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- [Treatment of back pain (ketoprofen and other methods)]. [Journal Article]
- Zh Nevrol Psikhiatr Im S S Korsakova 2014; 114(2):81-6.
- Behaviour of nonsteroidal anti-inflammatory drugs and eight of their metabolites during wastewater treatment studied by hollow fibre liquid phase microextraction and liquid chromatography mass spectrometry. [JOURNAL ARTICLE]
- Sci Total Environ 2014 Apr 9.:300-308.
In this work hollow fibre liquid phase microextraction combined with liquid chromatography mass spectrometry was applied for the determination of the nonsteroidal anti-inflammatory drugs (NSAIDs) ketoprofen, naproxen, diclofenac and ibuprofen as well as eight of their known human metabolites in wastewater samples. Extraction time and addition of tri-n-octylphosphine oxide (TOPO) to the liquid membrane were evaluated resulting in a method with an optimal extraction time of 5h and 5% (w/V) TOPO addition to the membrane liquid (di-n-hexyl ether). With the optimized method, enrichment factors ranged between 778 and 4830. The method was applied for analysis of samples collected from Källby wastewater treatment plant in the city of Lund, Sweden. Samples were collected from the influent, water entering as well as exiting the conventional activated sludge treatment and the effluent to study the behaviour of these compounds during the treatment process. All twelve substances were found in the influent and for all four drugs, higher concentrations were detected of the metabolites than the parent compounds. Highest concentrations were detected of o-desmethylnaproxen, 2-hydroxyibuprofen and carboxyibuprofen (average influent concentrations of 45, 35 and 63μg/L respectively). The study showed only partial removal during the primary treatment whereas both parent compounds and metabolites were efficiently removed during the activated sludge process. In the effluent all analytes were detected in concentrations below 1μg/L thus showing that either the investigated metabolites do not belong to the NSAID transformation products formed during the activated sludge treatment or they are also quickly further transformed within the treatment.
- Serious photocontact dermatitis induced by topical ketoprofen depends on the formulation. [JOURNAL ARTICLE]
- Eur J Dermatol 2014 Apr 11.
Background: Topical administration of ketoprofen to treat local subcutaneous pain significantly reduces gastrointestinal and cardiovascular adverse effects associated with oral delivery. However, this benefit must be weighed against the risk of photosensitisation/phototoxicity. Objective: To substantiate the safety and efficacy of topical ketoprofen delivery from a patch. Methods: Experiments were performed, and published information analysed, (a) to confirm the superior skin permeability and pharmacological activity of ketoprofen, and (b) to demonstrate the lower incidence of ketoprofen photosensitisation/phototoxicity when delivered from a topical patch. Results: Ketoprofen's photodegradation products were more photoallergic than the drug itself. The period post-ketoprofen treatment that skin should be protected from UV radiation (while the drug is cleared from the application site) was estimated. Conclusions: Photosensitisation to ketoprofen can be mitigated by a patch formulation, which protects the drug from direct UV exposure during skin application, and reduces the formation of even more photoallergic photodegradation products.
- Comparison of different sorbent materials for solid-phase extraction of selected drugs in human urine analyzed by UHPLC-UV. [JOURNAL ARTICLE]
- J Chromatogr B Analyt Technol Biomed Life Sci 2014 Mar 15.:22-28.
A procedure based on solid-phase extraction (SPE) followed by ultra-high-performance liquid chromatography (UHPLC) with UV detection has been developed for the analysis of multiple drugs in human urine. The compounds evaluated were aliskiren, prasugrel, rivaroxaban, prednisolone, propranolol, ketoprofen, nifedipine, naproxen, terbinafine, ibuprofen, diclofenac, sildenafil and acenocoumarol. Seventeen different solid phase extraction (SPE) cartridges were tested to evaluate their applicability for the isolation of drugs from human urine. Comparison were recovery of different drugs and reproducibility. The samples were analyzed by UHPLC using a Poroshell 120 EC-C18 column and acetonitrile -0.05% TFA in water as the mobile phase under gradient elution conditions. SPE combined with UHPLC-UV allowed the determination of drugs over a linear range of 0.01-30.0μg/mL, with limits of detection at 0.003-0.217μg/mL and precision of 0.8-7.1%. Phenyl (C6H5) sorbent was found to provide the most effective clean-up, removing the greatest amount of interfering substance and simultaneously ensuring analyte recoveries higher than 85.5% with relative standard deviations (RSD) <10%. The method was applied with good accuracy and precision in the determination of drugs in human urine obtained from patients treated with selected drugs.
