Temat: NSAIDs - Prolib Integro

Skocz do pozycji: 1.

Tytuł:: Hypersensitivity to aspirin : common eicosanoid alterations in urticaria and asthma
Autorzy:: Mastalerz, Lucyna
Szczeklik, Andrzej
Setkowicz, Małgorzata
Sanak, Marek
Opis:: Background: Aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs) can precipitate adverse reactions in two apparently different clinical conditions: bronchial asthma and chronic idiopathic urticaria (CIU). Recent evidence indicates that the reactions are triggered by the drugs that inhibit cyclooxygenase-1 but not cyclooxygenase-2. Objective: To assess whether patients with CIU and aspirin sensitivity share common eicosanoid alterations with patients who have aspirin-sensitive asthma. Methods: Seventy-four patients with CIU and a history of sensitivity to aspirin and NSAIDs underwent placebocontrolled oral aspirin challenge tests. Concentrations of urinary leukotriene E4 (uLTE4) were measured by ELISA and plasma stable prostaglandin D2 metabolite, 9a,11b prostaglandin F2 by GC/MS. All measurements were carried out at baseline and after aspirin dosing. Patients were genotyped for the leukotriene C4 synthase (LTC4S) promoter single nucleotide polymorphism. Results: In 30 of 74 patients, the aspirin challenge was positive, resulting in urticaria/angioedema. In these 30 patients, baseline uLTE4 levels were higher than in nonresponders and the healthy control subjects and increased further (significantly) after the onset of clinical reaction. No such increase occurred in subjects with negative aspirin challenge. Baseline uLTE4 levels correlated with severity of skin reactions. Plasma 9a,11b prostaglandin F2 levels rose significantly in both aspirin responders and nonresponders, although in the latter group the increase occurred later than in the former. In patients who reacted to aspirin, frequency of e444C allele of LTC4S was significantly higher than in patients who did not react. Conclusions: CIU with aspirin sensitivity is characterized by the eicosanoid alterations, which are similar to those present in aspirin-induced asthma.
Dostawca treści:: Repozytorium Uniwersytetu Jagiellońskiego

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Skocz do pozycji: 2.

Tytuł:: Synthesis, COX-1/2 inhibition and antioxidant activities of new oxicam analogues designed as potential chemopreventive agents
Autorzy:: Szczęśniak-Sięga, Berenika
Gębczak, Katarzyna
Gębarowski, Tomasz
Maniewska, Jadwiga
Tematy:: synthesis
chemoprevention
antioxidant
COX
NSAIDs
oxicams; Pokaż więcej
Wydawca:: Polskie Towarzystwo Biochemiczne
Powiązania:: https://bibliotekanauki.pl/articles/1038390.pdf Link otwiera się w nowym oknie
Opis:: Oxicams (e.g. piroxicam, meloxicam) are widely used nonsteroidal anti-inflammatory drugs (NSAIDs). A large body of evidence from epidemiological and preclinical studies has shown that NSAIDs have a chemopreventive effect on different types of cancer, especially in colorectal cancer. Moreover, mounting evidence from preclinical and clinical studies suggests that persistent inflammation functions as a driving force in the journey to cancer. What is more, inflammation induces reactive oxygen and nitrogen species, which cause damage to important cellular components (e.g., DNA, proteins and lipids), which can directly or indirectly contribute to malignant cell transformation. In this study, we discuss the synthesis and the resultant newly synthesized oxicam derivatives which are potentially chemopreventive, and at the same time antioxidant. Compound 9c, with the highest therapeutic index in the LoVo cancer cell line, was found to be the most efficient in ROS scavenging activity under conditions of oxidative stress.
Dostawca treści:: Biblioteka Nauki

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Skocz do pozycji: 3.

