or AgNPs and a day later, treated with resolvin D1 (RvD1) or vehicle (control) via oropharyngeal aspiration. Pulmonary lung toxicity was evaluated at 3-, 7-, 14-, and 21-days following AgNP exposure. MetS mice exposed to AgNPs and receiving vehicle treatment, demonstrated exacerbated pulmonary inflammatory responses compared to healthy mice. In the AgNP exposed mice receiving RvD1, pulmonary inflammatory response in MetS was reduced to levels comparable to healthy mice exposed to AgNPs. This included decreases in neutrophil influx and inflammatory cytokines, as well as elevated anti-inflammatory cytokines. CONCLUSIONS: Inefficient resolution may contribute to enhancements in MetS susceptibility to AgNP exposure causing an increased pulmonary inflammatory response. Treatments utilizing specific resolution mediators may be beneficial to individuals suffering MetS following inhalation exposures.
Asunto(s)
Síndrome Metabólico , Nanopartículas del Metal , Neumonía , Animales , Citocinas/metabolismo , Modelos Animales de Enfermedad , Ácidos Docosahexaenoicos , Inflamación/inducido químicamente , Nanopartículas del Metal/toxicidad , Ratones , Neumonía/inducido químicamente , Plata/toxicidadRESUMEN
BACKGROUND: Herbs usually contain a mixture of biologically active constituents, which can interact with numerous prescribed drugs and alter their safety profiles. OBJECTIVES: The current investigation was aimed to evaluate the effect of commonly used herbal products including black seed (Nigella sativa), garden cress (Lepidium sativum), and fenugreek (Trigonella foenum-graecum) on the pharmacokinetics and pharmacodynamics of clopidogrel using a Wistar rat model. METHODS: A GC-MS analysis revealed the presence of several phytoconstitutents (polyphenols) in the extracts of black seed, garden cress, and fenugreek. These polyphenols have the potential to interfere with clopidogrel effect. Plasma concentrations of clopidogrel were measured at different time points in the absence and presence of the concurrent use of tested herbal products and the pharmacokinetic parameters were calculated. Bleeding time was measured in various groups as a measure of the antiplatelet effect of clopidogrel. RESULTS: Area under the plasma concentration-time curves (AUC0-∞) of clopidogrel were 35.53 ±0.89 µg/ml*h (p<0.05), 26.01 ±0.90 µg/ml*h (p>0.05) and 32.80 ±2.51 µg/ml*h (p<0.05) in the black seed, garden cress and fenugreek group, respectively, compared with that of the control group (27.02 ±0.42 µg/ml*h). Treatment with black seed also caused an increase in clopidogrel Cmax by 31.52% (p<0.05) and with fenugreek by 21.42% (p<0.05); Cmax, did not changed with garden cress treatment (6.48 ±0.15 µg/ml versus 6.12 ±0.21 µg/ml, p>0.05). The pharmacodynamic evaluation of the antiplatelet effect of clopidogrel in the presence of herbal products treatment showed a significant prolongation in the bleeding time from a control baseline by ~22-26%, and by added ~8-12% in reference to clopidogrel therapeutic effect (p<0.05). CONCLUSION: The concurrent use of black seed, fenugreek, or garden cress can alter the pharmacokinetics and pharmacodynamics of clopidogrel to varying degrees due to the presence of various bioactive polyphenols. This is probably due to changes in drug disposition and its antiplatelet action. Further confirmation can determine the clinical relevance of these observations and identify the exact constituents responsible for such activities.
Asunto(s)
Coagulación Sanguínea/efectos de los fármacos , Clopidogrel/farmacocinética , Lepidium sativum , Nigella sativa , Fitoquímicos/farmacocinética , Polifenoles/farmacocinética , Antagonistas del Receptor Purinérgico P2Y/farmacocinética , Trigonella , Animales , Tiempo de Sangría/métodos , Interacciones de Hierba-Droga , Agregación Plaquetaria/efectos de los fármacos , Polifenoles/farmacología , RatasRESUMEN
Pre-existing conditions modulate sensitivity to numerous xenobiotic exposures such as air pollution. Specifically, individuals suffering from metabolic syndrome (MetS) demonstrate enhanced acute inflammatory responses following particulate matter inhalation. The mechanisms associated with these exacerbated inflammatory responses are unknown, impairing interventional strategies and our understanding of susceptible populations. We hypothesize MetS-associated lipid dysregulation influences mediators of inflammatory resolution signaling contributing to increased acute pulmonary toxicity. To evaluate this hypothesis, healthy and MetS mouse models were treated with either 18-hydroxy eicosapentaenoic acid (18-HEPE), 14-hydroxy docosahexaenoic acid (14-HDHA), 17-hydroxy docosahexaenoic acid (17-HDHA), or saline (control) via intraperitoneal injection prior to oropharyngeal aspiration of silver nanoparticles (AgNP). In mice receiving saline treatment, AgNP exposure resulted in an acute pulmonary inflammatory response that was exacerbated in MetS mice. A targeted lipid assessment demonstrated 18-HEPE, 14-HDHA, and 17-HDHA treatments altered lung levels of specialized pro-resolving lipid mediators (SPMs). 14-HDHA and 17-HDHA treatments more efficiently reduced the exacerbated acute inflammatory response in AgNP exposed MetS mice as compared to 18-HEPE. This included decreased neutrophilic influx, diminished induction of inflammatory cytokines/chemokines, and reduced alterations in SPMs. Examination of SPM receptors determined baseline reductions in MetS mice compared to healthy as well as decreases due to AgNP exposure. Overall, these results demonstrate AgNP exposure disrupts inflammatory resolution, specifically 14-HDHA and 17-HDHA derived SPMs, in MetS contributing to exacerbated acute inflammatory responses. Our findings identify a potential mechanism responsible for enhanced susceptibility in MetS that can be targeted for interventional therapeutic approaches.
