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Nonsteroidal anti-inflammatory drugs: prostaglandins, indications, and side effects
Ippokratis Pountos, Theodora Georgouli, Howard Bird, et al
International Journal of Interferon, Cytokine and Mediator Research , 2011, DOI: http://dx.doi.org/10.2147/IJICMR.S10200
Abstract: nsteroidal anti-inflammatory drugs: prostaglandins, indications, and side effects Review (6182) Total Article Views Authors: Ippokratis Pountos, Theodora Georgouli, Howard Bird, et al Published Date January 2011 Volume 2011:3 Pages 19 - 27 DOI: http://dx.doi.org/10.2147/IJICMR.S10200 Ippokratis Pountos1, Theodora Georgouli1, Howard Bird2, Peter V Giannoudis1 1Academic Department of Trauma and Orthopaedics, School of Medicine, 2Section of Musculoskeletal Disease, Leeds Institute of Molecular Medicine, University of Leeds, Leeds, UK Abstract: For centuries, nonsteroidal anti-inflammatory drugs (NSAIDs) have been part of our clinical practice. They started out as drugs with anti-inflammatory and analgesic action, and gradually their use has been expanded to new therapeutic targets, some of which are unrelated to their primary mode of action. Today, our armamentarium includes a large range of compounds, attesting to their utility in the treatment of clinical pathologies ranging from pain and inflammation to prevention and treatment of cancer. On the other hand, although NSAIDs share many common properties, their use poses risks, and physicians should be cognizant of their subtle differences and potential complications. In this context, this review article presents insight into NSAIDs’ pathophysiology and mode of action in the clinical setting, their indications, and their potential side effects.
Synthesis and Characterization of Naproxen-Salicylate Derivatives as Potential Dual-Targeted Inhibitors of Dihydrofolate Reductase  [PDF]
Syon Schlecht, Emily Gunderson, Ruthie Fowler, Takara Aguilar
Advances in Biological Chemistry (ABC) , 2024, DOI: 10.4236/abc.2024.144008
Abstract: Dihydrofolate reductase (DHFR) is an enzyme that catalyzes the reduction of dihydrofolate (DHF) to tetrahydrofolate (THF). Chemotherapy drugs such as methotrexate help to slow the progression of cancer by limiting the ability of dividing cells to make nucleotides by competitively inhibiting DHFR. Nonsteroidal anti-inflammatory drugs (NSAIDs) have been previously reported to exhibit competitive inhibition of DHFR, in addition to their primary action on cyclooxygenase enzymes. This interaction interferes with the enzymatic reduction of dihydrofolate to tetrahydrofolate, thereby impeding the folate metabolism pathway essential for nucleotide synthesis and cell proliferation. This activity stems from their structural resemblance to the p-aminobenzoyl-l-glutamate (pABG) moiety of folate, a substrate of DHFR. It has been established that NSAIDs containing a salicylate group (which has structural similarities to pABG), such as diflunisal, exhibit stronger DHFR-binding activity. In this study, we synthesized salicylate derivatives of naproxen with the aim of exploring their potential as inhibitors of DHFR. The interactions between these derivatives and human DHFR were characterized using a combination of biochemical, biophysical, and structural methods. Through polyacrylamide gel electrophoresis (PAGE) analysis, enzymatic assays, and quantitative ELISA, we investigated the binding affinity and inhibitory potency of the synthesized salicylate derivatives towards DHFR. The findings of this study suggest the potential of salicylate derivatives of naproxen as promising candidates for the inhibition of DHFR, thereby offering novel therapeutic opportunities for modulating the inflammatory process through multiple pathways. Further optimization of these derivatives could lead to the development of more efficacious dual-targeted analogs with enhanced therapeutic benefits.
