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- [Comparison of dexmedetomidine and propofol for short-term sedation in early postoperative period after cardiac surgery]. [English Abstract, Journal Article]
- Anesteziol Reanimatol 2014 Mar-Apr; (2):37-41.
To compare the efficacy of Dexmedetomidine and Propofol for short-term controlled sedation and analgesia in the early postoperative period after cardiac surgery.We performed open randomized prospective comparative study in 55 cardiovascular surgery patients. In the early postoperative period 28 patients received infusion of Dexmedetomidine (0.2-0.7 microg/kg per hour) while 27 patients--Propofol (0.3-2(system text of symbol)). Analgesia was carried out with Ketoprofen 100 mg/12h and additional 20 mg of Trimeperidine in case of pain intensity > or = 3 points (5-level verbal pain score). Sedation and agitation level (RASS scale), speed of awakening (Aldrete score), duration of mechanical ventilation and stay in the ICU, need for additional opioid injections, type and frequency of side effects were evaluated.We didn't find any significant differences in the duration of mechanical ventilation or rate of awakening after the end of infusion between the groups. Dexmedetomidine in the majority of cases resulted in mild or moderate sedation, Propofol--in deeper level of sedation. Retrograde amnesia was reached significantly more often (p < 0.05) in Dexmetomedine group. The daily dose of Trimeperidine in Propofol group was significantly higher (8 mg and 18 mg on average, p = 0.02). Differences in side effects between the groups were noted--bradycardia (Dexmetomedine--10 (39%), Propofol--3 (11%), p = 0.004) arterial hypotension (Dexmetomedine--9 (32%), Propofol--15 (59%), p = 0.002) and general malaise (Dexmetomedine--2 (7%), Propofol--6 (24%), p = 0.001). The length of stay in the ICU in Dexmetomedine group was significantly lower (1,1 days vs 2,6 days respectively, p = 0.006).To compare with Propofol Dexmetomedine induces less sedation level and more often provides retrograde amnesia with the same duration of mechanical ventilation and awakening rate. Dexmetomedine provides its own analgesic effect and shortens the length of patient's stay in ICU. Bradycardia was noted more frequently in Dexmedetomidine while arterial hypotension, general malaise and delirium--in Propofol group.
- [Assessment of pain relief in patients receiving different variants of multimodal analgesia after major gynecological surgery]. [English Abstract, Journal Article]
- Anesteziol Reanimatol 2014 Mar-Apr; (2):32-7.
The major gynecology surgery generally results in severe postoperative pain. Currently multimodal analgesia concept is widely used for the aim of postoperative pain relief optimization. According to this theory it is worth using the medication with different mechanism in order to increase analgesia qualify, decrease analgesic consumption and avoid adverse reaction. Unfortunately the surveys recently conducted have been pointed out the postoperative analgesia quality is still insufficient despite of using the concept mentioned above. One way to solve the problem is appearing in daily practice nefopam--centrally acting non-opioid analgesic that inhibits reuptake of serotonin, norepinephrine, and dopamine and also mitigates glutamatergic neurotransmission. In this trial we tried to assess the postoperative daily used analgesia quality and potency of preemptive multimodal analgesia model consisted of nefopam, ketoprofen, paracetamol and morphine.
- Ketoprofen enantioseparation with a Cinchona-alkaloid-based stationary phase: Enantiorecognition mechanism and release studies. [JOURNAL ARTICLE]
- J Sep Sci 2014 Jul 14.
With the present contribution we demonstrate that the base-line separation of ketoprofen enantiomers can be successfully achieved (α = 1.09; RS = 1.60) in the reversed-phase mode of elution with a commercially available anion-exchange-based chiral stationary phase, incorporating the quinine 2,6-diisopropylphenyl carbamate derivative as the enantioresolving unit. Focused modification of the eluent composition indicated a stereoselective role of hydrophobic and π-π interactions between the selector and selectand units, besides the prime ionic intermolecular interaction. The mechanistic hypotheses based on the chromatographic data were confirmed by in silico molecular dynamic simulations, which allowed us to establish the network of selector-selectand interactions underlying the stereorecognition process at a molecular level. The validated method was successfully used to evaluate the drug content and release profile of ketoprofen-loaded polymeric film, showing drug homogeneous distribution into the film and no preferential interactions between the polymer and one of the enantiomers, with the racemate released at each time point. This article is protected by copyright. All rights reserved.
- DJ-1 plays an important role in caffeic acid-mediated protection of the gastrointestinal mucosa against ketoprofen-induced oxidative damage. [JOURNAL ARTICLE]
- J Nutr Biochem 2014 Jun 12.
