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Sample records for veterinary non-steroidal anti-inflammatory

  1. Non-steroidal anti-inflammatory drug use and the risk of Parkinson's disease

    DEFF Research Database (Denmark)

    Manthripragada, Angelika D; Schernhammer, Eva S; Qiu, Jiaheng

    2011-01-01

    Experimental evidence supports a preventative role for non-steroidal anti-inflammatory drugs (NSAIDs) in Parkinson's disease (PD).......Experimental evidence supports a preventative role for non-steroidal anti-inflammatory drugs (NSAIDs) in Parkinson's disease (PD)....

  2. Hypersensitivity to non-steroidal anti-inflammatory drugs (NSAIDs)

    DEFF Research Database (Denmark)

    Nissen, Christoffer V; Bindslev-Jensen, Carsten; Mørtz, Charlotte G

    2015-01-01

    BACKGROUND: Non-steroidal anti-inflammatory drugs (NSAIDs) are reported to be the second most common cause of drug hypersensitivity. In 2011, experts from the EAACI/ENDA group and GA(2)LEN proposed a new classification system for NSAID hypersensitivity. The aim of this study was to classify...... responders reacted to non-pyrazolone drugs. Only one patient could not be classified according to the EAACI/ENDA system. An overlap between respiratory and cutaneous symptoms was found in 15/39 (38%) of patients. CONCLUSIONS: All but one of our patients could be classified according to the EAACI...

  3. Utilization of non-steroidal anti-inflammatory drugs in patients ...

    African Journals Online (AJOL)

    Non-steroidal anti-inflammatory drugs are widely prescribed worldwide. In Nigeria there is unrestricted access to these useful, yet potentially harmful drugs. We set out to assess the utilization of non-steroidal anti-inflammatory drugs in outpatients attending clinics in a Teaching Hospital in Nigeria. Consecutive patients were ...

  4. Hypersensitivity Reactions to Non-Steroidal Anti-Inflammatory Drugs.

    Science.gov (United States)

    Dona, Inmaculada; Salas, Maria; Perkins, James R; Barrionuevo, Esther; Gaeta, Francesco; Cornejo-Garcia, Jose A; Campo, Paloma; Torres, Maria Jose

    2016-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the leading causes of hypersensitivity reactions to drugs, and they are classified in two groups: those induced by nonspecific immunological mechanisms (non-allergic or cross-intolerance (CI) reactions), or by specific immunological mechanisms (allergic or selective reactions (SR)). The pathogenesis of CI is associated with their pharmacological activity (COX-1 inhibition), with symptoms due to an imbalance in the arachidonic acid pathway, independently of their chemical structure. SRs are mediated by specific IgE- or by a T-cell response and can be induced by a single NSAID or a class of chemically related NSAIDs, with patients tolerating chemically unrelated compounds. NSAIDs hypersensitivity reactions have been classified in five main groups: i) NSAIDs-exacerbated respiratory disease (NERD); ii) NSAIDs-exacerbated cutaneous disease (NECD); iii) NSAIDs-induced urticaria/angioedema (NIUA); iv) Single NSAID-induced urticaria/angioedema or anaphylaxis (SNIUAA); v) Single NSAID-induced delayed reactions (SNIDRs). Although this classification described above is widely accepted by most authors some phenotypes such as blended reactions do not fit. Therefore more research is needed in this topic. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  5. Renal toxicity of non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Black, H E

    1986-01-01

    Non-steroidal anti-inflammatory drugs represent the most heavily prescribed and used class of drugs in human medicine. Most are derivatives of either salicylates, propionic acid, indoleacetic acid, anthranilic acid, pyrazolone, or oxicams. They depress the synthesis of prostaglandins from arachidonic acid by reversible inhibition of the enzyme cyclooxygenase. In the kidney, prostaglandins PGE2 and PGI2 modulate the vasoconstrictor effects of angiotensin II, norepinephrine, and vasopressin. In the presence of volume contraction, anesthesia, or disease states associated with high levels of these hormones, prostaglandins regulate glomerular filtration, vascular resistance, and renin secretion. They additionally influence urine volume and sodium content. In man, a syndrome of analgesic abuse that has been identified worldwide occurs more frequently in females than males and can result in severe renal damage, most notably renal papillary necrosis. Most common laboratory animals are relatively resistant to developing the renal lesion associated with NSAIDs unless high doses are given over long periods of time and some withholding of water is introduced into the protocol. Diuresis with 5% dextrose and water is protective. Studies of paracetamol and salicylate have demonstrated that these compounds concentrate in the papillary tip of the kidney at concentrations of 4 to 13 times the plasma levels in dogs and rabbits, respectively. Renal papillary necrosis has been described in horses on maintenance doses of phenylbutazone where dehydration or reduced water consumption has occurred. The lesion can be reproduced experimentally if water is withheld during a portion of the dosing interval. An increased incidence of uroepithelial tumors have been reported in patients with a history of analgesic abuse.(ABSTRACT TRUNCATED AT 250 WORDS)

  6. Non-steroidal Anti-inflammatory Drugs in Raptors

    Science.gov (United States)

    Oaks, J. Lindsay; Meteyer, Carol U.; Miller, R. Eric; Fowler, Murray E.

    2012-01-01

    The use of analgesia has become standard, and appropriate, practice in avian medicine. As in mammals, pain control in avian patients is usually accomplished with opioids and nonsteroidal anti-inflammatory drugs (NSAIDs) used singly or in combination for a multimodal approach. Despite their usefulness, widespread use, and relative safety in clinical use, few controlled studies in birds have been conducted on efficacy, safety, and dosing. The guidelines for the use of NSAIDs in raptors and other birds have mainly been empirical. More recently, NSAIDs in free-living raptors have emerged as a major conservation issue with the discovery that diclofenac sodium was responsible for the population crash of three species of Gyps vultures in southern Asia. In this context, residues of veterinary NSAIDs in domestic animals are now considered environmental contaminants that can be significantly toxic to vultures and possibly other avian scavengers. Ironically, the disaster with Asian vultures has led to a considerable body of research on NSAIDs in raptors to the benefit of clinicians who now have scientific information available to help assess dosing, safety, toxicity, and pharmacokinetics of NSAIDs in their raptor patients.

  7. Antimicrobial activity of non-steroidal anti-inflammatory drugs with ...

    African Journals Online (AJOL)

    STORAGESEVER

    2009-12-29

    Dec 29, 2009 ... The non-steroidal anti-inflammatory drugs (NSAIDs) as the name implies are compounds of non- steroidal origin, with the capability of inhibiting/reducing inflammatory response associated with tissue injury which could be as a result of physical trauma, noxious chemicals or microorganisms. There is.

  8. Aspirin and its related non-steroidal anti-inflammatory drugs

    African Journals Online (AJOL)

    Aspirin and its related non-steroidal anti-inflammatory drugs. Aspirin or acetylsalicylic acid has been utilised by physicians for hundreds of years as an analgesic, anti-inflammatory and antipyretic (1). Derived from plant sources, such as the willow tree, it has the ability to induce apoptosis in cancer cells and stimulate.

  9. Non-steroidal anti-inflammatory drugs for acute gout.

    Science.gov (United States)

    van Durme, Caroline M P G; Wechalekar, Mihir D; Buchbinder, Rachelle; Schlesinger, Naomi; van der Heijde, Désirée; Landewé, Robert B M

    2014-09-16

    Gout is an inflammatory arthritis that is characterised by the deposition of monosodium urate crystals in synovial fluid and other tissues. The natural history of articular gout is generally characterised by three periods: asymptomatic hyperuricaemia, episodes of acute gout and chronic gouty arthritis. Non-steroidal anti-inflammatory drugs (NSAIDs) including selective cyclo-oxygenase-2 (COX-2) inhibitors (COXIBs) are commonly used to treat acute gout. Published guidelines recommend their use to treat acute attacks, using maximum recommended doses for a short time. To assess the benefit and safety of NSAIDs (including COXIBs) for acute gout. We searched the Cochrane Central Register of Controlled Trials (CENTRAL), MEDLINE and EMBASE for studies to 7 October 2013, the 2010 and 2011 ACR and EULAR abstracts and performed a handsearch of reference lists of articles. We searched the World Health Organization (WHO) trial register and ClinicalTrials.gov. We applied no date or language restrictions. We considered all published randomised controlled trials (RCTs) and quasi-randomised controlled clinical trials that compared NSAIDs with placebo or another therapy (including non-pharmacological therapies) for acute gout. Major outcomes were pain (proportion with 50% or more reduction in pain or mean pain when the dichotomous outcome was unavailable), inflammation (e.g. measured by joint swelling/erythema/tenderness), function of target joint, participant's global assessment of treatment success, health-related quality of life, withdrawals due to adverse events and total adverse events. Two review authors independently selected the studies for inclusion, extracted the data, performed a risk of bias assessment and assessed the quality of the evidence using the GRADE approach. We included 23 trials (2200 participants).One trial (30 participants) of low-quality evidence compared an NSAID (tenoxicam) with placebo. It found that significantly more participants had more than 50

  10. Ischaemic cardiovascular risk and prescription of non-steroidal anti-inflammatory drugs for musculoskeletal complaints

    NARCIS (Netherlands)

    Koffeman, A.R.; Valkhoff, V.E.; Jong, G.W. t; Warle-van Herwaarden, M.F.; Bindels, P.J.; Sturkenboom, M.C.; Luijsterburg, P.A.; Bierma-Zeinstra, S.M.

    2014-01-01

    OBJECTIVE: To determine the influence of ischaemic cardiovascular (CV) risk on prescription of non-steroidal anti-inflammatory drugs (NSAIDs) by general practitioners (GPs) in patients with musculoskeletal complaints. DESIGN: Cohort study. SETTING: A healthcare database containing the electronic GP

  11. effects of non-steroidal anti-inflammatory drugs on hypertension ...

    African Journals Online (AJOL)

    Objectives: To determine the impact of three non-steroidal anti-inflammatory drugs on the efficacy of two anti-hypertensive drugs. Design: Fifteen women with arthritis and hypertension who were receiving lisinoprii and. HCT, and administered sequentially in random order ibuprofen, sulindac, and diclofenac for one month ...

  12. The Pattern of Sale and Use of Non-Steroidal Anti-Inflammatory ...

    African Journals Online (AJOL)

    Purpose: The widespread use of non-steroidal anti-inflammatory drugs (NSAID) has meant that the adverse effects of these relatively safe drugs have become increasingly prevalent. This work examines the pattern of sale and use of NSAIDs as to call for caution in cases of misuse that may lead to renal, gastrointestinal and ...

  13. The Pattern of Sale and Use of Non-Steroidal Anti- Inflammatory ...

    African Journals Online (AJOL)

    Erah

    Purpose: The widespread use of non-steroidal anti-inflammatory drugs (NSAID) has meant that the adverse effects of these relatively safe drugs have become increasingly prevalent. This work examines the pattern of sale and use of NSAIDs as to call for caution in cases of misuse that may lead to renal, gastrointestinal and ...

  14. Postoperative non-steroidal anti-inflammatory drugs and colorectal anastomotic leakage

    DEFF Research Database (Denmark)

    Klein, Mads; Gögenur, Ismail; Rosenberg, Jacob

    2012-01-01

    Anastomotic leakage (AL) is the most important and one of the most serious complications after colorectal resections with primary anastomosis. Any factors that contribute to increase the risk of AL should be identified and - if possible - eliminated. Non-steroidal anti-inflammatory drugs (NSAIDs...

  15. Toxic effects of non-steroidal anti-inflammatory agents in rats ...

    African Journals Online (AJOL)

    The toxicosis of some non-steroidal anti-inflammatory drugs, piroxicam, indomethacin, phenylbutazone, and aspirin, which occasionally are locally used in Nigeria as rodenticides have been evaluated in rats using changes in the serum biochemical and haematological parameters as indices of toxicity. In the study, no ...

  16. Negative effect of non-steroidal anti-inflammatory drugs on the ...

    African Journals Online (AJOL)

    Ciprofloxacin, a second generation fluoroquinolone is often co-administered with non-steroidal anti-inflammatory drugs (NSAIDs) in life threatening situations in which Staphylococcus aureus infections are accompanied with pain and inflammation. This study was carried out to investigate possible in vitro interactions in co ...

  17. Non-steroidal anti-inflammatory drugs for chronic low back pain

    NARCIS (Netherlands)

    W.T.M. Enthoven (Wendy); P.D.D.M. Roelofs; R.A. Deyo (Richard); M.W. van Tulder (Maurits); B.W. Koes (Bart)

    2016-01-01

    textabstractBackground: Chronic back pain is an important health problem. Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used to treat people with low back pain, especially people with acute back pain. Short term NSAID use is also recommended for pain relief in people with chronic back

  18. Use of non-steroidal anti-inflammatory drugs and nutritional ...

    African Journals Online (AJOL)

    Background. The use of medications by football players in many populations is known to be high. Data on African players are scarce. Objective. To determine the magnitude of use of non-steroidal anti-inflammatory drugs (NSAIDs) and nutritional supplements by. Zimbabwean football players. Methods. We conducted a ...

  19. Use of non-steroidal anti-inflammatory drugs and nutritional ...

    African Journals Online (AJOL)

    Background. The use of medications by football players in many populations is known to be high. Data on African players are scarce. Objective. To determine the magnitude of use of non-steroidal anti-inflammatory drugs (NSAIDs) and nutritional supplements by Zimbabwean football players. Methods. We conducted a ...

  20. Antimicrobial activity of non-steroidal anti-inflammatory drugs with ...

    African Journals Online (AJOL)

    The non-steroidal anti-inflammatory drugs (NSAIDs) as the name implies are compounds of nonsteroidal origin, with the capability of inhibiting/reducing inflammatory response associated with tissue injury which could be as a result of physical trauma, noxious chemicals or microorganisms. There is however reason to ...

  1. Non-steroidal anti-inflammatory drugs for sciatica.

    Science.gov (United States)

    Rasmussen-Barr, Eva; Held, Ulrike; Grooten, Wilhelmus Ja; Roelofs, Pepijn Ddm; Koes, Bart W; van Tulder, Maurits W; Wertli, Maria M

    2016-10-15

    Nonsteroidal anti-inflammatory drugs (NSAIDs) are one of the most frequently prescribed drugs for the treatment of sciatica. A previous Cochrane review on the efficacy of NSAIDs summarised findings for acute and chronic low back pain (LBP) and sciatica. This is an update of the original review (2008) focusing on people suffering from sciatica. To determine the efficacy of NSAIDs in pain reduction, overall improvement, and reported side effects in people with sciatica. We performed electronic searches up to 24 June 2015 in the Cochrane Central Register of Controlled Trials (CENTRAL), MEDLINE, EMBASE, PubMed, and two trials registers. We searched reference lists of included studies and relevant reviews on the topics for additional trials. We included randomised controlled trials (double-blind, single-blind, and open-label) that assessed the efficacy of NSAIDs in sciatica. We included all trials that compared NSAIDs to placebo, to other NSAIDs, or to other medication. Additional interventions were allowed if there was a clear contrast for the treatment with NSAIDs in the trial. Three review authors independently assessed the risk of bias and extracted the data. Where feasible we calculated pooled results using Review Manager 5.3. We reported pain relief outcomes using mean difference (MD) with 95% confidence intervals (95% CI). We used risk ratios (RR) with 95% CI to report global improvement of treatment, adverse effects, and additional medication. We performed a meta-analysis if possible. We assessed level of evidence using the GRADE approach. We used standard methodological procedures recommended by The Cochrane Collaboration. We included 10 trials reported in 9 publications (N = 1651). Only one trial out of 10 was assessed at low risk of bias. Five trials used the currently recommended daily dose for the drug, and two trials used lower daily doses available over the counter. Three trials investigated NSAIDs no longer approved for human use. The follow-up duration

  2. Non-Steroidal Anti-Inflammatory Drugs: An Overview of Cardiovascular Risks

    Directory of Open Access Journals (Sweden)

    Mart A.F.J. van de Laar

    2010-07-01

    Full Text Available While aspirin may offer protection, other non-aspirin non-steroidal anti-inflammatory drugs (NSAIDs can cause serious cardiovascular side effects and complications. This has led to a general "black box" warning for cardiovascular adverse events for NSAIDs. This review explores the different mechanisms underlying the protective effects of aspirin, the NSAID associated renovascular effects causing hypertension, edema and heart failure, the cardiovascular effects causing myocardial infarction and stroke, and the possible deleterious interaction between NSAIDs and aspirin.

  3. Non-steroidal anti-inflammatory drugs and ulcer complications: a risk factor analysis for clinical decision-making

    DEFF Research Database (Denmark)

    Hansen, J M; Hallas, J; Lauritsen, Jens

    1996-01-01

    Use of non-steroidal anti-inflammatory drugs (NSAIDs) is recognized as an important cause of peptic ulcer complications. The aim of this nested case-control study was to identify risk factors for NSAID-related ulcer complications.......Use of non-steroidal anti-inflammatory drugs (NSAIDs) is recognized as an important cause of peptic ulcer complications. The aim of this nested case-control study was to identify risk factors for NSAID-related ulcer complications....

  4. Acute gastrointestinal permeability responses to different non-steroidal anti-inflammatory drugs

    Science.gov (United States)

    Smecuol, E; Bai, J; Sugai, E; Vazquez, H; Niveloni, S; Pedreira, S; Maurino, E; Meddings, J

    2001-01-01

    BACKGROUND AND AIMS—Non-steroidal anti-inflammatory drugs (NSAIDs) cause gastrointestinal damage both in the upper and lower gastrointestinal tract. New anti-inflammatory drugs have been developed in an attempt to improve their gastrointestinal side effect profile. Our objective was to compare the effect on gastrointestinal permeability of acute equieffective doses of four different NSAIDs; three were designed to reduce gastrointestinal mucosal injury.
MATERIALS—Healthy volunteers underwent sugar tests in a randomised fashion, 15 days apart, at: (1) baseline; (2) after two days of 75 mg slow release (microspheres) indomethacin; (3) after two days of 7.5 mg oral meloxicam which preferentially inhibits cyclooxygenase 2; and (4) after two days of 750 mg naproxen. A subgroup of subjects was tested after two days of 200 mg celecoxib. In each test, subjects ingested a solution containing sucrose, lactulose, and mannitol and sucralose, to evaluate gastroduodenal, intestinal, and colonic permeability, respectively.
RESULTS—Gastric permeability was significantly affected by naproxen (psucralose, was not significantly increased by any of the four drugs.
CONCLUSION—Our study provides evidence that the newly developed NSAIDs reduce gastric mucosal permeability significantly. However, most produced significant alteration of small intestinal permeability. In contrast, our results suggest that celecoxib seems to exhibit the most desirable gastrointestinal side effect profile.


Keywords: permeability; non-steroidal anti-inflammatory drugs; celecoxib; meloxican; small intestine; gastric injury PMID:11600467

  5. Non-Steroidal Anti-Inflammatory Drugs, Variation in Inflammatory Genes, and Aggressive Prostate Cancer

    Directory of Open Access Journals (Sweden)

    John S. Witte

    2010-10-01

    Full Text Available Increasing evidence suggests that prostatic inflammation plays a key role in the development of prostate cancer. It remains controversial whether non-steroidal anti-inflammatory drugs (NSAIDs reduce the risk of prostate cancer. Here, we investigate how a previously reported inverse association between NSAID use and the risk of aggressive prostate cancer is modulated by variants in several inflammatory genes. We found that NSAIDs may have differential effects on prostate cancer development, depending on one’s genetic makeup. Further study of these inflammatory pathways may clarify the mechanisms through which NSAIDs impact prostate cancer risk.

  6. Users? Knowledge About Adverse Effects of Non-steroidal Anti-inflammatory Drugs in Tirana, Albania

    OpenAIRE

    Roshi, Dajana; To?i, Ervin; Burazeri, Genc; Schr?der-B?ck, Peter; Malaj, Ledjan; Brand, Helmut

    2017-01-01

    Aim: To assess the level of knowledge of the adult users of non-steroidal anti-inflammatory drugs (NSAIDs) regarding their side effects and the socio-demographic factors associated with the use of these drugs in the adult population of Albania. Methods: This was a cross-sectional study including a representative sample of 199 individuals aged ?18 years (77% women; overall mean age: 30.3?10.0 years; overall response rate: 90%) who were users of NSAIDs recruited in ten different pharmacies in T...

  7. Non-steroidal anti-inflammatory drugs and renal response to exercise

    DEFF Research Database (Denmark)

    Olsen, Niels Vidiendal; Jensen, N G; Hansen, J M

    1999-01-01

    Nabumetone, a newer non-steroidal anti-inflammatory drug (NSAID) which preferentially blocks cyclo-oxygenase-2 activity, may be less nephrotoxic than indomethacin. This study tested whether nabumetone has effects different from those of indomethacin on exercise-induced changes in renal function...... and the renin-aldosterone system. In a randomized fashion, ten subjects were studied after indomethacin (100 mg), nabumetone (1 g) or no medication (control) administered orally at 22.00 hours on the day before each study day, and again at 8.00 hours upon arrival at the laboratory. Renal function was studied...

  8. Role of Non-Steroidal Anti-Inflammatory Drugs in Gynecology

    Directory of Open Access Journals (Sweden)

    Anna Livshits

    2010-07-01

    Full Text Available This review summarizes the current use of non-steroidal anti-inflammatory drugs (NSAIDs in obstetrics, gynecology and infertility. These medications are commonly used in different fields of reproductive medicine, for pain management after operative procedures and to relieve dysmenorrhea. In addition to their analgesic effect, NSAIDs are helpful in the management of menorrhagia by decreasing menstrual blood loss. NSAIDs alleviate pain associated with medical abortion, assist in undertaking natural cycle in-vitro fertilization by preventing follicular rupture and reducing premature ovulation, and serve as tocolytics in preterm labor. New NSAIDs may have a growing role in management of women's health.

  9. Postoperative non-steroidal anti-inflammatory drugs and colorectal anastomotic leakage

    DEFF Research Database (Denmark)

    Klein, Mads; Gögenur, Ismail; Rosenberg, Jacob

    2012-01-01

    Anastomotic leakage (AL) is the most important and one of the most serious complications after colorectal resections with primary anastomosis. Any factors that contribute to increase the risk of AL should be identified and - if possible - eliminated. Non-steroidal anti-inflammatory drugs (NSAIDs......) are often used for treating pain after surgical procedures, among these also colorectal resections. The objective of this Ph.d. thesis was to investigate whether the use of NSAIDs in the postoperative period increases the risk of AL, and investigate the effect on pathophysiological mechanisms. In order...

  10. A short history of anti-rheumatic therapy. III. Non steroidal anti-inflammatory drugs

    Directory of Open Access Journals (Sweden)

    P. Marson

    2011-06-01

    Full Text Available The chemical advances of the 20th century led to the synthesis of non steroidal anti-inflammatory drugs (NSAIDs, beginning from phenylbutazone and indomethacin and continuing with other new drugs, including ibuprofen, diclofenac, naproxen, piroxicam and, more recently, the highly selective COX-2 inhibitors (coxibs. This progress derived from the discovery of the mechanism of action of these drugs: the inhibition of synthesis of prostaglandins due to the cycloxigenase enzyme system, according to the experimental contributions of John R. Vane.

  11. Non-steroidal Anti-inflammatory Drugs Ranking by Nondeterministic Assessments of Probabilistic Type

    Directory of Open Access Journals (Sweden)

    Madalina luiza MOLDOVEANU

    2012-09-01

    Full Text Available With a number of common therapeutic prescriptions, common mechanisms, common pharmacological effects - analgesic, antipyretic and anti-inflammatory (acetaminophen excepted, common side effects (SE (platelet dysfunction, gastritis and peptic ulcers, renal insufficiency in susceptible patients, water and sodium retention, edemas, nephropathies, and only a few different characteristics – different chemical structures, pharmacokinetics and different therapeutic possibility, different selectivities according to cyclooxygenase pathway 1 and 2, non-steroidal anti-inflammatory drugs (NSAIDs similarities are more apparent than differences. Being known that in a correct treatment benefits would exceed risks, the question “Which anti-inflammatory drug presents the lowest risks for a patient?” is just natural. By the Global Risk Method (GRM and the Maximum Risk Method (MRM we have determined the ranking of fourteen NSAIDs considering the risks presented by each particular NSAID. Nimesulide, Etoricoxib and Celecoxib safety level came superior to the other NSAIDs, whereas Etodolac and Indomethacin present an increased side effects risk.

  12. Oral non-steroidal anti-inflammatory drug therapy for lung disease in cystic fibrosis.

    Science.gov (United States)

    Lands, Larry C; Stanojevic, Sanja

    2016-04-07

    Progressive lung damage causes most deaths in cystic fibrosis. Non-steroidal anti-inflammatory drugs (such as ibuprofen) may prevent progressive pulmonary deterioration and morbidity in cystic fibrosis. To assess the effectiveness of treatment with non-steroidal anti-inflammatory drugs in cystic fibrosis. We searched the Cochrane Cystic Fibrosis and Genetic Disorders Group Trials Register comprising references identified from comprehensive electronic database searches, hand searches of relevant journals and abstract books of conference proceedings. We contacted manufacturers of non-steroidal anti-inflammatory drugs.Latest search of the Group's Trials Register: 04 February 2016. Randomized controlled trials comparing oral non-steroidal anti-inflammatory drugs, at any dose for at least two months, to placebo in people with cystic fibrosis. Two authors independently assessed trials for inclusion the review and their potential risk of bias. The searches identified 10 trials; four are included (287 participants aged five to 39 years; maximum follow up of four years) and one is currently awaiting classification pending publication of the full trial report. Three trials compared ibuprofen to placebo (two from the same centre with some of the same participants); one trial assessed piroxicam versus placebo.The three ibuprofen trials were deemed to have good or adequate methodological quality, but used various outcomes and summary measures. Reviewers considered measures of lung function, nutritional status, radiological assessment of pulmonary involvement, intravenous antibiotic usage, hospital admissions, survival and adverse effects. Combined data from the two largest ibuprofen trials showed a significantly lower annual rate of decline for lung function, percent predicted forced expiratory volume in one second mean difference 1.32 (95% confidence interval 0.21 to 2.42); forced vital capacity mean difference 1.27 (95% confidence interval 0.26 to 2.28); forced expiratory

  13. Prediction by pharmacogenetics of safety and efficacy of non-steroidal anti- inflammatory drugs: a review.

    Science.gov (United States)

    Rollason, Victoria; Samer, Caroline Flora; Daali, Youssef; Desmeules, Jules Alexandre

    2014-03-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are the most frequently used drugs, either on prescription or over-thecounter (OTC). Their daily dosage is based on randomised controlled trials and an empirical clinical assessment of their efficacy and toxicity that allows dose adjustment. The individual response can however be altered by environmental and genetic pharmacokinetic and pharmacodynamic factors. This review summarizes the available pharmacogenetic data that explains part of the variability in response and occurrence of adverse drug reactions to NSAIDs treatment, with a thorough focus on CYP2C9, uridine diphosphate glucuronosyltransferases (UGTs) and cyclooxygenases (COX1 and COX2). Other polymorphisms that are currently being studied and could also explain the interindividual variability in the efficacy and safety of NSAIDs will also be considered.

  14. Non-steroidal anti-inflammatory drug use and risk of endometrial cancer

    DEFF Research Database (Denmark)

    Verdoodt, Freija; Friis, Søren; Dehlendorff, Christian

    2016-01-01

    OBJECTIVE: Non-steroidal anti-inflammatory drug (NSAID) use has been linked to a reduction in the risk of several cancer types. For endometrial cancer, however, results have been inconsistent. To summarize the available evidence on the risk of endometrial cancer associated with use of aspirin...... a random effects model. RESULTS: Six case-control and seven cohort studies were found eligible for our meta-analysis. We observed risk reductions in endometrial cancer associated with regular use of aspirin (case-control: 11%, cohort: 8%) and NA-NSAIDs (case-control: 9%, cohort: 6%), compared to non......-use. However, the pooled risk ratios were not statistically significant. Higher risk reductions were seen with high frequency of notably aspirin use (case-control: 37%, cohort: 20%). The inverse association between regular aspirin use and endometrial cancer risk was strongest among women with a body mass index...

  15. The Role of Non-Steroidal Anti-Inflammatory Drugs in the Chemoprevention of Breast Cancer

    Directory of Open Access Journals (Sweden)

    Sarah L. Horn

    2010-05-01

    Full Text Available Epidemiological evidence suggests that non-steroidal anti-inflammatory drugs (NSAIDs which act as cyclooxygenase (COX-2 inhibitors may reduce breast cancer incidence by up to 20%. These agents are often taken for pain relief by older women with osteoarthritis. Age is the major risk factor for breast cancer in women with 50% cases being diagnosed in those aged >65 years. NSAIDs reduce serum estradiol by 17% in post-menopausal women and since most of these who develop breast cancers have estrogen receptor positive tumours; this suggests a possible preventative role. Careful use of these agents could provide a strategy for both relief of symptoms of osteoarthritis and also breast cancer prevention. Instead of conducting a randomised trial, proof of efficacy could be from an adequately powered cohort study within the breast screening programme.

  16. Clinical pharmacology and therapeutic uses of non-steroidal anti-inflammatory drugs in the horse.

    Science.gov (United States)

    Lees, P; Higgins, A J

    1985-03-01

    Weak organic acids possessing anti-inflammatory, analgesic and antipyretic properties--commonly known as aspirin-like drugs--have been used in equine medicine for almost 100 years. These non-steroidal anti-inflammatory drugs (NSAIDs) may be classified chemically into two groups; the enolic acids such as phenylbutazone and carboxylic acids like flunixin, meclofenamate and naproxen. All NSAIDs have similar and possibly identical modes of action accounting for both their therapeutic and their toxic effects. They block some part of the cyclo-oxygenase enzyme pathway and thereby suppress the synthesis of several chemical mediators of inflammation, collectively known as eicosanoids. The available evidence indicates that some of the newer NSAIDs have a reasonable safety margin but further studies are required. The toxicity of phenylbutazone in the horse has been investigated very thoroughly in recent years and it has been shown to cause renotoxicity and, most significantly, ulceration of the gastrointestinal tract when relatively high doses are administered. Several factors may predispose towards phenylbutazone toxicity in the horse, including breed and age, but high dosage is considered to be particularly important. The absorption into, and fate within, the body of NSAIDs are considered and particular attention is drawn to the ways in which these pharmacokinetic properties relate to the drugs' toxicity and clinical efficacy. In reviewing current knowledge of the clinical pharmacology of this important group of drugs, it is hoped to provide the clinician with a rational, scientific basis for their safe and effective use in equine practice.

  17. Bio-Electro-Fenton process for the degradation of Non-Steroidal Anti-Inflammatory Drugs in wastewater

    DEFF Research Database (Denmark)

    Nadais, Helena; Li, Xiaohu; Alves, Nadine

    2018-01-01

    Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are ubiquitous municipal wastewater pollutants of which several are resistant to degradation in conventional wastewater treatment, and represent a major environmental health concern worldwide. An alternative treatment, the bio-electro-Fenton process,...

  18. Formulation,Optimization and Evaluation of Orally Disintegrating Tablet of Non-Steroidal Anti-inflammatory Drug

    OpenAIRE

    Patel Minal Arvindbhai; Shah Jigesh Ashwinbhai; Patel Kunal N.; Patel Bhavana A.; Patel Poras A.

    2012-01-01

    Piroxicam is a non steroidal anti-inflammatory drug with analgesic properties. The purpose of this studywas to develop a taste masked orally disintegrating tablet of poorly soluble Piroxicam by directcompression technique with β-cyclodextrin (ß-CD) complexes using various superdisintegrants likesodium starch glycolate, crospovidone XL and croscarmellose sodium. Complex was characterizedusing infrared spectroscopy, differential scanning calorimetry, % drug release study, gustatoryevaluation fo...

  19. Using UV-VIS spectrophotometry for determining ecotoxicity of selected non-steroidal anti-inflammatory drugs

    OpenAIRE

    Čapka, L. (Lukáš); Zlámalová Gargošová, H.; Vávrová, M.

    2015-01-01

    This paper presents the use of UV-VIS spectrophotometry as a means of determining ecotoxicity. The method is based on spectrophotometric measuring of micro-algae Pseudokirchneriella subcapitata in water suspension. Six non-steroidal anti-inflammatory drugs were selected as target compounds.

  20. Efficacy of non-steroidal anti-inflammatory drugs for low back pain: a systematic review of randomised clinical trials

    NARCIS (Netherlands)

    Koes, B. W.; Scholten, R. J.; Mens, J. M.; Bouter, L. M.

    1997-01-01

    To assess the efficacy of non-steroidal anti-inflammatory drugs (NSAIDs) for low back pain. Computer aided search of published randomised clinical trials and assessment of the methods of the studies. 26 randomised clinical trials evaluating NSAIDs for low back pain were identified. Score for quality

  1. Non-steroidal anti-inflammatory drugs (NSAIDs) for axial spondyloarthritis (ankylosing spondylitis and non-radiographic axial spondyloarthritis)

    NARCIS (Netherlands)

    Kroon, Feline P. B.; van der Burg, Lennart R. A.; Ramiro, Sofia; Landewé, Robert B. M.; Buchbinder, Rachelle; Falzon, Louise; van der Heijde, Désirée

    2015-01-01

    Axial spondyloarthritis (axSpA) comprises ankylosing spondylitis (radiographic axSpA) and non-radiographic (nr-)axSpA and is associated with psoriasis, uveitis and inflammatory bowel disease. Non-steroidal anti-inflammatory drugs (NSAIDs) are recommended as first-line drug treatment. To determine

  2. Mechanisms of peroxisome proliferator activated receptor γ regulation by non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Puhl, Ana C; Milton, Flora A; Cvoro, Aleksandra; Sieglaff, Douglas H; Campos, Jéssica C L; Bernardes, Amanda; Filgueira, Carly S; Lindemann, Jan Lammel; Deng, Tuo; Neves, Francisco A R; Polikarpov, Igor; Webb, Paul

    2015-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) display anti-inflammatory, antipyretic and analgesic properties by inhibiting cyclooxygenases and blocking prostaglandin production. Previous studies, however, suggested that some NSAIDs also modulate peroxisome proliferator activated receptors (PPARs), raising the possibility that such off target effects contribute to the spectrum of clinically relevant NSAID actions. In this study, we set out to understand how peroxisome proliferator activated receptor-γ (PPARγ/PPARG) interacts with NSAIDs using X-ray crystallography and to relate ligand binding modes to effects on receptor activity. We find that several NSAIDs (sulindac sulfide, diclofenac, indomethacin and ibuprofen) bind PPARγ and modulate PPARγ activity at pharmacologically relevant concentrations. Diclofenac acts as a partial agonist and binds to the PPARγ ligand binding pocket (LBP) in typical partial agonist mode, near the β-sheets and helix 3. By contrast, two copies of indomethacin and sulindac sulfide bind the LBP and, in aggregate, these ligands engage in LBP contacts that resemble agonists. Accordingly, both compounds, and ibuprofen, act as strong partial agonists. Assessment of NSAID activities in PPARγ-dependent 3T3-L1 cells reveals that NSAIDs display adipogenic activities and exclusively regulate PPARγ-dependent target genes in a manner that is consistent with their observed binding modes. Further, PPARγ knockdown eliminates indomethacin activities at selected endogenous genes, confirming receptor-dependence of observed effects. We propose that it is important to consider how individual NSAIDs interact with PPARγ to understand their activities, and that it will be interesting to determine whether high dose NSAID therapies result in PPAR activation.

  3. Helicobacter pylori-negative, non-steroidal anti-inflammatory drug: Negative idiopathic ulcers in Asia

    Science.gov (United States)

    Iijima, Katsunori; Kanno, Takeshi; Koike, Tomoyuki; Shimosegawa, Tooru

    2014-01-01

    Since the discovery of Helicobacter pylori (H. pylori) infection in the stomach, the bacteria infection and non-steroidal anti-inflammatory drugs (NSAIDs) use had been considered to be the 2 main causes of peptic ulcers. However, there have been recent reports of an increase in the proportion of peptic ulcers without these known risk factors; these are termed idiopathic peptic ulcers. Such trend was firstly indicated in 1990s from some reports in North America. In Asia, numerous studies reported that idiopathic ulcers accounted for a small percentage of all ulcers in the 1990s, but in the 2000s, multiple studies reported that the proportion of idiopathic ulcers had reached 10%-30%, indicating that the incidence of idiopathic ulcers in Asia has also been rising in recent years. While a decline in H. pylori infection rates of general population in Asia is seen as the main reason for the increased incidence of idiopathic ulcers, it is also possible that the absolute number of idiopathic ulcer cases has increased. Advanced age, serious systemic complication, and psychological stress are considered to be the potential risk factors for idiopathic ulcers. Management of idiopathic ulcers is challenging, at present, because there is no effective preventative measure against recurrence in contrast with cases of H. pylori-positive ulcers and NSAIDs-induced ulcers. As it is expected that H. pylori infection rates in Asia will decline further in the future, measures to treat idiopathic ulcers will also likely become more important. PMID:24574744

  4. Interactions between non-steroidal anti-inflammatory drugs and lipid membranes

    Science.gov (United States)

    Boggara, Mohan; Krishnamoorti, Ramanan

    2008-03-01

    Chronic usage of Non-steroidal anti-inflammatory drugs(NSAIDs) leads to gastrointestinal toxicity and clinical evidences point the cause to direct interactions between NSAIDs and phospholipid membranes. Also, NSAIDs pre-associated with phospholipid vesicles are shown to be safer and therapeutically more effective than unmodified ones. Our initial experiments and simulations on the partitioning of Aspirin and Ibuprofen clearly indicate role played by the drug structure in drug-membrane interactions. Those results motivated systematic molecular dynamics simulations of membranes with NSAIDs of different size, structure and pKa values. Our results suggest high partition coefficients for these NSAIDs in the membrane compared to water and thinning effect on the bilayer. Our small angle neutron scattering and reflectivity studies on DMPC-Ibuprofen systems indicate that the drug affects both ˜5 nm thick bilayer and overall ˜100 nm diameter vesicle, indicating that NSAIDs affect vesicles on various length scales. We will discuss the structural perturbations to membranes due to NSAIDs at clinically relevant molar ratios and their implications on the use of vesicles as delivery vehicles for NSAIDs.

