scholarly journals The positive and negative effects of using transdermal nonsteroidal anti-inflammatory drugs: chemoreactome analysis

2020 ◽  
Vol 12 (5) ◽  
pp. 123-129
Author(s):  
I. Yu. Torshin ◽  
O. A. Gromova ◽  
T. R. Grishina ◽  
V. A. Semenov

Transdermal nonsteroidal anti-inflammatory drugs (NSAIDs) are actively used for mild and moderate pain syndrome, muscle contusions and sprains, sports injuries, and the widest range of musculoskeletal diseases. The transdermal administration of NSAIDs aims to create sufficiently high drug concentrations in the lesion focus, provided that the side effects associated with its systemic action are maximally reduced.Objective: to comparatively simulate the effects of transdermal NSAIDs.Material and methods. Chemoreactome profiling of six NSAIDs (meloxicam, diclofenac, ibuprofen, ketoprofen, nimesulide, and dexketoprofen) was performed. The pharmacological capabilities of molecules were analyzed within the framework of a chemoreactome methodology, by comparing the chemical structure of the studied molecule with those of millions of other molecules, the pharmacological properties of which had already been studied in experimental and clinical studies. Training the artificial intelligence algorithms based on the big data available in in the databases PubChem/PHARMGKB, HMDB, STRING, and others was done with multi-level training quality control in the cross validation framework according to the combinatorial theory of solvability and the theory of feature value classification.Results and discussion. Meloxicam versus other NSAIDs accumulates primarily in the muscles and skin and, to a much lesser extent, in heart tissues, lymphocytes, gonads, and cartilage. This drug showed the greatest dose-dependent decongestant effect in the model of edema induced by croton oil. Analysis of the systemic effects of NSAIDs indicated that meloxicam might affect the metabolism of vitamins A, D, PP, and B6 to a lesser extent than other NSAIDs.Conclusion. The chemoreactomе analysis has demonstrated that meloxicam as a gel causing minimal side effects can be used effectively and long.

2017 ◽  
pp. 9-14
Author(s):  
L. Nazarenko ◽  

The article discusses the pathogenetic basis for the use of non-steroidal anti-inflammatory drugs (NSPVP) in obstetric practice for the treatment of pain syndrome in women with threatened abortion and pathological preliminary period. Provided with modern views on the mechanisms of analgesic clinical efficacy, side effects NSPVP. Provides information about the place of NSPVP during pregnancy, the risks to the fetus, the positive aspects in the conduct of women at risk of preterm birth, the pathological preliminary period. Key words: nonsteroidal anti-inflammatory drug, pain, premature birth, preliminary period.


2020 ◽  
Vol 14 (2) ◽  
pp. 123-130
Author(s):  
E. A. Taskina ◽  
N. G. Kashevarova ◽  
L. I. Alekseeva

The paper provides a review of the data available in the literature on the relationship of pain to the risk of OA progression. Network analyses and numerous studies, including those conducted at the V.A. Nasonova Research Institute of Rheumatology, have confirmed that pain syndrome is one of the significant predictors of knee OA progression. The major class of medications for OA pain includes nonsteroidal anti-inflammatory drugs. The paper gives data on the efficacy of meloxicam in OA patients, which is widely used in both Russia and other countries of the world. Meloxicam is characterized by a good safety profile in the gastrointestinal tract, cardiovascular and renal systems. It is the drug of choice in patients with musculoskeletal diseases, in particular OA. Good results in severe pain syndrome have been shown by a step-by-step regimen of meloxicam when the injection formulation of the drug is used in the first days of treatment, and then, to consolidate what has been gained from therapy, its oral dosage form is administered in terms of concomitant diseases.


2021 ◽  
Vol 19 (1) ◽  
pp. 45-52
Author(s):  
L. Yu. Orekhova ◽  
L. P. Shayda ◽  
V. Yu. Vashneva ◽  
Yu. A. Sycheva ◽  
V. N. Rakhova ◽  
...  