Health Related Quality of Life among Osteoarthritis Patients: A Comparison of Traditional Non-Steroidal Anti-Inflammatory Drugs and Selective COX-2 Inhibitors in the United Arab Emirates Using the SF-36  [PDF]
Mohammed Hassanein, Mohammed Shamssain, Nageeb Hassan
Pharmacology & Pharmacy (PP) , 2015, DOI: 10.4236/pp.2015.64025
Abstract: Objectives: Osteoarthritis (OA) has a dramatic impact on patients’ health related quality of life (HRQoL). Chronic use of analgesics and anti-inflammatory medications for pain management may improve symptoms but on long term may affect HRQoL negatively. The objective of the present study was to compare the impact of two different classes of analgesics, traditional non-steroidal anti-inflammatory drugs (NSAIDs) and selective cyclo-oxygenase-2 (COX-2) inhibitors on HRQoL among osteoarthritis patients using the SF-36 questionnaire. Methods: Clinic based cross-sectional study conducted at Al-Qassimi Hospital, Sharjah, United Arab Emirates (UAE), over a period of six months. Ethical Approval was obtained from the ethics committee at Al-Qassimi Clinical Research Center. Total of 200 osteoarthritis patients fulfilling the inclusion and exclusion criteria were involved in the study. Patients’ demographics were collected from their medical records. The Medical Outcome Study Short-Form 36 (SF-36) questionnaire was used to measure patients’ HRQoL. SF-36 data were scored using health outcomes scoring software 4.5. Results: Mean age of the subjects was 62.19 ± 9.81 years with females constituting 151 (75.5%) of the patients. In general, females scored lower in most of the HRQoL domains compared to males and there was significant difference between the two groups in the mental health (p = 0.005) & mental component (p = 0.042) domains. Compared to selective COX-2 inhibitors, patients on NSAIDs scored higher on all domains of SF-36 except physical functioning. There was significant difference in mental health domain for patients treated with NSAIDs (p = 0.02). Celecoxib was only better than NSAIDs in osteoarthritis patients with more than one musculoskeletal disorders in the domain of bodily pain (p = 0.009). Conclusion: NSAIDs-treated patients did not differ significantly from celecoxib-treated patients in all domains of the SF-36 except for the mental health domain.
Comportamento dos antitérmicos ibuprofeno e dipirona em crian？as febris
Magni, Ana Maria;Scheffer, Daniel Kashiwamura;Bruniera, Paula;
Jornal de Pediatria , 2011, DOI: 10.1590/S0021-75572011000100007
Abstract: objective: to evaluate temperature changes in febrile children that received a single oral dose of ibuprofen (10 mg/kg), the dose recommended for high fever, or dipyrone (15 mg/kg), the dose recommended by the manufacturer, at 2, 3, 4, 5, 6, 7 and 8 hours after administration. methods: this open-label randomized (1:1) controlled clinical tried enrolled 80 febrile boys and girls aged 6 months to 8 years with baseline axillary temperatures of 38.0 to 40.3 °c. the children were divided into two groups: high fever (> 39.1 °c) and low-grade fever (38.0 to 39.1 °c). the antipyretic effect was analyzed according to discontinuity, safety, response to treatment, tolerability and therapeutic efficacy. results: of the 80 children, 31 remained febrile during the 8 hours (38.8%), but 100% had a temperature decrease in the first 2 hours after the administration of either medication. in the high fever group, the temperature fell in 11 children treated with ibuprofen up to the 5th hour (100.00%) and in the 11 that received dipyrone, up to the third hour (100.00%). the difference in antipyretic efficacy of ibuprofen in the high fever group was statistically significant in the 3rd and 4th hours, and in the low-grade fever group, in the 3rd hour after medication. conclusions: a single oral dose of ibuprofen has a greater antipyretic efficacy than dipyrone, particularly when the fever is high. both drugs were well tolerated and safe in the short term.