  5. Non-steroidal anti-inflammatory drug prescriptions in hospital inpatients: are we assessing the risks?

    LENUS (Irish Health Repository)

    Kitchen, J

    2012-02-01

    AIM: To determine non-steroidal anti-inflammatory drug (NSAID) prescribing practices in a tertiary referral hospital. METHODS: A single time-point audit of drug kardexes and clinical notes of n = 388 patients on 2 July 2008 was carried out assessing demographics, gastrointestinal and coronary heart disease risk factors, renal function and co-prescribed medications. RESULTS: Fifty-seven of 388 (14.7%) hospital patients were on NSAIDs. Forty-nine were prescribed NSAID after admission. Nineteen (32.2%) were on regular NSAID (11\\/19 on PPI) and 38 patients were on PRN NSAID (12\\/38 on PPI). Seventeen of 49 patients were on other medications associated with gastrointestinal bleeding (10\\/17 were on PPI). Nineteen patients (33.3%) were >60 years. Eight patients had three or four risk factors for gastrointestinal bleeding; six were on PPI. Thirteen patients had two risks; 7 were on PPI. Six of 19 patients with one risk factor were on PPI. 40.3% had stage 2\\/3 chronic kidney disease. 35.1% had ischaemic heart disease. CONCLUSIONS: NSAIDs and PPIs are often prescribed inappropriately.

  6. Prevention of Renal Complications Induced by Non- Steroidal Anti-Inflammatory Drugs.

    Science.gov (United States)

    Ković, Sonja Vuč; Vujović, Katarina Savić; Srebro, Dragana; Medić, Branislava; Ilic-Mostic, Tatjana

    2016-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed for the treatment of pain, inflamation and fever. They are usually well tolerated in healthy persons, but in patients with risk factors (advanced age, renal impairment, heart failure, liver disease, concurrent medications with antihypertensive drugs), NSAIDs can induce serious renal adverse effects. They include sodium and water retention with edema, worsening of heart failure, hypertension, hyponatremia, hyperkalemia, acute kidney injury, chronic kidney disease, renal papillary necrosis and acute interstitial nephritis. The majority of these adverse effects are due to the inhibition of prostaglandins synthesis and they are dose and duration-dependent. Acute forms of kidney injuries are transient and often reversible upon drug withdrawal. Chronic use of NSAIDs in some patients may result in chronic kidney disease. It is recommended that patients at risk should have preventative strategies in place, including the use of the "lowest effective dose" of NSAID for the "shortest possible time" and monitoring renal function, fluid retention and electrolyte abnormalities. Patients who are taking antihypertensive medications should be monitored for high blood pressure and the doses of antihypertensive medications should be adjusted if needed. In general, the combination of NSAIDs and angiotensin inhibitors should be avoided. Some other preventive measures are dietary salt restriction, use of topical NSAIDs/non-pharmacological therapies and use of calcium channel blockers for treating hypertension.

  7. [Tolerance to coxibs in patients with intolerance to non-steroidal anti-inflammatory drugs (NSAIDs)].

    Science.gov (United States)

    Boehncke, S; Boehncke, W-H

    2005-10-07

    Non-steroidal anti-inflammatory drugs (NSAIDs) frequently cause pseudoallergic reactions. Recognition of two different prostaglandin synthase iso-enzymes led to the development of the so-called coxibs preferentially inhibiting cyclooxygenase-2. We studied tolerability of valdecoxib preferentially inhibitng cyclooxygenase-2 in patients with a history of intolerance to NSAIDs. 41 patients (30 female, 11male, age 14-74 years) with a history of intolerance to NSAIDs underwent scratch tests with these drugs and valdecoxib, followed by oral challenge with valdecoxib (maximum single dose: 20 mg; cumulative dose: 35mg) in a double-blind, placebo-controlled manner. The history of intolerance to NSAID comprised urticaria as the leading symptom (n = 26), followed by angioedema (n = 11) and anaphylactoid shock (n = 4). 21 patients reported reactions to only one NSAID, 15 identified 2 different triggering drugs, and 5 patients showed reactions to 3 different NSAIDs. Acetylsalicylic acid (n = 20) and diclofenac (n = 12) were the most frequent causative drugs. Upon oral challenge with valdecoxib, one patient developed generalized urticaria within 30 minutes following the last dose of valdecoxib; symptoms resolved after i. v. injection of 2 mg clemastine and 250 mg prednisolone. All other patients tolerated the oral challenge without adverse effects. Our results are in line with previous studies suggesting that preferential cyclooxygenase-2-inhibitors may safely be used by patients with known intolerance to NSAIDs.

  8. Adverse drug reactions in a primary care population prescribed non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Koffeman, Aafke R; Van Buul, Amanda R; Valkhoff, Vera E; Jong, Geert W 't; Bindels, Patrick J E; Sturkenboom, Miriam C J M; Van der Lei, Johan; Luijsterburg, Pim A J; Bierma-Zeinstra, Sita M A

    2015-01-01

    To determine how often patients with musculoskeletal (MSK) complaints prescribed a non-steroidal anti-inflammatory drug (NSAID) subsequently consult their general practitioner (GP) with a non-serious adverse drug reaction (ADR). Cohort study. A healthcare database containing the electronic GP medical records of over 1.5 million patients throughout the Netherlands. A total of 16 626 adult patients with MSK complaints prescribed an NSAID. The patients' medical records were manually assessed for the duration of NSAID use for a maximum of two months, and consultations for complaints predefined as potential ADRs were identified. Subsequently, the likelihood of an association with the NSAID use was assessed and these potential ADRs were categorized as likely, possible, or unlikely ADRs. In total, 961 patients (6%) consulted their GP with 1227 non-serious potential ADRs. In 174 patients (1%) at least one of these was categorized as a likely ADR, and in a further 408 patients (2.5%) at least one was categorized as a possible ADR. Dyspepsia was the most frequent likely ADR, followed by diarrhoea and dyspnoea (respectively 34%, 8%, and 8% of all likely ADRs). Of the patients with MSK complaints prescribed an NSAID, almost one in 30 patients re-consulted their GP with a complaint likely or possibly associated with the use of this drug. The burden of such consultations for non-serious ADRs should be taken into account by GPs when deciding whether treatment with an NSAID is appropriate.

  9. Cardiovascular pharmacogenetics of anti-thrombotic agents and non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Stitham, J; Vanichakarn, P; Ying, L; Hwa, J

    2014-01-01

    The use of antithrombotic agents, particularly antiplatelet drugs like aspirin and clopidogrel, has been instrumental in decreasing the risk for adverse cardiovascular events across a wide range of patients. However, despite the established benefits, the use of these medications remains suboptimal. There is a high degree of inter-individual variation in response to these treatments, whereby patients experience occlusive thromboembolic events, in spite of maintaining an appropriate treatment regimen. This has lead to the notion of antithrombotic "resistance" or "poor responders", which has been a growing concern amongst clinicians and other healthcare providers. Compounding this matter even further, reports of increased cardiovascular risk associated with the use of non-steroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen and naproxen, have revealed additional and unforeseen contributors to myocardial infarction and stroke. With all medications, striking a balance between the potential risks and benefits seems more art than science at times. However, given their widespread use and critical cardiovascular implications, further emphasis has been placed on understanding factors influencing antithrombotic and NSAID therapies. A major aim in cardiovascular pharmacogenetics is the discovery of genetic biomarkers that will allow for prospective screening and individualized prediction of drug efficacy and adverse reactions for these medications (both alone and together) within the context of cardiovascular disease.

  10. Nicolau Syndrome after Intramuscular Injection of Non-Steroidal Anti-Inflammatory Drugs (NSAID

    Directory of Open Access Journals (Sweden)

    Mehmet Dadaci

    2015-01-01

    Full Text Available Nicolau syndrome is a rare complication of intramuscular injection that leads to local ischemic necrosis of the skin and adipose tissue. In this paper, we discuss etiologies, risk factors, and treatment options for gluteal Nicolau syndrome referring to patients treated in our hospital. Our study includes 17 women who visited our clinic with symptoms of gluteal necrosis secondary to intramuscular injection. The following variables were taken into account: injection site, drug administered, frequency of injections, the person who administered the injections, needle size, and needle tip color. Magnetic resonance images obtained in the aftermath of intramuscular injection application were carefully analyzed for presence of necrosis, cyst formation and the thickness of the gluteal fat tissue layer. Drugs that had been received in intramuscular injection were exclusively non-steroidal anti-inflammatory drugs. Mean patient BMI was 41.8 (all patients were considered as obese, and mean gluteal fat thickness was 54 mm. Standard length of needles (3.8 cm had been used in procedures. The wounds were treated with primary closure in 11 patients and with local flap therapy in 6 patients. The observed necrosis was a consequence of misplaced gluteal injection, where drugs were injected into the adipose tissue instead of the muscle due to the extreme thickness of the fat layer, on one hand, and the inappropriate length of standard needles, on the other hand. Intramuscular injection should be avoided in obese patients whenever possible: if it is necessary, proper injection technique should be used.

  11. Nicolau Syndrome after intramuscular injection of non-steroidal anti-inflammatory drugs (NSAID)

    Science.gov (United States)

    Dadaci, Mehmet; Altuntas, Zeynep; Ince, Bilsev; Bilgen, Fatma; Tufekci, Osman; Poyraz, Necdet

    2015-01-01

    Nicolau syndrome is a rare complication of intramuscular injection that leads to local ischemic necrosis of the skin and adipose tissue. In this paper, we discuss etiologies, risk factors, and treatment options for gluteal Nicolau syndrome referring to patients treated in our hospital. Our study includes 17 women who visited our clinic with symptoms of gluteal necrosis secondary to intramuscular injection. The following variables were taken into account: injection site, drug administered, frequency of injections, the person who administered the injections, needle size, and needle tip color. Magnetic resonance images obtained in the aftermath of intramuscular injection application were carefully analyzed for presence of necrosis, cyst formation and the thickness of the gluteal fat tissue layer. Drugs that had been received in intramuscular injection were exclusively non-steroidal anti-inflammatory drugs. Mean patient BMI was 41.8 (all patients were considered as obese), and mean gluteal fat thickness was 54 mm. Standard length of needles (3.8 cm) had been used in procedures. The wounds were treated with primary closure in 11 patients and with local flap therapy in 6 patients. The observed necrosis was a consequence of misplaced gluteal injection, where drugs were injected into the adipose tissue instead of the muscle due to the extreme thickness of the fat layer, on one hand, and the inappropriate length of standard needles, on the other hand. Intramuscular injection should be avoided in obese patients whenever possible if it is necessary, proper injection technique should be used. PMID:25725145

  12. Acute renal failure, associated with non-steroidal anti-inflammatory drugs in healthy children.

    Science.gov (United States)

    Krause, Irit; Cleper, Roxana; Eisenstein, Bella; Davidovits, Miriam

    2005-09-01

    Seven patients aged 13 to 17.5 years developed acute renal failure after treatment with a variety of non-steroidal anti-inflammatory drugs (NSAID): naproxen, diclofenac, ibuprofen, dipyrone and paracetamol. Six of the patients used more than one kind of NSAID. None of the patients had previous history of renal disease or concomitant treatment with other drugs. The time interval between NSAID administration to the emergence of symptoms ranged from 1 to 4 days. The most common presenting symptoms were flank pain (4 patients), abdominal pain (3 patients) and vomiting (3 patients). All patients had normal urine output. Microscopic hematuria and proteinuria were found in 5 patients and leukocyturia in 2. Serum creatinine ranged from 1.3 to 8.3 mg% at presentation. Kidney biopsy was performed in 3 patients and showed findings consistent with mild interstitial inflammation in 1 patient, and normal renal tissue in 2. All patients were treated with intravenous fluids, 1 received corticosteroids. Renal function completely normalized in all patients within 7 to 16 days.

  13. Molecular Basis for Cyclooxygenase Inhibition by the Non-steroidal Anti-inflammatory Drug Naproxen

    Energy Technology Data Exchange (ETDEWEB)

    Duggan, Kelsey C.; Walters, Matthew J.; Musee, Joel; Harp, Joel M.; Kiefer, James R.; Oates, John A.; Marnett, Lawrence J. (Vanderbilt); (Pfizer)

    2010-11-15

    Naproxen ((S)-6-methoxy-{alpha}-methyl-2-naphthaleneacetic acid) is a powerful non-selective non-steroidal anti-inflammatory drug that is extensively used as a prescription and over-the-counter medication. Naproxen exhibits gastrointestinal toxicity, but its cardiovascular toxicity may be reduced compared with other drugs in its class. Despite the fact that naproxen has been marketed for many years, the molecular basis of its interaction with cyclooxygenase (COX) enzymes is unknown. We performed a detailed study of naproxen-COX-2 interactions using site-directed mutagenesis, structure-activity analysis, and x-ray crystallography. The results indicate that each of the pendant groups of the naphthyl scaffold are essential for COX inhibition, and only minimal substitutions are tolerated. Mutation of Trp-387 to Phe significantly reduced inhibition by naproxen, a result that appears unique to this inhibitor. Substitution of S or CH2 for the O atom of the p-methoxy group yielded analogs that were not affected by the W387F substitution and that exhibited increased COX-2 selectivity relative to naproxen. Crystallization and x-ray analysis yielded structures of COX-2 complexed to naproxen and its methylthio analog at 1.7 and 2.3 {angstrom} resolution, respectively. The combination of mutagenesis, structure analysis, and x-ray crystallography provided comprehensive information on the unique interactions responsible for naproxen binding to COX-2.

  14. Encouraging physician appropriate prescribing of non-steroidal anti-inflammatory therapies: protocol of a randomized controlled trial [ISRCTN43532635

    Directory of Open Access Journals (Sweden)

    Metge Colleen

    2004-08-01

    Full Text Available Abstract Background Traditional non-steroidal anti-inflammatory drugs (NSAIDs are a widely used class of therapy in the treatment of chronic pain and inflammation. The drugs are effective and can be relatively inexpensive thanks to available generic versions. Unfortunately the traditional NSAIDs are associated with gastrointestinal complications in a small proportion of patients, requiring costly co-therapy with gastro-protective agents. Recently, a new class of non-steroidal anti-inflammatory agents known as coxibs has become available, fashioned to be safer than the traditional NSAIDs but priced considerably higher than the traditional generics. To help physicians choose appropriately and cost-effectively from the expanded number of anti-inflammatory therapies, scientific bodies have issued clinical practice guidelines and third party payers have published restricted reimbursement policies. The objective of this study is to determine whether an educational intervention can prompt physicians to adjust their prescribing in accordance with these expert recommendations. Methods This is an ongoing, randomized controlled trial. All primary care physicians in Manitoba, Canada have been randomly assigned to a control group or an intervention study group. The educational intervention being evaluated consists of an audit and feedback mechanism combined with optional participation in a Continuing Medical Education interactive workshop. The primary outcome of the study is the change, from pre-to post-intervention, in physicians' appropriate prescribing of non-steroidal anti-inflammatory therapies for patients requiring chronic treatment. Three classes of non-steroidal anti-inflammatory therapies have been identified: coxib therapy, traditional NSAID monotherapy, and traditional NSAID therapy combined with gastro-protective agents. Appropriate prescribing is defined based on international clinical practice guidelines and the provincial drug reimbursement

  15. Psychological profiles of patients with upper gastrointestinal symptomatology induced by non-steroidal anti-inflammatory drugs.

    OpenAIRE

    Juby, A; Davis, P.

    1991-01-01

    Eighty three patients with classical or definite rheumatoid arthritis taking non-steroidal anti-inflammatory drugs (NSAIDs) were studied in an attempt to determine whether a patient's personality and psychological profile might contribute to the development of NSAID induced gastrointestinal symptomatology. It was found that the personality profile of the group of 45 asymptomatic patients was similar to that of a previously reported control group. In contrast, the 37 patients with gastrointest...

  16. Topical non-steroidal anti-inflammatory agents for diabetic cystoid macular oedema.

    Science.gov (United States)

    Sahoo, Soumendra; Barua, Ankur; Myint, Kay Thi; Haq, Adnaan; Abas, Adinegara B L; Nair, N S

    2015-02-16

    Diabetic cystoid macular oedema (CMO) is a condition which involves fluid accumulation in the inner portion of the retina. It often follows changes in retinal blood vessels which enhance the fluid to come out of vessels. Although it may be asymptomatic, symptoms are primarily painless loss of central vision, often with the complaint of seeing black spots in front of the eye.It is reported that CMO may resolve spontaneously, or fluctuate for months, before causing loss of vision. If left untreated or undiagnosed, progression of CMO may lead to permanent visual loss.It has been noted that patients with diabetic retinopathy have elevated inflammatory markers, and therefore it is likely that inflammation aids in the progression of vascular disease in these patients. Several topical non-steroidal anti-inflammatory drugs (NSAIDs) such as ketorolac 0.5%, bromfenac 0.09%, and nepafenac 0.1%, have therefore also been used topically to treat chronic diabetic CMO. Hence this review was conducted to find out the effects of topical NSAIDs in diabetic CMO. To assess the effects of topical non-steroidal anti-inflammatory drugs (NSAIDs) for diabetic cystoid macular oedema (CMO). We searched CENTRAL (which contains the Cochrane Eyes and Vision Group Trials Register) (2014, Issue 12), Ovid MEDLINE, Ovid MEDLINE In-Process and Other Non-Indexed Citations, Ovid MEDLINE Daily, Ovid OLDMEDLINE (January 1946 to January 2015), EMBASE (January 1980 to January 2015), Latin American and Caribbean Health Sciences Literature Database (LILACS) (January 1982 to January 2015), the ISRCTN registry (www.isrctn.com/editAdvancedSearch), ClinicalTrials.gov (www.clinicaltrials.gov) and the WHO International Clinical Trials Registry Platform (ICTRP) (www.who.int/ictrp/search/en). We did not use any date or language restrictions in the electronic searches for trials. We last searched the electronic databases on 12 January 2015. Randomised controlled trials (RCTs) and quasi-RCTs investigating the effects

  17. Impact of non-steroidal anti-inflammatory drugs on hypertensive disorders of pregnancy.

    Science.gov (United States)

    Wasden, Shane W; Ragsdale, Ellie S; Chasen, Stephen T; Skupski, Daniel W

    2014-10-01

    Non-steroidal anti-inflammatory drug (NSAID) use has the potential to adversely affect blood pressure in women with hypertensive disorders of pregnancy. We sought to evaluate this association. Women affected with severe hypertensive disorders of pregnancy were identified by retrospective chart review. The medication administration record was then used to identify controls (no NSAID exposure) until a sufficient number of patients were obtained, after which the cases (NSAID exposed) were identified in a chronological manner during the same study period until a 2:1 ratio was achieved. The primary outcome was the change in mean of all postpartum mean arterial pressures (MAP) throughout the hospital stay. Power analysis showed that 146 exposed and 73 unexposed subjects were necessary to obtain 90% power to detect a MAP difference of 10mmHg between the groups. Secondary outcomes included: initiation of anti-hypertensive medication, need for increased doses of anti-hypertension medication, and adverse events related to hypertension. 223 women had severe hypertensive disorders of pregnancy, of whom 75 (34%) were not exposed to NSAIDs and 148 (66%) were exposed. NSAID exposure was not associated with a difference in the average MAP postpartum (p=0.70), nor any of the secondary outcomes evaluated. Exposure to NSAIDs was less likely as serum creatinine increased (p=0.012). In women with severe hypertensive disorders of pregnancy, NSAIDs did not appear to increase the average postpartum MAP, increase the requirement for anti-hypertensive medications, or increase the rate of adverse postpartum events. Copyright © 2014 International Society for the Study of Hypertension in Pregnancy. Published by Elsevier B.V. All rights reserved.

  18. [Hypersensitivity reactions to non-steroidal anti-inflammatory drugs and tolerance to alternative drugs].

    Science.gov (United States)

    Calvo Campoverde, K; Giner-Muñoz, M T; Martínez Valdez, L; Rojas Volquez, M; Lozano Blasco, J; Machinena, A; Plaza, A M

    2016-03-01

    Hypersensitivity reactions to non-steroidal anti-inflammatory drugs (NSAIDs) are the most common reactions to drugs. The prevalence varies from 0.6 to 5.7% in general population, but there are no data available in children. The aim of this study is to determine the frequency of patients diagnosed with hypersensitivity to NSAIDs, and describe their clinical characteristics, type of hypersensitivity, and tolerance to alternative drugs. Retrospective study was conducted on children with suspected hypersensitivity to NSAIDs from January 2012 to December 2013. The diagnosis was confirmed by oral drug provocation test (DPT) to the drug involved in the group with a history of one episode, while in the group with a history of more than one episode with the same drug the diagnosis was based on clinical data. Subsequently, a DPT with acetylsalicylic acid (ASA) was done in order to classify hypersensitivity into selective or multiple. In those cases with a positive result, a DPT was performed with alternative drugs. Out of a total of 93 children studied, 26 were diagnosed with hypersensitivity to NSAIDs: 7 confirmed by oral DPT, and 19 based on clinical data. Multiple hypersensitivity was diagnosed in 50% of patients. Ibuprofen was involved in all reactions. The most common clinical manifestation was angioedema (44%). Acetaminophen was the best tolerated alternative drug. More than one quarter (28%) of the population studied was diagnosed with hypersensitivity to NSAIDs, and 50% had multiple hypersensitivity. Acetaminophen is a safe alternative in children with hypersensitivity to NSAIDs. Meloxicam may be an alternative in cases that do not tolerate acetaminophen. Copyright © 2015 Asociación Española de Pediatría. Published by Elsevier España, S.L.U. All rights reserved.

  19. Significant Acute Kidney Injury Due to Non-steroidal Anti-inflammatory Drugs: Inpatient Setting

    Directory of Open Access Journals (Sweden)

    Mehul Dixit

    2010-04-01

    Full Text Available In the United States non-steroidal anti-inflammatory drugs (NSAID are freely available over-the-counter. Because of the adverse effects on the kidneys and the popularity of these drugs, unregulated use of NSAIDs is an under recognized and potentially dangerous problem. Fifteen inpatients, mean age of 15.2 ± 2.3 years (five males, 10 females, were referred to nephrology for acute kidney injury. All patients admitted to taking ibuprofen and six also consumed naproxen. None of the patients had underlying renal diseases at the time of admission. Nine patients had proteinuria and 12 had hematuria (including one with gross hematuria. One patient had nephrotic syndrome but the condition resolved spontaneously without steroids and has remained in remission for four years. Two patients required dialysis. Only one of the dialyzed patients required steroid therapy for recovery of renal function. The mean duration of hospitalization was 7.4 ± 5.5 days. The serum creatinine peaked at 4.09 ± 4.24 (range 1.2-15.3 mg/dL. All patients recovered renal function with normalization of serum creatinine to 0.71 ± 0.15 mg/dL. The estimated GFR (glomerular filtration rate at peak of renal failure was 38.2 ± 20.5 mL/min but did improve to a baseline of 134 ± 26.2 mL/min (range 89-177, p < 0.01. However, the duration from onset to normalization of serum creatinine was 37 ± 42 days indicating that majority of patients had abnormal renal function for a prolonged period. In conclusion, NSAIDs pose a significant risk of renal failure for significant duration and as an entity may be under recognized.

  20. Perioperative use of non-steroidal anti-inflammatory drugs might impair dental implant osseointegration.

    Science.gov (United States)

    Winnett, Brent; Tenenbaum, Howard C; Ganss, Ben; Jokstad, Asbjørn

    2016-02-01

    To appraise whether adverse biological events following oral implant placement may be associated with perioperative use of non-steroidal anti-inflammatory drugs (NSAIDs). All patients treated in a university faculty postgraduate dental clinic between 1979 and 2012 that had experienced a failing and surgically removed dental implant (292 implants in 168 patients) were contacted to solicit additional information about their present dental and medical status and frequency of current and past use of NSAIDs. Potential associations between perioperative NSAIDs use and the occurrence of adverse biological events were explored by the use of 2 × 2 tables and two-tailed Fisher's exact tests. One hundred and four patients with initially 468 implants had experienced 238 implant failures, of which 197 were due to failing osseointegration (42%). Sixty of the participants, initially with 273 implants, had used NSAIDs perioperatively and experienced 44% implant failures, versus 38% in the non-NSAID cohort. The NSAID cohort experienced 3.2 times more cases of radiographic bone loss greater than 30% of the vertical height of their remaining implants and 1.9 times more cases of cluster failures, defined as failure of 50% or more of the implant(s) placed. Notwithstanding that a retrospective study design is open to potential bias, the current data indicate that dental implant osseointegration may be affected negatively by an inhibitory effect of NSAIDs on bone healing in vulnerable patients. Future and better clinical studies than the current should be designed to appraise more precisely the potential effects of NSAIDs on implant osseointegration in study populations that are not limited by stringent medical inclusion and exclusion criteria. © 2014 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

  1. Influence of non-steroidal anti-inflammatory drugs on antiplatelet effect of aspirin.

    Science.gov (United States)

    Yokoyama, H; Ito, N; Soeda, S; Ozaki, M; Suzuki, Y; Watanabe, M; Kashiwakura, E; Kawada, T; Ikeda, N; Tokuoka, K; Kitagawa, Y; Yamada, Y

    2013-02-01

    It has been reported that ibuprofen interferes with the antiplatelet effect of low-dose aspirin. This interaction is ascribed to steric hindrance at the active site of cyclooxygenase-1 by ibuprofen, when aspirin is administered after ibuprofen. However, whether other non-steroidal anti-inflammatory drugs (NSAIDs) interact with aspirin similarly is not well defined. The aim of this study was to assess the influence of nine NSAIDs on the antiplatelet effect of aspirin. We investigated the antiplatelet effect of NSAIDs using steady-state plasma concentration reported after usual doses. We studied the in vitro antiplatelet effect of NSAID alone, aspirin alone, aspirin before NSAID addition and aspirin after NSAID addition to platelet-rich plasma. The rates of platelet aggregation induced by collagen were determined. The final concentration of aspirin used was the 50% effective concentration (EC(50)) previously estimated in vitro. Ibuprofen and mefenamic acid interfere with the antiplatelet effect of aspirin when added before the latter. The rate of platelet aggregation was reduced by 48·1% and 22·7%, respectively. The other NSAIDs tested did not significantly affect the aspirin antiplatelet effect when exposure was prior to aspirin. None of the nine NSAIDs altered the aspirin effect if administration followed that of aspirin. Naproxen and flurbiprofen have significant antiplatelet effects at plasma concentrations seen with usual doses. Our in vitro model suggests that the antiplatelet effect of aspirin is significantly diminished when taken after, but not before, ibuprofen or mefenamic acid. None of the other NSAIDs tested had any effect irrespective of the timing of dosing. © 2012 Blackwell Publishing Ltd.

  2. New insights into the use of currently available non-steroidal anti-inflammatory drugs

    Directory of Open Access Journals (Sweden)

    Brune K

    2015-02-01

    Full Text Available Kay Brune,1 Paola Patrignani2 1Department of Experimental and Clinical Pharmacology and Toxicology, Friedrich-Alexander University Erlangen-Nuremberg, Erlangen, Germany; 2Department of Neuroscience, Imaging and Clinical Sciences, Center of Excellence on Aging, G d’Annunzio University, Chieti, Italy Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs, which act via inhibition of the cyclooxygenase (COX isozymes, were discovered more than 100 years ago. They remain a key component of the pharmacological management of acute and chronic pain. The COX-1 and COX-2 isozymes have different biological functions; analgesic activity is primarily (although not exclusively associated with inhibition of COX-2, while different side effects result from the inhibition of COX-1 and COX-2. All available NSAIDs, including acetaminophen and aspirin, are associated with potential side effects, particularly gastrointestinal and cardiovascular effects, related to their relative selectivity for COX-1 and COX-2. Since all NSAIDs exert their therapeutic activity through inhibition of the COX isozymes, strategies are needed to reduce the risks associated with NSAIDs while achieving sufficient pain relief. A better understanding of the inhibitory activity and COX-1/COX-2 selectivity of an NSAID at therapeutic doses, based on pharmacokinetic and pharmacodynamic properties (eg, inhibitory dose, absorption, plasma versus tissue distribution, and elimination, and the impact on drug tolerability and safety can guide the selection of appropriate NSAIDs for pain management. For example, many NSAIDs with moderate to high selectivity for COX-2 versus COX-1 can be administered at doses that maximize efficacy (~80% inhibition of COX-2 while minimizing COX-1 inhibition and associated side effects, such as gastrointestinal toxicity. Acidic NSAIDs with favorable tissue distribution and short plasma half-lives can additionally be dosed to provide near-constant analgesia while

  3. Non-steroidal anti-inflammatory drugs for the common cold.

    Science.gov (United States)

    Kim, Soo Young; Chang, Yoon-Jung; Cho, Hye Min; Hwang, Ye-Won; Moon, Yoo Sun

    2015-09-21

    Non-steroidal anti-inflammatory drugs (NSAIDs) have been widely used for the treatment of pain and fever associated with the common cold. To determine the effects of NSAIDs versus placebo (and other treatments) on signs and symptoms of the common cold, and to determine any adverse effects of NSAIDs in people with the common cold. We searched CENTRAL (2015, Issue 4, April), (January 1966 to April week 3, 2015), EMBASE (January 1980 to April 2015), CINAHL (January 1982 to April 2015) and ProQuest Digital Dissertations (January 1938 to April 2015). Randomised controlled trials (RCTs) of NSAIDS in adults or children with the common cold. Four review authors extracted data. We subdivided trials into placebo-controlled RCTs and head-to-head comparisons of NSAIDs. We extracted and summarised data on global analgesic effects (such as reduction of headache and myalgia), non-analgesic effects (such as reduction of nasal symptoms, cough, sputum and sneezing) and side effects. We expressed dichotomous outcomes as risk ratios (RR) with 95% confidence intervals (CI) and continuous data as mean differences (MD) or standardised mean differences (SMD). We pooled data using the fixed-effect and random-effects models. We included nine RCTs with 1069 participants, describing 37 comparisons: six were NSAIDs versus placebo and three were NSAIDs versus NSAIDs. The overall risk of bias in the included studies was mixed. In a pooled analysis, NSAIDs did not significantly reduce the total symptom score (SMD -0.40, 95% CI -1.03 to 0.24, three studies, random-effects model), or duration of colds (MD -0.23, 95% CI -1.75 to 1.29, two studies, random-effects model). For respiratory symptoms, cough did not improve (SMD -0.05, 95% CI -0.66 to 0.56, two studies, random-effects model) but the sneezing score significantly improved (SMD -0.44, 95% CI -0.75 to -0.12, two studies, random-effects model). For outcomes related to the analgesic effects of NSAIDs (headache, ear pain, and muscle and joint

  4. Non-steroidal anti-inflammatory drugs versus corticosteroids for controlling inflammation after uncomplicated cataract surgery.

    Science.gov (United States)

    Juthani, Viral V; Clearfield, Elizabeth; Chuck, Roy S

    2017-07-03

    Cataract is a leading cause of blindness worldwide. Cataract surgery is commonly performed but can result in postoperative inflammation of the eye. Inadequately controlled inflammation increases the risk of complications. Non-steroidal anti-inflammatory drugs (NSAIDs) and corticosteroids are used to prevent and reduce inflammation following cataract surgery, but these two drug classes work by different mechanisms. Corticosteroids are effective, but NSAIDs may provide an additional benefit to reduce inflammation when given in combination with corticosteroids. A comparison of NSAIDs to corticosteroids alone or combination therapy with these two anti-inflammatory agents will help to determine the role of NSAIDs in controlling inflammation after routine cataract surgery. To evaluate the comparative effectiveness of topical NSAIDs (alone or in combination with topical corticosteroids) versus topical corticosteroids alone in controlling intraocular inflammation after uncomplicated phacoemulsification. To assess postoperative best-corrected visual acuity (BCVA), patient-reported discomfort, symptoms, or complications (such as elevation of IOP), and cost-effectiveness with the use of postoperative NSAIDs or corticosteroids. To identify studies relevant to this review, we searched the Cochrane Central Register of Controlled Trials (CENTRAL), which contains the Cochrane Eyes and Vision Trials Register (2016, Issue 12), MEDLINE Ovid (1946 to December 2016), Embase Ovid (1947 to 16 December 2016), PubMed (1948 to December 2016), LILACS (Latin American and Caribbean Health Sciences Literature Database) (1982 to 16 December 2016), the metaRegister of Controlled Trials (mRCT) (www.controlled-trials.com; last searched 17 June 2013), ClinicalTrials.gov (www.clinicaltrials.gov; searched December 2016), and the WHO International Clinical Trials Registry Platform (ICTRP) (www.who.int/ictrp/search/en; searched December 2016). We included randomized controlled trials (RCTs) in which

  5. Topical non-steroidal anti-inflammatory drugs for analgesia in traumatic corneal abrasions.

    Science.gov (United States)

    Wakai, Abel; Lawrenson, John G; Lawrenson, Annali L; Wang, Yongjun; Brown, Michael D; Quirke, Michael; Ghandour, Omar; McCormick, Ryan; Walsh, Cathal D; Amayem, Ahmed; Lang, Eddy; Harrison, Nick

    2017-05-18

    Traumatic corneal abrasions are relatively common and there is a lack of consensus about analgesia in their management. It is therefore important to document the clinical efficacy and safety profile of topical ophthalmic non-steroidal anti-inflammatory drugs (NSAIDs) in the management of traumatic corneal abrasions. To identify and evaluate all randomised controlled trials (RCTs) comparing the use of topical NSAIDs with placebo or any alternative analgesic interventions in adults with traumatic corneal abrasions (including corneal abrasions arising from foreign body removal), to reduce pain, and its effects on healing time. We searched the Cochrane Central Register of Controlled Trials (CENTRAL) (which contains the Cochrane Eyes and Vision Trials Register) (2017, Issue 2), MEDLINE Ovid (1946 to 30 March 2017), Embase Ovid (1947 to 30 March 2017), LILACS (Latin American and Caribbean Health Sciences Literature Database) (1982 to 30 March 2017), OpenGrey (System for Information on Grey Literature in Europe) (www.opengrey.eu/); searched 30 March 2017, ZETOC (1993 to 30 March 2017), the ISRCTN registry (www.isrctn.com/editAdvancedSearch); searched 30 March 2017, ClinicalTrials.gov (www.clinicaltrials.gov); searched 30 March 2017 and the WHO International Clinical Trials Registry Platform (ICTRP) (www.who.int/ictrp/search/en); searched 30 March 2017. We did not use any date or language restrictions in the electronic searches for trials.We checked the reference lists of identified trials to search for further potentially relevant studies. RCTs comparing topical NSAIDs to placebo or any alternative analgesic interventions in adults with traumatic corneal abrasions. Two review authors independently performed data extraction and assessed risks of bias in the included studies. We rated the certainty of the evidence using GRADE. We included nine studies that met the inclusion criteria, reporting data on 637 participants.The studies took place in the UK, USA, Israel, Italy

  6. Effectiveness of various non-steroidal anti-inflammatory drugs in ...

    African Journals Online (AJOL)

    Purpose: To study the effectiveness of various nonsteroidal anti-inflammatory drugs (NSAIDs) in patients with vertebral fractures. Methods: A total of 78 patients (17 males and 61 females) with a mean age of 69.5 years were included. The major inclusion criterion was an osteoporotic vertebral fracture between T7 and L3.

  7. Trends in the non-steroidal anti-inflammatory drug market in six Central-Eastern European countries based on retail information.

    Science.gov (United States)

    Inotai, András; Hankó, Balázs; Mészáros, Agnes

    2010-02-01

    The objective of this study was to evaluate the non-steroidal anti-inflammatory drug market of six Central and Eastern European countries. Trends and similarities were compared across the examined countries. The Intercontinental Marketing Service Health database was used to determine consumption data between the years 2000 and 2007. We applied the anatomical therapeutical chemical-defined daily dose method, focussing on three major non-steroidal anti-inflammatory drug groups: conventional non-steroidal anti-inflammatory drugs, 'stronger cyclooxygenase 2 inhibitors' (all together as: non-cyclooxygenase 2 selective non-steroidal anti-inflammatory drugs) and selective cyclooxygenase 2 inhibitors. The main outcome measure was defined daily dose/1000 inhabitants/day. Different active agents have been distinguished between the three major groups. In total the non-steroidal anti-inflammatory drug group reached a 42.82-74.17 defined daily dose/1000 inhabitants/day volume in 2007, with an average total increase of 25.1% between 2002 and 2007. In the conventional non-steroidal anti-inflammatory drug group, diclofenac and ibuprofen have attained the highest consumption. Our results show a notable increase (325%, 2002-2007) of the 'stronger cyclooxygenase 2 inhibitor group' (nimesulide and meloxicam). Trends of selective cyclooxygenase 2 inhibitor volumes differ within the observed countries. Differences in the six countries concerning their NSAID consumption and market trends could not be explained with the inequalities in patient characteristics. The conventional NSAID retail gave the majority of the total NSAID market. The consumption of selective COX2 inhibitors in all of the six countries were much lower than in the US or Australia. The NSAID risk profile in the region is comparable to previous studies in other countries. Copyright (c) 2009 John Wiley & Sons, Ltd.

  8. Non-Steroidal Anti-inflammatory Drugs As Host-Directed Therapy for Tuberculosis: A Systematic Review

    Directory of Open Access Journals (Sweden)

    Vera M. Kroesen

    2017-06-01

    Full Text Available Lengthy, antimicrobial therapy targeting the pathogen is the mainstay of conventional tuberculosis treatment, complicated by emerging drug resistances. Host-directed therapies, including non-steroidal anti-inflammatory drugs (NSAIDs, in contrast, target host factors to mitigate disease severity. In the present Systematic Review, we investigate whether NSAIDs display any effects as therapy of TB and discuss possible mechanisms of action of NSAIDs as adjunctive therapy of TB. Ten studies, seven preclinical studies in mice and three clinical trials, were included and systematically reviewed. Our results point toward a beneficial effect of NSAIDs as adjunct to current TB therapy regimens, mediated by decreased lung pathology balancing host-immune reaction. The determination of the best timing for their administration in order to obtain the potential beneficial effects needs further investigation. Even if the preclinical evidence requires clinical evaluation, NSAIDs might represent a potential safe, simple, and cheap improvement in therapy of TB.

  9. Non-steroidal anti-inflammatory drugs and risk of cardiovascular disease in patients with rheumatoid arthritis

    DEFF Research Database (Denmark)

    Lindhardsen, Jesper; Gislason, Gunnar Hilmar; Jacobsen, Søren

    2013-01-01

    OBJECTIVE: To examine the risk of major cardiovascular disease associated with non-steroidal anti-inflammatory drugs (NSAIDs) in a large 'real-world' contemporary rheumatoid arthritis (RA) cohort. METHODS: A longitudinal cohort study was conducted with use of Danish nationwide individual......-level registry data on inpatient and outpatient health care provision, pharmacotherapy and income during 1997-2009. 17 320 RA patients were identified and matched with 69 280 controls (4 : 1) by age and sex. NSAID-associated risk of major cardiovascular disease defined as the combined endpoint of myocardial...... infarction, stroke or cardiovascular mortality was assessed in multivariable survival models. RESULTS: During follow-up (median 4.9 years) 6283 events occurred. The cardiovascular risk associated with overall NSAID use was significantly lower in RA patients than in controls (HR 1.22 (95% CI 1.09 to 1.37) vs...

