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1

Organ and prenatal toxicity of nonsteroidal anti-inflammatory drugs

100%

Dyndor K., Dworzanski W., Pliszczynska-Steuden M., Cendrowska-Pinkosz M., Chroscicki T., Dyndor P., Dworzanska A., Piasek E., Piech P., Ruchala M., Golec K., Hermanowicz-Dryka T.

Current Issues in Pharmacy and Medical Sciences

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2015

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vol. 28

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issue 3

200-203

EN

Non-selective cyclooxygenase (COX) inhibitors, commonly referred to as nonsteroidal anti-inflammatory drugs (NSAIDs), are among the most taken pharmaceuticals. In adults, they can have a series of side effects, including especially gastroenterotoxicity, hepatotoxicity, nephrotoxicity, chondrotoxicity, and neurotoxicity, and they can induce allergic reactions. Any exacerbation of symptoms depends on the chemical structure of the drug, its dosage and duration of exposure, individual sensitivity, comorbidities and the degree of inhibition of basic COX isoenzymes - the constitutive (COX-2) and induced (COX-1) expressions. However, data on prenatal toxicity are inconsistent. Classic nonselective COX inhibitors do not result in an increase in the risk of developing significant congenital defects; however, if used in the late-pregnancy period, they can have an adverse effect on the foetus, by inducing the premature closure of the ductus arteriosus and by producing a tocolytic effect. Individual reports also indicate the increased risk of developing heart and anterior abdominal wall defects, as well as hypospadias.

2

Changes of nitric oxide system and lipid peroxidation parameters in the digestive system of rats under conditions of acute stress, and use of nonsteroidal anti-inflammatory drugs

88%

Fomenko I., Bondarchuk T., Emelyanenko V., Denysenko N., Pavlo S., Ilkiv I., Lesyk R., Sklyarov A.

Current Issues in Pharmacy and Medical Sciences

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2015

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vol. 28

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issue 1

37-41

EN

The use of nonsteroidal anti-inflammatory drugs (NSAIDs) in combination with being physiologically stressed often occurs in in the course of different pathologies. This situation may result in the alteration of digestive system functioning. The effect of stress brings about changes in the activity of nitric oxide synthase (NOS), arginase, cyclooxygenase (COX) and lipid peroxidation, whereas the use of NSAIDs interrupts the multiple functions of the cell via the inhibition of prostaglandins (PGs) synthesis. Taking into account that NOS and COX-systems are connected in their regulation, the aim of the study was to determine the role played by NOS and lipid peroxidation under conditions of the combined action of NSAIDs and stress. In our study, male rats were used. The NSAIDs (naproxen - a non-selective COX inhibitor, celecoxib - a selective COX-2 blocker, and the compound 2A5DHT (which is the active substance of dual COX, and the lipoxygenase (LOX) inhibitor, darbufelone) were all administered at a dose 10 mg/kg, prior to water restraint stress (WRS). WRS brought about an increase of inducible NOS (iNOS) activity in the intestinal mucosal and muscular membranes, as well as in the pancreas. Because of this, constitutive NOS izoform (cNOS) and arginase activities decreased. Moreover, the MDA concentration increased, indicating the development of oxidative stress. In our work, pretreatment with naproxen, as in the WRS model, engendered a decrease in iNOS activity. What is more, administration of Celecoxib did not change iNOS activity, as compared to WRS alone, and it showed a tendency to reduce lipid peroxidation. In addition, 2A5DHT prior WRS brought about a decrease of iNOS activity, with the subsequent rise of cNOS activity. Of note, MDA concentration decreased in all studied organs, indicating the reduction of lipid peroxidation under the action of the darbufelone active substance.

3

Consumption and awareness of students about nonsteroidal anti-inflammatory drugs

88%

Wawryk-Gawda E., Chylinska-Wrzos P., Lis-Sochocka M., Jodlowska-Jedrych B.

Current Issues in Pharmacy and Medical Sciences

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2014

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vol. 27

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issue 3

175-178

EN

Nonsteroidal anti-inflammatory drugs (NSAIDs) are used by millions of people worldwide to neutralize pain that is of different origin, as well as to treat fever and inflammation. However, NSAIDs misuse/overuse can induce many adverse effects and some potentially serious complications. The aim of the our study was to ascertain young people’s knowledge about non-steroidal anti-inflammatory drugs. The research tool was a questionnaire. This study was carried out among students of the Medical University in Lublin, and it involved 236 persons of an average age of 20 years. The questions were intended to assess the frequency of NSAIDs use and the general knowledge that is held with respect to them. The results of this work show that more than 77% of the respondents confirmed that they use NSAIDs. Our results revealed no statistical correlation between the place of living or origin and the use of this drug. Hence, it can be said that while young adults quite often use NSAIDs, their knowledge about the dangers associated with the use of NSAIDs is low. Therefore, it is necessary to more intensively disseminate knowledge on the potential adverse effects of NSAID utilization.