Ketoprofen is widely used to alleviate pain and inflammation in clinical medicine; however, this drug may cause oxidative stress and lead to gastrointestinal (GI) ulcers. We previously reported that nuclear factor erythroid 2-related factor 2 (Nrf2) plays a crucial role in protecting cells against reactive oxygen species, and it facilitates the prevention of ketoprofen-induced GI mucosal ulcers. Recent reports suggested that Nrf2 becomes unstable in the absence of DJ-1/PARK7, attenuating the activity of Nrf2-regulated downstream antioxidant enzymes. Thus, increasing Nrf2 translocation by DJ-1 may represent a novel means for GI protection. In vitro, caffeic acid increases the nuclear/cytosolic Nrf2 ratio and the mRNA expression of the downstream antioxidant enzymes, ϒ-glutamyl cysteine synthetase, glutathione peroxidase, glutathione reductase, and heme oxygenase-1, by activating the JNK/p38 pathway in Int-407 cells. Moreover, knockdown of DJ-1 also reversed caffeic acid-induced nuclear Nrf2 protein expression in a JNK/p38-dependent manner. Our results also indicated that treatment of Sprague-Dawley rats with caffeic acid prior to the administration of ketoprofen inhibited oxidative damage and reversed the inhibitory effects of ketoprofen on the antioxidant system and DJ-1 protein expression in the GI mucosa. Our observations suggest that DJ-1 plays an important role in caffeic acid-mediated protection against ketoprofen-induced oxidative damage in the GI mucosa.
- [Meloxicam: the golden mean of nonsteroidal anti-inflammatory drugs]. [English Abstract, Journal Article]
- Ter Arkh 2014; 86(5):99-105.
Nonsteroidal anti-inflammatory drugs (NSAIDs) are most commonly used to treat acute and chronic pain in locomotor system (LMS) diseases. However, their administration may be accompanied by the development of dangerous complications as organic and functional disorders of the cardiovascular system (CVS) and gastrointestinal tract (GIT). Physicians have currently a wide range of NSAIDs at their disposal; but none of the representatives of this group can be considered the best. Thus, highly selective cyclooxygenase-2 inhibitors (Coxibs) are substantially safer for GIT; however, their use is clearly associated with the increased risk of severe cardiovascular events. Nonselective NSAIDs, such as naproxen or ketoprofen, are safer for CVS, but more frequently cause significant GIT organic and functional disorders. Moderately selective NSAIDs, such as meloxicam (movalis), conceivably could be the most acceptable choice for treating the majority of patients in this situation. This drug has been long and extensively used in global clinical practice and has gained the confidence of physicians and patients. The major benefits of meloxicam are its proven efficacy, convenient treatment regimen, relatively low risk of complications as organic and functional disorders of the GIT and CVD and good compatibility with low-dose aspirin.
- Irrigation of Root Vegetables with Treated Wastewater: Evaluating Uptake of Pharmaceuticals and the Associated Human Health Risks. [JOURNAL ARTICLE]
- Environ Sci Technol 2014 Jul 15.
To meet mounting water demands, treated wastewater has become an important source of irrigation. Thus, contamination of treated wastewater by pharmaceutical compounds (PCs) and the fate of these compounds in the agricultural environment are of increasing concern. This field study aimed to quantify PC uptake by treated wastewater-irrigated root crops (carrots and sweet potatoes) grown in lysimeters and to evaluate potential risks. In both crops, the nonionic PCs (carbamazepine, caffeine, and lamotrigine) were detected at significantly higher concentrations than ionic PCs (metoprolol, bezafibrate, clofibric acid, diclofenac, gemfibrozil, ibuprofen, ketoprofen, naproxen, sulfamethoxazole and sildenafil). PCs in leaves were found at higher concentrations than in the roots. Carbamazepine metabolites were found mainly in the leaves, where the concentration of the metabolite 10,11-epoxycarbamazepine was significantly higher than the parent compound. The health risk associated with consumption of wastewater-irrigated root vegetables was estimated using the threshold of toxicological concern (TTC) approach. Our data show that the TTC value of lamotrigine can be reached for a child at a daily consumption of half a carrot (~60 g). This study highlights that certain PCs accumulated in edible organs at concentrations above the TTC value should be categorized as contaminants of emerging concern.
- Comparison of the sensitivities of WaterLOGSY and saturation transfer difference NMR experiments. [JOURNAL ARTICLE]
- J Biomol NMR 2014 Jul 12.