  10. Role of non-steroidal anti-inflammatory drugs on intestinal permeability and nonalcoholic fatty liver disease.

    Science.gov (United States)

    Utzeri, Erika; Usai, Paolo

    2017-06-14

    The use of non-steroidal anti-inflammatory drugs (NSAIDs) is widespread worldwide thanks to their analgesic, anti-inflammatory and antipyretic effects. However, even more attention is placed upon the recurrence of digestive system complications in the course of their use. Recent data suggests that the complications of the lower gastro-intestinal tract may be as frequent and severe as those of the upper tract. NSAIDs enteropathy is due to enterohepatic recycling of the drugs resulting in a prolonged and repeated exposure of the intestinal mucosa to the compound and its metabolites. Thus leading to so-called topical effects, which, in turn, lead to an impairment of the intestinal barrier. This process determines bacterial translocation and toxic substances of intestinal origin in the portal circulation, leading to an endotoxaemia. This condition could determine a liver inflammatory response and might promote the development of non-alcoholic steatohepatitis, mostly in patients with risk factors such as obesity, metabolic syndrome and a high fat diet, which may induce a small intestinal bacterial overgrowth and dysbiosis. This alteration of gut microbiota may contribute to nonalcoholic fatty liver disease and its related disorders in two ways: firstly causing a malfunction of the tight junctions that play a critical role in the increase of intestinal permeability, and then secondly leading to the development of insulin resistance, body weight gain, lipogenesis, fibrogenesis and hepatic oxidative stress.

  11. Medicine information leaflets for non-steroidal anti-inflammatory drugs in Thailand.

    Science.gov (United States)

    Phueanpinit, Pacharaporn; Pongwecharak, Juraporn; Krska, Janet; Jarernsiripornkul, Narumol

    2016-02-01

    The importance of promoting the use of patient-oriented medicines leaflets is recognized in many countries. Leaflets should include basic information plus specific warnings, and be provided with all medicines, but there is little attempt at enforcement of these requirements in Thailand. To determine content and availability of Thai information leaflets for nonsteroidal anti-inflammatory drugs (NSAIDs). Leaflets for all NSAIDs available for purchase from 34 pharmacies in a large city were evaluated against a checklist and number of leaflets assessed against number of medicine packs available in each pharmacy. Of the 76 leaflets for ten different NSAIDs, 67 (88 %) were for locally manufactured products. Only 22 % of 76 leaflets were sufficient in number for distribution with medicines, while only 4 % had patient-oriented leaflets. No leaflet covered all topics in the checklist. Less than half included safety information, such as contraindications (46 %), precautions (47 %), and adverse drug reactions (34 %). Locally-produced leaflets provided less information than those for originator products and no leaflet included all the warnings required by Thai regulations. This study illustrates the variable availability and quality of NSAID information leaflets. The lack of accessible essential information about medicines in Thailand requires urgent attention to enable patients to minimise adverse reactions.

  12. Molecular mechanisms in the selectivity of non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Khan, Yasmin Shamsudin; Gutiérrez de Terán, Hugo; Åqvist, Johan

    2018-01-18

    Nonsteroidal anti-inflammatory drugs (NSAIDs) inhibit cyclooxygenase (COX) 1 and 2 with varying degrees of selectivity. A group of COX-2 selective inhibitors - coxibs - bind in a time-dependent manner through a three-step mechanism, utilizing a side-pocket in the binding site. Coxibs have been extensively probed to identify the structural features regulating the slow tight-binding mechanism responsible for COX-2 selectivity. In this study, we further probe a structurally and kinetically diverse data set of COX inhibitors in COX-2 by molecular dynamics and free energy simulations. We find that the features regulating the high affinities associated with time-dependency in COX depend on the inhibitor kinetics. In particular, most time-dependent inhibitors share a common structural binding mechanism, involving an induced-fit rotation of the side-chain of Leu531 in the main binding pocket. The high affinities of two-step slow tight-binding inhibitors and some slow reversible inhibitors can thus be explained by the increased space in the main binding pocket after this rotation. Coxibs that belong to a separate class of slow tight-binding inhibitors benefit more from the displacement of the neighboring side-chain of Arg513, exclusive to the COX-2 side-pocket. This displacement further stabilizes the aforementioned rotation of Leu531, and can explain the selectivity of coxibs for COX-2.

  13. toxicosis of non-steroidal anti-inflammatory agents in rats

    African Journals Online (AJOL)

    ABATAN

    plasma collected from 39 Mycobacterium bovis infected cattle and. 55 M. bovis free cattle were measured using atomic absorption ... derivative (B-PPD) and avian purified protein derivative (A-PPD) obtained from the Veterinary .... effects on biological system at a high rate. In biologic systems, free radicals may be centred on.

  14. Penetration and pharmacokinetics of non-steroidal anti-inflammatory drugs in rat prostate tissue.

    Science.gov (United States)

    Yellepeddi, Venkata K; Radhakrishnan, Jayashree; Radhakrishnan, Rajan

    2018-02-01

    Chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS) involves inflammation of the prostate and affects the quality of life of men of all ages. It is well reported in clinical studies that the treatment for CP/CPPS using nonsteroidal anti-inflammatory drugs (NSAIDs) produced favorable outcomes. However, currently, there are no guidelines on choice of the NSAIDs for the treatment of CP/CPPS. Therefore, in the current research study, we evaluated the prostate tissue penetration of four NSAIDs in rats to provide guidance on choice of NSAIDs for the treatment of CP/CPPS. Male Sprague-Dawley rats were administered orally with four NSAIDs viz. celecoxib, diclofenac, ibuprofen, and naproxen at 500 mg/kg dose. The animals were then sacrificed at various time points, and their prostate tissues were harvested. The NSAIDs were then extracted from the prostate tissues using liquid extraction technique, and their concentration in prostate tissue was quantified using high-performance liquid chromatography (HPLC). The prostate tissue penetration and related pharmacokinetic parameters were evaluated by non-compartmental analysis. The HPLC method for quantifying NSAIDs in prostate tissue resulted in single, sharp peaks without any interference and all validation parameters were within limits. Celecoxib showed the highest area under the curve (AUC) [146.50 ± 2.75 μg/mL*h] of all NSAID's. A two-factor analysis of variance (ANOVA) with replication indicated an overall statistically significant difference in the pharmacokinetic parameters for celecoxib, diclofenac, ibuprofen, and naproxen. This study for the first time reported the relative prostate tissue penetration of four NSAIDs. The pharmacokinetic data indicated that celecoxib has the highest penetration and retention in rat prostate tissues. Therefore, celecoxib may be considered as a better choice for the treatment CP/CPPS involving NSAIDs. © 2017 Wiley Periodicals, Inc.

  15. Non-steroidal anti-inflammatory drug in adjuvant treatment of intravitreal triamcinolone acetonide for macular edema

    Directory of Open Access Journals (Sweden)

    Xiao-Juan Liu

    2016-06-01

    Full Text Available AIM: To study the clinical value of non-steroidal anti-inflammatory drug in adjuvant treatment of intravitreal triamcinolone acetonide(IVTAfor macular edema caused by retinal vein occlusion(RVO. METHODS: Forty-eight eyes in 48 patients were randomly divided into trial and control group(24 eyes eachin this prospective study. In the trial group, additional pranoprofen drops was administered from 1d before IVTA to 30d after injection. Central foveal thickness(CFTwas measured with optical coherence tomography(OCT. Available documents of best corrected visual acuity(BCVA, CFT, intraocular pressure and complications pre- and post-injection at 3d, 1,2wk, 1 and 3mo were evaluated. RESULTS: After IVTA, BCVA was improved in both groups at different levels; but there was no statistically significant between two groups at each time point(P>0.05. The CFT values were 629±43μm vs 605±57μm before IVTA in the trail vs control groups(P>0.05. The values were 432±74μm vs 511±32μm(t=7.533, Pvs 379±29μm(t=13.212, Pvs control groups at 1 and 3mo after IVTA, respectively. Ocular hypertension occurred in 5 eyes after injection in trail group, and was controlled with anti-glaucoma medication and one eye with filtration surgery. Progression of cataract was noted in 3 of 35 phakic eyes and cataract surgery was performed in 2 eyes at 4-12mo after injection in trail group. Progression of cataract was noted in 4 eyes and cataract surgery was performed in 2 eyes at 4-12mo after injection in control group. No retinal detachment and endophthalmitis happened during the whole period of follow-up.CONCLUSION: Application of non-steroidal anti-inflammatory eye drops in perioperative period can be useful to improve the outcome of IVTA for macular edema, which needs further evaluation.

  16. 2-hydroxy arachidonic acid: a new non-steroidal anti-inflammatory drug.

    Directory of Open Access Journals (Sweden)

    Daniel H Lopez

    Full Text Available BACKGROUND: Nonsteroidal anti-inflammatory drugs (NSAIDs are a family of COX1 and COX2 inhibitors used to reduce the synthesis of pro-inflammatory mediators. In addition, inflammation often leads to a harmful generation of nitric oxide. Efforts are being done in discovering safer NSAIDs molecules capable of inhibiting the synthesis of pro-inflammatory lipid mediators and nitric oxide to reduce the side effects associated with long term therapies. METHODOLOGY/PRINCIPAL FINDINGS: The analogue of arachidonic acid (AA, 2-hydroxy-arachidonic acid (2OAA, was designed to inhibit the activities of COX1 and COX2 and it was predicted to have similar binding energies as AA for the catalytic sites of COX1 and COX2. The interaction of AA and 2OAA with COX1 and COX2 was investigated calculating the free energy of binding and the Fukui function. Toxicity was determined in mouse microglial BV-2 cells. COX1 and COX2 (PGH2 production activities were measured in vitro. COX1 and COX2 expression in human macrophage-like U937 cells were carried out by Western blot, immunocytochemistry and RT-PCR analysis. NO production (Griess method and iNOS (Western blot were determined in mouse microglial BV-2 cells. The comparative efficacy of 2OAA, ibuprofen and cortisone in lowering TNF-α serum levels was determined in C57BL6/J mice challenged with LPS. We show that the presence of the -OH group reduces the likelihood of 2OAA being subjected to H* abstraction in COX, without altering significantly the free energy of binding. The 2OAA inhibited COX1 and COX2 activities and the expression of COX2 in human U937 derived macrophages challenged with LPS. In addition, 2OAA inhibited iNOS expression and the production of NO in BV-2 microglial cells. Finally, oral administration of 2OAA decreased the plasma TNF-α levels in vivo. CONCLUSION/SIGNIFICANCE: These findings demonstrate the potential of 2OAA as a NSAID.

  17. Functionalized carbon nanotubes as the pseudostationary phase for capillary EKC separation of non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Huang, Yi-Jin; Wang, Guan-Ren; Huang, Kuan-Pin; Hsieh, Yu-Fang; Liu, Chuen-Ying

    2009-11-01

    Functionalized multiwalled carbon nanotubes (f-MWCNTs) can serve as the pseudostationary phase (PSP) for the capillary EKC separation of non-steroidal anti-inflammatory drugs (NSAIDs). To increase their hydrophilicity, we treated MWCNTs, with a sonochemical process in a concentrated nitric/sulfuric acid mixture. The oxidized MWCNTs were then characterized by FT-IR, transmission electron microscopy, and X-ray photoelectron spectroscopy. We evaluated the potential of the PSP and the effects of buffer composition, pH, addition of organic modifier, and injection temperature on the NSAID separation. The PSP created a network structure of pi-pi interactions, hydrophobic forces, hydrogen bonding, and electrostatic interactions to separate NSAIDs, providing a different separation mode from SDS micelles. We achieved complete separation of six NSAIDs using a mixture of a borate buffer (75 mM, pH 10) with methanol (5%, v/v) containing 0.02 mg/mL f-MWCNTs, an applied voltage of +12 kV and detection at 214 nm. Better precision was obtained with a low injection temperature. The method was also satisfactorily applied to the analysis of NSAIDs spiked into a urine sample.

  18. Removal of non-steroidal anti-inflammatory drugs ibuprofen and ketoprofen from water by emulsion liquid membrane.

    Science.gov (United States)

    Dâas, Attef; Hamdaoui, Oualid

    2014-02-01

    In this work, the removal of the worldwide non-steroidal anti-inflammatory drugs ibuprofen (IBP) and ketoprofen (KTP) by emulsion liquid membrane (ELM) was carried out. An ELM system is made up of hexane as diluent, Span 80 as the surfactant and sodium carbonate as the inner aqueous solution. Effect of experimental conditions that affect the extraction of IBP such as surfactant concentration, emulsification time, sulfuric acid concentration in external phase, acid type in external phase, internal phase concentration, type of internal phase, stirring speed, volume ratio of internal phase to membrane phase, treatment ratio, IBP initial concentration, diluent type and salt was investigated. The obtained results showed that by appropriate selection of the operational parameters, it was possible to extract nearly all of IBP molecules from the feed solution even in the presence of high concentration of salt. Under optimum operating conditions, the efficiencies of IBP removal from distilled water (99.3 %), natural mineral water (97.3 %) and sea water (94.0 %) were comparable, which shows that the ELM treatment process represents a very interesting advanced separation process for the removal of IBP from complex matrices such as natural and sea waters. Under the optimized experimental conditions, approximately 97.4 % KTP was removed in less than 20 min of contact time.

  19. Randomized trial of switching from prescribed non-selective non-steroidal anti-inflammatory drugs to prescribed celecoxib

    DEFF Research Database (Denmark)

    Macdonald, Thomas M; Hawkey, Chris J; Ford, Ian

    2017-01-01

    BACKGROUND: Selective cyclooxygenase-2 inhibitors and conventional non-selective non-steroidal anti-inflammatory drugs (nsNSAIDs) have been associated with adverse cardiovascular (CV) effects. We compared the CV safety of switching to celecoxib vs. continuing nsNSAID therapy in a European setting....... METHOD: Patients aged 60 years and over with osteoarthritis or rheumatoid arthritis, free from established CV disease and taking chronic prescribed nsNSAIDs, were randomized to switch to celecoxib or to continue their previous nsNSAID. The primary endpoint was hospitalization for non-fatal myocardial...... expected developed an on-treatment (OT) primary CV event and the rate was similar for celecoxib, 0.95 per 100 patient-years, and nsNSAIDs, 0.86 per 100 patient-years (HR = 1.12, 95% confidence interval, 0.81-1.55; P = 0.50). Comparable intention-to-treat (ITT) rates were 1.14 per 100 patient...

  20. Consumption patterns of non-steroidal anti-inflammatory drugs by the community without prescription in Dhaka City

    Directory of Open Access Journals (Sweden)

    Md. Khoshroz Samad

    2009-06-01

    Full Text Available A cross-sectional study on consumption patterns of non-steroidal anti-inflammatory drugs (NSAIDs by the community without prescription was conducted in Dhaka Metropolitan City. A total of 608 encounters from 16 pharmacies were interviewed from people found to purchase drugs of the pharmacy from their self demand. The commonest purchased NSAIDs per encounter was paracetamol (37.0%. Ibuprofen (13.8%, diclofenac sodium (12.7%, aspirin (7.4%, naproxen (6.9% and other group of NSAIDs (22.2% were also purchased. The influence by friends/relatives (30.3% previously advised by the doctor to purchase the NSAIDs for the same complaint were (29.1%; pharmacy salesmen’s advice (28.3% and other reasons (12.3%. The total cost of purchased NSAIDs per encounter were less than Tk. 5 (6.9%, Tk. 5 to less than Tk. 10 (45.4%, Tk. 10-25 (35.5% and more than Tk. 25 (12.2%. Single item of drug was purchased along with NSAIDs by 17.1% of encounters.

  1. Knowledge of Housewives Regarding Non Steroid Anti Inflammatory Drug Use on Joint Pain in Hegarmanah Village Jatinangor

    Directory of Open Access Journals (Sweden)

    Adi Mulyono Gondopurwanto

    2016-03-01

    Full Text Available Background: Joint pain is frequently found in daily life activities. The prevalence of joint pain increases within the age. One of the medicine used for joint pain is non-steroidal anti-inflammatory drug (NSAID. In connection with inappropriate usage and their side effects, this study aimed to seek the extent ofhousewives’ knowledge on the use of NSAID for joint pain in Hegarmanah village, Jatinangor subdistrict. Methods: This cross-sectional descriptive study was conducted in October 2013 to the housewives resided in Hegarmanah village, Jatinangor subdistrict, West Java. Questionaire sheet was distributed to each of 110 housewives that had been stratifiedly with randomized sample. The questionaire contained identity, age, education level, and knowledge of NSAID in related to joint pain. Results: Based on the data collected, 73 subjects had adequate level of the knowledge and 37 subjects were in a poor level of the knowledge. The proportion of respondents who knew that joint pain was the pain occurs in the joint was 99.1%, the proportion of respondents who knew that the pain relieving drugs are called NSAID group was 40.9%, the proportion of respondents who knew that NSAID had a side-effect was 73.6%, and the proportion of respondents who knew that the side-effect of NSAID is abdominal pain was 61.8%. Conclusions: Most of the housewives in Hegarmanah Subdistrict have adequate knowledge in the use ofNSAID for joint pain relief.

  2. [Use of topical non-steroidal anti-inflammatory agents in an urban health center. Comparison with the current evidence].

    Science.gov (United States)

    Yagüe-Sebastián, M M; Coscollar-Escartín, I; Muñoz-Albadalejo, P; López-Canales, M C; Villaverde-Royo, M V; Gutiérrez-Moreno, F

    2013-09-01

    To describe the prescribing of topical non-steroidal anti-inflammatory drugs (NSAIDs) in an urban health center (Zaragoza, Spain). A cross-sectional descriptive study was conducted on subjects who belonged to an urban center and were studied during the year 2010. The sample size with a confidence level of 95%, was calculated, a total of 843 prescriptions were analyzed. The sample was single random, and 150 cases were selected. The prevalence and confidence intervals were calculated. The statistical package STATA 9.1 was used for the calculations. The most used drug was diclofenac, in 27.33% (95% CI: 20.65-34.88). NSAIDs were most used in females. In 18% of the cases the area of application was the knee, followed by the 15% in the lower back area (95% CI: 10,22-21,78). There were no adverse reactions. Frequent use is made of topical NSAIDs in a basic health area. Current recommendations support the use in the knee and in the hand, but not in the back, where its use is common. The use of topical NSAIDs decreases side effects and drug interactions, therefore their use is recommended in patients on multiple drug therapy and in the elderly. Copyright © 2012 Sociedad Española de Médicos de Atención Primaria (SEMERGEN). Publicado por Elsevier España. All rights reserved.

  3. Non-steroidal anti-inflammatory drugs: use and co-treatment with potentially interacting medications in the elderly.

    Science.gov (United States)

    Vandraas, Kathrine F; Spigset, Olav; Mahic, Milada; Slørdal, Lars

    2010-08-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used in the elderly. NSAIDs may cause a series of adverse drug reactions, of which gastrointestinal, renovascular/cardiovascular and bleeding complications are of particular concern. Concomitant use of several other drugs may further increase the risk of these adverse effects. To examine the extent of chronic use of NSAIDs and co-prescription of drugs which may seriously interact with NSAIDs in elderly subjects, by using data from the Norwegian Prescription Database. A total of 7.3% of all individuals (71,681/984,457) over 60 years of age filled at least one prescription for reimbursed NSAIDs during the 1-year study period (2006). Co-prescription of medications which may interact with NSAIDs was prevalent for drugs used for hypertension and/or heart failure (59.5%), antithrombotic drugs (35.1%), systemic glucocorticoids (12.9%) and SSRI antidepressants (8.3%). As many as 4.8 and 3.8% of NSAID users were co-prescribed warfarin or oral methotrexate respectively. The frequent co-prescription of medications which may cause detrimental interactions in elderly chronic NSAID users adds to safety concerns regarding this widely prescribed class of drugs.

  4. Simultaneous determination of non-steroidal anti-inflammatory drugs and oestrogenic hormones in environmental solid samples.

    Science.gov (United States)

    Kumirska, Jolanta; Migowska, Natalia; Caban, Magda; Łukaszewicz, Paulina; Stepnowski, Piotr

    2015-03-01

    Pharmaceuticals are continually being released into the environment. Because of their physical and chemical properties, many of them or their bioactive metabolites can accumulate in sediments, sludge and soils, and induce adverse effects in terrestrial organisms. However, due to the very limited methods permitting the detection of these low-level concentration compounds in such complex matrices, their concentrations in natural solids remain largely unknown. In this paper, an analytical method for the simultaneous determination of thirteen pharmaceuticals (eight non-steroidal anti-inflammatory drugs and five oestrogenic hormones) in solid matrices was developed. The proposed MAE-SPE-GC-MS(SIM) method has been successfully validated providing a linear response over a concentration range of 1(17)-1000(1200)ng/g, depending on the pharmaceuticals, with correlation coefficients above 0.991. The method detection limits were in the range of 0.3-5.7 ng/g, absolute recoveries above 50%, except estrone. The developed method was applied in the analysis of the target compounds in sediment, sludge and soils collected in Poland giving primary data on their concentrations in such matrices in Poland. The obtained results confirmed that the proposed method can be successfully used in the analysis of real environmental solid samples. Copyright © 2014 Elsevier B.V. All rights reserved.

  5. Dynamic model of eicosanoid production with special reference to non-steroidal anti-inflammatory drug-triggered hypersensitivity.

    Science.gov (United States)

    Fajmut, Aleš; Emeršič, Tadej; Dobovišek, Andrej; Antić, Nataša; Schäfer, Dirk; Brumen, Milan

    2015-10-01

    The authors developed a mathematical model of arachidonic acid (AA) degradation to prostaglandins (PGs) and leukotrienes (LTs), which are implicated in the processes of inflammation and hypersensitivity to non-steroidal anti-inflammatory drugs (NSAIDs). The model focuses on two PGs (PGE2 and PGD2) and one LT (LTC4), their % increases and their ratios. Results are compared with experimental studies obtained from non-asthmatics (NAs), and asthmatics tolerant (ATA) or intolerant (AIA) to aspirin. Simulations are carried out for predefined model populations NA, ATA and three AIA, based on the differences of two enzymes, PG E synthase and/or LTC4-synthase in two states, that is, no-inflammation and inflammation. Their model reveals that the model population with concomitant malfunctions in both enzymes is the most sensitive to NSAIDs, since the duration and the capacity for bronchoconstriction risk are highest after simulated oral dosing of indomethacin. Furthermore, inflammation prolongs the duration of the bronchoconstriction risk in all AIA model populations, and the sensitivity analysis reveals multiple possible scenarios leading to hypersensitivity, especially if inflammatory processes affect the expression of multiple enzymes of the AA metabolic pathway. Their model estimates the expected fold-changes in enzyme activities and gives valuable information for further targeted transcriptomic/proteomic and metabolomic studies.

  6. Non steroidal anti-inflammatory drugs for preventing cystoid macular edema after cataract surgeries:a Meta-analysis

    Directory of Open Access Journals (Sweden)

    Xue-Jiao Xu

    2015-12-01

    Full Text Available AIM:To systematic evaluate the preventive effect of non-steroidal anti-inflammatory drugs(NSAIDson the cystoid macular edema(CMEafter the cataract surgery. METHODS:Searching literature which were published by March 2015 and which were the random control test(RCTon the preventive effect of NSAIDs on CME after the cataract surgery in PubMed, EMbase, Cochrane Library, MEDLINE, CNKI, Wanfang Data, Chongqing Weipu and Chinese biomedical literature database and through Internet with computer. Meanwhile, relevant articles, journals, conference papers and their reference were manually retrieved. According to inclusion and exclusion criteria,the study objects were limited.Revman5.0 software provided by the Cochrane Collaboration was used to analysis the incidence of CME after cataract surgeries.RESULTS:A total of 7 RCT were included in the study(1422 cases, 712 cases in the trial group, 710 cases in the control group. Using NSAIDs before and after cataract surgeries could significantly reduce the post-operative incidence of CME(OR=0.31, 95%CI:0.18~0.52, PCONCLUSION:Using NSAIDs before and after cataract surgeries can significantly reduce the incidence of postoperative CME. Due to the small sample size and the medium methodological quality, the conclusion is not powerful enough. More high-quality RCTs with larger sample size are needed to make the evaluation more objective, accurate and comprehensive.

  7. Consumption patterns of non-steroidal anti-inflammatory drugs by the community without prescription in Dhaka City

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    Md Khoshroz Samad

    2009-03-01

    Full Text Available A cross-sectional study on consumption patterns of non-steroidal anti-inflammatory drugs (NSAIDs by the community without prescription was conducted in Dhaka Metropolitan City. A total of 608 encounters from 16 pharmacies were interviewed from people found to purchase drugs of the pharmacy from their self demand. The commonest purchased NSAIDs per encounter was paracetamol (37.0%. Ibuprofen (13.8%, diclofenac sodium (12.7%, aspirin (7.4%, naproxen (6.9% and other group of NSAIDs (22.2% were also purchased. The influence by friends/relatives (30.3% previously advised by the doctor to purchase the NSAIDs for the same complaint were (29.1%; pharmacy salesmens advice (28.3% and other reasons (12.3%. The total cost of purchased NSAIDs per encounter were less than Tk. 5 (6.9%, Tk. 5 to less than Tk. 10 (45.4%, Tk. 10-25 (35.5% and more than Tk. 25 (12.2%. Single item of drug was purchased along with NSAIDs by 17.1% of encounters.

  8. Coordination Polymers Derived from Non-Steroidal Anti-Inflammatory Drugs for Cell Imaging and Drug Delivery.

    Science.gov (United States)

    Paul, Mithun; Dastidar, Parthasarathi

    2016-01-18

    A new series of Mn(II) coordination polymers, namely, [{Mn(L)(H2 O)2 }⋅2 Nap]∞ (CP1), [{Mn(L)(Ibu)2 (H2 O)2 }]∞ (CP2), [{Mn(L)(Flr)2 (H2 O)2 }]∞ (CP3), [{Mn(L)(Ind)2 (H2 O)2 }⋅H2 O]∞ (CP4), [{Mn2 (L)2 (μ-Flu)4 (H2 O)}⋅L]∞ (CP5), [{Mn2 (L)2 (μ-Tol)4 (H2 O)2 }]∞ (CP6) and [{Mn2 (L)2 (μ-Mef)4 (H2 O)2 }]∞ (CP7) (Nap=naproxen, Ibu=ibuprofen, Flr=flurbiprofen, Ind=indometacin, Flu=flufenamic acid, Tol=tolfenamic acid and Mef=mefenamic acid) derived from various non-steroidal anti-inflammatory drugs (NSAIDs) and the organic linker 1,2-bis(4-pyridyl)ethylene (L) have been synthesized with the aim of being used for cell imaging and drug delivery. Single-crystal X-ray diffraction (SXRD) studies revealed that the NSAID molecules were part of the coordination polymeric network either through coordination to the metal center (in the majority of the cases) or through hydrogen bonding. Remarkably, all the Mn(II) coordination polymers were found to be soluble in DMSO, thereby making them particularly suitable for the desired biological applications. Two of the coordination polymers (namely, CP1 and CP3) reported herein, were found to be photoluminescent both in the solid as well as in the solution state. Subsequent experiments (namely, MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide), and PGE2 (prostaglandin E2 ) assays) established their biocompatibility and anti-inflammatory response. In vitro studies by using a macrophage cell line (i.e., RAW 264.7) revealed that both CP1 and CP3 were excellent cell imaging agents. Finally, biodegradability studies under simulated physiological conditions in phosphate-buffered saline (PBS) at pH 7.6 showed that slow and sustained release of the corresponding NSAID was indeed possible from both CP1 and CP3. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  9. Campania Preventability Assessment Committee (Italy): A Focus on the Preventability of Non-steroidal Anti-inflammatory Drugs' Adverse Drug Reactions

    OpenAIRE

    Maurizio Sessa; Liberata Sportiello; Annamaria Mascolo; Cristina Scavone; Silvia Gallipoli; Gabriella di Mauro; Daniela Cimmaruta; Concetta Rafaniello; Annalisa Capuano

    2017-01-01

    Purpose: This study aims to investigate preventability criteria of adverse drug reactions (ADRs) involving non-steroidal anti-inflammatory drugs (NSAIDs) by analyzing individual case safety reports (ICSRs) sent through Campania region (Italy) spontaneous reporting system from July 2012 to October 2016. Methods: For all the ICSRs that reported NSAIDs as suspected drug, a trained multidisciplinary team of Campania Pharmacovigilance Regional Centre composed of clinical pharmacologists and pha...

  10. The safety of codeine in patients with non-steroidal anti-inflammatory drug hypersensitivity: a preliminary study.

    Science.gov (United States)

    Celebioglu, E; Karakaya, G; Kalyoncu, A F

    2013-01-01

    Drug provocation testing should be performed before safely prescribing an analgesic for patients that are hypersensitive to non-steroidal anti-inflammatory drugs (NSAIDs). Whether or not the direct histamine releasing effect of codeine renders it useful in NSAID-hypersensitive patients is unknown. This study aimed to determine if codeine could be recommended as a safe treatment option for NSAID-hypersensitive patients without the need for oral drug provocation testing. The study included NSAID-hypersensitive patients with and without concurrent asthma, rhinitis, and chronic urticaria that presented to the allergy clinic between 1 January 1991 and 31 December 2010. Patient data were collected from the allergy clinic computer database. Patients challenged with codeine were included in the codeine group. The non-codeine group included those patients that were tested with analgesics other than codeine. In total, data for 1071 patients, of whom 301 were in the codeine group, were analysed. The reaction rate to codeine was 7.3% and when compared in pairs, the rate was significantly lower than to meloxicam and nimesulide (odds ratios=0.26-0.31, respectively). The reaction rate to codeine did not differ from that to benzydamine, rofecoxib, and paracetamol. Symptomatic dermographism was associated (p=0.009) with test positivity to any drug. Although, codeine was among the safest alternative drugs and none of the patients had an anaphylactic reaction to it, thus a challenge with codeine may be considered especially in patients with dermographism. The results of this preliminary study should be confirmed in a prospective study including a control group. Copyright © 2012 SEICAP. Published by Elsevier Espana. All rights reserved.

  11. Combinatorial effect of non-steroidal anti-inflammatory drugs and NF-κB inhibitors in ovarian cancer therapy.

    Directory of Open Access Journals (Sweden)

    Luiz F Zerbini

    Full Text Available Several epidemiological studies have correlated the use of non-steroidal anti-inflammatory drugs (NSAID with reduced risk of ovarian cancer, the most lethal gynecological cancer, diagnosed usually in late stages of the disease. We have previously established that the pro-apoptotic cytokine melanoma differentiation associated gene-7/Interleukin-24 (mda-7/IL-24 is a crucial mediator of NSAID-induced apoptosis in prostate, breast, renal and stomach cancer cells. In this report we evaluated various structurally different NSAIDs for their efficacies to induce apoptosis and mda-7/IL-24 expression in ovarian cancer cells. While several NSAIDs induced apoptosis, Sulindac Sulfide and Diclofenac most potently induced apoptosis and reduced tumor growth. A combination of these agents results in a synergistic effect. Furthermore, mda-7/IL-24 induction by NSAIDs is essential for programmed cell death, since inhibition of mda-7/IL-24 by small interfering RNA abrogates apoptosis. mda-7/IL-24 activation leads to upregulation of growth arrest and DNA damage inducible (GADD 45 α and γ and JNK activation. The NF-κB family of transcription factors has been implicated in ovarian cancer development. We previously established NF-κB/IκB signaling as an essential step for cell survival in cancer cells and hypothesized that targeting NF-κB could potentiate NSAID-mediated apoptosis induction in ovarian cancer cells. Indeed, combining NSAID treatment with NF-κB inhibitors led to enhanced apoptosis induction. Our results indicate that inhibition of NF-κB in combination with activation of mda-7/IL-24 expression may lead to a new combinatorial therapy for ovarian cancer.

  12. Use of non-steroidal anti-inflammatory drugs in pregnancy: impact on the fetus and newborn.

    Science.gov (United States)

    Antonucci, Roberto; Zaffanello, Marco; Puxeddu, Elisabetta; Porcella, Annalisa; Cuzzolin, Laura; Pilloni, Maria Dolores; Fanos, Vassilios

    2012-05-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed in pregnancy to treat fever, pain and inflammation. Indications for chronic use of these agents during pregnancy are inflammatory bowel or chronic rheumatic diseases. Since the seventies, NSAIDs have been used as effective tocolytic agents: indomethacin has been the reference drug, delaying delivery for at least 48 hours and up to 7-10 days. Additionally, self-medication with NSAIDs is practiced by pregnant women. NSAIDs given to pregnant women cross the placenta and may cause embryo-fetal and neonatal adverse effects, depending on the type of agent, the dose and duration of therapy, the period of gestation, and the time elapsed between maternal NSAID administration and delivery. These effects derive from the action mechanisms of NSAIDs (mainly inhibition of prostanoid activity) and from the physiological changes in drug pharmacokinetics occurring during pregnancy. Increased risks of miscarriage and malformations are associated with NSAID use in early pregnancy. Conversely, exposure to NSAIDs after 30 weeks' gestation is associated with an increased risk of premature closure of the fetal ductus arteriosus and oligohydramnios. Fetal and neonatal adverse effects affecting the brain, kidney, lung, skeleton, gastrointestinal tract and cardiovascular system have also been reported after prenatal exposure to NSAIDs. NSAIDs should be given in pregnancy only if the maternal benefits outweigh the potential fetal risks, at the lowest effective dose and for the shortest duration possible. This article discusses in detail the placental transfer and metabolism of NSAIDs, and the adverse impact of prenatal NSAID exposure on the offspring.

  13. Oral drug challenges in non-steroidal anti-inflammatory drug-induced urticaria, angioedema and anaphylaxis.

    Science.gov (United States)

    Chaudhry, T; Hissaria, P; Wiese, M; Heddle, R; Kette, F; Smith, W B

    2012-06-01

    Urticaria, angioedema and anaphylaxis are common adverse reactions to non-steroidal anti-inflammatory drugs (NSAIDs). To investigate the clinical characteristics of NSAID-induced acute hypersensitivity reactions with structured oral drug challenges. Patients with NSAID-induced urticaria, angioedema or anaphylaxis were challenged with either the homologous NSAID to confirm diagnosis or a heterologous NSAID to investigate cross-reactivity. Data were analysed retrospectively and supplemented by a telephone questionnaire. Sixty-eight patients (mean age 48.3, 53 females) reported a total of 75 instances of NSAID-induced reactions of which 64% were purely cutaneous and 36% were systemic anaphylaxis. Ibuprofen was the most frequent cause of reactions (35%), however, diclofenac was the most frequent cause of anaphylaxis (48%). Seventeen out of 40 (43%) homologous NSAID challenges were positive; presentation with anaphylaxis or reaction to diclofenac predicted a positive challenge. Only 7 of 28 (25%) of heterologous NSAID challenges were positive. Structured challenges enabled us to identify 23 (34%) patients with selective reactivity to a single NSAID, 19 (28%) patients with cross-reactivity to multiple NSAIDs and 23 (34%) patients in whom NSAID hypersensitivity was not reproduced. Selective reactors presented most often with anaphylaxis and some had a background of beta-lactam antibiotic allergy. Cross-reactive patients often had a background of chronic urticaria and presented with milder reactions. In the absence of a reliable in vitro test, structured drug challenges allow identification of selective and cross-reactive NSAID hypersensitivity syndromes. NSAID-induced anaphylaxis is often associated with selective hypersensitivity and patients may not need to avoid other NSAIDs. © 2011 The Authors. Internal Medicine Journal © 2011 Royal Australasian College of Physicians.

  14. Special diaphragm-like strictures of small bowel unrelated to non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Wang, Ming-Liang; Miao, Fei; Tang, Yong-Hua; Zhao, Xue-Song; Zhong, Jie; Yuan, Fei

    2011-08-21

    To summarize clinical, endoscopic, radiologic and pathologic features of special diaphragm-like strictures found in small bowel, with no patient use of non-steroidal anti-inflammatory drugs (NSAIDs). From January 2000 to December 2009, 5 cases (2 men and 3 women, with a mean age of 41.6 years) were diagnosed as having diaphragm-like strictures of small bowel on imaging, operation and pathology. All the patients denied the use of NSAIDs. The clinical, endoscopic, radiologic and pathologic findings in these 5 patients were retrospectively reviewed from the hospital database. Images of capsule endoscopy (CE) and small bowel follow-through (SBFT) obtained in 3 and 3 patients, respectively, and images of double-balloon enteroscopy and computed tomography enterography (CTE) obtained in all 5 patients were available for review. All patients presented with long-term (2-16 years) symptoms of gastrointestinal bleeding and varying degrees of anemia. There was only one stricture in four cases and three lesions in one case, and all the lesions were located in the middle or distal segment of ileum. Circumferential stricture was shown in the small bowel in three cases in the CE image, but the capsule was retained in the small bowel of 2 patients. Routine abdomen computed tomography scan showed no other abnormal results except gallstones in one patient. The lesions were shown as circumferential strictures accompanied by dilated small bowel loops in the small bowel on the images of CTE (in all 5 cases), SBFT (in 2 cases) and double-balloon enteroscopy (in all cases). On microscopy, a chronic inflammatory infiltrate and circumferential diaphragm were found in all lesions. Diaphragm-like strictures of small bowel might be a special consequence of unclear damaging insults to the intestine, having similar clinical, endoscopic, radiologic and pathologic features.

  15. Non-steroidal Anti-inflammatory Drugs and Coxibs In Chemoprevention: A Commentary Based Primarily on Animal Studies

    Science.gov (United States)

    Fischer, Susan M.; Hawk, Ernest; Lubet, Ronald A.

    2011-01-01

    This article endeavors to evaluate the data on the efficacy of non-steroidal anti-inflammatory drugs (NSAIDs) and Coxibs in preclinical studies on cancer prevention carried out by the authors. The overall objective was to address questions that we see as significant for the field. The preclinical studies evaluated here are restricted to our rodent studies on colon/intestinal, bladder and non-melanoma skin cancer in which NSAIDs or celecoxib were administered as either prevention agents or therapeutic agents. These studies may shed light on several questions. Should human use of NSAIDs/Coxibs consider not only efficacy but also whether celecoxib is unique compared to other NSAIDs? Are standard NSAIDs as effective as celecoxib in animal studies? Is the efficacy of celecoxib in particular or NSAIDs in general due to their off-target effects or to their effects on COX-1 and COX-2? What is the likely efficacy of low dose aspirin? Some questions raised by human trials and human epidemiology are discussed and related to our observations in animal models. We also considered the problem with cardiovascular (CV) events and whether animal models are predictive of efficacy in humans. Based on human epidemiological studies and its CV profile, it appears that aspirin is the most promising NSAID for the prevention of human colon, bladder and skin cancer, although the animal data for aspirin is less conclusive. We hope that this discussion of the results in animal studies may help inform and shape human trials of these commonly employed, relatively inexpensive and highly effective classes of compounds. PMID:21778329

  16. [Effect of a non-steroidal anti-inflammatory agent, tolmetin sodium on exudative inflammation in experimental animals (author's transl)].