Tratamiento de la úlcera péptica
Calvo Romero,J. Ma.; Lima Rodríguez,E. Ma.;
Medifam , 2002, DOI: 10.4321/S1131-57682002000500002
Abstract: peptic ulcer (pu) has a high prevalence and incidence. it has been estimated that a 10% of the spanish population will develop a pu. helicobacter pylori (hp) infection and non-steroidal anti-inflammatory drugs (nsaid) are the major causes of pu. to erradicate hp infection almost always means healing of nsaid non associated pu and reduces very significantly the recurrence rates, obviating generally maintenance antisecretory therapy. proton-pump inhibitors are the treatment of choice for nsaid associated pu. there is no enough evidence to recommend or not to recommend the eradication of hp infection in patients with nsaid associated pu.
Endoscopia gastroduodenal após administra？？o de nimesulida, monofenilbutazona e meloxicam em c？es
Costa, P.R.S.;Araújo, R.B.;Costa, M.C.;Maia, R.E.N.;
Arquivo Brasileiro de Medicina Veterinária e Zootecnia , 2007, DOI: 10.1590/S0102-09352007000400014
Abstract: the gastroduodenal mucosa in dogs experimentally treated with nimesulide, monophenylbutazone and meloxicam was evaluated. there were four groups with eight dogs in each. groups one, two and three were given nimesulide, monophenylbutazone and meloxicam, respectively, during 21 days and group four was used as control. all animals were evaluated by gastroduodenoscopy before the study and on the 10th and 21st days. the dogs did not show any clinical or laboratorial changes during the study. the endoscopic evaluation of gastroduodenal mucosa showed only low degree lesions. these anti-inflammatory drugs showed to be safe for the gastrointestinal tract in healthy dogs.
Dexamethasone decreases migraine recurrence observed after treatment with a triptan combined with a nonsteroidal anti-inflammatory drug
Krymchantowski, Abouch V.;Barbosa, Jackeline Soraya;
Arquivos de Neuro-Psiquiatria , 2001, DOI: 10.1590/S0004-282X2001000500010
Abstract: background and objectives: triptans are effective drugs for the acute treatment of migraine. however, 30-40% of the patients commonly present recurrence before 24 hours therefore requiring another dose. nonsteroidal anti-inflammatory drugs (nsaid) such as tolfenamic acid and naproxen sodium combined with sumatriptan have demonstrated efficacy in reducing recurrence observed with the single use of this drug. steroids also have been suggested to treat refractory migraine and status migranosus. the aim of this study was to evaluate whether patients presenting frequent recurrence with the combination triptan plus nsaid, would decrease it with the association of dexamethasone. method: twenty three patients, 17 women and 6 men with migraine according to ihs criteria were prospectively studied. all patients presented frequent recurrence (3 60%, mean recurrence rate 74,8%) with the single use of sumatritpan 100mg or zolmitriptan 2,5mg or rizatriptan 10mg in at least 5 consecutive attacks, and didn't present a reduction of the recurrence rate superior than 20% with the combination of tolfenamic acid 200mg or rofecoxib 25mg in at least 5 other consecutive attacks (mean recurrence rate 60%). the patients had to treat 6 consecutive moderate or severe migraine attacks with their usual combination plus 4mg of dexamathasone with a maximum of twice a week, and fill out a diary reporting headache parameters. results: twenty patients, 16 women and 4 men completed the study. of those who completed the study, 11 took rizatriptan plus rofecoxib, 4 rizatriptan plus tolfenamic acid, 3 zolmitriptan plus rofecoxib, 1 zolmitriptan plus tolfenamic acid and 1 patient took sumatriptan plus tolfenamic acid, having the 20 patients taken as a third medication, a single tablet of 4mg of dexamethasone. all patients took oral formulations and none presented vomiting after that. among all 20 patients, one female and one male patient presented recurrence in 3 out of the 6 attacks (50%) while the remain
Analgesia e a？？o antiinflamatória da Arnica montana 12CH comparativamente ao cetoprofeno em c？es
Cassu, Renata Navarro;Collares, Carlos Meirelles;Alegre, Beatriz Porto;Ferreira, Rosangela Cristóv？o;Stevanin, Helaine;Bernardi, Camila ？ngela;