Tytuł:: Optimization of energy recovery processes from sunflower stalks using expired non-steroidal anti-inflammatory drugs (NSAIDs)
Autorzy:: Zubkova, Valentina
Baran, Stanisław
Strojwas, Andrzej
Opis:: The influence of the addition of expired paracetamol, naproxen, ibuprofen, and their blend on the course of pyrolysis of sunflower stalks was studied using the gravimetric technique as well as the techniques of IR and UV, XRD, and SEM and EDX spectroscopies. It was ascertained that ibuprofen has the highest effect in reduction of hydrocarbons in the composition of volatile pyrolysis products, which lowers the contribution of bands: saturated and unsaturated hydrocarbons by about 2.36 times; compounds with carbonyl groups by almost by three times; and the contribution of alcohols, phenols, and esters by 2.5 times in the FT-IR spectra. The reasons for a greater effectiveness of ibuprofen in reducing hydrocarbons in volatiles can be its lower temperature of decomposition and distinct composition of formed volatile pyrolysis products. Up to the temperature of 450 °C, paracetamol inhibits the migration of AAEMs from the pyrolyzed sample, the blend of pharmaceuticals accelerates the migration of all AAEMs except inorganics with Mg atoms. In the sediment of char of ibuprofen additive, there is a higher amount of Ca, Mg, and Cl atoms than in other chars, which can explain a greater influence of ibuprofen on the reduction of hydrocarbons in the composition of volatiles.
Dostawca treści:: Repozytorium Uniwersytetu Jagiellońskiego

Artykuł

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Skocz do pozycji: 4.

Tytuł:: A paradigm shift in the role of NSAIDs in COVID-19: new pathological mechanisms and potential treatment targets
Autorzy:: Ilie, Petre Cristian
Stefanescu, Simina
Veronese, Nicola
Tematy:: Paradigm Shift
NSAIDs
Covid-19
COX-2 inhibitors; Pokaż więcej
Wydawca:: Atena Research Association
Powiązania:: https://bibliotekanauki.pl/articles/1491092.pdf Link otwiera się w nowym oknie
Opis:: Objectives: The pathogeny of SARS-COV2 infection is currently not well defined. In this paper, we present a new perspective of how the SARS-CoV2 infection can lead to severe cases and potential pathways of preventing such cases. Methods: In the first part, we describe the role of cyclooxigenase 2 and in the second part, we describe the role of hypoxia inducible factor (HIF). Findings: We hypothesize that cyclooxigenase 2 and hypoxia inducible factor with subsequent inflammation and hypoxia can up-regulate each other in a vicious circle of feed-forward that can ultimately lead to “cytokine storm”. Conclusions: Breaking this cycle early potentially will have beneficial effects either by improving oxygenation (oxygen being given earlier in the course of the treatment) or by inhibiting COX-2. We also believe, that the use of COX-2 inhibitors early in the course of the disease can improve the outcome and clinical trial are urgently needed.
Dostawca treści:: Biblioteka Nauki

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Skocz do pozycji: 5.

Tytuł:: Evaluation of anti-inflammatory and ulcerogenic potential of zinc-ibuprofen and zinc-naproxen complexes in rats
Autorzy:: Librowski, Tadeusz
Marona, Henryk
Nowak, Gabriel
Gaweł, Magdalena
Szkaradek, Natalia
Młyniec, Katarzyna
Opis:: Because of numerous indications and high availability, non-steroidal anti-inflammatory drugs (NSAIDs) are among the most commonly prescribed and used medicines in the world. However, long-term therapy with and improper use of NSAIDs may lead to gastrointestinal damage. Therefore, improving the therapeutic index of the existing drugs has become a priority over the past decades. Considerable attention in the field has been concentrated on metal complexes of non-steroidal anti-inflammatory drugs. The aim of this study is to evaluate the effect of complexation with zinc on the anti-inflammatory and ulcerogenic effects of ibuprofen and naproxen after single and triple intragastric administration to rats. The anti-inflammatory effect was assessed in carrageenan-induced inflammatory edema in the hind paw of male albino Wistar rats. The mucosal lesions were inspected and evaluated for gross pathology. Single administration of both the investigated complexes, namely zinc-ibuprofen and zinc-naproxen (20 mg/kg equivalent to ibuprofen and naproxen, respectively) and their parent drugs and physical mixtures with zinc hydroaspartate (ZHA doses: 16.05 and 14.37 mg/kg), caused a significant reduction of the edema after the same time from the carrageenan injection in comparison to the control groups. However, no statistically significant differences between the investigated drugs were observed after their single administration. The mean ulceration score for the mixture of ibuprofen and ZHA was statistically lower than the mean score achieved in rats after treatment with ibuprofen alone. On the other hand, triple intragastric administration of the ZHA-ibuprofen and ZHA- naproxen combination showed substantial enhancement of the anti-inflammatory activity against control groups, as well as against the parent NSAIDs. The most potent anti-inflammatory activity was demonstrated after 2 h from the carrageenan injection in animals receiving ZHA together with naproxen. The edema growth was reduced in these animals by 80.9% as compared to the control group. This result was significantly higher than the results achieved in animals receiving zinc-naproxen (50.2%) or naproxen alone (47.9%). Both NSAID complexes with zinc and mixtures with ZHA alleviated ulcerations caused by parent NSAIDs; however, the mixtures of both ibuprofen and naproxen with ZHA after triple administration were the least damaging. In view of the above results, zinc supplementation during NSAID therapy may have a beneficial effect on ulcer prevention and healing by reducing the effective dose of the parent drug and increasing its potency.
Dostawca treści:: Repozytorium Uniwersytetu Jagiellońskiego