    Science.gov (United States)

    Nakamura, H; Yokoyama, Y; Motoyoshi, S; Ishii, K; Shimizu, M

    1979-07-01

    Effect of tolmetin sodium(Tol) on acute and subacute exudative inflammation was tested in experimental animals. Tol had a potent inhibitory activity (ED50 = 0.75 mg/kg, p.o.) on the increased vascular permeability induced by acetic acid in mice, and the potency was about 0.4 times that of indomethacin (Ind), and 6-93 times that of ibuprofen (Ibu), phenylbutazone(Phe) and aspirin(Asp). The inhibitory activity of Tol(ED50 = 18.2 mg/kg, p.o.) on UV-induced erythema in guinea pigs was about 0.3 times that of Ind. A recovery of the hind paw edema of rats, produced by a mixture of kaolin and carrageenin, was promoted by oral administration of Tol(2.5 approximately 20 mg/kg x 5/2 days). Tol(80 mg/kg/day, p.o.) showed a significant activity in inhibiting the exudation caused by croton oil in rats, and the activity was about 0.025 times that of Ind and greater than that of Ibu, Phe and Asp. Tol(100-800 microgram/ml) inhibited in a dose-dependent manner the phytohemagglutinin-induced blast transformation of cultured lymphocytes from rat thymus, as did salicylic acid. In vitro, Tol showed a potent activity similar to that of Ibu and Phe in preventing the denaturation of bovine serum albumin and the lysis of rat erythrocytes. From these results, it is suggested that Tol has a particularly potent inhibitory activity on acute exudative inflammation, and the mode of action may be attributed to a mechanism similar to that seen with other acidic non-steroidal anti-inflammatory drugs.

  17. Non-Steroidal Anti-Inflammatory Drugs and Aspirin Therapy for the Treatment of Acute and Recurrent Idiopathic Pericarditis

    Science.gov (United States)

    Schwier, Nicholas; Tran, Nicole

    2016-01-01

    Aspirin (ASA) and non-steroidal anti-inflammatory drugs (NSAIDs) are a mainstay of therapy for the treatment of idiopathic pericarditis (IP). A comprehensive review consisting of pertinent clinical literature, pharmacokinetic, and pharmacodynamic considerations, has not been released in recent years. This review will facilitate the clinician’s understanding of pharmacotherapeutic considerations for using ASA/NSAIDs to treat IP. Data were compiled using clinical literature consisting of case reports, cohort data, retrospective and prospective studies, and manufacturer package inserts. ASA, ibuprofen, indometacin, and ketorolac relatively have the most evidence in the treatment of IP, provide symptomatic relief of IP, and should be tapered accordingly. ASA is the drug of choice in patients with coronary artery disease (CAD), heart failure (HF), or renal disease, but should be avoided in patients with asthma and nasal polyps, who are naïve to ASA therapy. Ibuprofen is an inexpensive and relatively accessible option in patients who do not have concomitant CAD, HF, or renal disease. Indometacin is not available over-the-counter in the USA, and has a relatively higher incidence of central nervous system (CNS) adverse effects. Ketorolac is an intravenous option; however, clinicians must be mindful of the maximum dose that can be administered. While ASA/NSAIDs do not ameliorate the disease process of IP, they are part of first-line therapy (along with colchicine), for preventing recurrence of IP. ASA/NSAID choice should be dictated by comorbid conditions, tolerability, and adverse effects. Additionally, the clinician should be mindful of considerations such as tapering, high-sensitivity CRP monitoring, bleeding risk, and contraindications to ASA/NSAID therapy. PMID:27023565

  18. Evaluation of the analgesic and anti-inflammatory activity of fixed dose combination: Non-steroidal anti-inflammatory drugs in experimental animals

    Directory of Open Access Journals (Sweden)

    Amit Lahoti

    2014-01-01

    Conclusion: Combining paracetamol with ibuprofen enhances analgesic/anti-inflammatory activity over their individual component but potentiation of analgesic activity of diclofenac was not seen when paracetamol was added to it.

  19. Non-steroidal anti-inflammatory drugs (NSAIDs) for chronic non-cancer pain in children and adolescents.

    Science.gov (United States)

    Eccleston, Christopher; Cooper, Tess E; Fisher, Emma; Anderson, Brian; Wilkinson, Nick Mr

    2017-08-02

    Pain is a common feature of childhood and adolescence around the world, and for many young people, that pain is chronic. The World Health Organization guidelines for pharmacological treatments for children's persisting pain acknowledge that pain in children is a major public health concern of high significance in most parts of the world. While in the past pain was largely dismissed and was frequently left untreated, views on children's pain have changed over time, and relief of pain is now seen as important.We designed a suite of seven reviews on chronic non-cancer pain and cancer pain (looking at antidepressants, antiepileptic drugs, non-steroidal anti-inflammatory drugs, opioids, and paracetamol) in order to review the evidence for children's pain utilising pharmacological interventions.As the leading cause of morbidity in the world today, chronic disease (and its associated pain) is a major health concern. Chronic pain (that is pain lasting three months or longer) can arise in the paediatric population in a variety of pathophysiological classifications (nociceptive, neuropathic, or idiopathic) from genetic conditions, nerve damage pain, chronic musculoskeletal pain, and chronic abdominal pain, as well as for other unknown reasons.Non-steroidal anti-inflammatory drugs (NSAIDs) are used to treat pain, reduce fever, and for their anti-inflammation properties. They are commonly used within paediatric pain management. Non-steroidal anti-inflammatory drugs are currently licensed for use in Western countries, however they are not approved for infants under three months old. The main adverse effects include renal impairment and gastrointestinal issues. Common side effects in children include diarrhoea, headache, nausea, constipation, rash, dizziness, and abdominal pain. To assess the analgesic efficacy and adverse events of NSAIDs used to treat chronic non-cancer pain in children and adolescents aged between birth and 17 years, in any setting. We searched the Cochrane

  20. Solid lipid nanoparticles for the controlled delivery of poorly water soluble non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Kumar, Raj; Singh, Ashutosh; Garg, Neha; Siril, Prem Felix

    2018-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen (IBP) are among the most prescribed drugs across the globe. However, most NSAIDs are insoluble in water leading them to have poor bioavailability and erratic absorption. Moreover, NSAIDs such as IBP and ketoprofen (KP) have to be administered very frequently due to their short plasma half-life leading to side effects. Controlled release formulations of IBP, KP and nabumetone (NBT) based on solid lipid nanoparticles (SLNs) were successfully synthesised in the present study to solve the above-mentioned challenges that are associated with NSAIDs. SLNs were prepared in two steps; hot-melt homogenization followed by sonication to formulate SLNs with spherical morphology. While capmul® GMS-50K (capmul) was used as the lipid due to the high solubility of the studied drugs in it, gelucire® 50/13 (gelucire) was used as the surfactant. It was found that particle size was directly proportional to drug concentration and inversely proportional to surfactant concentration, volume of water added and temperature of water. Ultrasonication in a pulse mode with optimum duration of 15min was essential to obtain smaller nanoparticles through the formation of a nanoemulsion. Drug loaded SLNs with small particle size and narrow size distribution with good solid loading, encapsulation efficiency and drug loading percentage could be prepared using the optimised conditions. SLNs prepared at the optimised condition were characterized thoroughly by using different techniques such as dynamic light scattering (DLS), field emission scanning electron microscopy (FESEM), transmission electron microscopy (TEM), atomic force microscopy (AFM), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The cytotoxicity results showed that the prepared SLNs are non-toxic to Raw cell line. The drugs IBP, KP and NBT showed 53, 74 and 69% of percentage entrapment efficiency with

  1. Population-based analysis of non-steroidal anti-inflammatory drug use among children in four European countries in the SOS project: What size of data platforms and which study designs do we need to assess safety issues?

    NARCIS (Netherlands)

    V.E. Valkhoff (Vera); R. Schade (René); G.W. 't Jong (Geert); S.A. Romio (Silvana); M.J. Schuemie (Martijn); A. Arfe (Andrea); C. Garbe (Claus); R.M.C. Herings (Ron); S. Lucchi (Silvia); G. Picelli (Gino); J.C. Schink (Julian); H. Straatman (Huub); M. Villa (Marco); E.J. Kuipers (Ernst); M.C.J.M. Sturkenboom (Miriam)

    2013-01-01

    textabstractBackground: Data on utilization patterns and safety of non-steroidal anti-inflammatory drugs (NSAIDs) in children are scarce. The purpose of this study was to investigate the utilization of NSAIDs among children in four European countries as part of the Safety Of non-Steroidal

  2. [Cost-effectiveness analysis of celecoxib versus non-selective non-steroidal anti-inflammatory drug therapy for the treatment of osteoarthritis in Spain: A current perspective].

    Science.gov (United States)

    De Lossada, A; Oteo-Álvaro, Á; Giménez, S; Oyagüez, I; Rejas, J

    2016-01-01

    To assess the cost-effectiveness of celecoxib and non-selective non-steroidal anti-inflammatory drugs for the treatment of osteoarthritis in clinical practice in Spain. A decision-tree model using distribution, doses, treatment duration and incidence of GI and CV events observed in the pragmatic PROBE-designed «GI-Reasons» trial was used for cost-effectiveness. Effectiveness was expressed in terms of event averted and quality-adjusted life-years (QALY) gained. QALY were calculated based on utility decrement in case of any adverse events reported in GI-Reasons trial. The National Health System perspective in Spain was applied; cost calculations included current prices of drugs plus cost of adverse events occurred. The analysis was expressed as an incremental cost-effectiveness ratio per QALY gained and per event averted. One-way and probabilistic analyses were performed. Compared with non-selective non-steroidal anti-inflammatory drugs, at current prices, celecoxib treatment had higher overall treatment costs €201 and €157, respectively. However, celecoxib was associated with a slight increase in QALY gain and significantly lower incidence of gastrointestinal events (p<.001), with mean incremental cost-effectiveness ratio of €13,286 per QALY gained and €4,471 per event averted. Sensitivity analyses were robust, and confirmed the results of the base case. Celecoxib at current price may be considered as a cost-effective alternative vs. non-selective non-steroidal anti-inflammatory drugs in the treatment of osteoarthritis in daily practice in the Spanish NHS. Copyright © 2015 Sociedad Española de Médicos de Atención Primaria (SEMERGEN). Publicado por Elsevier España, S.L.U. All rights reserved.

  3. Impact of proton pump inhibitor treatment on gastrointestinal bleeding associated with non-steroidal anti-inflammatory drug use among post-myocardial infarction patients taking antithrombotics

    DEFF Research Database (Denmark)

    Olsen, A. M. S.; Lindhardsen, J.; Gislason, G. H.

    2015-01-01

    STUDY QUESTION What is the effect of proton pump inhibitors (PPIs) on the risk of gastrointestinal bleeding in post-myocardial infarction patients taking antithrombotics and treated with non-steroidal anti-inflammatory drugs (NSAIDs)? METHODS This was a nationwide cohort study based on linked...... plus antithrombotic therapy was estimated using adjusted time dependent Cox regression models. STUDY ANSWER AND LIMITATIONS The use of PPIs was independently associated with decreased risk of gastrointestinal bleeding in post-myocardial infarction patients taking antithrombotics and treated with NSAIDs...

  4. Cardiovascular risk with non-steroidal anti-inflammatory drugs: systematic review of population-based controlled observational studies.

    Directory of Open Access Journals (Sweden)

    Patricia McGettigan

    2011-09-01

    Full Text Available BACKGROUND: Randomised trials have highlighted the cardiovascular risks of non-steroidal anti-inflammatory drugs (NSAIDs in high doses and sometimes atypical settings. Here, we provide estimates of the comparative risks with individual NSAIDs at typical doses in community settings. METHODS AND FINDINGS: We performed a systematic review of community-based controlled observational studies. We conducted comprehensive literature searches, extracted adjusted relative risk (RR estimates, and pooled the estimates for major cardiovascular events associated with use of individual NSAIDs, in different doses, and in populations with low and high background risks of cardiovascular events. We also compared individual drugs in pair-wise (within study analyses, generating ratios of RRs (RRRs. Thirty case-control studies included 184,946 cardiovascular events, and 21 cohort studies described outcomes in >2.7 million exposed individuals. Of the extensively studied drugs (ten or more studies, the highest overall risks were seen with rofecoxib, 1.45 (95% CI 1.33, 1.59, and diclofenac, 1.40 (1.27, 1.55, and the lowest with ibuprofen, 1.18 (1.11, 1.25, and naproxen, 1.09 (1.02, 1.16. In a sub-set of studies, risk was elevated with low doses of rofecoxib, 1.37 (1.20, 1.57, celecoxib, 1.26 (1.09, 1.47, and diclofenac, 1.22 (1.12, 1.33, and rose in each case with higher doses. Ibuprofen risk was seen only with higher doses. Naproxen was risk-neutral at all doses. Of the less studied drugs etoricoxib, 2.05 (1.45, 2.88, etodolac, 1.55 (1.28, 1.87, and indomethacin, 1.30 (1.19, 1.41, had the highest risks. In pair-wise comparisons, etoricoxib had a higher RR than ibuprofen, RRR = 1.68 (99% CI 1.14, 2.49, and naproxen, RRR = 1.75 (1.16, 2.64; etodolac was not significantly different from naproxen and ibuprofen. Naproxen had a significantly lower risk than ibuprofen, RRR = 0.92 (0.87, 0.99. RR estimates were constant with different background risks for

  5. Synthesis and Biological Evaluation of Mutual Prodrugs of Carboxylic Group Containing Some Non-Steroidal Anti-Inflammatory Drugs and Propyphenazone.

    Science.gov (United States)

    Paliwal, Meenu; Sucheta; Ruchita; Jain, Shilpa; Monika; Himanshu

    2017-01-01

    The use of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) is not up to its potential because of their gastrointestinal side effects. Significant attention has been focused on the growth of bio-reversible derivatives, such as mutual prodrugs, to momentarily mask the acidic group of NSAIDs as a promising means of decreasing or eliminating the GI side effects. The aims of this paper are to synthesize the mutual prodrugs of selected NSAIDs (Ketorolac, niflumic acid, tolfenamic acid) with propyphenazone, a study on their several physicochemical characters, hydrolysis kinetics, antiinflammatory, analgesic activity and ulcerogenicity. Mutual prodrugs were synthesized and their structures were confirmed and characterized using IR, 1H NMR, 13C NMR, mass spectroscopy and their purity was established by elemental analysis. Synthesized prodrugs were subjected for pharmacokinetic studies, analgesic, anti-inflammatory activities and ulcerogenic index. In vitro hydrolysis study of synthesized prodrugs in enzyme-free simulated intestinal fluid (SIF, pH 7.4) and 80% human plasma showed encouraging hydrolysis rate following first order kinetics while found stable in simulated gastric fluid (SGF, pH 1.2). Considerable decrease in ulcerogenic index and better anti-inflammatory activities were found in most of the cases as compared to their parent drugs. Among all prodrugs, viz. KE and NG showed excellent pharmacological response. A very less irritation to gastric mucosal was observed with the synthesized prodrugs than their parent drugs and can be considered for sustained drug release. Encouraging hydrolysis rate in SIF and 80% human plasma, improved analgesic and anti-inflammatory activities and reduced ulcerogenic liabilities of synthesized prodrugs revealed enhancement in the therapeutic index of the parent drugs. On the basis of above observation, it is concluded that mutual prodrugs approach can be applied to obtain synergistic effect for analgesic and anti inflammatory

  6. Low-dose aspirin, non-steroidal anti-inflammatory drugs, selective COX-2 inhibitors and breast cancer recurrence

    DEFF Research Database (Denmark)

    Cronin-Fenton, Deirdre P; Heide-Jørgensen, Uffe; Ahern, Thomas P

    2016-01-01

    BACKGROUND: Aspirin, nonsteroidal anti-inflammatory drugs (NSAIDs), and selective COX-2 inhibitors may improve outcomes in breast cancer patients. We investigated the association of aspirin, NSAIDs, and use of selective COX-2 inhibitors with breast cancer recurrence. METHODS: We identified incide...

  7. Knowledge and perceptions of the risks of non-steroidal anti-inflammatory drugs among orthopaedic patients in Thailand

    OpenAIRE

    Phueanpinit, Pacharaporn; Pongwecharak, Juraporn; Krska, Janet; Jarernsiripornkul, Narumol

    2016-01-01

    Background There is a high incidence of adverse effects from non-steroidal antiinflammatory drugs (NSAIDs) in Thailand, but patients’ perceptions and knowledge of NSAID risks is unknown. Objective This study aims to assess patients’ perceptions and knowledge of NSAID risks and factors affecting them. Setting University hospital in North-East of Thailand. Method A Cross-sectional study conducted over 4 months, using a self-administered questionnaire. Patients prescribed NSAIDs for at least one...

  8. Phenylacetic acids and the structurally related non-steroidal anti-inflammatory drug diclofenac bind to specific gamma-hydroxybutyric acid sites in rat brain

    DEFF Research Database (Denmark)

    Wellendorph, Petrine; Høg, Signe; Skonberg, Christian

    2009-01-01

    Gamma-Hydroxybutyric acid (GHB) is a proposed neurotransmitter or neuromodulator with a yet unresolved mechanism of action. GHB binds to both specific high-affinity GHB binding sites and to gamma-aminobutyric acid subtype B (GABA(B)) receptors in the brain. To separate specific GHB effects from...... GABA(B) receptor effects, it is imperative to develop GHB selective and potent compounds. We generated the compound, 4-(biphen-4-yl)-4-hydroxybutyric acid, which is the 4-hydroxyl analogue of the non-steroidal anti-inflammatory drug (NSAID) fenbufen (referred to as gamma-hydroxyfenbufen). When measured...... in a rat brain homogenate [(3)H]NCS-382 binding assay, gamma-hydroxyfenbufen inhibited [(3)H]NCS-382 binding with a 10-fold higher affinity than GHB (K(i) 0.44 microM), thus establishing it as a novel lead structure. The active metabolite of fenbufen, 4-biphenylacetic acid inhibited [(3)H]NCS-382 binding...

  9. Use of Polymer Inclusion Membranes (PIMs) as support for electromembrane extraction of non-steroidal anti-inflammatory drugs and highly polar acidic drugs.

    Science.gov (United States)

    Cristina, Román-Hidalgo; María Jesús, Martín-Valero; Rut, Fernández-Torres; Miguel Ángel, Bello-López

    2018-03-01

    The use of polymer inclusion membranes (PIMs) as support of 1-octanol liquid membrane in electromembrane extraction (EME) procedure is proposed. Synthesis of PIMs were optimized to a composition of 29% (w/w) of cellulose triacetate as base polymer and 71% (w/w) of Aliquat®336 as cationic carrier. Flat PIMs of 25µm thickness and 6mm diameter were used. EME protocol was implemented for the simultaneous extraction of four non-steroidal anti-inflammatory drugs (NSAIDs) (salicylic acid, ketoprofen, naproxen and ibuprofen) and four highly polar acidic drugs (anthranilic acid, nicotinic acid, amoxicillin and hippuric acid). Posterior HPLC separation of the extracted analytes was developed with diode array detection. Recoveries in the 81-34% range were obtained. EME procedure was applied to human urine samples. Copyright © 2017 Elsevier B.V. All rights reserved.

  10. Analysis of effect of non-steroidal anti-inflammatory drugs on teeth and oral tissues during orthodontic treatment. Report based on literature review.

    Science.gov (United States)

    Krasny, Marta; Zadurska, Małgorzata; Cessak, Grzegorz; Fiedor, Piotr

    2013-01-01

    In view of high availability and diversity of non-steroidal anti-inflammatory drugs (NSAIDs) on Polish market it is important for orthodontists to be aware of NSAID effect on the range of orthodontic tooth movement as well as the risk of root resorption in the moved teeth and other adverse effects, which might occur within oral cavity. The disadvantages of NSAID non-selective inhibition of COX include common oral inflammatory conditions, gingival bleeding, and disturbances of salivary secretion. Both, the selective and non-selective COX inhibitors, meloxicam excluded, used to alleviate the pain of orthodontic tooth movement, impede the movement of teeth. Paracetamol, explicitly indicated by most authors as the safest NSAID, seems to be the drug of choice in view of no influence on the range of tooth movement, the risk of root resorption or other adverse effects within oral cavity.

  11. The effect of non-steroidal anti-inflammatory drugs on the metabolism of /sup 14/C-arachidonic acid by human gingival tissue in vitro

    Energy Technology Data Exchange (ETDEWEB)

    Elattar, T.M.; Lin, H.S.; Tira, D.E.

    1983-09-01

    We investigated the effect of non-steroidal anti-inflammatory drugs on prostaglandins (PGs) and 12-hydroxyeicosatetraenoic acid (12-HETE) formation by inflamed human gingival tissues. Gingival tissue homogenates were incubated with /sup 14/C-arachidonic acid in the presence of indomethacin, piroxicam, or ibuprofen, and the organic solvent extracts were chromatographed on silica gel plates with standards for radiometric assay. There was a significant negative trend between the doses (10(-7)-10(-3) M) of each of indomethacin, piroxicam, and ibuprofen, and the amounts of PGF2 alpha, PGE2, PGD2, and 15-keto-PGE2 produced. All three drugs have a significant inhibitory effect on PGs and 12-HETE production at 10(-3) M when compared with the control. The rank order effectiveness of the drugs, at 10(-3) M, on PG inhibition was indomethacin greater than piroxicam greater than ibuprofen, and on 12-HETE inhibition was indomethacin greater than ibuprofen greater than piroxicam.

  12. [Safe prescription recommendations for non steroidal anti-inflammatory drugs: Consensus document ellaborated by nominated experts of three scientific associations (SER-SEC-AEG)].

    Science.gov (United States)

    Lanas, Angel; Benito, Pere; Alonso, Joaquín; Hernández-Cruz, Blanca; Barón-Esquivias, Gonzalo; Perez-Aísa, Angeles; Calvet, Xavier; García-Llorente, José Francisco; Gobbo, Milena; Gonzalez-Juanatey, José R

    2014-03-01

    This article outlines key recommendations for the appropriate prescription of non steroidal anti-inflammatory drugs to patients with different musculoskeletal problems. These recommendations are based on current scientific evidence, and takes into consideration gastrointestinal and cardiovascular safety issues. The recommendations have been agreed on by experts from three scientific societies (Spanish Society of Rheumatology [SER], Spanish Association of Gastroenterology [AEG] and Spanish Society of Cardiology [SEC]), following a two-round Delphi methodology. Areas that have been taken into account encompass: efficiency, cardiovascular risk, gastrointestinal risk, liver risk, renal risk, inflammatory bowel disease, anemia, post-operative pain, and prevention strategies. We propose a patient management algorithm that summarizes the main aspects of the recommendations. Copyright © 2013 Elsevier España, S.L. and AEEH y AEG. All rights reserved.

  13. Safe prescription recommendations for non steroidal anti-inflammatory drugs: consensus document ellaborated by nominated experts of three scientific associations (SER-SEC-AEG).

    Science.gov (United States)

    Lanas, Angel; Benito, Pere; Alonso, Joaquín; Hernández-Cruz, Blanca; Barón-Esquivias, Gonzalo; Perez-Aísa, Ángeles; Calvet, Xavier; García-Llorente, José Francisco; Gobbo, Milena; Gonzalez-Juanatey, José R

    2014-01-01

    This article outlines key recommendations for the appropriate prescription of non steroidal anti-inflammatory drugs to patients with different musculoskeletal problems. These recommendations are based on current scientific evidence, and takes into consideration gastrointestinal and cardiovascular safety issues. The recommendations have been agreed on by experts from three scientific societies (Spanish Society of Rheumatology [SER], Spanish Association of Gastroenterology [AEG] and Spanish Society of Cardiology [SEC]), following a two-round Delphi methodology. Areas that have been taken into account encompass: efficiency, cardiovascular risk, gastrointestinal risk, liver risk, renal risk, inflammatory bowel disease, anemia, post-operative pain, and prevention strategies. We propose a patient management algorithm that summarizes the main aspects of the recommendations. Copyright © 2013 Elsevier España, S.L. All rights reserved.

  14. The Effects of Two Non-Steroidal Anti-Inflammatory Drugs, Bromfenac 0.1% and Ketorolac 0.45%, on Cataract Surgery.

    Science.gov (United States)

    Jung, Ji Won; Chung, Byung Hoon; Kim, Eung Kweon; Seo, Kyoung Yul; Kim, Tae-im

    2015-11-01

    To compare the additive effects of two types of non-steroidal anti-inflammatory drugs (NSAIDs), bromfenac 0.1% or ketorolac 0.45%, relative to topical steroid alone in cataract surgery. A total 91 subjects scheduled to undergo cataract operation were randomized into three groups: Group 1, pre/postoperative bromfenac 0.1%; Group 2, pre/postoperative preservative-free ketorolac 0.45%; and Group 3, postoperative steroid only, as a control. Outcome measures included intraoperative change in pupil size, postoperative anterior chamber inflammation control, change in macular thickness and volume, and ocular surface status after operation. Both NSAID groups had smaller intraoperative pupil diameter changes compared to the control group (pmiosis, postoperative inflammation, and macular changes more effectively than postoperative steroid alone.

  15. Quantification and qualification of complication risks at use of non-steroid anti-inflammatory drugs as a basis for recommendations on their use and prophylaxis

    Directory of Open Access Journals (Sweden)

    Andrey Evgenyevich Karateev

    2014-03-01

    Full Text Available Non-steroid anti-inflammatory drugs (NSAID were and still remain the main means for arresting acute and controlling chronic pains in therapeutic practice. However, serious complications that may be caused by these drugs essentially limit their application. Therapists need distinct and reasonable guidelines on NSAID prescription depending on presence of a comorbid pathology and risk factors associated with the gastrointestinal tract and cardiovascular system. World renowned experts have been actively studying this problem. The main aspects of NSAID efficiency and safety are discussed in this study; the risk factors are ranked according to their significance; and an algorithm of reasonable drug prescription, including prevention of potential complications, is proposed.

  16. Effects of non-steroidal anti-inflammatory drugs on cyanobacteria and algae in laboratory strains and in natural algal assemblages.

    Science.gov (United States)

    Bácsi, István; B-Béres, Viktória; Kókai, Zsuzsanna; Gonda, Sándor; Novák, Zoltán; Nagy, Sándor Alex; Vasas, Gábor

    2016-05-01

    In recent years measurable concentrations of non-steroidal anti-inflammatory drugs (NSAIDs) have been shown in the aquatic environment as a result of increasing human consumption. Effects of five frequently used non-steroidal anti-inflammatory drugs (diclofenac, diflunisal, ibuprofen, mefenamic acid and piroxicam in 0.1 mg ml(-1) concentration) in batch cultures of cyanobacteria (Synechococcus elongatus, Microcystis aeruginosa, Cylindrospermopsis raciborskii), and eukaryotic algae (Desmodesmus communis, Haematococcus pluvialis, Cryptomonas ovata) were studied. Furthermore, the effects of the same concentrations of NSAIDs were investigated in natural algal assemblages in microcosms. According to the changes of chlorophyll-a content, unicellular cyanobacteria seemed to be more tolerant to NSAIDs than eukaryotic algae in laboratory experiments. Growth of eukaryotic algae was reduced by all drugs, the cryptomonad C. ovata was the most sensitive to NSAIDs, while the flagellated green alga H. pluvialis was more sensitive than the non-motile green alga D. communis. NSAID treatments had weaker impact in the natural assemblages dominated by cyanobacteria than in the ones dominated by eukaryotic algae, confirming the results of laboratory experiments. Diversity and number of functional groups did not change notably in cyanobacteria dominated assemblages, while they decreased significantly in eukaryotic algae dominated ones compared to controls. The results highlight that cyanobacteria (especially unicellular ones) are less sensitive to the studied, mostly hardly degradable NSAIDs, which suggest that their accumulation in water bodies may contribute to the expansion of cyanobacterial mass productions in appropriate environmental circumstances by pushing back eukaryotic algae. Thus, these contaminants require special attention during wastewater treatment and monitoring of surface waters. Copyright © 2016 Elsevier Ltd. All rights reserved.

  17. Investigation of anticholinergic and non-steroidal anti-inflammatory prodrugs which reduce chemically induced skin inflammation.

    Science.gov (United States)

    Young, Sherri C; Fabio, Karine M; Huang, Mou-Tuan; Saxena, Jaya; Harman, Meredith P; Guillon, Christophe D; Vetrano, Anna M; Heck, Diane E; Flowers, Robert A; Heindel, Ned D; Laskin, Jeffrey D

    2012-02-01

    As part of a continuous effort to develop efficient counter measures against sulfur mustard injuries, several unique NSAID prodrugs have been developed and screened for anti-inflammatory properties. Presented herein are three classes of prodrugs which dually target inflammation and cholinergic dysfunction. Compounds 1-28 contain common NSAIDs linked either to choline bioisosteres or to structural analogs of acetylcholinesterase (AChE) inhibitors. These agents have shown utility as anti-vesicants and anti-inflammatory agents when screened in a mouse ear vesicant model (MEVM) against both 2-chloroethyl ethyl sulfide (CEES), a blistering agent, and 12-O-tetradecanoylphorbol-13-acetate (TPA), a common topical irritant. Many of the prodrugs have activity against CEES, with 5, 18, 22 and 27 reducing inflammation by more than 75% compared with a control. Compounds 12, 13, 15 and 22 show comparable activity against TPA. Promising activity in the MEVM is related to half-lives of NSAID release in plasma, moderate to high lipophilicity, and some degree of inhibition of AChE, a potential contributor to sulfur mustard-mediated tissue damage. Copyright © 2011 John Wiley & Sons, Ltd.

  18. Investigation of Anticholinergic and Non-steroidal Anti-inflammatory Prodrugs which Reduce Chemically-induced Skin Inflammation

    Science.gov (United States)

    Young, Sherri C.; Fabio, Karine M.; Huang, Mou-Tuan; Saxena, Jaya; Harman, Meredith P.; Guillon, Christophe D.; Vetrano, Anna M.; Heck, Diane E.; Flowers, Robert A.; Heindel, Ned D.; Laskin, Jeffrey D.

    2013-01-01

    As part of a continuous effort to develop efficient countermeasures against sulfur mustard injuries, several unique NSAID prodrugs have been developed and screened for anti-inflammatory properties. Presented herein are three classes of prodrugs which dually target inflammation and cholinergic dysfunction. Compounds 1–28 contain common NSAIDs linked either to choline bioisosteres or to structural analogs of acetylcholinesterase (AChE) inhibitors. These agents have shown utility as anti-vesicants and anti-inflammatory agents when screened in a mouse ear vesicant model (MEVM) against both 2-chloroethyl ethyl sulfide (CEES), a blistering agent, and 12-O-tetradecanoylphorbol-13-acetate (TPA), a common topical irritant. Many of the prodrugs have activity against CEES, with 5, 18, 22 and 27 reducing inflammation by more than 75 % compared to a control. Compounds 12, 13, 15 and 22 show comparable activity against TPA. Promising activity in the MEVM is related to half-lives of NSAID-release in plasma, moderate to high lipophilicity, and some degree of inhibition of AChE, a potential contributor to sulfur mustard-mediated tissue damage. PMID:21319177

  19. High on treatment platelet reactivity against aspirin by non-steroidal anti-inflammatory drugs--pharmacological mechanisms and clinical relevance.

    Science.gov (United States)

    Hohlfeld, T; Saxena, A; Schrör, K

    2013-05-01

    Inhibition of platelet function by aspirin results from irreversible inhibition of platelet cyclooxygenase (COX)-1. While sufficient inhibition is obtained at antiplatelet doses (75-325 mg/day) in most (≥95%) treated patients, the antiplatelet effect of aspirin and subsequent cardiovascular risk reduction is much less in clinical settings and disease-dependent. Several reasons for this "high on treatment platelet reactivity" are known. This paper reviews the evidence for an interaction between aspirin and other COX inhibitors, namely non-steroidal anti-inflammatory drugs (NSAIDs). Numerous experimental studies demonstrated a pharmacodynamic interaction between aspirin and NSAIDs. This likely occurs within the hydrophobic substrate channel of platelet COX-1 and might be explained by molecular competition between inhibitor drugs and substrate (arachidonic acid) at overlapping binding sites. This interaction is found with some compounds, notably ibuprofen and dipyrone (metamizole), but not with others, such as diclofenac and acetaminophen (paracetamol). Hence, this interaction is not a class effect of NSAIDs and/or non-steroidal analgesics but rather due to specific structural requirements which still remain to be defined. In vivo studies on healthy subjects and patients tend to confirm this type of interaction as well as large differences between NSAIDs and non-steroidal analgesics, respectively. These interactions may be clinically relevant and may increase the cardiovascular risk in long-term treatment for primary and secondary cardiovascular prevention in patients with chronic inflammation, such as rheumatoid arthritis. These patients have an elevated risk for myocardial infarctions and may require chronic antiplatelet treatment by aspirin in addition to treatment of inflammatory pain.

  20. Effects of paracetamol, non-steroidal anti-inflammatory drugs, acetylsalicylic acid, and opioids on bone mineral density and risk of fracture: results of the Danish Osteoporosis Prevention Study (DOPS)

    DEFF Research Database (Denmark)

    Vestergaard, Peter; Hermann, P; Jensen, J-E B

    2012-01-01

    Pain medication has been associated with fractures. We found higher weight in paracetamol and non-steroidal anti-inflammatory drugs (NSAID) users and lower vitamin D levels in opioid and acetylsalicylic acid users. None of the pain medications influenced bone mineral density or loss. NSAID were a...

  1. Determination of the total concentration of highly protein-bound drugs in plasma by on-line dialysis and column liquid chromatography : application to non-steroidal anti-inflammatory drugs

    NARCIS (Netherlands)

    Herráez-Hernández, R; van de Merbel, N C; Brinkman, U A

    1995-01-01

    The potential of on-line dialysis as a sample preparation procedure for compounds highly bound to plasma proteins is evaluated, using non-steroidal anti-inflammatory drugs as model compounds and column liquid chromatography as the separation technique. Different strategies to reduce the degree of

  2. Time-trends in the prescribing of gastroprotective agents to primary care patients initiating low-dose aspirin or non-steroidal anti-inflammatory drugs: a population-based cohort study

    NARCIS (Netherlands)

    M.F.W.V. Warlé-Van Herwaarden (Margaretha); A.R. Koffeman (Aafke); V.E. Valkhoff (Vera); G.W. 't Jong (Geert); C. Kramers; M.C.J.M. Sturkenboom (Miriam); P.A. de Smet (Peter)

    2015-01-01

    textabstractAims Low-dose aspirin (LDA) and non-steroidal-anti-inflammatory drugs (NSAIDs) both increase the risk of upper gastrointestinal events (UGIEs). In the Netherlands, recommendations regarding the prescription of gastroprotective agents (GPAs) in LDA users were first issued in 2009 in the

  3. Time-trends in the prescribing of gastroprotective agents to primary care patients initiating low-dose aspirin or non-steroidal anti-inflammatory drugs: a population-based cohort study

    NARCIS (Netherlands)

    Warle-van Herwaarden, M.F.; Koffeman, A.R.; Valkhoff, V.E.; Jong, G.W. t; Kramers, C.; Sturkenboom, M.C.; Smet, P.A.G.M. de

    2015-01-01

    AIMS: Low-dose aspirin (LDA) and non-steroidal-anti-inflammatory drugs (NSAIDs) both increase the risk of upper gastrointestinal events (UGIEs). In the Netherlands, recommendations regarding the prescription of gastroprotective agents (GPAs) in LDA users were first issued in 2009 in the

  4. Cause for concern in the use of non-steroidal anti-inflammatory medications in the community -a population-based study

    Directory of Open Access Journals (Sweden)

    Adams Robert J

    2011-07-01

    Full Text Available Abstract Background Non-steroidal anti-inflammatory (NSAID medications are a common cause of reported adverse drug side-effects. This study describes the prevalence of non-steroidal anti-inflammatory (NSAID use (other than low-dose aspirin and the presence of co-existing relative contraindications to NSAID use and chronic conditions in a representative population sample. Methods Data were analysed from 3,206 adults attending first follow-up of the North West Adelaide Health Study (NWAHS in 2004 - 2006, a longitudinal representative population study. Medications were brought into study clinic visits by participants. Clinical assessment included measured blood pressure, kidney function, serum cholesterol, blood glucose. Questionnaires assessed demographics, lifestyle risk factors, physician-diagnosed chronic conditions. Data were weighted to census measures by region, age group, gender, and probability of selection in the household, to provide population representative estimates. Pearson's Chi-square tests determined significant differences in proportions. Multiple logistic regression was used to examine associations of socio-demographic characteristics with use of NSAIDs. Results Of 3,175 participants, 357 (11.2%, and 16% of those aged > 55 years, reported using either non-specific NSAIDs or COX-2 inhibitors, other than low-dose aspirin. Among people using NSAIDs, 60.8% had hypertension, 30.8% had Stage 3 or higher chronic kidney disease, 17.2% had a history of cardiovascular disease (CVD and 20.7% had a > 15% 10-year CVD risk. The prevalence of NSAID use among people with hypertension was 16%, with kidney disease 15.9%, and a history of CVD 20.0%. Among people taking diuretics, 24.1% were also taking NSAIDs, and of those taking medications for gastro-esophageal reflux, 24.7% were on NSAIDs. Prescription-only COX-2 inhibitors, but not other NSAIDs, were used more by people > 75 years than by 35-54 year olds (OR 3.7, 95% CI 2.0, 6.7, and also were

  5. Safety of celecoxib in patients with adverse skin reactions to acetaminophen (paracetamol) and nimesulide associated or not with common non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Liccardi, Gennaro; Salzillo, Antonello; Piccolo, Amedeo; Senna, Gianenrico; Piscitelli, Eugenia; D'Amato, Maria; D'Amato, Gennaro

    2005-02-01

    Acetaminophen (paracetamol--P) and Nimesulide (N) are widely used analgesic-antipyretic/anti-inflammatory drugs. The rate of adverse hypersensitivity reactions to these agents is generally low. On the contrary non-steroidal anti-inflammatory drugs (NSAIDs) are commonly involved in such reactions. Celecoxib (CE) is a novel drug, with high selectivity and affinity for COX-2 enzyme. We evaluated the tolerability of CE in a group of patients with documented history of adverse cutaneous reactions to P and N associated or not to classic NSAIDs. We studied 9 patients with hypersensitivity to P and N with or without associated reactions to classic NSAIDs. The diagnosis of P and N-induced skin reactions was based in vivo challenge. The placebo was blindly administered at the beginning of each challenge. After three days, a cumulative dosage of 200 mg of CE in refracted doses were given. After 2-3 days, a single dose of 200 mg was administered. All patients were observed for 6 hours after each challenge, and controlled again after 24 hours to exclude delayed reactions. The challenge was considered positive if one or more of the following appeared: erythema, rush or urticaria-angioedema. No reaction was observed with placebo and eight patients (88.8%) tolerated CE. Only one patient developed a moderate angioedema of the lips. Only one hypersensitivity reaction to CE was documented among 9 P and N-highly NSAIDs intolerant patients. Thus, we conclude that CE is a reasonably safe alternative to be used in subjects who do not tolerate P and N.