4

Synthesis, COX-1/2 inhibition and antioxidant activities of new oxicam analogues designed as potential chemopreventive agents

75%

Szczęśniak-Sięga B., Gębczak K., Gębarowski T., Maniewska J.

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2018

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vol. 65

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issue 2

199-207

EN

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.

5

Endoplasmic reticulum stress response in the roadway for the effects of non-steroidal anti-inflammatory drugs

63%

Mügge F. L. B., Silva A. M.

Endoplasmic Reticulum Stress in Diseases

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2015

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vol. 2

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issue 1

EN

Over the past decade, a handful of evidence has been provided that nonsteroidal anti-inflammatory drugs (NSAIDs) display effects on the homeostasis of the endoplasmic reticulum (ER). Their uptake into cells will eventually lead to activation or inhibition of key molecules that mediate ER stress responses, raising not only a growing interest for a pharmacological target in ER stress responses but also important questions how the ER-stress mediated effects induced by NSAIDs could be therapeutically advantageous or not. We review here the toxicity effects and therapeutic applications of NSAIDs involving the three majors ER stress arms namely PERK, IRE1, and ATF6. First, we provide brief introduction on the well-established and characterized downstream events mediated by these ER stress players, followed by presentation of the NSAIDs compounds and mode of action, and finally their effects on ER stress response. NSAIDs present promising drug agents targeting the components of ER stress in different aspects of cancer and other diseases, but a better comprehension of the mechanisms underlying their benefits and harms will certainly pave the road for several diseases’ therapy.

6

Oznaczanie niesteroidowych leków przeciwzapalnych w surowicy ludzkiej techniką GC/MS: optymalizacja procedury ekstrakcyjnej leków

63%

Kurkiewicz S., Dzierżęga-Lęcznar A., Stępień K.

Annales Academiae Medicae Silesiensis

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2011

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vol. 65

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issue 3

28-33

EN

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.

PL

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.

7

The treatment of severe chronic pain in an elderly patient - case report

51%

Kocot-Kępska M., Przeklasa-Muszyńska A., Dobrogowski J.

Ból

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2014

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vol. 15

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issue 2

42-47

EN

Chronic pain is a disease in its own right and requires a multimodal treatment including pharmacotherapy, interventional procedures, rehabilitation, psychotherapy and neuromodulation. Multimodal pharmacotherapy remains the main and best available method of symptomatic chronic pain treatment. In clinical practice, the choice of analgesics is based on the pharmacological properties, the risk of side effects, ease of use, and availability of the drug,. A special group of patients with chronic pain are elderly patients in whom, due to changes in the pharmacokinetics of drugs, many limitations and contraindications to the use of analgesics are present. In the paper an elderly patient suffering from severe pain was described, in whom the use of drugs with different mechanisms of action in the transdermal and topical form provided the effective pain control while minimizing risk of side effects.

PL

Ból przewlekły jest chorobą samą w sobie, wymaga kompleksowego leczenia z uwzględnieniem farmakoterapii, zabiegów interwencyjnych, rehabilitacji, psychoterapii oraz neuromodulacji. Farmakoterapia multimodalna pozostaje nadal główną i najbardziej dostępną metodą leczenia objawowego bólu przewlekłego. W praktyce klinicznej wybór analgetyków opiera się na własnościach farmakologicznych leku, ryzyku objawów niepożądanych, łatwości stosowania leku oraz jego dostępności. Szczególną grupę pacjentów z bólem przewlekłym stanowią osoby w wieku podeszłym, u których ze względu na zmiany w farmakokinetyce leków istnieje wiele ograniczeń i przeciwwskazań do stosowania analgetyków. W pracy opisano pacjentkę w wieku podeszłym cierpiącą z powodu silnego bólu, u której zastosowanie leków o różnym mechanizmie działania aplikowanych w postaci przezskórnej pozwoliło na skuteczną kontrolę bólu przy zminimalizowanym ryzyku objawów niepożądanych.

Refine search results

Organ and prenatal toxicity of nonsteroidal anti-inflammatory drugs

Changes of nitric oxide system and lipid peroxidation parameters in the digestive system of rats under conditions of acute stress, and use of nonsteroidal anti-inflammatory drugs

Consumption and awareness of students about nonsteroidal anti-inflammatory drugs

Synthesis, COX-1/2 inhibition and antioxidant activities of new oxicam analogues designed as potential chemopreventive agents

Endoplasmic reticulum stress response in the roadway for the effects of non-steroidal anti-inflammatory drugs

Oznaczanie niesteroidowych leków przeciwzapalnych w surowicy ludzkiej techniką GC/MS: optymalizacja procedury ekstrakcyjnej leków

The treatment of severe chronic pain in an elderly patient - case report