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Skocz do pozycji: 6.

Tytuł:: Assessment of Lipophilicity Descriptors of Selected NSAIDs Obtained at Different TLC Stationary Phases
Autorzy:: Plenis, Alina
Starek, Małgorzata
Zagrobelna, Marta
Dąbrowska, Monika
Opis:: Lipophilicity study of selected NSAIDs, the group of the bioactive compounds usually used in humans and animals medicine, with the use of experimental and calculation methods was evaluated. LogP values are proposed and compared as descriptors of the lipophilicity of eleven compounds (from oxicams and coxibs). Obtained data were designated by thin-layer chromatography (TLC) in various chromatographic conditions, with stationary phases with different properties. The mobile phase systems were prepared by mixing the respective amounts of water and organic modifier, methanol and acetone, in the range of 30 to 80% (v/v) in 5% increments. Retention parameters (R$_{F}$, R$_{M}$ and R$_{M0}$) were calculated and statistically evaluated to establish correlations. All experimentally determined R$_{M0}$ values were compared with partition coefficients obtained by computational methods using linear regression analysis. Moreover, in order to extract information about the lipophilicity of compounds from large retention datasets, two chemometric approaches, namely principal component analysis (PCA) and cluster analysis (CA) were carried out. Established models of lipophilicity may have the potential to predict the biological activity of a number of drugs. The presented knowledge may also be of use during drug discovery processes, broadening the knowledge of potential ways to modify the physicochemical properties of chemical compounds.
Dostawca treści:: Repozytorium Uniwersytetu Jagiellońskiego

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Skocz do pozycji: 7.