  6. Analysis of the use and adverse effects of non-steroidal anti-inflammatory drugs: A pilot study

    Directory of Open Access Journals (Sweden)

    Perić Aneta

    2006-01-01

    Full Text Available Background/Aim. The use and adverse effects of nonsteroidal anti-inflammatory drugs (NSAIDs in outpatients with rheumatic diseases has not yet been studied enough. The aim of this study was to evaluate the data about the efficacy and safety of NSAIDs obtained from the questionnaires submitted to the outpatients receiving these drugs. Methods. The patients who had been prescribed any of NSAIDs within the period from June to September, 2004 were included in the study. The answers obtained from the questionnaires were statistically analyzed by means of χ2-test. Results. At the time of the study, 150 patients had been prescribed ibuprofen or some other NSAID. Out of the total number of dispensed questionnaires (n = 150, only 45 (30% were shown to be correctly filled-in. Their analysis showed that 64.4% of the patients had suffered from rheumatic diseases for more than five years, and had regularly used NSAIDs. The average age of these patients was about 70 years, and the number of females was double as high as that of the males. The most frequently used NSAIDs were diclofenac and ibuprofen (46.14%, and 23.24%, respectively. According to the answers given by the patients, the most often adverse reactions were gastric complaints such as nausea (11.1%, and stomach pain (8.9%. Due to this, the majority of the patients (64.4% used some of the antiulcer drugs, most often ranitidine (31.1%. Conclusion. The results of this pilot study revealed that among the outpatients suffering from rheumatic diseases, the number of females was double as high as the number of males, that these patients were of the mean age of 70 years, and that their diseases lasted longer than five years. Gastric complains such as nausea and gastric pain of mild intensity were the most often adverse effects of NSAIDs reported by our patients. It could be the consequence of the predominant use of diclofenac and ibuprofen, NSAIDs with mild to moderate ulcerogenic potential, as well as the

  7. Non-Steroid Anti-Inflammatory Drugs Are Better than Acetaminophen on Fever Control at Acute Stage of Fracture.

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    Kuang-Ting Yeh

    Full Text Available In addition to adequate surgical fixation and an aggressive rehabilitation program, pain relief is one of the most critical factors in the acute stage of fracture treatment. The most common analgesics are nonsteroid anti-inflammatory drugs and Acetaminophen, both of which relieve pain and reduce body temperature. In clinical experiences, they exhibit effective pain control; however, their influence on body temperature remains controversial. This study is aimed at determining the effects of analgesics at the acute stage of traumatic fracture by performing a clinical retrospective study of patients with fractures and a fracture animal model. The retrospective study revealed that, in the acetaminophen group, the mean value of postmedication body temperature (BT was significantly higher than that of the premedication BT. The change in BT was highly related with the medication rather than other risk factors. Forty eight 12-week-old male Wistar rats were divided into 6 groups: a control group, fracture group, fracture-Acetaminophen group, Acetaminophen group, fracture-Arcoxia group, and Arcoxia group. Fracture rats were prepared by breaking their unilateral tibia and fibula. Their inflammation conditions were evaluated by measuring their serum cytokine level and their physiological status was evaluated by estimating their central temperature, heart rate, and mean blood pressure. The hepatic adverse effects were assessed by measuring the serum levels of aspartate aminotransferase (sGOT and alanine aminotransferase (sGPT. The central temperature in the fracture-Acetaminophen group exceeded that in the groups fed normal saline water or Arcoxia. Accumulated hepatic injury was presented as steadily ascending curves of sGOT and sGPT. Inflammation-related cytokine levels were not higher in the Acetaminophen fracture group and were significantly lower in the fracture-Arcoxia group. Fever appeared to be aggravated by acetaminophen and more related to the

  8. On the use of carbon blacks as potential low-cost adsorbents for the removal of non-steroidal anti-inflammatory drugs from river water.

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    Cuerda-Correa, Eduardo M; Domínguez-Vargas, Joaquín R; Olivares-Marín, Francisco J; de Heredia, Jesús Beltrán

    2010-05-15

    The adsorption of two non-steroidal anti-inflammatory drugs (NSAIDs), namely naproxen and ketoprofen, has been studied. Low-cost carbonaceous materials such as carbon blacks have been used as the adsorbents. The influence of temperature (20-60 degrees C), pH (3-11), ionic strength (0.01-0.1M), textural properties of the adsorbents (S(BET) and pore volumes) and aqueous matrix on the adsorption process has been analyzed. The adsorption isotherms have been determined both in milli-Q aqueous solution and water from the Guadiana river. Ionic strength and pH exert a noticeable influence on the process. In general, the removal is favored at low values of temperature and pH. On the contrary, an increase of the ionic strength seems to favor the adsorption process. The use of more porous adsorbents results in a more effective removal of the pollutants. Finally, the use of natural river water results in a noticeable increase of the removal capacity of naproxen and, particularly, ketoprofen. The experimental results proved that, under the optimal operation conditions, up to 517mg/g of naproxen and 400mg/g of ketoprofen may be adsorbed, which demonstrates the promising potential of these adsorbents for the removal of the pharmaceuticals under study. Copyright (c) 2010 Elsevier B.V. All rights reserved.

  9. Influence of matrix effect on the performance of the method for the official residue control of non-steroidal anti-inflammatory drugs in animal muscle.

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    Olejnik, Małgorzata; Jedziniak, Piotr; Szprengier-Juszkiewicz, Teresa; Zmudzki, Jan

    2013-02-15

    During the development and validation of mass spectrometry based method in residue control analysis, it is recommended to evaluate the level of the matrix effect. Often its level is relatively high, despite extensive sample purification. The matrix effect in the method for the determination of non-steroidal anti-inflammatory drugs in animal muscle was tested using a post-extraction addition technique. The experiment was performed to assess the impact of chromatographic conditions and design of ion source on the results. Additionally, the impact of phospholipids was tested. The matrix effect signal varied from 36% (64% ion suppression) to 192% (92% ion enhancement), depending on the analyte and species. The internal standard corrected matrix effect was generally lower but was still high for some analytes. Both chromatographic conditions and ion source design have influence on the level of matrix effect; however, this effect was no longer observed after compensation with internal standards. Currently, no commonly accepted criteria exist for the interpretation of results of determination of matrix effects; such criteria have been proposed in this paper, based on guidelines for bioanalytical methods and results of the study. Copyright © 2012 John Wiley & Sons, Ltd.

  10. The effectiveness of prophylactic proton pump inhibitors for prevention of non-steroidal anti inflammatory drugs associated gastric and duodenal ulcers in elderly.

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    Kheiri, Babikir; Mabrouk, Ahmed; Ahmed, Imran; Khan, Hashim; Sheikh, Azeem S

    2014-01-01

    Aims was undertaken to ensure concomitant usage of proton pump inhibitors (PPIs) with Non-Steroidal Anti-inflammatory Drugs (NSAIDs) in Elderly, in order to avoid upper gastrointestinal (GI) symptoms and ulcers. Reviewing of 386 patients' prescription on the EMIS (Egton Medical Information Systems) Web, on April 2014. Checking who have not been prescribed PPIs with NSAIDs, offering them appointment for prescription and discussion about risks and benefits of PPIs. Re-audit of 390 patients' prescription on the EMIS Web, on July 2014. Exclusion criteria in the audit and re-audit were; NSAIDs usage for more than 3 years, contra-indications for PPIs, and patients who declined inclusion in the audit. In the first audit cycle, a total of 386 patients' prescription reviewed, 23 (6%) patients were not prescribed PPIs with NSAIDs and were eligible for PPIs prescription. Those patients were contacted by post, an appointment arranged for them and prescribed the PPIs. 12 weeks later a re-audit was done, showed that all patients (100%) who are prescribed NSAIDs are prescribed prophylactic PPIs. None of the patients who are prescribed NSAIDs and PPIs concomitantly developed upper GI symptoms or ulcers. The audit increased the awareness of the junior doctors of the importance of concomitant prescription of PPIs with NSAIDs, in accordance with the electronic Medical Compendium (eMC) guidelines, to prevent upper GI symptoms and ulcers. That was reflected in the re-audit having 100% of the patients prescribed NSAIDs and PPIs concomitantly.

  11. Modulations in the intestinal disaccharide hydrolases and membrane dynamics: effect of non-steroidal anti-inflammatory drugs aspirin and nimesulide.

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    Kaushal, Naveen; Sanyal, S N

    2007-01-01

    The present study was designed to evaluate the influence of two commonly prescribed non-steroidal anti-inflammatory drugs (NSAIDs), aspirin and nimesulide on the biochemical composition and membrane dynamics of rat intestine. Female Wistar rats were divided into three different groups viz: Group I (Control), Group II (aspirin-treated, 50 mg/kg body weight) and Group III (nimesulide-treated, 10 mg/kg body weight). After 28 days, biochemical estimations in both drug treated groups showed an increase in sucrase, lactase, maltase and alkaline phosphatase as compared to the control. Alterations in the intestinal membrane dynamics by fluidity studies and Fourier Transform Infra Red (FTIR) spectroscopy also showed considerable changes. The alterations in the histoarchitecture of the intestine were also seen, which correlated well with the changes in structure and composition of the intestine. The use of NSAIDs like aspirin and nimesulide may cause the gastrointestinal side effects due to initial changes in the enzyme activities and membrane dynamics.

  12. Side-Effects of Non-Steroidal Anti-Inflammatory Drugs on the Liver in Dogs and Hepatoprotective Effect of Plant Remedies

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    Szweda Magdalena

    2014-10-01

    Full Text Available Hepatoprotective effect of plant drugs against hepatic tissue injury induced by non-steroidal anti-inflammatory drugs (NSAIDs was assessed on Beagle dogs. The adverse effects of carprofen and robenacoxib on the hepatic tissue were evaluated on the basis of histopathological examination of liver sections. It was demonstrated that the use of NSAIDs with liquorice and composed plant remedy Pectosol¯ caused a reduction of hepatic adverse effects induced by the administration of NSAIDs. This fact indicates a hepatoprotective effect of the tested plant remedies during the treatment with NSAIDs. However, the results require further studies on a larger group of animals. Liquorice and Pectosol¯ reduce the hepatic side effects, which develop after the treatment with carprofen and, to a lesser extent, robenacoxib in young Beagles. Such studies allow to investigate the negative and positive effects of using robenacoxib and carprofen in dogs and, therefore, help to limit the NSAID-induced side effects on the liver in these animals.

  13. 7B.02: THE ASSOCIATION BETWEEN NON-STEROIDAL ANTI-INFLAMMATORY DRUGS AND BLOOD PRESSURE CONTROL IN HYPERTENSIVE PATIENTS AND THE RELATION TO GENDER.

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    Ljungman, C; Kahan, T; Schiöler, L; Wettermark, B; Boström, K Bengtsson; Hasselström, J; Manhem, K

    2015-06-01

    Approximately 25% of hypertensive patients >65 years are treated for arthrosis, which is the most common cause of long term use of non-steroidal anti-inflammatory drugs (NSAID). NSAID inhibits prostaglandin synthesis and interacts with the renin angiotensin system. The objective of this study was to investigate if concomitant use of NSAID in hypertensive patients is associated with a lower possibility to reach target blood pressure hypertension from the Swedish primary Care Cardiovascular Database (SPCCD) in 2007-2008. Patient characteristics, antihypertensive drug class, dispensations of NSAIDs, comorbidities and blood pressure measurements were analyzed. The proportion of days covered (PDC) with prescription was calculated in order to analyze the NSAID use and the PDC was grouped 80% of days covered with prescription during 180 days prior to the last blood pressure measurement. In all 6700 patients had at least one prescription of NSAID. Patients with NSAID were younger (67.9 ± 11.2 vs 69.4 ± 11.9 years, p hypertensive patients does not seem to be associated with a higher blood pressure level. The use of NSAIDs is not associated with a reduced ability of achieving target blood pressure. Thus, hypertensive patients do not à priori need to be discouraged to use NSAID.

  14. Status of non-steroidal anti-inflammatory drugs use and its association with chronic kidney disease: a cross-sectional survey in China.

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    Pan, Yujing; Zhang, Luxia; Wang, Fang; Li, Xiaomei; Wang, Haiyan

    2014-10-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) have been reported to be associated with adverse effects including kidney injury, while relevant studies from developing countries are limited. We aimed to explore the status of NSAIDs use in China, as well as cross-sectional association between NSAIDs intake and presence of chronic kidney disease (CKD). A national representative sample of 47,204 adults in China was used. Prevalence of regular NSAIDs use was reported. Age- and sex- matched controls of NSAIDs users were then selected. The association between NSAIDs use and kidney injury were analyzed using logistic regression. Altogether 1129 participants reported regular use of NSAIDs, with the adjusted prevalence of 3.6% (95% CI, 3.2%-3.9%). And 76.9% of them (n = 868) had taken phenacetin-containing analgesics, with an adjusted prevalence of 3.2% (95% CI, 2.9%-3.5%). After adjusting for potential confounders, long-term NSAIDs intake (≥ 48 months) was associated with eGFR < 60 mL/min per 1.73 m2, with an OR of 2.36 (95% CI, 1.28-4.37). Regular use of NSAIDs, especially phenacetin-containing drugs, is prevalent in China. And long-term NSAIDs intake (≥ 48 months) was independently associated with reduced renal function. © 2014 Asian Pacific Society of Nephrology.

  15. In Vitro Interactions between Non-Steroidal Anti-Inflammatory Drugs and Antifungal Agents against Planktonic and Biofilm Forms of Trichosporon asahii.

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    Suteng Yang

    Full Text Available Increasing drug resistance has brought enormous challenges to the management of Trichosporon spp. infections. The in vitro antifungal activities of non-steroidal anti-inflammatory drugs (NSAIDs against Candida spp. and Cryptococcus spp. were recently discovered. In the present study, the in vitro interactions between three NSAIDs (aspirin, ibuprofen and diclofenac sodium and commonly used antifungal agents (fluconazole, itraconazole, voriconazole, caspofungin and amphotericin B against planktonic and biofilm cells of T. asahii were evaluated using the checkerboard microdilution method. The spectrophotometric method and the XTT reduction assay were used to generate data on biofilm cells. The fractional inhibitory concentration index (FICI and the ΔE model were compared to interpret drug interactions. Using the FICI, the highest percentages of synergistic effects against planktonic cells (86.67% and biofilm cells (73.33% were found for amphotericin B/ibuprofen, and caspofungin/ibuprofen showed appreciable percentages (73.33% for planktonic form and 60.00% for biofilm as well. We did not observe antagonism. The ΔE model gave consistent results with FICI (86.67%. Our findings suggest that amphotericin B/ibuprofen and caspofungin/ibuprofen combinations have potential effects against T. asahii. Further in vivo and animal studies to investigate associated mechanisms need to be conducted.

  16. The influence of non-steroidal anti-inflammatory drugs and paracetamol used for pain control of orthodontic tooth movement: a systematic review

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    ADRIANO S. CORRÊA

    2017-08-01

    Full Text Available ABSTRACT The present study aimed to perform a systematic literature review to determine if there is a non-steroidal anti-inflammatory drug (NSAID that interferes less within tooth movement. This research was performed according to the PRISMA statement. Articles were searched in eight electronic databases (PubMed, Scopus, Embase, Web of Science, LILACS, SciELO, Google Scholar, and Open Grey. Only experimental studies on male Wistar rats were selected, which included experiments related to the influence of NSAIDs on orthodontic movement. Studies in animals with pathological conditions, literature review articles, letters to the editor and/or editorials, case reports, abstracts, books, and book chapters were excluded. Each of the steps of this systematic literature review was performed by two examiners independently. Results: the total sample consisted of 505 articles, from which 6 studies were eligible after a qualitative analysis. From the drugs assessed, paracetamol was unanimous for not interfering within orthodontic movement when compared to the control group. However, drugs such as aspirin, ibuprofen, sodium diclofenac, and selective cyclooxygenase-2 inhibitors caused a reduction in tooth movement when compared to the control group. Conclusion: paracetamol could be considered the drug of choice for pain relief because it interferes less within tooth movement.

  17. Use of aspirin, non-steroidal anti-inflammatory drugs, and acetaminophen (paracetamol), and risk of psoriasis and psoriatic arthritis: a cohort study.

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    Wu, Shaowei; Han, Jiali; Qureshi, Abrar A

    2015-02-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) have been reported to induce or exacerbate psoriasis. We aimed to evaluate the association between several widely used analgesics, including aspirin, non-aspirin NSAIDs, and acetaminophen (paracetamol), and risk of psoriasis and psoriatic arthritis (PsA) in a large cohort of US women, the Nurses' Health Study II (1991-2005). Information on regular use of aspirin, NSAIDs, and acetaminophen was collected for 95,540 participants during the follow-up. During 1,321,280 person-years of follow-up, we documented 646 incident psoriasis cases and 165 concomitant PsA cases. Compared to women who reported no use, regular acetaminophen and NSAIDs users with more than 10 years of use had multivariate hazard ratios of 3.60 [95% confidence interval (CI): 2.02-6.41] and 2.10 (95% CI: 1.11-3.96) for PsA, respectively. There was no clear association between aspirin and risk of psoriasis or PsA. In conclusion, long-term acetaminophen and NSAIDs use may be associated with an increased risk of PsA. Special attention on psoriasis and PsA screening may be needed for those who are prescribed for acetaminophen and NSAIDs for long-term periods.

  18. The appropriate use of non-steroidal anti-inflammatory drugs in rheumatic disease: opinions of a multidisciplinary European expert panel.

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    Burmester, Gerd; Lanas, Angel; Biasucci, Luigi; Hermann, Matthias; Lohmander, Stefan; Olivieri, Ignazio; Scarpignato, Carmelo; Smolen, Josef; Hawkey, Chris; Bajkowski, Adam; Berenbaum, Francis; Breedveld, Ferdinand; Dieleman, Peter; Dougados, Maxime; MacDonald, Thomas; Mola, Emilio Martin; Mets, Tony; Van den Noortgate, Nele; Stoevelaar, Herman

    2011-05-01

    Given the safety issues of non-steroidal anti-inflammatory drugs (NSAID) and the robustness of guidelines, making treatment choices in daily clinical practice is increasingly difficult. This study aimed systematically to analyse the opinions of a multidisciplinary European expert panel on the appropriateness of different NSAID, with or without the use of a proton pump inhibitor (PPI), in individual patients with chronic rheumatic disease. /Using the Research and Development/University of California at Los Angeles appropriateness method, the appropriateness of five (non-)selective NSAID with or without a PPI was assessed for 144 hypothetical patient profiles, ie, unique combinations of cardiovascular and gastrointestinal risk factors. Appropriateness statements were calculated for all indications. All options without PPI were considered appropriate in patients with no gastrointestinal/cardiovascular risk factors. Cyclooxygenase-2 selective inhibitors (C2SI) alone and non-selective NSAID plus PPI were preferred for patients with elevated gastrointestinal risk and low cardiovascular risk. Naproxen plus PPI was favoured in patients with high cardiovascular risk. For the combination of high gastrointestinal/high cardiovascular risk the use of any NSAID was discouraged; if needed, naproxen plus PPI or a C2SI plus PPI could be considered. The panel results may support treatment considerations at the level of individual patients, according to their gastrointestinal/cardiovascular risk profile.

  19. Synthesis, crystal structure and spectroscopy of bioactive Cd(II) polymeric complex of the non-steroidal anti-inflammatory drug diclofenac sodium: Antiproliferative and biological activity

    Science.gov (United States)

    Tabrizi, Leila; Chiniforoshan, Hossein; McArdle, Patrick

    2015-02-01

    The interaction of Cd(II) with the non-steroidal anti-inflammatory drug diclofenac sodium (Dic) leads to the formation of the complex [Cd2(L)41.5(MeOH)2(H2O)]n(L = Dic), 1, which has been isolated and structurally characterized by X-ray crystallography. Diclofenac sodium and its metal complex 1 have also been evaluated for antiproliferative activity in vitro against the cells of three human cancer cell lines, MCF-7 (breast cancer cell line), T24 (bladder cancer cell line), A-549 (non-small cell lung carcinoma), and a mouse fibroblast L-929 cell line. The results of cytotoxic activity in vitro expressed as IC50 values indicated the diclofenac sodium and cadmium chloride are non active or less active than the metal complex of diclofenac (1). Complex 1 was also found to be a more potent cytotoxic agent against T-24 and MCF-7 cancer cell lines than the prevalent benchmark metallodrug, cisplatin, under the same experimental conditions. The superoxide dismutase activity was measured by Fridovich test which showed that complex 1 shows a low value in comparison with Cu complexes. The binding properties of this complex to biomolecules, bovine or human serum albumin, are presented and evaluated. Antibacterial and growth inhibitory activity is also higher than that of the parent ligand compound.

  20. Non-steroidal anti-inflammatory drugs decrease E2F1 expression and inhibit cell growth in ovarian cancer cells.

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    Blanca L Valle

    Full Text Available Epidemiological studies have shown that the regular use of non-steroidal anti-inflammatory (NSAIDs drugs is associated with a reduced risk of various cancers. In addition, in vitro and experiments in mouse models have demonstrated that NSAIDs decrease tumor initiation and/or progression of several cancers. However, there are limited preclinical studies investigating the effects of NSAIDs in ovarian cancer. Here, we have studied the effects of two NSAIDs, diclofenac and indomethacin, in ovarian cancer cell lines and in a xenograft mouse model. Diclofenac and indomethacin treatment decreased cell growth by inducing cell cycle arrest and apoptosis. In addition, diclofenac and indomethacin reduced tumor volume in a xenograft model of ovarian cancer. To identify possible molecular pathways mediating the effects of NSAID treatment in ovarian cancer, we performed microarray analysis of ovarian cancer cells treated with indomethacin or diclofenac. Interestingly, several of the genes found downregulated following diclofenac or indomethacin treatment are transcriptional target genes of E2F1. E2F1 was downregulated at the mRNA and protein level upon treatment with diclofenac and indomethacin, and overexpression of E2F1 rescued cells from the growth inhibitory effects of diclofenac and indomethacin. In conclusion, NSAIDs diclofenac and indomethacin exert an anti-proliferative effect in ovarian cancer in vitro and in vivo and the effects of NSAIDs may be mediated, in part, by downregulation of E2F1.

  1. Characterisation of cyclooxygenase 1 and 2 expression in mouse resident peritoneal macrophages in vitro; interactions of non steroidal anti-inflammatory drugs with COX2.

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    Tordjman, C; Coge, F; Andre, N; Rique, H; Spedding, M; Bonnet, J

    1995-05-17

    Resident peritoneal macrophages exposed to inflammatory stimuli (zymosan, lipopolysaccharide (LPS)) represent a widely used model for studying arachidonic acid metabolism and for screening of prostaglandin (PG) synthesis inhibitors. In the present study, cyclooxygenase 1 (COX1) was shown constitutively expressed in mouse adherent and non-adherent macrophages whereas expression of COX2 was observed only in adherent cells, even when cultured in minimal conditions (Ca-, Mg- and serum-free medium). The COX2 expression was amplified by arachidonic acid cascade stimulating agents (Ca, Mg, zymosan) and by LPS in a time-dependant manner; PGE2 by itself amplified LPS-induced COX2 expression. In well-defined experimental conditions of COX2 expression (LPS-stimulated adherent macrophages), we studied specific interactions of some representative anti-inflammatory drugs with COX2 enzymatic activity and expression. By contrast with dexamethasone, which reduced PGE2 release together with a strong reduction of COX2 expression (protein and mRNA), non steroidal anti-inflammatory drugs (NSAIDs) reduced PGE2 synthesis without any effect at the COX2 mRNA level. This reduction of PGE2 production by NSAIDs resulted from either an exclusive enzymatic inhibition (aspirin, NS398, 6-Methoxy naphtyl acetic acid) or an enzymatic inhibition associated with a slight decrease of COX2 protein level (indomethacin). For paracetamol and salicylic acid, two weak inhibitors of COX enzymatic activity, reduction of PGE2 synthesis appeared to be related to reduced level of COX2. These findings show that the macrophage can be used as a cellular model to study specifically COX1 and COX2. In this cell type, COX2 expression is dependent on adhesion, enhanced by stimulation of arachidonic acid metabolism, and auto amplified by PGE2. Furthermore, the results indicate that known NSAIDs differ in their interaction with cyclooxygenase, being able to inhibit either COX2 enzymatic activity, and/or COX2 expression

  2. Possible link between history of hypersensitivity to a specific non-steroidal anti-inflammatory drug (NSAID) and positive results following challenge test to alternative NSAIDS.

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    Trombetta, Domenico; Imbesi, Selene; Vita, Giuseppe; Isola, Stefania; Minciullo, Paola Lucia; Saija, Antonella; Gangemi, Sebastiano

    2009-01-01

    In subjects with hypersensitivity reactions to non-steroidal anti-inflammatory drugs (NSAIDs), the choice of suitable alternative drugs with the lowest risk of reaction is imperative for therapeutic management. A safe method to exclude drug hypersensitivity is to perform a challenge test for an alternative drug. The present study was conducted to: obtain more information about the safety of NSAIDs; assess the risk of reaction following the administration of a selective or nonselective cyclooxygenase 2 (COX-2) inhibitor in patients with a history of adverse reactions to NSAIDs; investigate if age and/or gender play a role in the susceptibility to develop adverse reactions to NSAIDs. This retrospective study includes 524 patients with a history of hypersensitivity to NSAIDs admitted to undergo challenge test to an alternative anti-inflammatory drug. Statistical significance was achieved when odds ratio (OR) and risk ratio (RR) values were >1. 8.39% of patients with hypersensitivity reactions to NSAIDs showed a positive challenge test for the alternative drug. Challenge tests for nonselective COX-2 inhibitors were positive in 16.2% of patients with previous reaction to a same drug class and in 12.9% of patients with a history of reaction to selective COX-2 inhibitors. No positive challenge test to a non-selective COX-2 inhibitor was found in patients with a history of hypersensitivity to nimesulide (CAS 51803-78-2). Challenge tests for selective COX-2 inhibitors were positive in 4.6% of patients with a previous reaction to nonselective COX-2 inhibitors and in 7.2% of patients with a history of reaction to selective COX-2 inhibitors. The RR of a positive challenge test to a non-selective COX-2 inhibitor was significant in patients who had a history of reaction to an analogous compound (P 0.21, OR 1.31, RR 1.26). In this study, selective COX-2 inhibitors represented the class of NSAIDs less frequently reported as responsible of adverse reaction. These data underline

  3. Association of individual non-steroidal anti-inflammatory drugs and chronic kidney disease: a population-based case control study.

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    Ylenia Ingrasciotta

    Full Text Available Non-steroidal anti-inflammatory agents (NSAIDs are known to be associated with renal damage. No clear evidence exists regarding differential risk of chronic kidney disease (CKD, specifically, across various NSAIDs.The aim of this population-based case-control study was to evaluate the association between use of individual NSAIDs and risk of CKD in a general population of Southern Italy.A nested case-control study was carried out using the general practice Arianna database, identifying incident CKD patients as cases and matched controls from 2006 to 2011. The date of first CKD diagnosis was defined as the index date (ID. Conditional logistic regressions were performed to estimate the risk of CKD associated with NSAIDs by class and individual drugs as compared to non-use during different time windows (within one year, six or three months prior to ID, with the latter being defined as current users. Among current users, the effect of cumulative exposure to these drugs was evaluated.Overall, 1,989 CKD cases and 7,906 matched controls were identified. A statistically significant increase in the risk of CKD was found for current users of oxicams (adjusted OR: 1.68; 95% CI: 1.15-2.44 and concerning individual compounds, for ketorolac (adj. OR: 2.54; 95% CI: 1.45-4.44, meloxicam (adj. OR: 1.98; 95% CI: 1.01-3.87 and piroxicam (adj. OR: 1.95; 95% CI: 1.19-3.21.The risk of CKD varies across individual NSAIDs. Increased risk has been found for ketorolac, which may precipitate subclinical CKD through acute renal damage, and long-term exposure to oxicams, especially meloxicam and piroxicam.

  4. Asthma and Rhinitis Induced by Selective Immediate Reactions to Paracetamol and Non-steroidal Anti-inflammatory Drugs in Aspirin Tolerant Subjects.

    Science.gov (United States)

    Pérez-Alzate, Diana; Blanca-López, Natalia; Doña, Inmaculada; Agúndez, José A; García-Martín, Elena; Cornejo-García, José A; Perkins, James R; Blanca, Miguel; Canto, Gabriela

    2016-01-01

    In subjects with non-steroidal anti-inflammatory drugs (NSAIDs)- exacerbated respiratory disease (NERD) symptoms are triggered by acetyl salicylic acid (ASA) and other strong COX-1 inhibitors, and in some cases by weak COX-1 or by selective COX-2 inhibitors. The mechanism involved is related to prostaglandin pathway inhibition and leukotriene release. Subjects who react to a single NSAID and tolerate others are considered selective responders, and often present urticaria and/or angioedema and anaphylaxis (SNIUAA). An immunological mechanism is implicated in these reactions. However, anecdotal evidence suggests that selective responders who present respiratory airway symptoms may also exist. Our objective was to determine if subjects might develop selective responses to NSAIDs/paracetamol that manifest as upper/lower airways respiratory symptoms. For this purpose, we studied patients reporting asthma and/or rhinitis induced by paracetamol or a single NSAID that tolerated ASA. An allergological evaluation plus controlled challenge with ASA was carried out. If ASA tolerance was found, we proceeded with an oral challenge with the culprit drug. The appearance of symptoms was monitored by a clinical questionnaire and by measuring FEV1 and/or nasal airways volume changes pre and post challenge. From a total of 21 initial cases, we confirmed the appearance of nasal and/or bronchial manifestations in ten, characterized by a significant decrease in FEV1% and/or a decrease in nasal volume cavity after drug administration. All cases tolerated ASA. This shows that ASA tolerant subjects with asthma and/or rhinitis induced by paracetamol or a single NSAID without skin/systemic manifestations exist. Whether these patients represent a new clinical phenotype to be included within the current classification of hypersensitivity reactions to NSAIDs requires further investigation.

  5. Fabrication of aluminum terephthalate metal-organic framework incorporated polymer monolith for the microextraction of non-steroidal anti-inflammatory drugs in water and urine samples.

    Science.gov (United States)

    Lyu, Dan-Ya; Yang, Cheng-Xiong; Yan, Xiu-Ping

    2015-05-08

    Polymer monolith microextraction (PMME) based on capillary monolithic column is an effective and useful technique to preconcentrate trace analytes from environmental and biological samples. Here, we report the fabrication of a novel aluminum terephthalate metal-organic framework (MIL-53(Al)) incorporated capillary monolithic column via in situ polymerization for the PMME of non-steroidal anti-inflammatory drugs (NSAIDs) (ketoprofen, fenbufen and ibuprofen) in water and urine samples. The fabricated MIL-53(Al) incorporated monolith was characterized by X-ray powder diffractometry, scanning electron microscopy, Fourier transform infrared spectrometry, and nitrogen adsorption experiment. The MIL-53(Al) incorporated monolith gave larger surface area than the neat polymer monolith. A 2-cm long MIL-53(Al) incorporated capillary monolith was applied for PMME coupled with high-performance liquid chromatography for the determination of the NSAIDs. Potential factors affecting the PMME were studied in detail. Under the optimized conditions, the developed method gave the enhancement factors of 46-51, the linear range of 0.40-200μgL(-1), the detection limits (S/N=3) of 0.12-0.24μgL(-1), and the quantification limits (S/N=10) of 0.40-0.85μgL(-1). The recoveries for spiked NSAIDs (20μgL(-1)) in water and urine samples were in the range of 77.3-104%. Besides, the MIL-53(Al) incorporated monolith was stable enough for 120 extraction cycles without significant loss of extraction efficiency. The developed method was successfully applied to the determination of NSAIDs in water and urine samples. Copyright © 2015 Elsevier B.V. All rights reserved.

  6. Biological evaluation of bismuth non-steroidal anti-inflammatory drugs (BiNSAIDs): stability, toxicity and uptake in HCT-8 colon cancer cells.

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    Hawksworth, Emma L; Andrews, Philip C; Lie, Wilford; Lai, Barry; Dillon, Carolyn T

    2014-06-01

    Recent studies showed that the metal-coordinated non-steroidal anti-inflammatory drug (NSAID), copper indomethacin, reduced aberrant crypt formation in the rodent colon cancer model, while also exhibiting gastrointestinal sparing properties. In the present study, the stability and biological activity of three BiNSAIDs of the general formula [Bi(L)3]n, where L=diflunisal (difl), mefenamate (mef) or tolfenamate (tolf) were examined. NMR spectroscopy of high concentrations of BiNSAIDs (24h in cell medium, 37°C) indicated that their structural stability and interactions with cell medium components were NSAID specific. Assessment of cell viability using the [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium]bromide (MTT) assay showed that the toxicity ranking of the BiNSAIDs paralleled those of the respective free NSAIDs: diflHbismuth content was observed following treatment with [Bi(tolf)3]. Since NMR studies indicated that [Bi(tolf)3] was the most stable BiNSAID and that cellular uptake of bismuth correlated with structural stability it appears that bismuth uptake is assisted by the NSAID. Microprobe SR-XRF imaging showed that the intracellular fate of bismuth was independent of the specific BiNSAID treatment whereby all BiNSAID-treated cells showed bismuth accumulation in the cytoplasm within 24-h exposure. The size and location of the hot spots (0.3-5.8μm(2)), were consistent with cellular organelles such as lysosomes. Copyright © 2014 Elsevier Inc. All rights reserved.

  7. Effects of Preoperative Non-Steroidal Anti-Inflammatory Drugs on Pain Mitigation and Patients’ Shoulder Performance Following Rotator Cuff Repair

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    Alireza Rouhani

    2014-12-01

    Full Text Available Purpose: Pain is one of the most important factors adversely affecting clinical outcomes of operated patients. The present study aims at evaluating effects of preoperative COX2 non-steroidal anti-inflammatory inhibitors on pain mitigation and performance of patients with shoulder rotator cuff tear. Methods: This case-control study was conducted on 60 patients suffering from rotator cuff injury candidate for arthroscopic repair. The patients were classified in two parallel and matched groups. One group (case group was treated using Celecoxib (200mg/12h started 48 hours before surgery and continued for 10 days after operation. In the control group, the placebo was prescribed in the same way. Postoperative pain, side effects, sleep disturbance, and short-term outcomes were compared between two groups using DASH questionnaire. Results: Postoperative pain in the Celecoxib group significantly decreased in comparison with the control one. The difference was statistically meaningful (P<0.001. Well motion ability was seen in 80% of patients of the Celecoxib group. It was 26.6% in the placebo group since pain inhibited them from exercising more motions. In this regard, there was a statistically meaningful difference between these two groups (P=0.02. Sleep disturbance was meaningfully at higher levels in the placebo group (P=0.001. Following up the patients for three months, it was made clear that performance of the Celecoxib group was better than that of the placebo one. Conclusion: COX2 inhibitors are well efficient in patients’ pain management after arthroscopic rotator cuff repair surgery. It results in less life complications, less sleep disturbances, improvement of patients’ short-term clinical outcome, and more quick recovery.

  8. Long-term use of non-steroidal anti-inflammatory drugs and the risk of myocardial infarction in the general population

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    González-Pérez Antonio

    2005-11-01

    Full Text Available Abstract Background Recent data indicate that chronic use of coxibs leads to an increased occurrence of thrombotic cardiovascular events. This raises the question as to whether traditional non-steroidal anti-inflammatory drugs (tNSAIDs might also produce similar hazards. Our aim has been to evaluate the association between the chronic use of tNSAIDs and the risk of myocardial infarction (MI in patients. Methods We performed a nested case-control analysis with 4,975 cases of acute MI and 20,000 controls, frequency matched to cases by age, sex, and calendar year. Results Overall, current use of tNSAID was not associated with an increased risk of MI (RR:1.07;95%CI: 0.95–1.21. However, we found that the relative risk (RR of MI for durations of tNSAID treatment of >1 year was 1.21 (95% CI, 1.00–1.48. The corresponding RR was 1.34 (95% CI, 1.06–1.70 for non-fatal MI. The effect was independent from dose. The small risk associated with long-term use of tNSAIDs was observed among patients not taking low-dose aspirin (RR: 1.29; 95% CI, 1.01–1.65. The effect of long-term use for individual tNSAIDs ranged from a RR of 0.87 (95% CI, 0.47–1.62 with naproxen to 1.38 (95% CI, 1.00–1.90 with diclofenac. Conclusion This study adds support to the hypothesis that chronic treatment with some tNSAIDs is associated with a small increased risk of non-fatal MI. Our data are consistent with a substantial variability in cardiovascular risks between individual tNSAIDs.

  9. Crystal structure of a mixed-ligand silver(I complex of the non-steroidal anti-inflammatory drug diclofenac and pyrimidine

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    Sevim Hamamci Alisir

    2016-10-01

    Full Text Available In the title mixed-ligand silver(I coordination polymeric complex with the non-steroidal anti-inflammatory drug diclofenac (C14H11Cl2NO2 (diclH and pyrimidine (pym, namely poly[{μ2-2-[2-(2,6-dichloroanilinophenyl]acetato-κ2O:O′}(μ2-pyrimidine-κ2N1:N3silver(I], [Ag(C14H10Cl2NO2(C4H4N2]n or [Ag(μ-dicl(μ-pym]n, the very distorted tetrahedral AgN2O2 coordination centres comprise two N-atom donors from bridging pym ligands [Ag—N = 2.381 (3 and 2.412 (3 Å] and two carboxylate O-atom donors from dicl ligands [Ag—O = 2.279 (2 and 2.280 (2 Å], which bridge Ag atoms, giving a centrosymmetric dinuclear units with a short Ag...Ag separation [2.8931 (5 Å]. Within the units are short intraligand C—Cl...π(pym interactions [3.6409 (15 Å]. The units are linked through the bridging N atoms of the pym ligand into a two-dimensional sheet–polymer structure lying parallel to (100 and stabilized by inter-ring π–π interactions between the pym ligands [Cg...Cg = 3.4199 (17 Å]. Additional inter-unit C—H...O and C—H...Cg hydrogen-bonding interactions between the sheets give an overall three-dimensional structure.