Asunto(s)
Mediadores de Inflamación/metabolismo , Metabolismo de los Lípidos/efectos de los fármacos , Pulmón/efectos de los fármacos , Síndrome Metabólico/complicaciones , Nanopartículas del Metal/toxicidad , Neumonía/inducido químicamente , Compuestos de Plata/toxicidad , Animales , Antiinflamatorios/farmacología , Citocinas/genética , Citocinas/metabolismo , Dieta Alta en Grasa , Modelos Animales de Enfermedad , Ácidos Docosahexaenoicos/farmacología , Regulación de la Expresión Génica , Ácidos Hidroxieicosatetraenoicos/farmacología , Metabolismo de los Lípidos/genética , Pulmón/metabolismo , Masculino , Síndrome Metabólico/tratamiento farmacológico , Síndrome Metabólico/genética , Síndrome Metabólico/metabolismo , Ratones Endogámicos C57BL , Neumonía/genética , Neumonía/metabolismo , Neumonía/prevención & control , Transducción de SeñalRESUMEN
Extensive research has been carried out during the last few decades, providing a detailed account of thousands of discovered phytochemicals and their biological activities that have the potential to be exploited for a wide variety of medicinal purposes. These phytochemicals, which are pharmacologically important for clinical use, primarily consist of polyphenols, followed by terpenoids and alkaloids. There are numerous published reports indicating the primary role of phytochemicals proven to possess therapeutic potential against several diseases. However, not all phytochemicals possess significant medicinal properties, and only some of them exhibit viable biological effects. Naringenin, a flavanone found in citrus fruits, is known to improve immunity, repair DNA damage, and scavenge free radicals. Despite the very low bioavailability of naringenin, it is known to exhibit various promising biological properties of medicinal importance, including anti-inflammatory and antioxidant activities. This review focuses on the various aspects related to naringenin, particularly its physicochemical, pharmacokinetic, and pharmacodynamic properties. Furthermore, various pharmacological activities of naringenin, such as anticancer, antidiabetic, hepatoprotective, neuroprotective, cardioprotective, nephroprotective, and gastroprotective effects, have been discussed along with their mechanisms of action.
RESUMEN
PURPOSE: Drug utilization studies have proven to be an effective tool in the evaluation of rational drug use in different health care systems, including oncology. The drug utilization studies were used in many institutes to ensure the safe, effective and appropriate use of drugs being prescribed. The main aim of this study was to assess the utilization pattern of anticancer drugs in breast cancer patients. METHOD: A retrospective cross-sectional observational study was carried out at King Saud University Medical City (KSUMC) for 1 year from January 2016 to December 2016. All female patients diagnosed with breast cancer during this year were included in the study. RESULTS: A total of 101 patients were included in this study. Most patients received an average of three anticancer drugs. The most commonly prescribed medication was fluorouracil, epirubicin, and cyclophosphamide (FEC) regimen, which was used in 81% of patients. Combinations of FEC + docetaxel and FEC + docetaxel + trastuzumab were received by43% and 23% of patients, respectively. Docetaxel was the most commonly used drug in neoadjuvant setting, whereas letrozole and trastuzumab were prescribed more frequently in hormonal and targeted therapies, respectively. The total drug expenditure on anticancer therapy was approximately 3.8 million Saudi Riyals (S.R), with adjuvant therapy constituting over half of the total spending. In neoadjuvant settings, the spending cost for hormonal therapy was the highest. The condition of most breast cancer patients was improved during the study period, whereas only 29% of the included patients progressed. CONCLUSION: FEC was the most common regimen used in this study, consistent with the National Comprehensive Cancer Network (NCCN) guideline recommendation. Our results indicated that adherence to a clinical guideline and recommended medication regimens improved patient outcomes. Our finding indicate how analyzing drug utilization pattern could benefit institutions in managing inventory and efficiently using health care resources.