Relevance. To date, the prescription of nonsteroidal anti-inflammatory drugs for the treatment of complicated forms of caries, accompanied by a pronounced pain syndrome, is still needed. The main criteria to be met by NSAIDs used by patients are: adequacy of clinical situation, safety, effectiveness. However, if the choice of therapeutic agent is made without taking into account the accompanying somatic pathology, there is a risk of harm to the patient's health, both on the recommendation of the attending physician, and when the patient himself using the drug. The use of NSAIDs in medical practice is often fraught with serious adverse events (AEs), primarily from the gastrointestinal tract (GIT), cardiovascular system (CVS), etc. The task of the doctor, who prescribes NSAIDs to the patient, is to minimize the negative effects of these drugs on digestive and cardiovascular system of the patient while achieving the optimal analgesic and anti-inflammatory effects.Aim. To study the peculiarities of non-steroidal anti-inflammatory drugs in the treatment of complicated caries in patients with concomitant somatic pathology.Materials and methods. Retrospective review of domestic and foreign publications, questionnaire survey of dentists concerning prescribed NSAIDs, and generalized recommendations for prescribing these drugs taking into account the features of general medical diseases were carried out.Results. Basing on literature data and own clinical observations, the most frequently prescribed drugs for pain reaction relief in patients with complicated forms of caries were singled out and recommendations for prescription of NSAIDs in patients with generalosomatic diseases were suggested.Conclusions. This work offers recommendations for the use of NSAIDs in dental patients with concomitant somatic pathology.


2021 ◽  
Vol 9 (C) ◽  
pp. 239-242
Author(s):  
Siti Salima ◽  
Ali Budi Harsono ◽  
Aisyah Aisyah ◽  
Kemala Mantilidewi

BACKGROUND: One of the harshest side effects following anticancer agent treatments is chemotherapy-induced neuropathic pain. After surgical staging, chemotherapy combination of paclitaxel carboplatin could be a choice of therapy for Stage II or more advanced stage of ovarian cancer. Different side effects may appear after the application of paclitaxel. CASE REPORT: Here, we show an uncommon case of paclitaxel-acute pain syndrome (P-APS), and how we deal with such cases according to our experiences. One uncommon side effect is P-APS, which can be treated effectively with the administration of non-steroidal anti-inflammatory drugs, corticosteroid, and supportive therapy. CONCLUSION: One uncommon side effect of Paclitaxel induced neuropathic can be treated effectively with the administration of non-steroidal anti inflammatory drugs, corticosteroid, and supportive therapy.


2020 ◽  
Author(s):  
Elin Nyman ◽  
Maria Lindh ◽  
William Lövfors ◽  
Christian Simonsson ◽  
Alexander Persson ◽  
...  

Both initiation and suppression of inflammation are hallmarks of the immune response. If not balanced, the inflammation may cause extensive tissue damage, which is associated with common diseases, e.g. asthma and atherosclerosis. Anti-inflammatory drugs often come with severe side effects driven by high and fluctuating drug concentrations. To remedy this, drugs with sustained anti-inflammatory responses are desirable. However, we still lack a quantitative mechanistic understanding of such sustained effects. Here, we study the anti-inflammatory response to a common glucocorticoid drug, Dexamethasone. We find a sustained response 22 hours after drug removal. With hypothesis testing using mathematical modeling, we unravel the underlying mechanism – a slow release of Dexamethasone from the receptor-drug complex. The developed model is in agreement with time-resolved training and testing data, and is used to simulate hypothetical treatment schemes. This work opens up for a more knowledge-driven drug development, to find sustained anti-inflammatory responses and fewer side effects.


Materials ◽  
2021 ◽  
Vol 14 (11) ◽  
pp. 2715
Author(s):  
Rodica Ana Ungur ◽  
Viorela Mihaela Ciortea ◽  
Laszlo Irsay ◽  
Alina Deniza Ciubean ◽  
Bogdana Adriana Năsui ◽  
...  