  10. Non-steroidal anti-inflammatory drugs, Cyclooxygenase-2 inhibitors and paracetamol use in Queensland and in the whole of Australia

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    Tett Susan E

    2008-09-01

    Full Text Available Abstract Background Cross national drug utilization studies can provide information about different influences on physician prescribing. This is important for medicines with issues around safety and quality of use, like non selective non-steroidal anti-inflammatory drugs (ns-NSAIDs and cyclo-oxygenase-2 (COX-2 inhibitors. To enable comparison of prescription medicine use across different jurisdictions with a range of population sizes, data first need to be compared within Australia to understand whether use in a smaller sub-population may be considered as representative of the total use within Australia. The aim of this study was to compare the utilization of non selective NSAID, COX-2 inhibitors and paracetamol between Queensland and Australia. Method Dispensing data were obtained for concession beneficiaries for Australia for ns-NSAIDs, COX-2 inhibitors and paracetamol subsidized by the PBS over the period 1997–2003. The same data were purchased for Queensland. Data were converted to Defined Daily Dose (DDD/1000 beneficiaries/day (World Health Organization anatomical therapeutic chemical classification, 2005. Results Total NSAID and paracetamol consumption were similar in Australia and Queensland. Ns-NSAID use decreased sharply with the introduction of COX-2 inhibitors (from approximately 80 to 40 DDD/1000 beneficiaries/day. Paracetamol was constant (approximately 45 DDD/1000 beneficiaries/day. COX-2 inhibitors consumption was initially higher in Queensland than in the whole of Australia. Conclusion Despite initial divergence in celecoxib use between Queensland and Australia, the use of ns-NSAIDs, COX-2 inhibitors and paracetamol overall, in concession beneficiaries, was comparable in Australia and Queensland.

  11. An investigation of the concomitant use of angiotensin-converting enzyme inhibitors, non-steroidal anti-inflammatory drugs and diuretics.

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    Bucsa, C; Moga, D C; Farcas, A; Mogosan, C; Dumitrascu, D L

    2015-08-01

    To determine in retrospective data the prevalence at hospital discharge of co-prescribing angiotensin-converting enzyme inhibitors (ACE-I) and non-steroidal anti-inflammatory drugs (NSAIDs) and ACE-I/NSAIDs and diuretics and to identify factors associated with the co-prescription. Secondary, we evaluated the extent of serum creatinine and potassium monitoring in patients treated with ACE-I and these associations and determined the prevalence of values above the upper normal limit (UNL) in monitored patients. Hospitalized patients with ACE-I in their therapy at discharge were included in 3 groups as follows: ACE-I, DT (double therapy with ACE-I and NSAIDs) and TT (triple therapy with ACE-I, NSAIDs and diuretics) groups. We evaluated differences on demographic characteristics, co-morbidities, medications, laboratory monitoring and quantified the patients with serum creatinine and potassium levels above the UNL using descriptive statistics. Logistic regression analysis with backward elimination was performed to identify significant predictors of combination therapy. Of 9960 admitted patients, 1214 were prescribed ACE-I, 40 were prescribed ACE-I/NSAIDs and 22 were prescribed ACE-I/NSAIDs/diuretics (3.13% and 1.72%, respectively, of the patients prescribed with ACE-I). Serum creatinine and potassium were monitored for the great majority of patients from all groups. The highest percentage of hyperkalemia was found in the DT group (10% of the patients) and of serum creatinine above UNL in the TT group (45.45%). The logistic regression final model showed that younger patients and monitoring for potassium were significantly associated with combination therapy. The prevalence of patients receiving DT/TT was relatively low and their monitoring during hospitalization was high. Factors associated with the combinations were younger patients and patients not tested for serum potassium.

  12. Non-steroidal anti-inflammatory drugs and paracetamol in self-therapy of various disorders in students of different fields of study.

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    Wiliński, Jerzy; Lechowicz, Marta; Kameczura, Tomasz; Głowacki, Mikołaj; Kameczura, Anna; Chrapusta, Anna; Wiliński, Bogdan

    2015-01-01

    Over-the-counter non-steroidal anti-inflammatory drugs (NSAIDs) and paracetamol are most commonly the first-line pharmacotherapy in combating different pain and inflammatory disorders and fever. Unfortunately, those drugs might have serious side effects, especially when they are used in an inappropriate way. The aim of the study was to explore various aspects of NSAIDs and paracetamol use in the self-therapy of miscellaneous disorders in young adults. The questionnaire-based survey comprised 250 consecutive students aged 22.1 ± 1.9 years (189 women) of diverse fields of study. The drugs were applied in clinical conditions in which they should be avoided including asthma attack (1.2%), vomiting (2.4%), malaise and depression (3.6%), in autumn and winter as a preventive measure against infections (14.0%), heart-burn (2.0%) and during food poisoning (16.0%). As many as 6.0% of the students claimed that studied medications are ultimately free of adverse reactions. Men more frequently than women used NSAIDs and paracetamol during alcohol consumption (49.2% vs 30.7%, p = 0.009, respectively) but less often were aware that there are maximum doses of medications which should not be exceeded (57.4% vs 76.7%, p = 0.003, respectively). The students of medical-related degree courses (n = 82) compared with individuals of other subjects (n = 168) declared they more often have the custom of always reading medications' leaflets (46.3% vs 31.0%, p = 0.017, respectively). Side effects of medicines were reported by 65 participants - 26.0%. In conclusion, students' knowledge about NSAIDs and paracetamol is low. Participants do not search for information on drug related endangerments, the medication group choice for the given disorder is often inappropriate and the drugs are applied in conditions in which they are contraindicated.

  13. Tolerance to coxibs in patients with intolerance to non-steroidal anti-inflammatory drugs (NSAIDs): a systematic structured review of the literature.

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    Weberschock, Tobias Bernd; Müller, Sylke-Monina; Boehncke, Sandra; Boehncke, Wolf-Henning

    2007-07-01

    Adverse events triggered by non-steroidal anti-inflammatory drugs (NSAIDs) are among the most common drug-related intolerance reactions in medicine; they are possibly related to inhibition of cyclooxygenase-1. Coxibs, preferentially inhibiting cyclooxygenase-2, may therefore represent safe alternatives in patients with NSAID intolerance. We reviewed the literature in a systematic and structured manner to identify and evaluate studies on the tolerance of coxibs in patients with NSAID intolerance. We searched MEDLINE (1966-2006), the COCHRANE LIBRARY (4th Issue 2006) and EMBASE (1966-2006) up to December 9, 2006, and analysed all publications included using a predefined evaluation sheet. Symptoms and severity of adverse events to coxibs were analysed based on all articles comprising such information. Subsequently, the probability for adverse events triggered by coxibs was determined on analyses of double-blind prospective trials only. Among 3,304 patients with NSAID intolerance, 119 adverse events occurred under coxib medication. All adverse events, except two, have been allergic/urticarial in nature; none was lethal, but two were graded as life-threatening (grade 4). The two non-allergic adverse events were described as a grade 1 upper respiratory tract haemorrhage, and a grade 1 gastrointestinal symptom, respectively. In 13 double-blind prospective studies comprising a total of 591 patients with NSAID intolerance, only 13 adverse reactions to coxib provocations were observed. The triggering coxibs were rofecoxib (2/286), celecoxib (6/208), etoricoxib (4/56), and valdecoxib (1/41). This review documents the good tolerability of coxibs in patients with NSAID intolerance, for whom access to this class of drugs for short-term treatment of pain and inflammation is advantageous.

  14. Variants of CEP68 Gene Are Associated with Acute Urticaria/Angioedema Induced by Multiple Non-Steroidal Anti-Inflammatory Drugs

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    Cornejo-García, José Antonio; Flores, Carlos; Plaza-Serón, María C.; Acosta-Herrera, Marialbert; Blanca-López, Natalia; Doña, Inmaculada; Torres, María J.; Mayorga, Cristobalina; Guéant-Rodríguez, Rosa M.; Ayuso, Pedro; Fernández, Javier; Laguna, José J.; Agúndez, José A. G.; García-Martín, Elena; Guéant, Jean-Louis; Canto, Gabriela; Blanca, Miguel

    2014-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are the most consumed drugs worldwide because of their efficacy and utility in the treatment of pain and inflammatory diseases. However, they are also responsible for an important number of adverse effects including hypersensitivity reactions. The most important group of these reactions is triggered by non-immunological, pharmacological mechanisms catalogued under the denomination of cross-intolerance (CRI), with acute urticaria/angioedema induced by multiple NSAIDs (MNSAID-UA) the most frequently associated clinical entity. A recent genome-wide association study identified the gene encoding the centrosomal protein of 68 KDa (CEP68) as the major locus associated with aspirin intolerance susceptibility in asthmatics. In this study, we aimed to assess the role of this locus in susceptibility to CRI to NSAIDs by examining 53 common gene variants in a total of 635 patients that were classified as MNSAID-UA (n = 399), airway exacerbations (n = 110) or blended pattern (n = 126), and 425 controls. We found in the MNSAID-UA group a number of variants (17) associated (lowest p-value = 1.13×10−6), including the non-synonymous Gly74Ser variant (rs7572857) previously associated with aspirin intolerance susceptibility in asthmatics. Although not being significant in the context of multiple testing, eight of these variants were also associated with exacerbated respiratory disease or blended reactions. Our results suggest that CEP68 gene variants may play an important role in MNSAID-UA susceptibility and, despite the different regulatory mechanisms involved depending on the specific affected organ, in the development of hypersensitivity reactions to NSAIDs. PMID:24618698

  15. Campania Preventability Assessment Committee (Italy: A Focus on the Preventability of Non-steroidal Anti-inflammatory Drugs' Adverse Drug Reactions

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    Maurizio Sessa

    2017-05-01

    Full Text Available Purpose: This study aims to investigate preventability criteria of adverse drug reactions (ADRs involving non-steroidal anti-inflammatory drugs (NSAIDs by analyzing individual case safety reports (ICSRs sent through Campania region (Italy spontaneous reporting system from July 2012 to October 2016.Methods: For all the ICSRs that reported NSAIDs as suspected drug, a trained multidisciplinary team of Campania Pharmacovigilance Regional Centre composed of clinical pharmacologists and pharmacists with pluriannual experience in Pharmacovigilance assessed preventability by using the P-method.Results: In all 19,039 ICSRs were sent to Campania Pharmacovigilance Regional Centre, of which 550 reported NSAIDs as suspected drug. In total, 94 cases (17.1% out of 550 ICSRs were preventable. In the 94 preventable cases, 201 critical criteria were detected of which 182/201 (90.5% related to healthcare professionals' practices, 0/201 (0.0% to drug quality, and 19/201 (9.5% to patient behavior. The most detected critical criteria were the necessary medication not given (52/182; 28.6%, labeled drug–drug interaction (36/182; 19.7%, incorrect drug administration duration (31/182; 16.9%, wrong indication (26/182; 14.2%, therapeutic duplication (18/182; 10.0%, and documented hypersensitivity to administered drug or drug class (10/182; 5.6%. In seventeen (18.1% preventable cases, there were 19 critical criteria involving non-compliance (15/19 critical criteria; 78.9% and self-medication with the non-over-the-counter drugs (4/19 critical criteria; 21.1%. In all, 17 out 94 (18.1% preventable cases involved over-the-counter drugs.Conclusion: A call for action for Campania Pharmacovigilance Regional Centre is necessary in order to promote initiatives to increase the awareness of healthcare professionals and citizens on the risk associated with inappropriate use of NSAIDs.

  16. Drug interactions between antihypertensive drugs and non-steroidal anti-inflammatory agents: a descriptive study using the French Pharmacovigilance database.

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    Fournier, Jean-Pascal; Sommet, Agnès; Durrieu, Geneviève; Poutrain, Jean-Christophe; Lapeyre-Mestre, Maryse; Montastruc, Jean-Louis

    2014-04-01

    Drug-drug interactions (DDIs) between antihypertensive drugs and non-steroidal anti-inflammatory drugs (NSAIDs) can lead to adverse drug reactions (ADRs). Guidelines are available to help prescribers deal with these drug associations, but their implementation is not well evaluated. The aims of this study were to assess the prevalence of NSAIDs exposure in patients treated with antihypertensive drugs, using the French Pharmacovigilance database, and explore the ADRs related to DDIs between antihypertensive drugs and NSAIDs. Over the 11, 442 notifications of ADRs recorded in this database in patients treated with oral antihypertensive drugs between 2008 and 2010, 517 (4.5 and 95% CI: 4.1-4.9) also included exposure to NSAIDs. These subjects were more frequently women, took more drugs in general, and were younger and less frequently treated with antiplatelet drugs. In 24.2% of them (125 patients), a DDI between NSAIDs and antihypertensive drugs was potentially the cause of the reported ADR. Acute renal failure caused by DDIs between NSAIDs and angiotensin-converting enzyme inhibitors (ACEIs), angiotensin receptor blockers (ARBs), or diuretics was the most frequently reported ADR (20.7%). Finally, in the French Pharmacovigilance database, around one-fourth of associations NSAIDs  +  antihypertensive drugs are associated with a 'serious' ADR (mainly acute renal failure), suggesting that this well-known DDI is not enough taken into account by prescribers. © 2012 The Authors Fundamental and Clinical Pharmacology © 2012 Société Française de Pharmacologie et de Thérapeutique.

  17. Clinically important improvement in the WOMAC and predictor factors for response to non-specific non-steroidal anti-inflammatory drugs in osteoarthritic patients: a prospective study

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    Hmamouchi Ihsane

    2012-01-01

    Full Text Available Abstract Background The aims of the present study were first to detect MCID for WOMAC in a Moroccan population, and second, to identify the best pre-treatment predictors on the change of health after treatment by non-specific, non-steroidal anti-inflammatory drugs (NSAIDs, and to evaluate whether the predictors were dependent on the choice of the response criterion. Methods The study involved 173 patients with osteoarthritis in whom primary care physicians decided to start treatment with non-selective NSAIDs. Assessments at admission and after 6 weeks were conducted. In order to determine the threshold levels associated with a definition of clinically important improvement, the receiver operating characteristic method was used. Three different measures of response to a 6-week NSAIDs treatment were used: one indirect measure (MCID in the total WOMAC score, one direct measure (transition question and a combination of both criteria. Results Eighty patients (46.3% reported "a slightly better" general health status compared to that of 6 weeks before NSAIDs treatment. The MCID proportion is a 16.0% reduction in WOMAC. The most stable pre-treatment predictors on the improvement of health after treatment by NSAIDs were the absence of previous knee injury and a high level of education. Conclusions In our data, a 16.0% reduction of the total WOMAC score from baseline was associated with the highest degree of improvement on the transition scale category. This cut-off point had good accuracy, and should be appropriate for use in the interpretation of clinical studies results, as well as in clinical care.

  18. Clinically important improvement in the WOMAC and predictor factors for response to non-specific non-steroidal anti-inflammatory drugs in osteoarthritic patients: a prospective study

    Science.gov (United States)

    2012-01-01

    Background The aims of the present study were first to detect MCID for WOMAC in a Moroccan population, and second, to identify the best pre-treatment predictors on the change of health after treatment by non-specific, non-steroidal anti-inflammatory drugs (NSAIDs), and to evaluate whether the predictors were dependent on the choice of the response criterion. Methods The study involved 173 patients with osteoarthritis in whom primary care physicians decided to start treatment with non-selective NSAIDs. Assessments at admission and after 6 weeks were conducted. In order to determine the threshold levels associated with a definition of clinically important improvement, the receiver operating characteristic method was used. Three different measures of response to a 6-week NSAIDs treatment were used: one indirect measure (MCID in the total WOMAC score), one direct measure (transition question) and a combination of both criteria. Results Eighty patients (46.3%) reported "a slightly better" general health status compared to that of 6 weeks before NSAIDs treatment. The MCID proportion is a 16.0% reduction in WOMAC. The most stable pre-treatment predictors on the improvement of health after treatment by NSAIDs were the absence of previous knee injury and a high level of education. Conclusions In our data, a 16.0% reduction of the total WOMAC score from baseline was associated with the highest degree of improvement on the transition scale category. This cut-off point had good accuracy, and should be appropriate for use in the interpretation of clinical studies results, as well as in clinical care. PMID:22269793

  19. Intravenous self-administration of benzydamine, a non-steroidal anti-inflammatory drug with a central cannabinoidergic mechanism of action.

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    Avvisati, Riccardo; Meringolo, Maria; Stendardo, Emiliana; Malavasi, Elisa; Marinelli, Silvia; Badiani, Aldo

    2018-03-01

    Benzydamine (BZY) is a non-steroidal anti-inflammatory drug used for the topical treatment of inflammations of the oral and vaginal mucosae. Virtually nothing is known about the central pharmacological actions of BZY. Yet there are reports of voluntary systemic overdosage of BZY in drug addicts, resulting in a euphoric, hallucinatory state. In the present study, we investigated the reinforcing properties of BZY in a rat self-administration paradigm. We found that BZY has a powerful reinforcing effect and that this effect is greatly facilitated in animals that already had substance experience, having previously self-administered heroin and cocaine, indicating cross sensitization between BZY and other common drugs of abuse. We then assessed the effect of BZY on prelimbic cortex-to-nucleus accumbens glutamatergic transmission, using field recordings in rat parasagittal brain slices. BZY dose-dependently reduced both field excitatory post synaptic potential amplitude and paired pulse ratio, suggesting a presynaptic mechanism of action. Similarly to the in vivo paradigm, also the electrophysiological effects of BZY were potentiated in slices from animals that had undergone cocaine and heroin self-administration. Furthermore, BZY-induced Long Term Depression (LTD)-like responses in the prelimbic cortex-to-nucleus accumbens circuitry were significantly reduced in the presence of the CB1 receptor antagonist AM251. These findings provide firm evidence of the abuse liability of BZY and suggest a possible cannabinoidergic mechanism of action. Further research is needed in order to give insights into the molecular mechanism underlying BZY psychoactive and reinforcing effects, to better understand its abuse potential. © 2017 Society for the Study of Addiction.

  20. Exposure to non-steroidal anti-inflammatory drugs during pregnancy and the risk of selected birth defects: a prospective cohort study.

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    Marleen M H J van Gelder

    Full Text Available Since use of non-steroidal anti-inflammatory drugs (NSAIDs during pregnancy is common, small increases in the risk of birth defects may have significant implications for public health. Results of human studies on the teratogenic risks of NSAIDs are inconsistent. Therefore, we evaluated the risk of selected birth defects after prenatal exposure to prescribed and over-the-counter NSAIDs.We used data on 69,929 women enrolled in the Norwegian Mother and Child Cohort Study between 1999 and 2006. Data on NSAID exposure were available from a self-administered questionnaire completed around gestational week 17. Information on pregnancy outcome was obtained from the Medical Birth Registry of Norway. Only birth defects suspected to be associated with NSAID exposure based upon proposed teratogenic mechanisms and previous studies were included in the multivariable logistic regression analyses. A total of 3,023 women used NSAIDs in gestational weeks 0-12 and 64,074 women did not report NSAID use in early pregnancy. No associations were observed between overall exposure to NSAIDs during pregnancy and the selected birth defects separately or as a group (adjusted odds ratio 0.7, 95% confidence interval 0.4-1.1. Associations between maternal use of specific types of NSAIDs and the selected birth defects were not found either, although an increased risk was seen for septal defects and exposure to multiple NSAIDs based on small numbers (2 exposed cases; crude odds ratio 3.9, 95% confidence interval 0.9-15.7.Exposure to NSAIDs during the first 12 weeks of gestation does not seem to be associated with an increased risk of the selected birth defects. However, due to the small numbers of NSAID-exposed infants for the individual birth defect categories, increases in the risks of specific birth defects could not be excluded.

  1. Evaluation of biological endpoints in crop plants after exposure to non-steroidal anti-inflammatory drugs (NSAIDs): implications for phytotoxicological assessment of novel contaminants.

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    Schmidt, Wiebke; Redshaw, Clare H

    2015-02-01

    Human pharmaceuticals have been detected in the terrestrial environment at µg to mg kg(-1) concentrations. Repeated application of sewage sludge (biosolids) and increasing reclaimed wastewater use for irrigation could lead to accumulation of these novel contaminants in soil systems. Despite this, potential phytotoxicological effects on higher plants have rarely been evaluated. These studies aimed to test effects upon germination, development, growth and physiology of two crop plants, namely radish (Raphanus sativus Spakler 3) and lettuce (Lactuca sativa All Year Around), after exposure to different, but structurally related non-steroidal anti-inflammatory drugs (NSAIDs) at environmentally relevant concentrations. A range of biological endpoints comprising biomass, length, water content, specific root and shoot length, root to shoot ratio, daily progress of stages of cell elongation and organ emergence (primary root, hypocotyl elongation, cotyledon emergence, cotyledon opening, and no change), as well as photosynthetic measurements were evaluated. Compounds from the fenamic acid class were found to affect R. sativus root endpoints (root length and water content), while ibuprofen affected early root development of L. sativa. In general, phytotoxicological effects on root endpoints demonstrated that impacts upon higher plants are not only compound specific, but also differ between plant species. It was found that the usage of a wide range of biological endpoints (all simple, cost-effective and ecologically relevant) were beneficial in detecting differences in plant responses to NSAID exposure. Due to paucity and discrepancy within the few previously available phytotoxicological studies with pharmaceuticals, it is now essential to allocate time and resources to consider development of suitable chronic toxicity tests, and some suggestions regarding this are presented. Copyright © 2014 Elsevier Inc. All rights reserved.

  2. Molecular modeling and simulation studies of recombinant laccase from Yersinia enterocolitica suggests significant role in the biotransformation of non-steroidal anti-inflammatory drugs

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    Singh, Deepti; Rawat, Surender [Laboratory of Enzymology and Recombinant DNA Technology, Department of Microbiology, Maharshi Dayanand University, Rohtak 124001, Haryana (India); Waseem, Mohd; Gupta, Sunita; Lynn, Andrew [School of Computational & Integrative Sciences, Jawaharlal Nehru University, New Delhi 110067 (India); Nitin, Mukesh; Ramchiary, Nirala [School of Life Sciences, Jawaharlal Nehru University, New Delhi 110067 (India); Sharma, Krishna Kant, E-mail: kekulsharma@gmail.com [Laboratory of Enzymology and Recombinant DNA Technology, Department of Microbiology, Maharshi Dayanand University, Rohtak 124001, Haryana (India)

    2016-01-08

    The YacK gene from Yersinia enterocolitica strain 7, cloned in pET28a vector and expressed in Escherichia coli BL21 (DE3), showed laccase activity when oxidized with 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) and guaiacol. The recombinant laccase protein was purified and characterized biochemically with a molecular mass of ≈58 KDa on SDS-PAGE and showed positive zymogram with ABTS. The protein was highly robust with optimum pH 9.0 and stable at 70 °C upto 12 h with residual activity of 70%. Kinetic constants, K{sub m} values, for ABTS and guaiacol were 675 μM and 2070 μM, respectively, with corresponding Vmax values of 0.125 μmol/ml/min and 6500 μmol/ml/min. It also possess antioxidative property against BSA and Cu{sup 2+}/H{sub 2}O{sub 2} model system. Constant pH MD simulation studies at different protonation states of the system showed ABTS to be most stable at acidic pH, whereas, diclofenac at neutral pH. Interestingly, aspirin drifted out of the binding pocket at acidic and neutral pH, but showed stable binding at alkaline pH. The biotransformation of diclofenac and aspirin by laccase also corroborated the in silico results. This is the first report on biotransformation of non-steroidal anti-inflammatory drugs (NSAIDs) using recombinant laccase from gut bacteria, supported by in silico simulation studies. - Highlights: • Laccase from Yersinia enterocolitica strain 7 was expressed in Escherichia coli BL21 (DE3). • Recombinant laccase was found to be thermostable and alkali tolerant. • The in silico and experimental studied proves the biotransformation of NSAIDs. • Laccase binds to ligands differentially under different protonation state. • Laccase also possesses free radical scavenging property.

  3. Molecular modeling and simulation studies of recombinant laccase from Yersinia enterocolitica suggests significant role in the biotransformation of non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Singh, Deepti; Rawat, Surender; Waseem, Mohd; Gupta, Sunita; Lynn, Andrew; Nitin, Mukesh; Ramchiary, Nirala; Sharma, Krishna Kant

    2016-01-08

    The YacK gene from Yersinia enterocolitica strain 7, cloned in pET28a vector and expressed in Escherichia coli BL21 (DE3), showed laccase activity when oxidized with 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) and guaiacol. The recombinant laccase protein was purified and characterized biochemically with a molecular mass of ≈58 KDa on SDS-PAGE and showed positive zymogram with ABTS. The protein was highly robust with optimum pH 9.0 and stable at 70 °C upto 12 h with residual activity of 70%. Kinetic constants, Km values, for ABTS and guaiacol were 675 μM and 2070 μM, respectively, with corresponding Vmax values of 0.125 μmol/ml/min and 6500 μmol/ml/min. It also possess antioxidative property against BSA and Cu(2+)/H2O2 model system. Constant pH MD simulation studies at different protonation states of the system showed ABTS to be most stable at acidic pH, whereas, diclofenac at neutral pH. Interestingly, aspirin drifted out of the binding pocket at acidic and neutral pH, but showed stable binding at alkaline pH. The biotransformation of diclofenac and aspirin by laccase also corroborated the in silico results. This is the first report on biotransformation of non-steroidal anti-inflammatory drugs (NSAIDs) using recombinant laccase from gut bacteria, supported by in silico simulation studies. Copyright © 2015 Elsevier Inc. All rights reserved.

  4. Effects of photobiomodulation therapy and topical non-steroidal anti-inflammatory drug on skeletal muscle injury induced by contusion in rats-part 2: biochemical aspects.

    Science.gov (United States)

    Tomazoni, Shaiane Silva; Frigo, Lúcio; Dos Reis Ferreira, Tereza Cristina; Casalechi, Heliodora Leão; Teixeira, Simone; de Almeida, Patrícia; Muscara, Marcelo Nicolas; Marcos, Rodrigo Labat; Serra, Andrey Jorge; de Carvalho, Paulo de Tarso Camillo; Leal-Junior, Ernesto Cesar Pinto

    2017-11-01

    Muscle injuries trigger an inflammatory process, releasing important biochemical markers for tissue regeneration. The use of non-steroidal anti-inflammatory drugs (NSAIDs) is the treatment of choice to promote pain relief due to muscle injury. NSAIDs exhibit several adverse effects and their efficacy is questionable. Photobiomodulation therapy (PBMT) has been demonstrated to effectively modulate inflammation induced from musculoskeletal disorders and may be used as an alternative to NSAIDs. Here, we assessed and compared the effects of different doses of PBMT and topical NSAIDs on biochemical parameters during an acute inflammatory process triggered by a controlled model of contusion-induced musculoskeletal injury in rats. Muscle injury was induced by trauma to the anterior tibial muscle of rats. After 1 h, rats were treated with PBMT (830 nm, continuous mode, 100 mW of power, 35.71 W/cm 2 ; 1, 3, and 9 J; 10, 30, and 90 s) or diclofenac sodium (1 g). Our results demonstrated that PBMT, 1 J (35.7 J/cm 2 ), 3 J (107.1 J/cm 2 ), and 9 J (321.4 J/cm 2 ) reduced the expression of tumor necrosis factor alpha (TNF-α) and cyclooxygenase-2 (COX-2) genes at all assessed times as compared to the injury and diclofenac groups (p injury group (p injury group). In addition, PBMT (1, 3, and 9 J) effectively reduced levels of cytokines TNF-α, interleukin (IL)-1β, and IL-6 at all assessed times as compared to the injury and diclofenac groups (p muscle contusion injuries.

  5. Non-steroidal anti-inflammatory drugs use is associated with reduced risk of inflammation-associated cancers: NIH-AARP study.

    Directory of Open Access Journals (Sweden)

    Fatma M Shebl

    Full Text Available Chronic inflammation has been linked to cancers, and use of non-steroidal anti-inflammatory drugs (NSAIDs has been associated with reduced risk of several cancers. To further refine the magnitude of NSAID-related associations, in particular for cancers related to inflammation, such as alcohol-, infection-, obesity-, and smoking-related cancers, as well as for less common cancers, we evaluated the use of NSAIDs and cancer risk in a very large cohort. We used propensity scores to account for potential selection bias and hypothesized that NSAID use is associated with decreased cancer incidence.We conducted a prospective study among 314,522 participants in the NIH-AARP Diet and Health Study. Individuals who completed the lifestyle questionnaire, which included NSAID use, in 1996-1997 were followed through 2006. Information on cancer incidence was ascertained by linking to cancer registries and vital status databases.During 2,715,994 person-years of follow-up (median 10.1 person-years, there were 51,894 incident cancers. Compared with non-users of NSAIDs, individuals who reported use in the 12 months prior to interview had a significantly lower risk of all inflammation-related cancer, alcohol-related, infection-related, obesity-related, and smoking-related cancers [hazard ratio (HR (95% CI 0.90 (0.87-0.93, 0.80 (0.74-0.85, 0.82 (0.78-0.87, 0.88 (0.84-0.92, and 0.88 (0.85-0.92 respectively].After accounting for potential selection bias, our data showed an inverse association between NSAID use and alcohol-related, infection-related, obesity-related, and smoking-related cancers and support the hypothesis that inflammation is related to an increased risk of certain cancers.

  6. Effect of therapeutic plasma concentrations of non-steroidal anti-inflammatory drugs on the production of reactive oxygen species by activated rat neutrophils

    Directory of Open Access Journals (Sweden)

    Paino I.M.M.

    2005-01-01

    Full Text Available The release of reactive oxygen specie (ROS by activated neutrophil is involved in both the antimicrobial and deleterious effects in chronic inflammation. The objective of the present investigation was to determine the effect of therapeutic plasma concentrations of non-steroidal anti-inflammatory drugs (NSAIDs on the production of ROS by stimulated rat neutrophils. Diclofenac (3.6 µM, indomethacin (12 µM, naproxen (160 µM, piroxicam (13 µM, and tenoxicam (30 µM were incubated at 37ºC in PBS (10 mM, pH 7.4, for 30 min with rat neutrophils (1 x 10(6 cells/ml stimulated by phorbol-12-myristate-13-acetate (100 nM. The ROS production was measured by luminol and lucigenin-dependent chemiluminescence. Except for naproxen, NSAIDs reduced ROS production: 58 ± 2% diclofenac, 90 ± 2% indomethacin, 33 ± 3% piroxicam, and 45 ± 6% tenoxicam (N = 6. For the lucigenin assay, naproxen, piroxicam and tenoxicam were ineffective. For indomethacin the inhibition was 52 ± 5% and diclofenac showed amplification in the light emission of 181 ± 60% (N = 6. Using the myeloperoxidase (MPO/H2O2/luminol system, the effects of NSAIDs on MPO activity were also screened. We found that NSAIDs inhibited both the peroxidation and chlorinating activity of MPO as follows: diclofenac (36 ± 10, 45 ± 3%, indomethacin (97 ± 2, 100 ± 1%, naproxen (56 ± 8, 76 ± 3%, piroxicam (77 ± 5, 99 ± 1%, and tenoxicam (90 ± 2, 100 ± 1%, respectively (N = 3. These results show that therapeutic levels of NSAIDs are able to suppress the oxygen-dependent antimicrobial or oxidative functions of neutrophils by inhibiting the generation of hypochlorous acid.

  7. Crystal structures of three classes of non-steroidal anti-inflammatory drugs in complex with aldo-keto reductase 1C3.

    Directory of Open Access Journals (Sweden)

    Jack U Flanagan

    Full Text Available Aldo-keto reductase 1C3 (AKR1C3 catalyses the NADPH dependent reduction of carbonyl groups in a number of important steroid and prostanoid molecules. The enzyme is also over-expressed in prostate and breast cancer and its expression is correlated with the aggressiveness of the disease. The steroid products of AKR1C3 catalysis are important in proliferative signalling of hormone-responsive cells, while the prostanoid products promote prostaglandin-dependent proliferative pathways. In these ways, AKR1C3 contributes to tumour development and maintenance, and suggest that inhibition of AKR1C3 activity is an attractive target for the development of new anti-cancer therapies. Non-steroidal anti-inflammatory drugs (NSAIDs are one well-known class of compounds that inhibits AKR1C3, yet crystal structures have only been determined for this enzyme with flufenamic acid, indomethacin, and closely related analogues bound. While the flufenamic acid and indomethacin structures have been used to design novel inhibitors, they provide only limited coverage of the NSAIDs that inhibit AKR1C3 and that may be used for the development of new AKR1C3 targeted drugs. To understand how other NSAIDs bind to AKR1C3, we have determined ten crystal structures of AKR1C3 complexes that cover three different classes of NSAID, N-phenylanthranilic acids (meclofenamic acid, mefenamic acid, arylpropionic acids (flurbiprofen, ibuprofen, naproxen, and indomethacin analogues (indomethacin, sulindac, zomepirac. The N-phenylanthranilic and arylpropionic acids bind to common sites including the enzyme catalytic centre and a constitutive active site pocket, with the arylpropionic acids probing the constitutive pocket more effectively. By contrast, indomethacin and the indomethacin analogues sulindac and zomepirac, display three distinctly different binding modes that explain their relative inhibition of the AKR1C family members. This new data from ten crystal structures greatly broadens

  8. Non-steroidal anti-inflammatory high digestive bleeding hospital income / Ingresos hospitalarios por hemorragia digestiva alta por antiinflamatorios no esteroidicos

    Directory of Open Access Journals (Sweden)

    Valls MD

    2004-12-01

    Full Text Available From year 1997 the Requena Hospital Pharmacy Service maintain a program of detection and prevention of drugs-related problems hospital income (DRPI. The program is coordinated with the Primary Care Pharmacy Service for the establishment of the preventive measures. The DRPI program establishes feedback, collective and/or individualized, on the agents of health of the Health Area and on the population in general, according to the cases, as it bases for the prevention of DRPIs. Methods: The detection of IDRP is made by means of revision of the diagnoses gathered in the admission book of the Emergency Department and the HIGIA database. Clinical records of the patients are retrospectively analyzed. Medical criteria, specifically gathered in clinical history, are accepted for the imputability establishment. Results: In period 1997-2003, 195 drug-related high digestive hemorrhage hospital income (HDH have been detected: 188 by non-steroidal anti-inflammatory drugs (NSAID, in two cases the NSAID could not settle down cause, 3 by ticlopidine, 3 by metamizole and 1 by clopidogrel. In 45 cases (23% the involved medicine was over the counter (OTC, 58 cases were related to low doses aspirin (AAS, 15 cases related to the association of NSAIDs or NSAIDs with low doses AAS and 70 cases were produced by non-aspirin-NSAIDs or non-OTC-AAS to doses of 500mg. 80% of the cases of HDH by AAS to low doses took place in patients of 69 years old or older. In 85% of the cases of HDH by non-aspirin- NSAID or non-OTC-AAS of 500mg with gastro-protection criteria this had not been used. In the three cases of HDH by metamizole patients were older than 80 years and with HDH antecedents. Conclusions: The low use of gastroprotection between the affected population of HDH by NSAIDs in spite of the existence of clear factors of risk concludes. Gastroprotection in patients dealt with low doses AAS and equal or greater age about 69 years although the age were the only factor of risk

  9. A healthy lifestyle index is associated with reduced risk of colorectal adenomatous polyps among non-users of non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Tabung, Fred K; Steck, Susan E; Burch, James B; Chen, Chin-Fu; Zhang, Hongmei; Hurley, Thomas G; Cavicchia, Philip; Alexander, Melannie; Shivappa, Nitin; Creek, Kim E; Lloyd, Stephen C; Hebert, James R

    2015-02-01

    In a Columbia, South Carolina-based case-control study, we developed a healthy lifestyle index from five modifiable lifestyle factors (smoking, alcohol intake, physical activity, diet, and body mass index), and examined the association between this lifestyle index and the risk of colorectal adenomatous polyps (adenoma). Participants were recruited from a local endoscopy center and completed questionnaires related to lifestyle behaviors prior to colonoscopy. We scored responses on each of five lifestyle factors as unhealthy (0 point) or healthy (1 point) based on current evidence and recommendations. We added the five scores to produce a combined lifestyle index for each participant ranging from 0 (least healthy) to 5 (healthiest), which was dichotomized into unhealthy (0-2) and healthy (3-5) lifestyle scores. We used logistic regression to calculate odds ratios (OR) and 95% confidence intervals (CI) for adenoma with adjustment for multiple covariates. We identified 47 adenoma cases and 91 controls. In the main analyses, there was a statistically nonsignificant inverse association between the dichotomous (OR 0.54; 95% CI 0.22, 1.29) and continuous (OR 0.75; 95% CI 0.51, 1.10) lifestyle index and adenoma. Odds of adenoma were significantly modified by the use of non-steroidal anti-inflammatory drugs (NSAIDs) (p(interaction) = 0.04). For participants who reported no use of NSAIDs, those in the healthy lifestyle category had a 72% lower odds of adenoma as compared to those in the unhealthy category (OR 0.28; 95% CI 0.08, 0.98), whereas a one-unit increase in the index significantly reduced odds of adenoma by 53% (OR 0.47; 95% CI 0.26, 0.88). Although these findings should be interpreted cautiously given our small sample size, our results suggest that higher scores from this index are associated with reduced odds of adenomas, especially in non-users of NSAIDs. Lifestyle interventions are required to test this approach as a strategy to prevent colorectal adenomatous

  10. Regular and low-dose aspirin, other non-steroidal anti-inflammatory medications and prospective risk of HER2-defined breast cancer: the California Teachers Study.