Ciência Rural , 2011, DOI: 10.1590/S0103-84782011001000018
Abstract: this study aimed to evaluate the analgesic and anti-inflammatory effects of arnica montana 12ch comparatively to ketoprofen in dogs undergoing ovariohysterectomy. sixteen female dogs were randomly distributed in two groups of eight animals and received 1mg kg-1 of ketoprofen (tc) and 5 globules of arnica montana 12ch (ta) by oral route. after 60 minutes, the dogs were sedated with acepromazine (0.05mg kg-1, iv), followed by anesthetic induction with propofol (5mg kg-1 iv) and maintained with isoflurane. heart rate, respiratory rate, systolic blood pressure, arterial blood gases, serum cortisol concentration and degree of analgesia and inflammation were measured. additional morphine (0.5mg kg-1im) was given when the analgesia was insufficient. statistical analyses were performed by anova and tukey tests (p<0.05). cardiopulmonary stability was observed in both treatments during the surgery. the degree of analgesia and inflammation did not differ between groups. rescue analgesia was administered to two dogs from each group. it was concluded that arnica montana 12ch provides similar analgesic and anti-inflammatory effects when compared with ketoprofen, suggesting that this treatment is a safe and effective option to dogs undergoing ovariohysterectomy.
Protocolo de control del dolor y la inflamación postquirúrgica: Una aproximación racional
Romero-Ruiz,Manuel Ma; Herrero-Climent,Mariano; Torres-Lagares,Daniel; Gutiérrez-Pérez,José Luis;
RCOE , 2006, DOI: 10.4321/S1138-123X2006000200005
Abstract: one of the most important goals in oral surgery must be to reduce postsurgical symptoms following any surgical procedure. in order to obtain this objective it is very important to know the postoperative inflammation physiopathology. scientific evidence has emphasized the importance of pre-emptive and preoperative treatment to control all the variables related with postoperative pain and swelling. the preventive philosophy must be associated with a rational use of analgesic and anti-inflammatory drugs. in this paper, based on the scientific evidence but also on our clinical experience, we review the different therapeutic measures that we can apply before, during and after the surgical procedure. we also describe a pharmacological protocol that is easily applicable in our offices in order to control postoperative symptoms.
Diclofenac sodium topical solution with dimethyl sulfoxide, a viable alternative to oral nonsteroidal anti-inflammatories in osteoarthritis: review of current evidence
Fuller P, Roth SH
Journal of Multidisciplinary Healthcare , 2011, DOI: http://dx.doi.org/10.2147/JMDH.S23209
Abstract: lofenac sodium topical solution with dimethyl sulfoxide, a viable alternative to oral nonsteroidal anti-inflammatories in osteoarthritis: review of current evidence Review (5258) Total Article Views Authors: Fuller P, Roth SH Published Date July 2011 Volume 2011:4 Pages 223 - 231 DOI: http://dx.doi.org/10.2147/JMDH.S23209 Philip Fuller1, Sanford Roth2 1Covidien, Hazelwood, MO; 2Arizona Research and Education, Arthritis Research Laboratory, Arizona State University, Phoenix, AZ, USA Abstract: Topical nonsteroidal anti-inflammatory drugs (NSAIDs) may offer a safer alternative to their oral counterparts for the management of osteoarthritis. Diclofenac sodium topical solution with dimethyl sulfoxide (TDiclo) was evaluated in five randomized, controlled trials and is indicated for treatment of the signs and symptoms associated with osteoarthritis of the knee. Three studies showed that TDiclo is superior to placebo and vehicle control with respect to pain, physical function, and perception of osteoarthritis symptoms. Two studies showed that benefits are similar to those of oral diclofenac, with one study demonstrating statistical equivalence. The most common adverse event associated with TDiclo in these studies was dry skin. Incidences of gastrointestinal adverse events and abnormal levels of liver enzymes were lower with TDiclo compared with oral diclofenac in active-controlled studies. Based on these studies, TDiclo represents a practical, evidence-based option for the management of osteoarthritis of the knee.
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