- Trace analysis of benzophenone-derived compounds in surface waters and sediments using solid-phase extraction and microwave-assisted extraction followed by gas chromatography-mass spectrometry. [JOURNAL ARTICLE]
- Anal Bioanal Chem 2014 Mar 30.
This study describes a procedure for determining eight benzophenone-derived compounds in surface waters and sediments. These include the pharmaceutical ketoprofen, its phototransformation products 3-ethylbenzophenone and 3-acetylbenzophenone, and five benzophenone-type ultraviolet (UV) filters. The proposed analytical method involves the pre-concentration of water samples by solid-phase extraction (SPE) and microwave-assisted extraction (MAE) of sediment samples followed by derivatization and analysis by gas chromatography-mass spectrometry. Different parameters were investigated to achieve optimal method performance. Recoveries of 91 to 96 % from water samples were obtained using HLB Oasis SPE cartridges, whereas MAE of sediments (30 min at 150 °C) gave recoveries of 80 to 99 %. Limits of detection were between 0.1 and 1.9 ng L(-1) for water samples and from 0.1 to 1.4 ng g(-1) for sediment samples. The developed method was applied to environmental samples and revealed the presence of UV filters in the majority of the surface waters with up to 690 ng L(-1) of 2-hydroxy-4-methoxybenzophenone. By contrast, ketoprofen (≤2,900 ng L(-1)) and its degradation products (≤320 ng L(-1)) were found in only two rivers, both receiving wastewater treatment plant effluents. Sediment analysis revealed benzophenone to be present in concentrations up to 650 ng g(-1), whereas concentrations of other compounds were considerably lower (≤32 ng L(-1)). For the first time, quantifiable amounts of two ketoprofen transformation products in the aqueous environment are reported.
- Effects of ketoprofen for prevention of postoperative cognitive dysfunction in aged rats. [JOURNAL ARTICLE]
- J Anesth 2014 Mar 28.
Postoperative cognitive dysfunction is a common geriatric complication that may be associated with increased mortality. Here, we investigated the effects of postoperative analgesia with ketoprofen on cognitive functions in aged animals and compared its effectiveness to morphine. Rats were randomly allocated to one of four groups: isoflurane anesthesia without surgery (group C), isoflurane anesthesia with laparotomy (group IL), and isoflurane anesthesia with laparotomy plus postoperative analgesia with ketoprofen or morphine. There was no difference in postoperative locomotor activity among groups. In group IL, postoperative pain levels assessed by the Rat Grimace Scale significantly increased until 8 h after surgery, which was similarly inhibited by both ketoprofen and morphine. Cognitive function was assessed using radial arm maze testing for 12 consecutive days from postoperative day 3. Results showed that the number of memory errors in group IL were significantly higher than those in goup C. However, both ketoprofen and morphine could attenuate the increase in memory errors following surgery to a similar degree. Conversely, ketoprofen showed no effect on cognitive function in the nonsurgical rats that did not experience pain. Our findings suggest that postoperative analgesia with ketoprofen can prevent the development of surgery-associated memory deficits via its pain-relieving effects.
- Effects of castration method and frequency of intramuscular injections of ketoprofen on behavioral and physiological indicators of pain in beef cattle. [Journal Article]
- J Anim Sci 2014 Apr; 92(4):1686-97.
Two experiments were conducted to determine the effect of a single or multiple intramuscular (i.m.) injection of ketoprofen and castration technique on physiological and behavioral indicators of pain in beef calves. A total of 150 bull calves (284.8 ± 22.7 kg BW) were used in both experiments, each 1 conducted as a 3 × 2 factorial design, where main factors included castration technique-no castration (CT), surgical (SU), or band (BA)-and drug administration-physiological solution (PS) or i.m. injection of ketoprofen (KP; 3 mg Anafen/kg BW) in the neck of calves. Animals were weighed weekly during the experiment to calculate ADG. Behavioral responses indicative of pain and discomfort during the castration procedure were documented using a visual analog score (VAS) by an experienced observer who was blind to the treatments. Movements of the animals in the chute during castration were quantified using a strain gauge system mounted on the head gate to evaluate the escape response of the cattle. Pens were equipped with an automated feed bunk monitoring system enabling feed intake and feeding behavior to be continuously monitored for each individual. Thermographic images of the scrotal area were evaluated 24 and 0.5 h before castration, 0.5, 1, 24, 48, and 270 h postcastration, and weekly thereafter until the end of the trial. Blood samples were obtained postcastration to evaluate changes in total white blood cell (WBC) count and neutrophil-to-lymphocyte (N:L) ratio. Saliva samples were taken 24 and 0.5 h before castration, immediately after castration, and 0.5, 1, 2, 5, 24, and 48 h and then 5, 7, and 14 d after castration to determine cortisol concentration. Scrotal temperature, VAS, total WBC, N:L ratio, salivary cortisol, mobility, and pressure exerted in the chute were greater (P < 0.05) and ADG and feed intake were lower (P < 0.05) in SU than in CT animals within the first week after castration. Also, BA calves had a greater (P < 0.05) scrotal temperature around wk 4 after castration and a lower feed intake and ADG at wk 2 and 3 and wk 6 and 7 after castration, respectively, compared to CT. Treatment KP had limited effects on reducing the indicators of pain associated with SU or BA, suggesting that further studies will be needed to assess the posology of the i.m. administration of ketoprofen to improve the consistency of its effects as a pain mitigation strategy after castration.