    Science.gov (United States)

    Clarke, Christina A; Canchola, Alison J; Moy, Lisa M; Neuhausen, Susan L; Chung, Nadia T; Lacey, James V; Bernstein, Leslie

    2017-05-01

    Regular users of aspirin may have reduced risk of breast cancer. Few studies have addressed whether risk reduction pertains to specific breast cancer subtypes defined jointly by hormone receptor (estrogen and progesterone receptor) and human epidermal growth factor receptor 2 (HER2) expression. This study assessed the prospective risk of breast cancer (overall and by subtype) according to use of aspirin and other non-steroidal anti-inflammatory medications (NSAIDs) in a cohort of female public school professionals in California. In 1995 - 1996, participants in the California Teachers Study completed a baseline questionnaire on family history of cancer and other conditions, use of NSAIDs, menstrual and reproductive history, self-reported weight and height, living environment, diet, alcohol use, and physical activity. In 2005-2006, 57,164 participants provided some updated information, including use of NSAIDs and 1457 of these participants developed invasive breast cancer before January 2013. Multivariable Cox proportional hazards regression models provided hazard rate ratios (HRR) for the association between NSAID use and risk of invasive breast cancer as well as hormone receptor- and HER2-defined subtypes. Developing breast cancer was associated inversely with taking three or more tablets of low-dose aspirin per week (23% of participants). Among women reporting this exposure, the HRR was 0.84 (95% confidence interval (CI) 0.72-0.98) compared to those not taking NSAIDs and this was particularly evident in women with the hormone receptor-positive/HER2-negative subtype (HRR = 0.80, 95% CI 0.66-0.96). Use of three or more tablets of "other" NSAIDs was marginally associated with lower risk of breast cancer (HRR = 0.79, 95% CI 0.62-1.00). Other associations with NSAIDs were generally null. Our observation of reduced risk of breast cancer, among participants who took three or more tablets of low-dose aspirin weekly, is consistent with other reports looking at

  11. Hospital pharmacists' roles and attitudes in providing information on the safety of non-steroidal anti-inflammatory drugs in Thailand.

    Science.gov (United States)

    Phueanpinit, Pacharaporn; Jarernsiripornkul, Narumol; Pongwecharak, Juraporn; Krska, Janet

    2014-12-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used for patients to manage pain and inflammation, especially in older adults. Failure to cope with some adverse drug reactions (ADRs) of NSAIDs could lead to more serious symptoms, therefore, providing useful information about medicine is an important step in protecting patients from developing serious ADRs. The pharmacy service should be a frequent source of medicine information for patients, however in Thailand, little is known about pharmacists' provision of safety information to patients for management and prevention of these ADRs. Aims of this study were to determine Thai hospital pharmacists' roles in providing drug safety information and to assess their attitudes towards the importance of giving drug safety education to patients. All government hospitals in north-eastern Thailand. This study was a cross-sectional survey. A total of 761 pharmacists in 287 hospitals in north-eastern Thailand were selected by stratified random sampling. Self-administered questionnaires were sent by post, with two reminders. Proportion of hospital pharmacists providing ADR information on NSAIDs to patients, factors affecting this provision, and pharmacist attitudes towards drug safety education for patients. The response rate was 54.8% (N = 417), the majority of respondents worked in community hospitals (57.2%). A total of 347 pharmacists (83.6%) had informed patients about ADRs, although less than half had informed patients about ADR monitoring and management (36.6% and 44.1% respectively). The proportion of time spent in direct patient contact, type of hospital, and other routine work were associated with the frequency of drug safety information provision. Pharmacists had moderately good attitudinal scores towards drug safety education (62.2 ± 5.4), with significantly higher scores found in those who provided most ADR information to patients (60.3 ± 5.2 vs. 62.6 ± 5.4, P = 0.002). The majority (82.2%) agreed that

  12. Non-steroidal anti-inflammatory drugs for the treatment of pain and immobility-associated osteoarthritis: consensus guidance for primary care

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    Adebajo Ade

    2012-03-01

    Full Text Available Abstract Background Osteoarthritis is a common presentation in primary care, and non-selective non-steroidal anti-inflammatory drugs (sometimes also referred to as traditional NSAIDs or tNSAIDs and selective cyclo-oxygenase 2 inhibitors (COX-2 inhibitors are commonly used to treat it. The UK's National Institute for Health and Clinical Excellence (NICE recommends taking patient risk factors into account when selecting a tNSAID or a COX-2 inhibitor, but GPs have lacked practical guidance on assessing patient risk. Methods A multi-disciplinary group that included primary care professionals (PCPs developed an evidence-based consensus statement with an accompanying flowchart that aimed at providing concise and specific guidance on NSAID use in osteoarthritis treatment. An open invitation to meet and discuss the issue was made to relevant healthcare professionals in South Yorkshire. A round table meeting was held that used a modified nominal group technique, aimed at generating opinions and ideas from all stakeholders in the consensus process. A draft developed from this meeting went through successive revisions until a consensus was achieved. Results Four statements on the use of tNSAIDs and COX-2 inhibitors (and an attached category of evidence were agreed: 1 tNSAIDs are effective drugs in relieving pain and immobility associated with osteoarthritis. COX-2 inhibitors are equally effective; 2 tNSAIDs and COX-2 inhibitors vary in their potential gastrointestinal, liver, and cardio-renal toxicity. This risk varies between individual treatments within both groups and is increased with dose and duration of treatment; 3 COX-2 inhibitors are associated with a significantly lower gastrointestinal toxicity compared to tNSAIDs. Co-prescribing of aspirin reduces this advantage; 4 PPIs should always be considered with a tNSAID and with a COX-2 inhibitor in higher GI risk patients. An accompanying flowchart to guide management was also agreed. Conclusions

  13. Safety and efficacy of long-term esomeprazole 20 mg in Japanese patients with a history of peptic ulcer receiving daily non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Sugano, Kentaro; Kinoshita, Yoshikazu; Miwa, Hiroto; Takeuchi, Tsutomu

    2013-03-26

    Non-steroidal anti-inflammatory drugs (NSAIDs) are an effective and common treatment for chronic pain disorders, but long-term use is associated with risk of potentially life-threatening gastrointestinal adverse events (AEs). The proton pump inhibitor esomeprazole has been found to be effective for gastroprotection in NSAID users, but few long-term studies have been conducted in Japan. This was an open-label, multicentre, single-arm, prospective 1-year study of treatment with esomeprazole (20 mg once daily) in Japanese patients (aged ≥20 years) with endoscopic evidence of previous peptic ulcer and receiving daily oral NSAID therapy (at a stable dose) for a chronic condition. Eligibility was not dictated by type of oral NSAID. The primary objective was to determine long-term safety and tolerability of esomeprazole. Efficacy for prevention of peptic ulcers was also determined (Kaplan-Meier method). All statistical analyses were descriptive. A total of 130 patients (73.1% women, mean age 62.1 years, 43.8% Helicobacter pylori-positive) received treatment with esomeprazole in addition to long-term NSAID therapy (most commonly for rheumatoid arthritis [n=42] and osteoarthritis [n=34]). Loxoprofen, meloxicam and diclofenac were the most commonly used NSAIDs; cyclo-oxygenase (COX)-2 selective agents were used by 16.2% of patients (n=21). Long-term compliance with esomeprazole (capsule counts) was >75% for the majority of patients. Although 16.9% of patients (n=22) experienced AEs judged to be possibly related to treatment with esomeprazole, they were mostly mild and transient. The most commonly reported possibly treatment-related AEs were abnormal hepatic function, headache, increased γ-glutamyltransferase levels and muscle spasms (2 patients each). Overall, 95.9% (95% confidence interval: 92.3, 99.4) of patients remained ulcer free at 1 year. Long-term treatment with esomeprazole (20 mg once daily) is well tolerated and efficacious for preventing ulcer recurrence in

  14. Dermal Cell Damage Induced by Topical Application of Non-Steroidal Anti-Inflammatory Drugs is Suppressed by Trehalose Co-Lyophilization in Ex Vivo Analysis

    National Research Council Canada - National Science Library

    KAYASUGA-KARIYA, Yuko; IWANAGA, Shintaroh; FUJISAWA, Ayano; LIN, Lee-Shuan; SUZUKI, Shigeki; CHUNG, Ung-il; SASAKI, Nobuo; SHIMOHATA, Nobuyuki; MOCHIZUKI, Manabu

    2013-01-01

    ... effect of trehalose was reinforced by co-lyophilization of NSAIDs with trehalose. The anti-inflammatory effect of co-lyophilized NSAIDs with trehalose was comparable to that seen with NSAIDs alone in a rat model...

  15. Inhibition of tolbutamide 4-methylhydroxylation by a series of non-steroidal anti-inflammatory drugs in V79-NH cells expressing human cytochrome P4502C10

    NARCIS (Netherlands)

    Kappers, W.A.; Groene, E.M. de; Kleij, L.A.; Witkamp, R.F.; Zweers-Zeilmaker, W.M.; Feron, V.J.; Horbach, G.J.

    1996-01-01

    1. To study the role of cytochrome P4502C10 in the metabolism of the non-steroidal antiinflammatory drugs (NSAIDs) diclofenac, phenylbutazone, fenoprofen, ibuprofen, flurbiprofen, ketoprofen and naproxen, a cell line was developed stably expressing CYP2C10 cDNA. A retroviral vector construct,

  16. Paracetamol (acetaminophen) or non-steroidal anti-inflammatory drugs, alone or combined, for pain relief in acute otitis media in children.

    Science.gov (United States)

    Sjoukes, Alies; Venekamp, Roderick P; van de Pol, Alma C; Hay, Alastair D; Little, Paul; Schilder, Anne Gm; Damoiseaux, Roger Amj

    2016-12-15

    Acute otitis media (AOM) is one of the most common childhood infectious diseases and a significant reason for antibiotic prescriptions in children worldwide. Pain from middle ear infection and pressure behind the eardrum is the key symptom of AOM. Ear pain is central to children's and parents' experience of the illness. Because antibiotics provide only marginal benefits, analgesic treatment including paracetamol (acetaminophen) and non-steroidal anti-inflammatory drugs (NSAIDs) is regarded as the cornerstone of AOM management in children. Our primary objective was to assess the effectiveness of paracetamol (acetaminophen) or NSAIDs, alone or combined, compared with placebo or no treatment in relieving pain in children with AOM. Our secondary objective was to assess the effectiveness of NSAIDs compared with paracetamol in children with AOM. We searched the Cochrane Central Register of Controlled Trials (CENTRAL), Issue 7, July 2016; MEDLINE (Ovid, from 1946 to August 2016), Embase (from 1947 to August 2016), CINAHL (from 1981 to August 2016), LILACS (from 1982 to August 2016) and Web of Science (from 1955 to August 2016) for published trials. We screened reference lists of included studies and relevant systematic reviews for additional trials. We searched WHO ICTRP, ClinicalTrials.gov, and the Netherlands Trial Registry (NTR) for completed and ongoing trials (search date 19 August 2016). We included randomised controlled trials (RCTs) comparing the effectiveness of paracetamol or NSAIDs, alone or combined, for pain relief in children with AOM. We also included trials of paracetamol or NSAIDs, alone or combined, for children with fever or upper respiratory tract infections (URTIs) if we were able to extract subgroup data on pain relief in children with AOM either directly or after obtaining additional data from study authors. Two review authors independently assessed methodological quality of the included trials and extracted data. We used the GRADE approach to rate

  17. [Risk of fatal/non-fatal events in patients with previous coronary heart disease/acute myocardial infarction and treatment with non-steroidal anti-inflammatory drugs].

    Science.gov (United States)

    Muñoz Olmo, L; Juan Armas, J; Gomariz García, J J

    2017-09-04

    Primary Care is the fundamental axis of our health system and obliges us to be consistent with our prescriptions. The non-steroidal anti-inflammatory drugs (NSAIDs) have been associated with increased cardiovascular risk and increased risk of all causes of death, as well as acute myocardial infarction (AMI) in patients with a previous myocardial infarction. Pain and cardiac patient management are 2 basic pillars in our daily activity, and we must know the limitations of NSAIDs in patients with established cardiovascular risk. We present a review of the scientific literature with primary interest in the role of NSAIDs and cardiovascular risk. The objective is to determine the relationship between the consumption of different NSAIDs and the fatal and non-fatal events among patients with known coronary disease. This is a review of the scientific literature with primary interest in the role of NSAIDs and cardiovascular risk. The literature review was conducted in PubMed search engines like Tripdatabase and with certain keywords. Of the 15 original papers found, 9 did not correspond completely to the central focus, so the approach was decided from 6 original articles from the past 5 years, which address the central focus of increased cardiovascular risk found (fatal and non-fatal events) in patients with prior cardiovascular disease or AMI being prescribed NSAIDs for any reason. The risk of fatal/non-fatal events in each of the studies is expressed by the odds ratio (OR)/hazard ratio (HR), defined as the probability of an event occurring. A moderate risk was observed for ibuprofen. It increases the risk of acute coronary syndrome after 5 years of cardiovascular event, especially in the 2nd year (OR 1.63; 95% CI 1.42-1.87). It also increases the risk of stroke (HR 1.23; 95% IC 1.10-1.38). Cyclo-oxygenase-2 inhibitors were the third risk group, after nabumetone and diclofenac. Celecoxib increases risk from the 14th day of treatment (HR 2.3; 95% CI 1.79-3.02), having an OR

  18. The efficacy of non-narcotic analgesics on post-operative endodontic pain: A systematic review and meta-analysis: The efficacy of non-steroidal anti-inflammatory drugs and/or paracetamol on post-operative endodontic pain.

    Science.gov (United States)

    Shirvani, A; Shamszadeh, S; Eghbal, M J; Asgary, S

    2017-09-01

    The objective of this review was to evaluate the efficacy of non-narcotic analgesics including non-steroidal anti-inflammatory drugs (NSAIDs) and/or paracetamol in the treatment of post-operative endodontic pain. Additionally, we aimed to examine the possible association of study covariates on the pain scores using meta-regression analysis. An electronic search was performed in 2016. After data extraction and quality assessment of the included studies (n = 27, representing 2188 patients), meta-analysis was performed using a random-effect inverse variance method. Meta-regression analysis was conducted to examine the associations between effect sizes and study-level covariates (P endodontic pain by administration of NSAIDs and/or paracetamol. However, analgesic regimens should be considered as important determinants when prescribing a pharmacological adjuvant. © 2017 John Wiley & Sons Ltd.

  19. In vitro evaluation of the effects of anti-fungals, benzodiazepines and non-steroidal anti-inflammatory drugs on the glucuronidation of 19-norandrosterone: implications on doping control analysis.

    Science.gov (United States)

    Palermo, Amelia; Alessi, Beatrice; Botrè, Francesco; de la Torre, Xavier; Fiacco, Ilaria; Mazzarino, Monica

    2016-09-01

    We have studied whether the phase II metabolism of 19-norandrosterone, the most representative metabolite of 19-nortestosterone (nandrolone), can be altered in the presence of other drugs that are not presently included on the Prohibited List of the World Anti-Doping Agency. In detail, we have evaluated the effect of non-prohibited drugs belonging to the classes of anti-fungals, benzodiazepines, and non-steroidal anti-inflammatory drugs on the glucuronidation of 19-norandrosterone. In vitro assays based on the use of either pooled human liver microsomes or specific recombinant isoforms of uridine diphosphoglucuronosyl-transferase were designed and performed to monitor the formation of 19-norandrosterone glucuronide from 19-norandrosterone. Determination of 19-norandrosterone (free and conjugated fraction) was performed by gas chromatography - mass spectrometry after sample pretreatment consisting of an enzymatic hydrolysis (performed only for the conjugated fraction), liquid/liquid extraction with tert-butylmethyl ether, and derivatization to form the trimethylsilyl derivative. In parallel, a method based on reversed-phase liquid chromatography coupled to tandem mass spectrometry in positive electrospray ionization with acquisition in selected reaction monitoring mode was also developed to identify the non-prohibited drugs considered in this study. Incubation experiments have preliminarily shown that the glucuronidation of 19-norandrosterone is principally carried out by UGT2B7 (39%) and UGT2B17 (31%). Inhibition studies have shown that the yield of the glucuronidation reaction is reduced in the presence of the anti-fungals itraconazole, ketoconazole, and miconazole, of the benzodiazepine triazolam and of the non-steroidal anti-inflammatory drugs diclofenac and ibuprofen, while no alteration was recorded in the presence of all other compounds considered in this study. Copyright © 2015 John Wiley & Sons, Ltd. Copyright © 2015 John Wiley & Sons, Ltd.

  20. Therapeutic potential of a non-steroidal bifunctional anti-inflammatory and anti-cholinergic agent against skin injury induced by sulfur mustard

    Energy Technology Data Exchange (ETDEWEB)

    Chang, Yoke-Chen; Wang, James D.; Hahn, Rita A.; Gordon, Marion K.; Joseph, Laurie B. [Department of Pharmacology and Toxicology, Rutgers University, Piscataway, NJ (United States); Heck, Diane E. [Department of Environmental Science, New York Medical College, Valhalla, NY (United States); Heindel, Ned D. [Department of Chemistry, Lehigh University, Bethlehem, PA (United States); Young, Sherri C. [Department of Chemistry, Muhlenberg College, Allentown, PA (United States); Sinko, Patrick J. [Department of Pharmaceutics, Rutgers University, Piscataway, NJ (United States); Casillas, Robert P. [MRIGlobal, Kansas City, MO (United States); Laskin, Jeffrey D. [Environmental and Occupational Medicine, Robert Wood Johnson Medical School, Rutgers University, Piscataway, NJ (United States); Laskin, Debra L. [Department of Pharmacology and Toxicology, Rutgers University, Piscataway, NJ (United States); Gerecke, Donald R., E-mail: gerecke@eohsi.rutgers.edu [Department of Pharmacology and Toxicology, Rutgers University, Piscataway, NJ (United States)

    2014-10-15

    Sulfur mustard (bis(2-chloroethyl) sulfide, SM) is a highly reactive bifunctional alkylating agent inducing edema, inflammation, and the formation of fluid-filled blisters in the skin. Medical countermeasures against SM-induced cutaneous injury have yet to be established. In the present studies, we tested a novel, bifunctional anti-inflammatory prodrug (NDH 4338) designed to target cyclooxygenase 2 (COX2), an enzyme that generates inflammatory eicosanoids, and acetylcholinesterase, an enzyme mediating activation of cholinergic inflammatory pathways in a model of SM-induced skin injury. Adult SKH-1 hairless male mice were exposed to SM using a dorsal skin vapor cup model. NDH 4338 was applied topically to the skin 24, 48, and 72 h post-SM exposure. After 96 h, SM was found to induce skin injury characterized by edema, epidermal hyperplasia, loss of the differentiation marker, keratin 10 (K10), upregulation of the skin wound marker keratin 6 (K6), disruption of the basement membrane anchoring protein laminin 322, and increased expression of epidermal COX2. NDH 4338 post-treatment reduced SM-induced dermal edema and enhanced skin re-epithelialization. This was associated with a reduction in COX2 expression, increased K10 expression in the suprabasal epidermis, and reduced expression of K6. NDH 4338 also restored basement membrane integrity, as evidenced by continuous expression of laminin 332 at the dermal–epidermal junction. Taken together, these data indicate that a bifunctional anti-inflammatory prodrug stimulates repair of SM induced skin injury and may be useful as a medical countermeasure. - Highlights: • Bifunctional anti-inflammatory prodrug (NDH4338) tested on SM exposed mouse skin • The prodrug NDH4338 was designed to target COX2 and acetylcholinesterase. • The application of NDH4338 improved cutaneous wound repair after SM induced injury. • NDH4338 treatment demonstrated a reduction in COX2 expression on SM injured skin. • Changes of skin repair

  1. Toxic effects of the non-steroidal anti-inflammatory drug diclofenac. Part II: cytological effects in liver, kidney, gills and intestine of rainbow trout (Oncorhynchus mykiss).

    Science.gov (United States)

    Triebskorn, R; Casper, H; Heyd, A; Eikemper, R; Köhler, H-R; Schwaiger, J

    2004-06-10

    In the present study, cytopathology was investigated in the liver, kidney, gills and gut of rainbow trout (Oncorhynchus mykiss) exposed to five different concentrations (1, 5, 20, 100 and 500 microg/L) of the anti-inflammatory drug diclofenac under laboratory conditions. The lowest observed effect concentration (LOEC) for cytological alterations in liver, kidney and gills was 1 microg/L. In the gut, however, no diclofenac-induced cytopathology occurred. As the most prominent reactions induced by diclofenac (1) in the kidney, a severe accumulation of protein in the tubular cells (so called hyaline droplet degeneration), macrophage infiltration and structural alterations (dilation, vesiculation) of the endoplasmic reticulum (ER) in the proximal and distal renal tubules were observed. Furthermore, shortening of podocytes and their retraction from the basal lamina, a thickening of the basal lamina, the formation of desmosomes, and necrosis of endothelial cells in the renal corpuscles occurred; (2) in the liver, the most striking reactions were the collapse of the cellular compartmentation as well as the glycogen depletion of hepatocytes; (3) in the gills, pillar cell necrosis, hypertrophy of chloride cells, and epithelium lifting became evident in the secondary lamellae.

  2. Pre-hospital Use of Non-steroidal Anti-inflammatory Drugs (NSAIDs) is Associated with a Reduced Incidence of Trauma-Induced Coagulopathy

    Science.gov (United States)

    Neal, Matthew D.; Brown, Joshua B.; Moore, Ernest E.; Cuschieri, Joseph; Maier, Ronald V.; Minei, Joseph P.; Billiar, Timothy R.; Peitzman, Andrew B.; Cohen, Mitchell J.; Sperry, Jason L.; Inflammation, The

    2014-01-01

    Objective To determine if pre-hospital NSAID use may lead to a reduced incidence of Trauma-Induced Coagulopathy (TIC) in severely injured patients. Summary Background Data TIC is present in up to one-quarter of severely injured trauma patients and is linked to worse outcomes after injury. Evidence linking TIC to inflammation has emerged, however, the mechanism behind this association is still under investigation. NSAIDs are commonly used anti-inflammatory drugs, but their effects on TIC and outcomes after injury are largely unexplored. Methods We performed a secondary analysis of the Inflammation and the Host Response to Injury Large Scale Collaborative Program (Glue Grant) dataset. Prehospital medications and co-morbidities were analyzed via logistic regression analysis for association with TIC as defined by laboratory (INR>1.5) or clinical (transfusion > 2 units of fresh frozen plasma (FFP) or > 1 pack of platelets in 6 hours) parameters. Results Prehospital NSIAD use was independently associated with a 72% lower risk of TIC and was the only medication amongst 15 analyzed to retain significance in the model. Stepwise logistic regression also demonstrated that preadmission use of NSAIDs was independently associated with a 66% lower risk of clinically significant coagulopathy. These findings were independent of co-morbid conditions linked to NSAID use. Conclusions NSAID use prior to admission for severe injury is associated with a reduced incidence of TIC. These findings provide further evidence to a potential leak between TIC and inflammation. PMID:24424149

  3. Non-steroidal anti-inflammatory drug use and ovarian cancer risk: findings from the NIH-AARP Diet and Health Study and systematic review

    Science.gov (United States)

    Murphy, Megan A.; Trabert, Britton; Yang, Hannah P.; Park, Yikyung; Brinton, Louise A.; Hartge, Patricia; Sherman, Mark E.; Hollenbeck, Albert; Wentzensen, Nicolas

    2012-01-01

    Background Chronic inflammation has been proposed as a risk factor for ovarian cancer. Some data suggest that anti-inflammatory medications may be protective against ovarian cancer; however, results have been inconsistent. Methods We evaluated the risk of epithelial ovarian cancer with regular use of NSAIDs prospectively in the NIH-AARP Diet and Health Study, using Cox proportional hazard models. We also examined the risk of common subtypes of epithelial ovarian cancer (serous, mucinous, endometrioid, clear cell and other epithelial) with regular use of NSAIDs. In addition, we performed meta-analyses summarizing the risk of ovarian cancer with “regular use” of NSAIDs in previously published studies. Results We did not observe a significant association between regular use of NSAIDs with ovarian cancer risk in the AARP cohort (aspirin: RR 1.06, 95% CI 0.87–1.29; non-aspirin NSAIDs: RR 0.93, 95% CI 0.74–1.15); however summary estimates from prospective cohort studies demonstrated that use of non-aspirin NSAIDs may reduce the risk of ovarian cancer (RR 0.88, 95% CI 0.77–1.01). Although not significant, we found that mucinous tumors were inversely associated with non-aspirin NSAID use (RR 0.69, 95% CI 0.23–2.10) in the AARP cohort, which was supported by the meta-analysis (RR 0.69, CI 0.50–0.94.) Conclusion Although results from the NIH-AARP cohort study were not statistically significant, our meta-analysis suggests that non-aspirin NSAIDs may be protective against ovarian cancer. Additional analyses, focusing on dose, duration, and frequency of NSAID use and accounting for ovarian cancer heterogeneity are necessary to further elucidate the association between NSAID use and ovarian cancer risk. PMID:22972000

  4. Gastroprotective and Ulcer Healing Effects of Camel Milk and Urine in HCl/EtOH, Non-steroidal Anti-inflammatory Drugs (Indomethacin), and Water-Restraint Stress-induced Ulcer in Rats.

    Science.gov (United States)

    Hu, Zijuan; Chang, Xiaoman; Pan, Qing; Gu, Kebin; Okechukwu, Patrick Nwabueze

    2017-01-01

    Camel milk has been reportedly used to treat dropsy, jaundice, tuberculosis, and diabetes while camel urine is used to treat diarrhea and cancer. However, there is no scientific evidence on the antiulcer activity of camel milk and urine. Thus, the present is designed to investigate the gastroprotective and ulcer healing effect of camel milk and urine on experimentally induced gastric ulcer models in rats. The gastroprotective effect was investigated in HCl/EtOH, water-restraint stress (WRS) and non-steroidal anti-inflammatory drugs (indomethacin)-induced ulcer models while ulcer healing activity was investigated in indomethacin-induced ulcer model. Cimetidine (100 mg/kg) was used as a standard antiulcer drug. Acute toxicity study done up to a dosage of 10 ml/kg of camel milk and urine showed no signs of toxicity and mortality among the rats, indicating the present dosage of 5 ml/kg is safe to be administered to the rats. In the HCl/EtOH model, oral administration of cimetidine (100 mg/kg), camel urine (5 ml/kg), and camel milk (5 ml/kg) significantly (P ulcer inhibition of 100% while camel milk showed an inhibition of 50%. Similarly, in the indomethacin-induced ulcer model, cimetidine, camel milk, and urine showed an ulcer inhibition of 100, 33.3, and 66.7%, respectively. In addition, camel milk and urine also showed a significant (P ulcer healing effect of 100% in indomethacin-induced ulcer model, with no ulcers observed as compared to that of cimetidine, which offers a healing effect of 60.5%. The antiulcer activity of camel milk and urine may be attributed to its cytoprotective mechanism and antioxidant properties. Acute toxicity findings revealed the dosage of 10 ml/kg of camel milk and urine seems no toxic and indicating the dosage of 5 ml/kg is safe to be administered to the ratsOral administration of cimetidine (100 mg/kg), camel urine (5 ml/kg), and camel milk (5 ml/kg) significantly inhibited gastric lesions by 83.7, 60.5 and 100% in the HCl

  5. Regular use of acetaminophen or acetaminophen-codeine combinations and prescription of rescue therapy with non-steroidal anti-inflammatory drugs: a population-based study in primary care.

    Science.gov (United States)

    Vannacci, Alfredo; Lombardi, Niccolò; Simonetti, Monica; Fornasari, Diego; Fanelli, Andrea; Cricelli, Iacopo; Cricelli, Claudio; Lora Aprile, Pierangelo; Lapi, Francesco

    2017-06-01

    There are contrasting positions concerning the benefit-risk ratio of acetaminophen use for osteoarthritis (OA)-related pain. To clarify the effectiveness of acetaminophen or acetaminophen-codeine combinations according to their regimen of use, we evaluated whether being a regular user (adherent) of these medications decreased the occurrence of rescue therapy with non-steroidal anti-inflammatory drugs (NSAIDs). Using the Health Search IMS Health Longitudinal Patient Database, we formed a cohort of patients aged ≥18 years and newly treated with acetaminophen or acetaminophen-codeine combinations for OA between 1 January 2001 and 31 December 2013. These patients were followed up for one year in which they were categorized as regular or irregular users of these medications according to a variable medication possession ratio (VMPR) ≥ 50% or lower. We operationally defined the rescue therapy as the use of any NSAIDs prescribed for OA-related pain. Overall, 40,029 patients (69.5% females; mean age: 68 ± 13.57) treated with acetaminophen or acetaminophen-codeine combinations formed the cohort. After the first year of treatment, regular users showed a statistically significantly lower risk of being prescribed with rescue therapy with NSAIDs (OR = 0.89; 95% CI 0.84-0.96). These findings show that regular use of acetaminophen or acetaminophen-codeine combinations may reduce the need for NSAIDs to treat OA-related pain.

  6. More on the "Triple Whammy": antihypertensive drugs, non-steroidal anti-inflammatory agents and acute kidney injury - a case/non-case study in the French pharmacovigilance database.

    Science.gov (United States)

    Fournier, Jean-Pascal; Sommet, Agnès; Durrieu, Geneviève; Poutrain, Jean-Christophe; Lapeyre-Mestre, Maryse; Montastruc, Jean-Louis

    2014-08-01

    It has been suggested that the risk of acute kidney injury (AKI) increases with the number of drugs associated between non-steroidal anti-inflammatory drugs (NSAIDs), angiotensin converting enzyme inhibitors (ACEis) [or angiotensin receptor blockers (ARBs)] and diuretics. We aimed to investigate whether the number of drugs associated between NSAIDs, ACEis, ARBs and diuretics was associated to disproportionate reporting of AKI in the French Pharmacovigilance Database. In reports of Adverse Drug Reactions (ADRs) recorded between 01 January 2008 and 31 December 2010, we selected patients whose medications included at least one oral antihypertensive drug. We used a case/non-case methodology. Cases were AKI and non-cases were all the remaining reports. Among the 11,442 ADR reports in patients under antihypertensive drug recorded in the French Pharmacovigilance Database, 837 ADRs were AKI (7.3%, 95% CI 6.8-7.8). AKI and the number of drugs associated were disproportionately reported (one drug alone: adjusted ROR 2.19, 95% CI: 1.65-2.89, two drugs: adjusted ROR 5.27, 95% CI: 4.00-6.94, three and more: adjusted ROR 16.46, 95% CI: 11.38-23.80). There was no significant association between NSAIDs' half-lives and reporting of AKI (adjusted ROR=0.54, 95% CI: 0.25-1.15). Given the widespread use of these hazardous drugs in general population, caution is needed when they are associated.

  7. The pharmacology and activity of non-steroidal anti-inflammatory drugs (NSAIDs: a review of their use as an adjuvant treatment in patients with HBV and HCV chronic hepatitis

    Directory of Open Access Journals (Sweden)

    Sirio Fiorino

    2013-03-01

    Full Text Available Introduction: Different DNA and RNA viruses exploit common strategies to support their persistence and replication in infected individuals. In particular, the hepatitis B virus (HBV and the hepatitis C virus (HCV cause major health problems worldwide. These pathogens exert an immunosuppressive role by inducing the persistent activation of cyclooxygenase-2 (COX-2 and an increased synthesis of prostaglandin E2 (PGE2. The suppression of this proinflammatory network by non-steroidal anti-inflammatory drugs (NSAIDs has been proposed as a therapeutic approach to decrease viral replication. Materials and methods: In this review, the role of inflammation in the support of viral replication and NSAIDs and ketoprofen pharmacology are briefly discussed. In addition, studies that have investigated the use of NSAIDs for the treatment of HBV and HCV chronic hepatitis, which were identified by a systematic literature search of PubMed and MEDLINE, are reported. Results: To date, pegylated-interferon (PEG-IFN and/or nucleot(side analogues and PEG-IFN and ribavirin remain the standard therapy for HBV and HCV chronic hepatitis, respectively. Discussion: The use of NSAIDs in patients with chronic viral hepatitis has only a ‘‘historical’’ interest. Nevertheless, the possible usefulness of ketoprofen with PEG-IFN and ribavirin for HCVinfected patients, non-responders to standard therapy or with genotype 1, should be evaluated in future clinical studies.

  8. Analysis of non-steroidal anti-inflammatory drugs in milk using QuEChERS and liquid chromatography coupled to mass spectrometry: triple quadrupole versus Q-Orbitrap mass analyzers.

    Science.gov (United States)

    Rúbies, Antoni; Guo, Lili; Centrich, Francesc; Granados, Mercè

    2016-08-01

    We developed a Quick, Easy, Cheap, Effective, Rugged, and Safe (QuEChERS) method for the high throughput determination of 10 non-steroidal anti-inflammatory drugs (NSAIDs) in milk samples using high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) with a triple quadrupole (QqQ) instrument and an electrospray ionization (ESI) source. The new extraction procedure is highly efficient, and we obtained absolute recoveries in the range 78.1-97.1 % for the extraction and clean-up steps. Chromatographic separation is performed in the gradient mode with a biphenyl column and acidic mobile phases consisting of water and acetonitrile containing formic acid. The chromatographic run time was about 12 min, and NSAID peaks showed a good symmetry factor. For MS/MS detection, we used multiple reaction monitoring (MRM) mode, using ESI in both positive and negative modes. Our method has been validated in compliance with the European Commission Decision 657/2002/EC, and we obtained very satisfactory results in inter-laboratory testing. Furthermore, we explored the use of a hybrid high resolution mass spectrometer, combining a quadrupole and an Orbitrap mass analyzer, for high resolution (HR) MS/MS detection of NSAIDs. We achieved lower NSAID quantification limits with Q-Orbitrap high resolution mass spectrometry (HRMS/MS) detection than those achieved with the QqQ instrument; however, its main feature is its very high selectivity, which makes HRMS/MS particularly suitable for confirmatory analysis.

  9. The effects of two non-steroidal anti-inflammatory drugs on the mobility of laying hens with keel bone fractures.

    Science.gov (United States)

    Nasr, Mohammed Af; Nicol, Christine J; Wilkins, Lindsay; Murrell, Joanna C

    2015-03-01

    Investigate the effects of administration of meloxicam and carprofen on the mobility of hens with and without keel fractures. Within each of two experiments a 'blinded' randomised cross over design whereby birds received either the test drug (carprofen or meloxicam) or saline. Two groups of Lohman Brown hens with and without keel bone fractures. The first group (n = 63) was treated with carprofen 25 mg kg(-1) and saline subcutaneously, twice. The second group (n = 40) was treated with meloxicam (5 mg kg(-1) ) and saline subcutaneously. The latency of birds to fly down from perches 50, 100 and 150 cm above the ground was measured after each treatment. Data from experiment 1 and 2 were analysed separately; the effects of drug treatment compared with saline on landing time for birds with and without keel bone fractures were evaluated using MLwiN. In both experiments latency to fly down from perches was longer in hens with keel fractures and there was a significant interaction between perch height and fracture status. For carprofen, at the 50 cm, 100 cm and 150 cm perch heights, birds with fractures took (mean ± SD) 2.5 ± 2.9, 6.8 ± 9.7 and 11.5 ± 13.2 seconds respectively to fly down compared with 1.3 ± 0.5, 2.3 ± 1.2 and 4.2 ± 3.1 seconds for birds without fractures. For meloxicam, at the 50 cm, 100 cm and 150 cm perch heights, birds with fractures took 2.9 ± 2.5, 49.8 ± 85.4 and 100.3 ± 123.6 seconds respectively compared with 0.7 ± 0.5, 2.5 ± 7.1 and 3.0 ± 4.6 seconds to fly down for birds without fractures. There was no significant effect of carprofen or meloxicam treatment. These data provide further confirmation that keel fractures reduce the willingness of birds to move from perches. © 2014 Association of Veterinary Anaesthetists and the American College of Veterinary Anesthesia and Analgesia.

  10. Effects of β-D-mannuronic acid, as a novel non-steroidal anti-inflammatory medication within immunosuppressive properties, on IL17, RORγt, IL4 and GATA3 gene expressions in rheumatoid arthritis patients

    Directory of Open Access Journals (Sweden)

    Barati A

    2017-03-01

    Full Text Available Anis Barati,1 Ahmad Reza Jamshidi,2,* Hossein Ahmadi,1 Zahra Aghazadeh,1 Abbas Mirshafiey1,* 1Department of Immunology, School of Public Health, 2Iranian Institute for Health Sciences Research, Rheumatology Research Center, Shariati Hospital, Tehran University of Medical Sciences, Tehran, Iran *These authors contributed equally to this work Abstract: Rheumatoid arthritis (RA is the most common form of chronic inflammatory arthritis characterized by pain, swelling and destruction of joints, with a resultant disability. Disease-modifying anti-rheumatic drugs (DMARDs and biological drugs can interfere with the disease process. In this study, the effect of β-D-mannuronic acid (M2000 as a novel non-steroidal anti-inflammatory drug (NSAID with immunosuppressive and anti-inflammatory effects together with antioxidant effects was evaluated on IL17, RORγt, IL4 and GATA3 gene expression in 12 RA patients. Previously, M2000 driven from sodium alginate (natural product; patented, DEU: 102016113018.4 has shown a notable efficacy in experimental models of multiple sclerosis, RA and nephrotic syndrome. This study was performed on 12 patients with RA who had an inadequate response to conventional treatments. During this trial, patients were permitted to continue the conventional therapy excluding NSAIDs. M2000 was administered orally at a dose of 500 mg twice daily for 12 weeks. The peripheral blood mononuclear cells (PBMCs were collected before and after treatment to evaluate the expression levels of IL4, GATA3, IL17 and RORγt. The gene expression results showed that M2000 has a potent efficacy, so that it could not only significantly decrease IL17 and RORγt levels but also increase IL4 and GATA3 levels after 12 weeks of treatment. Moreover, the gene expression results were in accordance with the clinical and preclinical assessments. In conclusion, M2000 as a natural novel agent has therapeutic and immunosuppressive properties on RA patients (identifier

  11. Postscreening follow-up of the Finnish Prostate Cancer Screening Trial on putative prostate cancer risk factors: vitamin and mineral use, male pattern baldness, pubertal development and non-steroidal anti-inflammatory drug use.

    Science.gov (United States)

    Sarre, Sami; Määttänen, Liisa; Tammela, Teuvo L J; Auvinen, Anssi; Murtola, Teemu J

    2016-08-01

    Objective The etiology of prostate cancer (PCa) is still unclear. This study aimed to investigate the association between PCa risk and the indicators of endogenous androgen production at puberty, male pattern baldness, over-the-counter use of non-steroidal anti-inflammatory drugs and vitamin supplement use. Materials and methods Participants in the third round of the Finnish Prostate Cancer Screening Trial were sent a survey on possible PCa risk factors and 11,795 out of 12,740 (93%) men returned the questionnaire. PCa cases were identified from the Finnish Cancer Registry. Results During the median follow-up of 6.6 years, 757 PCa cases were diagnosed and 21 men died from PCa. Compared to earlier onset, puberty onset after 15 years of age was associated with a borderline significant decrease in PCa risk [hazard ratio (HR) 0.87, 95% confidence interval (CI) 0.75-1.00] but not with PCa mortality. Weekly use of ibuprofen was associated with an increased risk of PCa overall (HR 1.43, 95% CI 1.08-1.91) and with metastatic PCa (HR 1.49, 95% CI 1.12-1.99) compared to less frequent use. No statistically significant association was found between vitamin use and PCa. Conclusions This study suggests that the timing of initiation of endogenous androgen production at puberty may have importance for later PCa development. Current use of over-the-counter ibuprofen is associated with an increased risk of PCa. There was no evidence of any protective effects of vitamin use on PCa risk.