The WaterLOGSY (WL) and saturation transfer difference (STD) NMR experiments have proven to be extremely useful techniques to characterize interactions between small molecules and large biomolecules. In this work we compare the relative sensitivities of WL and STD NMR using 3 experimental systems: ketoprofen (KET)-bovine serum albumin (BSA), tert-butyl hydroquinone (TBHQ)-hemagglutinin (HA), and chloramphenicol (CAM)-ribosome (70S). In all cases we find that WL is more sensitive than STD for a given experimental time with the ratios ranging from 3.2 for KET-BSA to 16 for TBHQ-HA and CAM-70S. We attribute the increased sensitivity of WL to be due to simultaneous saturation of multiple sources of cross correlation, including direct NOEs of (1)H of water and exchangeable groups and indirect NOEs of (1)H-C groups. We suggest that the outstanding sensitivity of WL make it ideally suited for drug screening efforts targeting very large biomolecules at relatively low concentrations.
- Effect of ketoprofen on pre-weaning piglet mortality on commercial farms. [JOURNAL ARTICLE]
- Vet J 2014 Jun 6.
The effect of ketoprofen on pre-weaning piglet mortality was evaluated in a large-scale study on commercial farms. Sows (n= 1486) from 15 farms were included. Half of the sows received 3 mg/kg ketoprofen in a single intramuscular administration within 12 h after farrowing. The other half remained untreated. Pre-weaning mortality was lower in the ketoprofen-treated group than in the control group (8.43% vs. 10.24%, respectively; P= 0.010). The major impact of ketoprofen on mortality was seen between days 2 and 7 postpartum (mortality rates of 2.75% vs. 4.02% for treated and control groups, respectively; P= 0.001). In addition, ketoprofen treatment was associated with a higher number of piglets weaned per litter than when no treatment was given (10.0 vs. 9.84, respectively; P= 0.012).
- Occurrence of pharmaceuticals in urban wastewater of north Indian cities and risk assessment. [JOURNAL ARTICLE]
- Environ Monit Assess 2014 Jul 9.
Six pharmaceuticals of different categories, such as nonsteroidal anti-inflammatory drugs (ibuprofen, ketoprofen, naproxen, diclofenac), anti-epileptic (carbamazepine), and anti-microbial (trimethoprim), were investigated in wastewater of the urban areas of Ghaziabad and Lucknow, India. Samples were concentrated by solid phase extraction (SPE) and determined by high-performance liquid chromatography (HPLC) methods. The SPE-HPLC method was validated according to the International Conference on Harmonization guidelines. All the six drugs were detected in wastewater of Ghaziabad, whereas naproxen was not detected in Lucknow wastewater. Results suggest that levels of these detected drugs were relatively higher in Ghaziabad as compared to those in Lucknow, and diclofenac was the most frequently detected drug in both the study areas. Detection of these drugs in wastewater reflects the importance of wastewater inputs as a source of pharmaceuticals. In terms of the regional distribution of compounds in wastewater of two cities, higher spatial variations (coefficient of variation 112.90-459.44 %) were found in the Lucknow wastewater due to poor water exchange ability. In contrast, lower spatial variation (162.38-303.77 %) was observed in Ghaziabad. Statistical analysis results suggest that both data were highly skewed, and populations in two study areas were significantly different (p < 0.05). A risk assessment based on the calculated risk quotient (RQ) in six different bioassays (bacteria, duckweed, algae, daphnia, rotifers, and fish) showed that the nonsteroidal anti-inflammatory drugs (NSAIDs) posed high (RQ >1) risk to all the test species. The present study would contribute to the formulation of guidelines for regulation of such emerging pharmaceutical contaminants in the environment.
- Fast ibuprofen, ketoprofen and naproxen simultaneous determination in human serum for clinical toxicology by GC-FID. [JOURNAL ARTICLE]
- Clin Biochem 2014 Jul 6.
The aim of this study was to develop and validate a gas chromatographic method with flame ionization detection (GC-FID) for the measurement of ibuprofen, naproxen and ketoprofen for clinical toxicology purposes.100μL of plasma was treated with methyl chloroformate and derivatized analytes were extracted with hexane. Optimal conditions of the derivatization procedure have been found using the experimental chemometric design (face-centered central composite design). The selectivity and efficiency of the procedure was confirmed by GC-MS.The assay was linear in the concentration range of 10-400μgmL(-1), with adequate accuracy and precision for GC-FID (98-106.7%, CV≤9.1%, respectively) and for GC-MS (99.3-105.5%, CV≤9.2%, respectively).The entire sample preparation procedure is completed within 5min and the quantitative results are available within 35min. The method was successfully applied to quantify the selected compounds in serum of patients from emergency units.