- [Nonspecific low-back pain: from symptomatic treatment to pathogenesis-based treatment]. [English Abstract, Journal Article]
- Zh Nevrol Psikhiatr Im S S Korsakova 2014; 114(2):51-5.
To study the efficacy and safety of artrosilene in the combination with piascledine in patients with low-back pain.Sixty patients, 42 women and 18 men (mean age 53,6±10,4 years) with chronic nonspecific low-back pain were treated with artrosilene (ketoprofen lysine salt) in the combination with the chondro protector piascledine (a mix of avocado and soybean oil extracts).There the persistent decrease in the intensity of pain syndrome and severity of vertebral syndrome and improvement of quality of life.The drugs can be recommended for treatment of nonspecific low-back pain.
- Removal and fate of micropollutants in a sponge-based moving bed bioreactor. [JOURNAL ARTICLE]
- Bioresour Technol 2014 Mar 5.:311-319.
This study investigated the removal of micropollutants using polyurethane sponge as attached-growth carrier. Batch experiments demonstrated that micropollutants could adsorb to non-acclimatized sponge cubes to varying extents. Acclimatized sponge showed significantly enhanced removal of some less hydrophobic compounds (logD<2.5), such as ibuprofen, acetaminophen, naproxen, and estriol, as compared with non-acclimatized sponge. The results for bench-scale sponge-based moving bed bioreactor (MBBR) system elucidated compound-specific variation in removal, ranging from 25.9% (carbamazepine) to 96.8% (β-Estradiol 17-acetate) on average. In the MBBR system, biodegradation served as a major removal pathway for most compounds. However, sorption to sludge phase was also a notable removal mechanism of some persistent micropollutants. Particularly, carbamazepine, ketoprofen and pentachlorophenol were found at high concentrations (7.87, 6.05 and 5.55μg/g, respectively) on suspended biosolids. As a whole, the effectiveness of MBBR for micropollutant removal was comparable with those of activated sludge processes and MBRs.
- Relationship Between Blood Levels and the Anti-Hyperalgesic Effect of Ketoprofen in the Rat. [JOURNAL ARTICLE]
- Drug Dev Res 2014 Jan 21.
Preclinical Research The relationship between blood levels of ketoprofen and its anti-hyperalgesic effects was examined in rat using the carrageenan-evoked thermal hyperalgesia model. Female adult Wistar rats were injected with carrageenan into the plantar surface of the right hind paw. Immediately after, rats were administered with ketoprofen po and hindpaw withdrawal latency measured and micro-whole blood samples were obtained over six hours via a cannula inserted in the caudal artery. Ketoprofen levels were measured by HPLC. Ketoprofen concentration increased in a dose-dependent manner and was reflected in dose-dependent anti-hyperalgesic effect. The pharmacokinetic and pharmacodynamic parameters expressed as mean ± s.e.m. following administration of 1, 3.2, and 10 mg/kg ketoprofen were: Cmax 1.27 ± 0.08, 3.44 ± 0.20 and 11.76 ± 0.81 μg/mL; AUClast 4.16 ± 0.17, 11.63 ± 0.65 and 28.15 ± 1.32 μg h/mL; and Emax observed (AUCE ): 65.41 ± 7.79, 92.06 ± 6.46 and 98.42 ± 7.53%. A direct relationship between blood concentrations and the anti-hyperalgesic effect of ketoprofen followed a maximum effect model equation. The results indicate that the anti-hyperalgesic effect of ketoprofen in the carrageenan pain model can be predicted by the pharmacokinetic properties of ketoprofen.