The non-steroidal anti-inflammatory drugs (NSAIDs) are the most used drugs in knee OA (osteoarthritis) treatment. Despite their efficiency in pain and inflammation alleviation, NSAIDs accumulate in the environment as chemical pollutants and have numerous genetic, morphologic, and functional negative effects on plants and animals. Ultrasound (US) therapy can improve pain, inflammation, and function in knee OA, without impact on environment, and with supplementary metabolic beneficial effects on cartilage compared to NSAIDs. These features recommend US therapy as alternative for NSAIDs use in knee OA treatment.


2019 ◽  
Vol 25 (1) ◽  
pp. 3-6 ◽  
Author(s):  
Manas A. Rane ◽  
Alexander Gitin ◽  
Benjamin Fiedler ◽  
Lawrence Fiedler ◽  
Charles H. Hennekens

Introduction: Nonsteroidal anti-inflammatory drugs (NSAIDs) include aspirin, naproxen, diclofenac, and ibuprofen, as well as selective cyclooxygenase 2 inhibitors such as celecoxib. Their use is common, as well as their side effects which cause 100 000 hospitalizations and 17 000 deaths annually. Recently, the US Food and Drug Administration strengthened its warning about the risks of cardiovascular disease (CVD) attributed to nonaspirin NSAIDs. Methods: When the sample size is large, randomization provides control of confounding not possible to achieve with any observational study. Further, observational studies and, especially, claims data have inherent confounding by indication larger than the small to moderate effects being sought. Results: While trials are necessary, they must be of sufficient size and duration and achieve high compliance and follow-up. Until then, clinicians should remain uncertain about benefits and risks of these drugs. Conclusions: Since the totality of evidence remains incomplete, health-care providers should consider all these aforementioned benefits and risks, both CVD and beyond, in deciding whether and, if so, which, NSAID to prescribe. The factors in the decision of whether and, if so, which NSAID to prescribe for relief of pain from inflammatory arthritis should not be limited to risks of CVD or gastrointestinal side effects but should also include potential benefits including improvements in overall quality of life resulting from decreases in pain or impairment from musculoskeletal pain syndromes. The judicious individual clinical decision-making about the prescription of NSAIDs to relieve pain based on all these considerations has the potential to do much more good than harm.


2021 ◽  
Vol 28 ◽  
Author(s):  
Josiane Viana Cruz ◽  
Joaquín María Campos Rosa ◽  
Njogu Mark Kimani ◽  
Silvana Giuliatti ◽  
Cleydson Breno Rodrigues dos Santos

: This article presents a simplified view of celecoxib as a potential inhibitor in the treatment of inflammatory diseases. The enzyme cyclooxygenase (COX) has, predominantly, two isoforms called cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX-2). The former plays a constitutive role that is related to homeostatic effects in renal and platelets, while the latter is mainly responsible for induction of inflammatory effects. Since COX-2 plays an important role in the pathogenesis of inflammatory diseases, it has been signaled as a target for the planning of anti-inflammatory intermediates. Many inhibitors developed and planned for COX-2 inhibition have presented side effects to humans, mainly in the gastrointestinal and/or cardiovascular tract. Therefore, it is necessary to design new potential COX-2 inhibitors, which are relatively safe and without side effects. To this end, of the generation of non-steroidal anti-inflammatory drugs from “coxibs”, celecoxib is the only potent selective COX-2 inhibitor that is still commercially available. Thus, the compound celecoxib became a commercial prototype inhibitor for the development of anti-inflammatory agents for COX-2 enzyme. In this review, we provide highlights where such inhibition should provide a structural basis for the design of promising new non-steroidal anti-inflammatory drugs (NSAIDs) which act as COX-2 inhibitors with lesser side effects on the human body.


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