Tytuł:: Ocena wpływu wielokrotnego podania wodoroasparginianu cynku na aktywność przeciwzapalną ketoprofenu
The evaluation of influence of repeated administration of zinc hydroaspartate on anti-inflammatory activity of ketoprofen.
Autorzy:: Lipkowska, Anna
Opis:: Nonsteroidal anti-inflammatory drugs are commonly used as analgesics and antipyretic drugs. Despite their availability they are not devoid of side effects, especially from the digestive system. Zinc is one of the most important microelements in human body. It influences on functions of many systems and organs. Even small deficiency of this element results in disturbances of various systems i.a. the digestive or immunological system. It was investigated its beneficial effect on the inflammatory process. The aim of this study was to evaluate the influence of multiple administration of zinc hydroaspartate on anti-inflammatory and analgesic activity of ketoprofen and its impact on gastric mucosa. Tests were carried out on rats, male Wistar. The study lasted 14 days. During this time rats were recived zinc hydroaspartate in three ways: ip dissolved in water, po dissolved in water and po dissolved in 0,5% methylcellulose solution. To determine anti-inflammatory activity of ketoprofen was used a method consisting of 4-measurement of paw edema after carragen injection (before injectione, in 1st, 2nd, and 3rd hour after injection). The analgesic activity was measured by using analgesymetr in 3rd hour after injection. The following results were obtained. It was shown statistically significant in antiedematous activity of ketoprofen according to the way of administration of zinc hydroaspartate. Zinc hydroaspartate dissolved in water and given per os increased antiedematous activity of ketoprofen, while zinc hydroaspartate given in methylcellulose solution decreased drug activity. The dose-dependence of ketoprofen wasn’t observed. The best results were obtained for the ketoprofen used in dose of 10 mg/kg b.w. It was observed that ketoprofen had the supreme antiedematous activity in 2nd hour after administration. Conducted studies do not give the unequivocal answer about gastroprotective activity of zinc hydroaspartate. Its influence on gastric mucosa is dependent on the way of administration and the type of solvent.
Niesteroidowe leki przeciwzapalne są powszechnie stosowane jako środki przeciwbólowe i przeciwgorączkowe. Pomimo ich dostępności nie są one pozbawione działań niepożadanych, szczególnie ze strony przewodu pokarmowego. Cynk jest jednym z najważniejszych mikroelementów w ludzkim organizmie. Wpływa na funkcje wielu układów i narządów. Już niewielki niedobór tego pierwiastka skutkuje zaburzeniami m. in. Układu pokarmowego czy immunologicznego. Doświadczalnie wykazano korzystny wpływ cynku na przebieg procesu zapalnego. Celem niniejszej pracy była ocena wpływu wielokrotnego podania wodoroasparaginianu cynku na aktywność przeciwzapalna i przeciwbólową ketoprofenu oraz jego wpływu na błonę śluzową zołądka. Badania przeprowadzono na szczurach, samcach rasy Wistar. Eksperyment trwał 14 dni. Przez ten czas szczury otrzymywały wodoroasparaginian: ip rozpuszczony w wodzie, po ropuszczony w wodzie oraz po rozpuszczony w 0.5% roztworze metylocelulozy. W 14 dniu podawano po ketoprofen. Do oznaczania aktywności przeciwzapalnej wykorzystano metodę 4-krotnego pomiaru obrzęku po wstrzyknięciu karagenu (przed wstrzyknięciem, po 1,2 i 3 godzinie od podania). Aktywność przeciwbólową mierzono przy uzyciu analgezymetru w trzeciej godzinie od iniekcji. Otrzymano następujące wyniki. Wykazano statystycznie istotne różnice w aktywności przeciwobrzękowej ketoprofenu zależnie od sposobu podania wodoroasparaginianu cynku. Wodoroasparaginian rozpuszczony w wodzie i podawany po nasilał aktywność przeciwobrzękową ketoprofenu, natomiast wodoroasparaginian rozpuszczony roztworze metylocelulozy osłabiał działanie leku. Nie zaobserwowano natomiast dawkozależności ketoprofenu. Najlepsze wyniki uzyskano dla dawki 10mg/kg m.c. Zauważono, że ketoprofen wykazywał nasilniejszą aktywność przeciwobrzękową w 2 godzinie od podania. Przeprowadzone badania nie pozwalają jednoznacznie określić gastroprotekcyjnego działania wodoroasparaginianu cynku. Zależnie od drogi podania i rozpuszczalnika uzyskano różny wpływ na błonę śluzową żołądka.
Dostawca treści:: Repozytorium Uniwersytetu Jagiellońskiego

Inne

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Skocz do pozycji: 8.

Tytuł:: Ketoprofen – miejscowe leczenie przeciwbólowe i przeciwzapalne
Ketoprofen – Local Treatment for Pain Relief and Anti-Inflammation
Autorzy:: Kuthan, Robert
Tematy:: Ketoprofen
topical application
pain relief
nonsteroidal anti-inflammatory drug (NSAIDs; Pokaż więcej
Wydawca:: Wydawnictwo Naukowe Medyk sp. z o.o.
Powiązania:: https://bibliotekanauki.pl/articles/32374875.pdf Link otwiera się w nowym oknie
Opis:: Artykuł omawia skuteczność ketoprofenu, niesteroidowego leku przeciwzapalnego, stosowanego miejscowo w łagodzeniu bólu związanego z różnymi schorzeniami, takimi jak urazy sportowe, zapalenie stawów czy ból kręgosłupa. Badania kliniczne potwierdzają jego efektywność w redukcji dolegliwości bólowych u dorosłych i dzieci w porównaniu do placebo oraz innych substancji terapeutycznych. Mechanizm działania ketoprofenu opiera się na hamowaniu enzymów COX-1 i COX-2 oraz redukcji produkcji prostaglandyn, co zmniejsza objawy zapalenia. Miejscowe stosowanie ketoprofenu pozwala na osiągnięcie wysokich stężeń leku w obszarze bólu przy minimalnym narażeniu ogólnoustrojowym, a to sprzyja skutecznemu łagodzeniu bólu. Dodatkowo artykuł podkreśla korzyści z zastosowania ketoprofenu miejscowo w leczeniu bólu związanego z zabiegami stomatologicznymi i ortodontycznymi.
The article discusses the effectiveness of ketoprofen, a nonsteroidal anti-inflammatory drug used topically, in alleviating pain associated with various conditions such as sports injuries, joint inflammation, and back pain. Clinical studies confirm its efficacy in reducing pain symptoms in adults and children compared to placebo and other therapeutic substances. The mechanism of action of ketoprofen is based on inhibiting COX-1 and COX-2 enzymes and reducing prostaglandin production, which alleviates inflammation symptoms. Topical application of ketoprofen allows for achieving high drug concentrations in the pain area with minimal systemic exposure, promoting effective pain relief. Additionally, the article highlights the benefits of using ketoprofen topically in treating pain associated with dental and orthodontic procedures.
Dostawca treści:: Biblioteka Nauki