RESUMEN
The purpose of this study was to investigate the population pharmacokinetics (PK) of cefuroxime in patients undergoing coronary artery bypass graft (CABG) surgery. In this observational pharmacokinetic study, multiple blood samples were collected over a 48-h interval of intravenous cefuroxime administration. The samples were analyzed by using a validated high-performance liquid chromatography (HPLC) method. Population pharmacokinetic models were developed using Monolix (version 4.4) software. Pharmacokinetic-pharmacodynamic (PD) simulations were performed to explore the ability of different dosage regimens to achieve the pharmacodynamic targets. A total of 468 blood samples from 78 patients were analyzed. The PK for cefuroxime were best described by a two-compartment model with between-subject variability on clearance, the volume of distribution of the central compartment, and the volume of distribution of the peripheral compartment. The clearance of cefuroxime was related to creatinine clearance (CLCR). Dosing simulations showed that standard dosing regimens of 1.5 g could achieve the PK-PD target of the percentage of the time that the free concentration is maintained above the MIC during a dosing interval (fTMIC) of 65% for an MIC of 8 mg/liter in patients with a CLCR of 30, 60, or 90 ml/min, whereas this dosing regimen failed to achieve the PK-PD target in patients with a CLCR of ≥125 ml/min. In conclusion, administration of standard doses of 1.5 g three times daily provided adequate antibiotic prophylaxis in patients undergoing CABG surgery. Lower doses failed to achieve the PK-PD target. Patients with high CLCR values required either higher doses or shorter intervals of cefuroxime dosing. On the other hand, lower doses (1 g three times daily) produced adequate target attainment for patients with low CLCR values (≤30 ml/min).
Asunto(s)
Antibacterianos/farmacocinética , Antibacterianos/uso terapéutico , Puente Cardiopulmonar/métodos , Cefuroxima/farmacocinética , Cefuroxima/uso terapéutico , Puente de Arteria Coronaria/métodos , Adolescente , Adulto , Anciano , Anciano de 80 o más Años , Cromatografía Líquida de Alta Presión , Femenino , Humanos , Masculino , Pruebas de Sensibilidad Microbiana , Persona de Mediana Edad , Método de Montecarlo , Adulto Joven , beta-Lactamas/farmacocinética , beta-Lactamas/uso terapéuticoRESUMEN
Stigmasterol (99.9% pure) was isolated from Azadirachta indica and its chemopreventive effect on 7,12-dimethylbenz[a]anthracene (DMBA)-induced skin cancer was investigated in Swiss albino mice. Skin tumors were induced by topical application of DMBA and promoted by croton oil. To assess the chemopreventive potential of stigmasterol, it was orally administered at a concentration of 200 mg/kg and 400 mg/kg three times weekly for 16 weeks. Reduction in tumor size and cumulative number of papillomas were seen as a result of treatment with stigmasterol. The average latency period was significantly increased as compared with the carcinogen-treated control. Stigmasterol induced a significant decrease in the activity of serum enzymes, such as aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, and bilirubin as compared with the control. Stigmasterol significantly increased glutathione, superoxide dismutase, and catalase as compared with the control. Elevated levels of lipid peroxide and DNA damage in the control group were significantly inhibited by administration of stigmasterol. From the present study, it can be inferred that stigmasterol has chemopreventive activity in an experimental model of cancer. This chemopreventive activity may be linked to the oxidative stress of stigmasterol. The antigenotoxic properties of stigmasterol are also likely to contribute to its chemopreventive action.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Azadirachta/química , Neoplasias Cutáneas/prevención & control , Estigmasterol/farmacología , 9,10-Dimetil-1,2-benzantraceno/toxicidad , Animales , Antineoplásicos Fitogénicos/administración & dosificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Aceite de Crotón/toxicidad , Daño del ADN/efectos de los fármacos , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Femenino , Masculino , Ratones , Estrés Oxidativo/efectos de los fármacos , Neoplasias Cutáneas/patología , Estigmasterol/administración & dosificación , Estigmasterol/aislamiento & purificaciónRESUMEN
Tocotrienol-rich fraction of palm oil, which contains the isomers of vitamin E, was shown to possess potent anticancer activity against mammary adenocarcinoma cell lines. Its clinical use, however, is limited by poor oral bioavailability and short half-life. Previously, we developed tocotrienol-rich lipid nanoemulsions for intravenous administration. The objective of this study was to investigate the effect of surface grafted polyethylene glycol (PEG) on the properties of the nanoemulsions. PEGylation was achieved by the addition of equimolar PEG groups using poloxamer or 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(polyethylene glycol)2000] (PEG2000-DSPE). The effect of PEG surface topography on the antiproliferative activity of nanoemulsions against mammary adenocarcinoma cells, their susceptibility to protein adsorption, and its effect on blood hemolysis and circulation time was investigated. Nanoemulsions PEGylated with poloxamer or PEG2000-DSPE were stable under physical stress. Poloxamer nanoemulsion, however, displayed higher uptake and potency against MCF-7 tumor cells in 2D and 3D culture and increased hemolytic effect and susceptibility to IgG adsorption, which was reflected in its rapid clearance and short circulation half-life (1.7 h). Conversely, PEGylation with PEG2000-DSPE led to a 7-fold increase in mean residence time (12.3 h) after IV injection in rats. Reduced activity in vitro and improved circulation time suggested strong shielding of plasma proteins from the droplets. Differences between the nanoemulsions were attributed to polymer imbibitions and the differences in PEG conformation and density on the surface of the droplets.