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Skocz do pozycji: 9.

Autorzy:: Mullol, Joaquim
Hagemann, Jan
Sanak, Marek
Bobolea, Irina
Klimek, Ludger
Dostawca treści:: Repozytorium Uniwersytetu Jagiellońskiego

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Skocz do pozycji: 10.

Tytuł:: Oznaczanie niesteroidowych leków przeciwzapalnych w surowicy ludzkiej techniką GC/MS: optymalizacja procedury ekstrakcyjnej leków
GC/MS determination of non-steroidal anti-infl ammatory drugs in human serum: an optimization of the drug extraction procedure
Autorzy:: Kurkiewicz, Sławomir
Dzierżęga-Lęcznar, Anna
Stępień, Krystyna
Tematy:: gc/ms
sililacja
ekstrakcja do fazy stałej
nlpz
silylation
spe
serum
nsaids; Pokaż więcej
Wydawca:: Śląski Uniwersytet Medyczny w Katowicach
Powiązania:: https://bibliotekanauki.pl/articles/1038346.pdf Link otwiera się w nowym oknie
Opis:: Determination of non-steroidal anti-infl ammatory drugs (NSAIDs) in human and animal physiological fl uids requires the use of appropriate pro-cedures permitting rapid and effi cient recovery of the drugs from biological matrices. The aim of this study was to compare various methods of NSAIDs extraction from human serum that is essential for GC/MS analysis of the drugs. Commercially available biochemistry control human serum supplemented with ibuprofen, paracetamol, fl urbiprofen, nabumeton, naproxen, ketoprofen, mefenamic acid and diclofenac sodium salt was used. Solid phase extraction, HybridSPE- -PPT technology and liquid-liquid extraction were applied for NSAIDs isolation from the serum. GC/MS analysis of the drugs was preceded by their derivatization to trimethylsilyl esters with BSTFA. The highest extraction effi ciency and the best separation of the drugs from endogenous components of the serum were achieved using the solid phase extraction on octadecyl-bonded silica.
Oznaczanie niesteroidowych leków przeciwzapalnych (NLPZ) w płynach fizjologicznych ludzi i zwierząt wymaga zastosowania szybkich i wydajnych procedur izolacji tych leków z biologicznej matrycy. Celem pracy było porównanie różnych metod ekstrakcji NLPZ z surowicy ludzkiej, jako etapu poprzedzającego analizę tych leków techniką GC/MS. W badaniach wykorzystano dostępną handlowo surowicę stosowaną jako materiał kontrolny w oznaczeniach biochemicznych, do której dodano ibuprofen, paracetamol, flurbiprofen, nabumeton, naproksen, ketoprofen, kwas mefenamowy oraz sól sodową diklofenaku. W celu wyizolowania NLPZ z surowicy zastosowano ekstrakcję do fazy stałej, technikę HybridSPE- -PPT oraz ekstrakcję ciecz-ciecz. Leki poddano derywatyzacji do pochodnych trimetylosililowych za pomocą BSTFA, a następnie analizowano techniką GC/MS. Najwyższą wydajność ekstrakcji oraz najlepszy stopień oddzielenia NLPZ od endogennych składników surowicy uzyskano metodą ekstrakcji do fazy stałej w postaci żelu krzemionkowego z aktywnymi grupami oktadecylowymi.
Dostawca treści:: Biblioteka Nauki

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