  12. Use of non-steroidal anti-inflammatory drugs that elevate cardiovascular risk: an examination of sales and essential medicines lists in low-, middle-, and high-income countries.

    Directory of Open Access Journals (Sweden)

    Patricia McGettigan

    Full Text Available BACKGROUND: Certain non-steroidal anti-inflammatory drugs (NSAIDs (e.g., rofecoxib [Vioxx] increase the risk of heart attack and stroke and should be avoided in patients at high risk of cardiovascular events. Rates of cardiovascular disease are high and rising in many low- and middle-income countries. We studied the extent to which evidence on cardiovascular risk with NSAIDs has translated into guidance and sales in 15 countries. METHODS AND FINDINGS: Data on the relative risk (RR of cardiovascular events with individual NSAIDs were derived from meta-analyses of randomised trials and controlled observational studies. Listing of individual NSAIDs on Essential Medicines Lists (EMLs was obtained from the World Health Organization. NSAID sales or prescription data for 15 low-, middle-, and high-income countries were obtained from Intercontinental Medical Statistics Health (IMS Health or national prescription pricing audit (in the case of England and Canada. Three drugs (rofecoxib, diclofenac, etoricoxib ranked consistently highest in terms of cardiovascular risk compared with nonuse. Naproxen was associated with a low risk. Diclofenac was listed on 74 national EMLs, naproxen on just 27. Rofecoxib use was not documented in any country. Diclofenac and etoricoxib accounted for one-third of total NSAID usage across the 15 countries (median 33.2%, range 14.7-58.7%. This proportion did not vary between low- and high-income countries. Diclofenac was by far the most commonly used NSAID, with a market share close to that of the next three most popular drugs combined. Naproxen had an average market share of less than 10%. CONCLUSIONS: Listing of NSAIDs on national EMLs should take account of cardiovascular risk, with preference given to low risk drugs. Diclofenac has a risk very similar to rofecoxib, which was withdrawn from worldwide markets owing to cardiovascular toxicity. Diclofenac should be removed from EMLs.

  13. Screening procedure for detection of non-steroidal anti-inflammatory drugs and their metabolites in urine as part of a systematic toxicological analysis procedure for acidic drugs and poisons by gas chromatography-mass spectrometry after extractive methylation.

    Science.gov (United States)

    Maurer, H H; Tauvel, F X; Kraemer, T

    2001-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used as analgesic and anti-rheumatic drugs, and they are often misused. A gas chromatographic-mass spectrometric (GC-MS) screening procedure was developed for their detection in urine as part of a systematic toxicological analysis procedure for acidic drugs and poisons after extractive methylation. The compounds were separated by capillary GC and identified by computerized MS in the full-scan mode. Using mass chromatography with the ions m/z 119, 135, 139, 152, 165, 229, 244, 266, 272, and 326, the possible presence of NSAIDs and their metabolites could be indicated. The identity of positive signals in such mass chromatograms was confirmed by comparison of the peaks underlying full mass spectra with the reference spectra recorded during this study. This method allowed the detection of therapeutic concentrations of acemetacin, acetaminophen (paracetamol), acetylsalicylic acid, diclofenac, diflunisal, etodolac, fenbufen, fenoprofen, flufenamic acid, flurbiprofen, ibuprofen, indometacin, kebuzone, ketoprofen, lonazolac, meclofenamic acid, mefenamic acid, mofebutazone, naproxen, niflumic acid, phenylbutazone, suxibuzone, tiaprofenic acid, tolfenamic acid, and tolmetin in urine samples. The overall recoveries of the different NSAIDs ranged between 50 and 80% with coefficients of variation of less than 15% (n = 5), and the limits of detection of the different NSAIDs were between 10 and 50 ng/mL (S/N = 3) in the full-scan mode. Extractive methylation has proved to be a versatile method for STA of various acidic drugs, poisons, and their metabolites in urine. It has also successfully been used for plasma analysis.

  14. A novel therapeutic approach targeting rheumatoid arthritis by combined administration of morin, a dietary flavanol and non-steroidal anti-inflammatory drug indomethacin with reference to pro-inflammatory cytokines, inflammatory enzymes, RANKL and transcription factors.

    Science.gov (United States)

    Sultana, Farhath; Rasool, MahaboobKhan

    2015-03-25

    The present study was designed to assess the combined efficacy of morin, a dietary flavanol and non-steroidal anti-inflammatory drug indomethacin against adjuvant-induced arthritis in rats, an experimental model for rheumatoid arthritis. Arthritis was induced by intradermal injection of complete freund's adjuvant (0.1 ml) into the right hind paw of the Wistar albino rats. Morin (30 mg/kg b.wt), indomethacin (3 mg/kg b.wt) and combination of morin and indomethacin were administered intraperitoneally (from 11th to 20th day) after adjuvant injection. We have found that the activities/levels of lysosomal acid hydrolases (acid phosphatase, β-galactosidase, N-acetyl glucosaminidase and cathepsin-D), glycoproteins (hexose and hexosamine), urinary constituents (hydroxyproline and glycosaminoglycans), reactive oxygen species (LPO and NO), elastase, inflammatory mediators (TNF-α, IL-1β, MCP-1, VEGF and PGE2) and paw edema were significantly increased in arthritic rats compared to controls. Whereas, the anti-oxidant status (SOD, CAT, GPx, glutathione, and ceruloplasmin), body weight and bone collagen was found to be decreased. The mRNA expression of pro-inflammatory cytokines (TNF-α, IL-1β, IL-17, IL-6 and MCP-1), inflammatory enzymes (iNOS and COX-2), RANKL, and transcription factors (NF-kB p65 and AP-1) was found upregulated in the ankle joints of arthritic rats in qRT-PCR analysis. In addition, the increased protein expression of NF-kB p65 and COX-2 was also detected by immunohistochemical analysis. On the other hand, the above said imbalances were regulated back effectively to near normal as evidenced by the histopathological and radiological analysis on combined treatment with morin and indomethacin. Our study indicates that the combination therapy was more effective than either single drug alone in suppressing the pathogenesis of RA. Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.

  15. Concurrent use of diuretics, angiotensin converting enzyme inhibitors, and angiotensin receptor blockers with non-steroidal anti-inflammatory drugs and risk of acute kidney injury: nested case-control study.

    Science.gov (United States)

    Lapi, Francesco; Azoulay, Laurent; Yin, Hui; Nessim, Sharon J; Suissa, Samy

    2013-01-08

    To assess whether a double therapy combination consisting of diuretics, angiotensin converting enzyme inhibitors, or angiotensin receptor blockers with addition of non-steroidal anti-inflammatory drugs (NSAIDs) and the triple therapy combination of two of the aforementioned antihypertensive drugs to which NSAIDs are added are associated with an increased risk of acute kidney injury. Retrospective cohort study using nested case-control analysis. General practices contributing data to the UK Clinical Practice Research Datalink linked to the Hospital Episodes Statistics database. A cohort of 487,372 users of antihypertensive drugs. Rate ratios with 95% confidence intervals of acute kidney injury associated with current use of double and triple therapy combinations of antihypertensive drugs with NSAIDs. During a mean follow-up of 5.9 (SD 3.4) years, 2215 cases of acute kidney injury were identified (incidence rate 7/10,000 person years). Overall, current use of a double therapy combination containing either diuretics or angiotensin converting enzyme inhibitors or angiotensin receptor blockers with NSAIDs was not associated with an increased rate of acute kidney injury. In contrast, current use of a triple therapy combination was associated with an increased rate of acute kidney injury (rate ratio 1.31, 95% confidence interval 1.12 to 1.53). In secondary analyses, the highest risk was observed in the first 30 days of use (rate ratio 1.82, 1.35 to 2.46). A triple therapy combination consisting of diuretics with angiotensin converting enzyme inhibitors or angiotensin receptor blockers and NSAIDs was associated with an increased risk of acute kidney injury. The risk was greatest at the start of treatment. Although antihypertensive drugs have cardiovascular benefits, vigilance may be warranted when they are used concurrently with NSAIDs.

  16. Non-steroidal anti-inflammatory drug use in chronic pain conditions with special emphasis on the elderly and patients with relevant comorbidities: management and mitigation of risks and adverse effects.

    Science.gov (United States)

    Wehling, Martin

    2014-10-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most frequently used drugs, and this widespread use is complicated by safety issues. A Literature review was conducted. NSAIDs are a leading cause of drug-related morbidity, especially in the elderly and patients with comorbidities. Most adverse effects are related to generalized inhibition of the major targets of NSAIDs: cyclooxygenases I and II. These enzymes are not only involved in pain and inflammation pathogenesis but are also required in the gastrointestinal (GI) tract for mucosal protection and gut motility, and in the kidneys for functional integrity. Thus, the mechanisms of NSAID toxicity are well understood, but the consequences are largely uncontrolled in clinical practice. GI ulcers, including bleeding ulcers, may occur in several percent of all chronic unprotected, high-dose NSAID users. Renal side effects may precipitate renal failure, resulting in acute dialysis and chronic retention. This includes sodium retention, resulting in arterial hypertension, heart failure, and atherosclerotic events. Cardiovascular risk may be tripled by chronic high-dose NSAID use in long-term clinical trials though "real-life studies" indicate lower risk ratios. Off-target side effects include allergic reactions, drug-induced liver injury, and central nervous system effects. Management of pain and inflammation must consider those risks and find alternative drugs or approaches to limit the negative impact of NSAIDs on mortality and morbidity. Alternative drugs, low-dose/short-term use, but especially non-pharmacologic approaches, such as physiotherapy, exercise, neurophysiologic measures, and local therapies, need to be further utilized. The appalling equation "less pain-more deaths/morbidity" ultimately necessitates treatment optimization in the individual patient.

  17. The effects of selected drugs, including chlorpromazine and non-steroidal anti-inflammatory agents, on polyclonal IgG synthesis and interleukin 1 production by human peripheral blood mononuclear cells in vitro.

    Science.gov (United States)

    Martinez, F; Coleman, J W

    1989-01-01

    We tested a range of drugs for their effects on in vitro polyclonal IgG synthesis by human peripheral blood mononuclear cells (PBMC) stimulated with the lectin pokeweed mitogen (PWM). The test drugs were selected on the basis of reported disruptive effects on immune function in vivo. IgG production between day 4 and days 7 or 8 of culture was measured by biotin-streptavidin sandwich ELISA. The anti-psychotic agent chlorpromazine (0.55-1.7 microM) enhanced IgG synthesis to approximately double control levels. In contrast, the non-steroidal anti-inflammatory drugs (NSAIDs) indomethacin, piroxicam, ibuprofen and aspirin inhibited IgG synthesis by up to 50%, with a rank order of potency that reflects their activity as inhibitors of cyclo-oxygenase. Phenytoin, procainamide, propylthiouracil, methimazole, D-penicillamine and D-penicillamine-L-cysteine all failed to modulate IgG synthesis at non-toxic concentrations. The potentiation and inhibition of IgG synthesis by chlorpromazine and indomethacin, respectively, was observed only when the drug was present during the first 24 h of culture. Neither chlorpromazine nor indomethacin, at non-toxic concentrations, affected PHA- and PWM-stimulated proliferation of PBMC. In addition, chlorpromazine, indomethacin and piroxicam, at concentrations which produced maximal modulation of IgG synthesis, and D-penicillamine and D-penicillamine-L-cysteine at 10 microM failed to influence production of interleukin-1-like activity. We conclude that chlorpromazine and NSAIDs, although they exert opposite effects on IgG synthesis, act at an early stage of B cell differentiation that appears to be independent of interleukin 1 synthesis and early proliferative events. PMID:2788047

  18. Evaluation of preventive and therapeutic activity of novel non-steroidal anti-inflammatory drug, CG100649, in colon cancer: Increased expression of TNF-related apoptosis-inducing ligand receptors enhance the apoptotic response to combination treatment with TRAIL.

    Science.gov (United States)

    Woo, Jong Kyu; Kang, Ju-Hee; Jang, Yeong-Su; Ro, Seonggu; Cho, Joong Myung; Kim, Hwan-Mook; Lee, Sang-Jin; Oh, Seung Hyun

    2015-04-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) have been suggested as the potential new class of preventive or therapeutic antitumor agents. The aim of the present study was to evaluate the antitumor activity of the novel NSAID, CG100649. CG100649 is a novel NSAID dual inhibitor for COX-2 and carbonic anhydrase (CA)-I/-II. In the present study, we investigated the alternative mechanism by which CG100649 mediated suppression of the colon cancer growth and development. The anchorage‑dependent and -independent clonogenic assay showed that CG100649 inhibited the clonogenicity of human colon cancer cells. The flow cytometric analysis showed that CG100649 induced the G2/M cell cycle arrest in colon cancer cells. Animal studies showed that CG100649 inhibited the tumor growth in colon cancer xenograft in nude mice. Furthermore, quantitative PCR and FACS analysis demonstrated that CG100649 upregulated the expression of TNF-related apoptosis-inducing ligand (TRAIL) receptors (DR4 and DR5) but decreased the expression of decoy receptors (DcR1 and DcR2) in colon cancer cells. The results showed that CG100649 treatment sensitized TRAIL‑mediated growth suppression and apoptotic cell death. The combination treatment resulted in significant repression of the intestinal polyp formation in APCmin/+ mice. Our data clearly demonstrated that CG100649 contains preventive and therapeutic activity for colon cancer. The present study may be useful for identification of the potential benefit of the NSAID CG100649, for the achievement of a better treatment response in colon cancer.

  19. Determination of acidic non-steroidal anti-inflammatory drugs in aquatic samples by liquid chromatography-triple quadrupole mass spectrometry combined with carbon nanotubes-based solid-phase extraction.

    Science.gov (United States)

    Reinholds, I; Pugajeva, I; Zacs, Dz; Lundanes, E; Rusko, J; Perkons, I; Bartkevics, V

    2017-10-18

    A solid-phase extraction (SPE) method based on multi-walled carbon nanotubes (CNT) was developed for the determination of 12 acidic non-steroidal anti-inflammatory drugs (NSAIDs) in surface waters and tap water. Pristine and functionalised CNTs were evaluated as sorbent materials. Batch experiments were used to optimise sorption and desorption conditions (sorbent type and amount, adsorption time, pH). The adsorption equilibrium was reached after 8 to 48 h duration, which increased with the pH of solution. Non-agglomerated pristine CNTs (20 mg) showed the most optimal adsorption (94 to 100%) for all of the analytes after a 30-min contact period in acidified water solutions (100 mL). The compounds retained at those conditions were recovered by 40 to 95% by using 5% ammonium hydroxide in methanol as the desorbing solution at ambient conditions. A comprehensive liquid chromatography coupled to triple quadrupole mass spectrometry (LC-QqQ-MS/MS) was used for the analysis of real water samples. The method showed sufficient recovery (65-125%) and good precision (2-14% relative standard deviation (RSD)). The limits of detection and quantification ranged between 0.01 and 1.3 ng L-1 and 0.04 and 3.9 ng L-1. Only diclofenac and ibuprofen were found in the analysed surface water samples from Latvia (n = 10) and Norway (n = 14). Diclofenac was found at 1.7-8.4 ng L-1 concentration in two samples of surface waters, whereas the concentrations of ibuprofen ranged between 1.0 and 9.2 ng L-1 in seven samples collected in Norway and 3.9-17 ng L-1 in three samples from Latvia.

  20. Effect of different non-steroidal anti-inflammatory drugs, aspirin, nimesulide and celecoxib on the disaccharide hydrolases and histoarchitecture of the rat intestinal brush border membrane Efecto de diferentes fármacos anti-inflamatorios no esteroideos, aspirina, nimesulida y celecoxib, sobre las hidrolasas de disacárido y la histo-arquitectura de la membrana del borde en cepillo intestinal de la rata

    OpenAIRE

    N. Sood; N. Kaushal; S. N. Sanyal

    2008-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are known to cause gastrointestinal damage. New anti-inflammatory drugs have been developed in an attemptto improve their gastrointestinal side effect profile which however failed to do so. Therefore, the objective of the present study was to compare the effect of three different NSAIDs, aspirin, nimesulide and celecoxib on the intestinal brush border membrane (BBM) marker enzymes and correlate these alterations to the histoarchtecture of the int...

  1. Enhancement of antinociception by coadminstration of minocycline and a non-steroidal anti-inflammatory drug indomethacin in naïve mice and murine models of LPS-induced thermal hyperalgesia and monoarthritis

    Directory of Open Access Journals (Sweden)

    Masocha Willias

    2010-12-01

    Full Text Available Abstract Background Minocycline and a non-steroidal anti-inflammatory drug (NSAID indomethacin, have anti-inflammatory activities and are both used in the management of rheumatoid arthritis. However, there are no reports on whether coadministration of these drugs could potentiate each other's activities in alleviating pain and weight bearing deficits during arthritis. Methods LPS was injected to BALB/c mice intraperitoneally (i.p. to induce thermal hyperalgesia. The hot plate test was used to study thermal nociception in naïve BALB/c and C57BL/6 mice and BALB/c mice with LPS-induced thermal hyperalgesia and to evaluate antinociceptive effects of drugs administered i.p. Monoarthritis was induced by injection of LPS intra-articularly into the right hind (RH limb ankle joint of C57BL/6 mice. Weight bearing changes and the effect of i.p. drug administration were analyzed in freely moving mice using the video-based CatWalk gait analysis system. Results In naïve mice indomethacin (5 to 50 mg/kg had no significant activity, minocycline (25 to 100 mg/kg produced hyperalgesia to thermal nociception, however, coadministration of minocycline 50 mg/kg with indomethacin 5 or 10 mg/kg produced significant antinociceptive effects in the hot plate test. A selective inhibitor of COX-1, FR122047 (10 mg/kg and a selective COX-2 inhibitor, CAY10404 (10 mg/kg had no significant antinociceptive activities to thermal nociception in naïve mice, however, coadministration of minocycline, with CAY10404 but not FR122047 produced significant antinociceptive effects. In mice with LPS-induced hyperalgesia vehicle, indomethacin (10 mg/kg or minocycline (50 mg/kg did not produce significant changes, however, coadministration of minocycline plus indomethacin resulted in antinociceptive activity. LPS-induced RH limb monoarthritis resulted in weight bearing (RH/left hind (LH limb paw pressure ratios and RH/LH print area ratios deficits. Treatment with indomethacin (1 mg/kg or

  2. Enhancement of antinociception by coadminstration of minocycline and a non-steroidal anti-inflammatory drug indomethacin in naïve mice and murine models of LPS-induced thermal hyperalgesia and monoarthritis

    Science.gov (United States)

    2010-01-01

    Background Minocycline and a non-steroidal anti-inflammatory drug (NSAID) indomethacin, have anti-inflammatory activities and are both used in the management of rheumatoid arthritis. However, there are no reports on whether coadministration of these drugs could potentiate each other's activities in alleviating pain and weight bearing deficits during arthritis. Methods LPS was injected to BALB/c mice intraperitoneally (i.p.) to induce thermal hyperalgesia. The hot plate test was used to study thermal nociception in naïve BALB/c and C57BL/6 mice and BALB/c mice with LPS-induced thermal hyperalgesia and to evaluate antinociceptive effects of drugs administered i.p. Monoarthritis was induced by injection of LPS intra-articularly into the right hind (RH) limb ankle joint of C57BL/6 mice. Weight bearing changes and the effect of i.p. drug administration were analyzed in freely moving mice using the video-based CatWalk gait analysis system. Results In naïve mice indomethacin (5 to 50 mg/kg) had no significant activity, minocycline (25 to 100 mg/kg) produced hyperalgesia to thermal nociception, however, coadministration of minocycline 50 mg/kg with indomethacin 5 or 10 mg/kg produced significant antinociceptive effects in the hot plate test. A selective inhibitor of COX-1, FR122047 (10 mg/kg) and a selective COX-2 inhibitor, CAY10404 (10 mg/kg) had no significant antinociceptive activities to thermal nociception in naïve mice, however, coadministration of minocycline, with CAY10404 but not FR122047 produced significant antinociceptive effects. In mice with LPS-induced hyperalgesia vehicle, indomethacin (10 mg/kg) or minocycline (50 mg/kg) did not produce significant changes, however, coadministration of minocycline plus indomethacin resulted in antinociceptive activity. LPS-induced RH limb monoarthritis resulted in weight bearing (RH/left hind (LH) limb paw pressure ratios) and RH/LH print area ratios deficits. Treatment with indomethacin (1 mg/kg) or minocycline (50 mg

  3. Online eluent-switching technique coupled anion-exchange liquid chromatography–ion trap tandem mass spectrometry for analysis of non-steroidal anti-inflammatory drugs in pig serum.

    Science.gov (United States)

    Chang, Kai Chun; Lin, Jyh Shiun; Cheng, Cheanyeh

    2015-11-27

    A novel method for online extraction, pH-gradient separation, and analysis of nine non-steroidal anti-inflammatory drugs (NSAIDs) was developed by coupling online eluent-switching technique to single anion-exchange chromatographic column/ion trap mass spectrometer (MS) and used for monitoring NSAIDs residues in pig serum. A neutral eluent and a pH-gradient eluent were used for extraction and separation of NSAIDs, respectively. Each of nine NSAIDs has an MS precursor ion of either [M−H]− or [M−Na]−. The extracted ion chromatogram for a specific product ion of each NSAID was used for its quantitative analysis. The dynamic linear ranges of calibration curves were all 0–200 ng mL−1 (R2 > 0.9950). The analysis accuracies estimated by spiking standard concentrations at 20, 100, and 200 ng mL−1 were 80.5–99.9%. The corresponding intra-day and inter-day precisions (RSD%) were 2.5–14.5% and 2.9–15.2%, respectively. The limit of detection/limit of quantitation of NSAIDs were 1.3/4.3, 0.5/1.6, 0.2/0.5, 2.5/8.2, 1.5/4.9, 0.6/2.1, 0.6/2.0, 0.5/1.7, and 0.6/2.1 ng mL−1 for carprofen, diclofenac, flunixin, ibuprofen, ketoprofen, meclofenamic acid sodium, mefenamic acid, niflumic acid, and tolfenamic acid, respectively. After 1 h injection of a dose containing 2 mg kg−1 weight pig of flunixin and tolfenamic acid to the pigs, a residue amount of 3480 ± 36 ng mL−1 and 431 ± 13 ng mL−1, respectively, was reached for the incurred pig serum specimens and both residues were reduced to about 20 ng mL−1 at the time of 24 h.

  4. Effects of glucosamine sulfate on the use of rescue non-steroidal anti-inflammatory drugs in knee osteoarthritis: Results from the Pharmaco-Epidemiology of GonArthroSis (PEGASus) study.

    Science.gov (United States)

    Rovati, Lucio C; Girolami, Federica; D'Amato, Massimo; Giacovelli, Giampaolo

    2016-02-01

    The use of Symptomatic Slow-Acting Drugs in Osteoarthritis (SYSADOAs) may be expected to decrease the use of concomitant medications for rescue analgesia, including non-steroidal anti-inflammatory drugs (NSAIDs). The Pharmaco-Epidemiology of GonArthroSis (PEGASus) study was designed to assess this possibility. PEGASus was a cohort study of continuous recruitment of patients with "dynamic" exposure to the investigated SYSADOA (crystalline glucosamine sulfate, glucosamine hydrochloride, chondroitin sulfate, diacerein, and avocado-soybean unsaponifiables, all at approved dosages). Investigators were rheumatologists or general practitioners randomly selected from French telephone lists. Patients diagnosed with knee osteoarthritis (OA) were recruited when consulting an investigator for a symptom flare and were prescribed, or not, one of the SYSADOAs as per clinical judgment. Follow-up visits were as per routine medical practice in the 12 months following enrollment, with telephone interviews after 1 month and at 4-month intervals thereafter up to 24 months. Use of NSAIDs was recorded, as well as the dynamism of treatment exposure consisting of continuing the prescribed SYSADOA, switching, discontinuation or initiation of a SYSADOA. Patient exposure was expressed in 2-month time units, with any NSAID use as Yes/No binary outcome during each unit. Odds ratios [OR and 95% confidence interval (CI)] of NSAID use were calculated for periods of exposure to each SYSADOA, by multivariate logistic regression for an 80% power and 95% confidence to see a decrease of at least 15%. This report consists of the full data pertaining to crystalline glucosamine sulfate, while results of other SYSADOAs were summarized as available from the French Health Authority (HAS) website (www.has-sante.fr). Of 6451 patients in the PEGASus cohort, 315 patients received crystalline glucosamine sulfate, they were exposed for 481 2-month time units and had an incident use of NSAIDs of 18.7%. In the

  5. Simultaneous analysis of non-steroidal anti-inflammatory drugs and estrogenic hormones in water and wastewater samples using gas chromatography-mass spectrometry and gas chromatography with electron capture detection

    Energy Technology Data Exchange (ETDEWEB)

    Migowska, Natalia; Caban, Magda; Stepnowski, Piotr; Kumirska, Jolanta, E-mail: kumirska@chem.univ.gda.pl

    2012-12-15

    Non-steroidal anti-inflammatory drugs are the group of pharmaceuticals that is most often found in the environment, whereas estrogenic hormones are considered to be potent endocrine disruptors. However, the fate and persistence of these compounds in the environment are still unclear. In this study we propose two approaches for determining these compounds in environmental water samples: GC-MS using time windows and operating in selected ion-monitoring mode (SIM) and, for the first time, gas chromatography with electron capture detection (GC-ECD). The identification criteria of both methods fulfilled the requirements of Directive 2002/657/EC. The use of time windows improved the sensitivity of GC-MS measurements. In GC-MS analysis the pharmaceuticals were determined as trimethylsilyl, in GC-ECD as pentafluoropropionyl derivatives. The influence of such parameters as the type of reagent, type of solvent, reaction time, reaction temperature and microwave irradiation in a household microwave oven on the efficacy of silylation was investigated. Derivatization using N,O-bis(trimethylsilyl)trifluoroacetamide (BSTFA) and 1% trimethylchlorosilane (TMCS) in pyridine (1:1, v/v) for 30 min in 60 Degree-Sign C was found to be optimal. Optimization of the solid phase extraction procedure (SPE) confirmed that the application of Oasis HLB cartridges, the acidification of loading samples to pH 2 and the use of methanol as eluent gave the best absolute recoveries (ARs) of the target compounds. The following ARs of all the compounds were achieved: 58.2-106.8% in influent wastewater, 77.8-103.4% in effluent wastewater and 81.2-101.9% in surface water samples. Validation of the SPE-GC-MS method enables 13 pharmaceuticals to be determined with MDLs between 3.3 and 343.6 ng/L, depending on the analytes and matrices. GC-ECD analysis enables the determination of 6 pharmaceuticals in surface water samples with MDLs between 0.7 and 5.4 ng/L. The proposed methods were successfully used for

  6. Safety and efficacy of long-term esomeprazole 20 mg in Japanese patients with a history of peptic ulcer receiving daily non-steroidal anti-inflammatory drugs

    Science.gov (United States)

    2013-01-01

    Background Non-steroidal anti-inflammatory drugs (NSAIDs) are an effective and common treatment for chronic pain disorders, but long-term use is associated with risk of potentially life-threatening gastrointestinal adverse events (AEs). The proton pump inhibitor esomeprazole has been found to be effective for gastroprotection in NSAID users, but few long-term studies have been conducted in Japan. Methods This was an open-label, multicentre, single-arm, prospective 1-year study of treatment with esomeprazole (20 mg once daily) in Japanese patients (aged ≥20 years) with endoscopic evidence of previous peptic ulcer and receiving daily oral NSAID therapy (at a stable dose) for a chronic condition. Eligibility was not dictated by type of oral NSAID. The primary objective was to determine long-term safety and tolerability of esomeprazole. Efficacy for prevention of peptic ulcers was also determined (Kaplan-Meier method). All statistical analyses were descriptive. Results A total of 130 patients (73.1% women, mean age 62.1 years, 43.8% Helicobacter pylori-positive) received treatment with esomeprazole in addition to long-term NSAID therapy (most commonly for rheumatoid arthritis [n=42] and osteoarthritis [n=34]). Loxoprofen, meloxicam and diclofenac were the most commonly used NSAIDs; cyclo-oxygenase (COX)-2 selective agents were used by 16.2% of patients (n=21). Long-term compliance with esomeprazole (capsule counts) was >75% for the majority of patients. Although 16.9% of patients (n=22) experienced AEs judged to be possibly related to treatment with esomeprazole, they were mostly mild and transient. The most commonly reported possibly treatment-related AEs were abnormal hepatic function, headache, increased γ-glutamyltransferase levels and muscle spasms (2 patients each). Overall, 95.9% (95% confidence interval: 92.3, 99.4) of patients remained ulcer free at 1 year. Conclusion Long-term treatment with esomeprazole (20 mg once daily) is well tolerated and

  7. Use of Fixed Dose Combination (FDC Drugs in India: Central Regulatory Approval and Sales of FDCs Containing Non-Steroidal Anti-Inflammatory Drugs (NSAIDs, Metformin, or Psychotropic Drugs.

    Directory of Open Access Journals (Sweden)

    Patricia McGettigan

    2015-05-01

    Full Text Available In 2012, an Indian parliamentary committee reported that manufacturing licenses for large numbers of fixed dose combination (FDC drugs had been issued by state authorities without prior approval of the Central Drugs Standard Control Organization (CDSCO in violation of rules, and considered that some ambiguity until 1 May 2002 about states' powers might have contributed. To our knowledge, no systematic enquiry has been undertaken to determine if evidence existed to support these findings. We investigated CDSCO approvals for and availability of oral FDC drugs in four therapeutic areas: analgesia (non-steroidal anti-inflammatory drugs [NSAIDs], diabetes (metformin, depression/anxiety (anti-depressants/benzodiazepines, and psychosis (anti-psychotics.This was an ecologic study with a time-trend analysis of FDC sales volumes (2007-2012 and a cross-sectional examination of 2011-2012 data to establish the numbers of formulations on the market with and without a record of CDSCO approval ("approved" and "unapproved", their branded products, and sales volumes. Data from the CDSCO on approved FDC formulations were compared with sales data from PharmaTrac, a database of national drug sales. We determined the proportions of FDC sales volumes (2011-2012 arising from centrally approved and unapproved formulations and from formulations including drugs banned/restricted internationally. We also determined the proportions of centrally approved and unapproved formulations marketed before and after 1 May 2002, when amendments were made to the drug rules. FDC approvals in India, the United Kingdom (UK, and United States of America (US were compared. For NSAID FDCs, 124 formulations were marketed, of which 34 (27% were centrally approved and 90 (73% were unapproved; metformin: 25 formulations, 20 (80% approved, five (20% unapproved; anti-depressants/benzodiazepines: 16 formulations, three (19% approved, 13 (81% unapproved; anti-psychotics: ten formulations, three (30

  8. Gastrointestinal mucosal injury following repeated daily oral administration of conventional formulations of indometacin and other non-steroidal anti-inflammatory drugs to pigs: a model for human gastrointestinal disease.

    Science.gov (United States)

    Rainsford, K D; Stetsko, P I; Sirko, S P; Debski, S

    2003-05-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) vary in their propensity to cause damage in different regions of the gastrointestinal (GI) tract in laboratory animals and humans. This may depend on the type of drug formulation as well as the intrinsic pharmacological properties of the drugs. The purpose of this study was to determine the effects of NSAIDs, with cyclooxygenase 1 and 2 inhibitory activity but with different potency as inhibitors of prostaglandin production, when given orally as tablet/capsule formulations of NSAIDs for 10 days to pigs, a species that has close resemblance in structure and function of the tract to that in humans. Three capsule or tablet formulations of NSAIDs were given orally to pigs for 10 days. GI bleeding was measured by determination of radioactive iron in the faeces from (59)Fe-pre-labelled red blood cells. The blood loss was compared with the pathological changes in the GI mucosa observed at autopsy, mucosal myeloperoxidase (MPO) activity as an index of leucocyte infiltration, and plasma and mucosal concentrations of the drugs at termination assayed by high-performance liquid chromatography. Mucosal damage and bleeding varied according to the type of NSAID. Gastroduodenal ulcers and lesions occurred with the cyclooxygenase inhibitors indometacin (indomethacin) (Indocid capsules 10 or 5 mg kg(-1) day(-1) b.i.d.), aspirin (USP tablets 150 mg kg(-1) day(-1) b.i.d) and naproxen (Apotex tablets 50 or 75 mg kg(-1) day(-1) b.i.d.), and there was an increase in the cumulative (i.e. 10-day) blood loss at higher doses of indometacin and naproxen, and with aspirin. There was no statistically significant increase in gastric or intestinal mucosal MPO activity in the non-damaged mucosa with these drugs and this was confirmed by histological observations in non-lesioned areas of the mucosa. Indometacin produced focal ulcers in the caecum but this was not observed with the other drugs. All the NSAIDs produced significant blood loss coincident

  9. Safety of non-steroidal anti-inflammatory drugs, including aspirin and paracetamol (acetaminophen) in people receiving methotrexate for inflammatory arthritis (rheumatoid arthritis, ankylosing spondylitis, psoriatic arthritis, other spondyloarthritis).

    Science.gov (United States)

    Colebatch, Alexandra N; Marks, Jonathan L; Edwards, Christopher J

    2011-11-09

    Methotrexate is routinely used in the treatment of inflammatory arthritis. There have been concerns regarding the safety of using concurrent non-steroidal anti-inflammatory drugs (NSAIDs), including aspirin, or paracetamol (acetaminophen), or both, in these people. To systematically appraise and summarise the scientific evidence on the safety of using NSAIDs, including aspirin, or paracetamol, or both, with methotrexate in inflammatory arthritis; and to identify gaps in the current evidence, assess the implications of those gaps and to make recommendations for future research to address these deficiencies. We searched the Cochrane Central Register of Controlled Trials (CENTRAL) (The Cochrane Library, second quarter 2010); MEDLINE (from 1950); EMBASE (from 1980); the Cochrane Database of Systematic Reviews (CDSR) and the Database of Abstracts of Reviews of Effects (DARE). We also handsearched the conference proceedings for the American College of Rheumatology (ACR) and European League against Rheumatism (EULAR) (2008 to 2009) and checked the websites of regulatory agencies for reported adverse events, labels and warnings. Randomised controlled trials and non-randomised studies comparing the safety of methotrexate alone to methotrexate with concurrent NSAIDs, including aspirin, or paracetamol, or both, in people with inflammatory arthritis. Two authors independently assessed the search results, extracted data and assessed the risk of bias of the included studies. Seventeen publications out of 8681 identified studies were included in the review, all of which included people with rheumatoid arthritis using various NSAIDs, including aspirin. There were no identified studies for other forms of inflammatory arthritis.For NSAIDs, 13 studies were included that used concurrent NSAIDs, of which nine studies examined unspecified NSAIDs. The mean number of participants was 150.4 (range 19 to 315), mean duration 2182.9 (range 183 to 5490) days, although the study duration was

  10. ANTI-INFLAMMATORY EFFECT OF Myrtus nivellei Batt & Trab ...

    African Journals Online (AJOL)

    2015-01-15

    inflammatoy activity; Myrtus nivellei ... EXTRACTION AND SAMPLE PREPARATION. Ground samples of Myrtus nivellei were .... [1] Mahdi EJ. Aspirin and its related non-steroidal anti-inflammatory drugs. Libyan Journal of. Medecine.

  11. Synthesis and anti-inflammatory evaluation of novel thiadiazol ...

    African Journals Online (AJOL)

    In the search for new potential non-steroidal anti-inflammatory agents, some novel Mefenamic acid derivatives were synthesized and confirmed by spectroscopic data. The anti-inflammatory activities of these compounds were evaluated by the croton oil-induced ear oedema test in mice. The preliminary pharmacological ...

  12. Investigation of the anti-inflammatory and anti- nociceptive activities ...

    African Journals Online (AJOL)

    PRECIOUS

    2009-06-15

    Jun 15, 2009 ... by non-steroidal anti-inflammatory drugs (NSAID), tole- rance and dependence induced by opiates, use of these drugs as anti-inflammatory and anti-nociceptive agents. *Corresponding author. E-mail: pmasika@ufh.ac.za. Fax: +27. 40 6022583. have not been successful in all cases (Adedapo et al.,. 2008).

  13. A cluster randomised stepped wedge trial to evaluate the effectiveness of a multifaceted information technology-based intervention in reducing high-risk prescribing of non-steroidal anti-inflammatory drugs and antiplatelets in primary medical care: The DQIP study protocol

    Directory of Open Access Journals (Sweden)

    Dreischulte Tobias

    2012-03-01

    Full Text Available Abstract Background High-risk prescribing of non-steroidal anti-inflammatory drugs (NSAIDs and antiplatelet agents accounts for a significant proportion of hospital admissions due to preventable adverse drug events. The recently completed PINCER trial has demonstrated that a one-off pharmacist-led information technology (IT-based intervention can significantly reduce high-risk prescribing in primary care, but there is evidence that effects decrease over time and employing additional pharmacists to facilitate change may not be sustainable. Methods/design We will conduct a cluster randomised controlled with a stepped wedge design in 40 volunteer general practices in two Scottish health boards. Eligible practices are those that are using the INPS Vision clinical IT system, and have agreed to have relevant medication-related data to be automatically extracted from their electronic medical records. All practices (clusters that agree to take part will receive the data-driven quality improvement in primary care (DQIP intervention, but will be randomised to one of 10 start dates. The DQIP intervention has three components: a web-based informatics tool that provides weekly updated feedback of targeted prescribing at practice level, prompts the review of individual patients affected, and summarises each patient's relevant risk factors and prescribing; an outreach visit providing education on targeted prescribing and training in the use of the informatics tool; and a fixed payment of 350 GBP (560 USD; 403 EUR up front and a small payment of 15 GBP (24 USD; 17 EUR for each patient reviewed in the 12 months of the intervention. We hypothesise that the DQIP intervention will reduce a composite of nine previously validated measures of high-risk prescribing. Due to the nature of the intervention, it is not possible to blind practices, the core research team, or the data analyst. However, outcome assessment is entirely objective and automated. There will

  14. Desensitization to acetyl-salicylic acid as a treatment for non-steroid anti-inflammatory drugs (NSAIDs-exacerbated respiratory disease = Desensibilización al ácido acetil-salicílico como tratamiento para la enfermedad respiratoria exacerbada por antiinflamatorios no esteroides

    Directory of Open Access Journals (Sweden)

    Cardona Villa, Ricardo

    2014-07-01

    Full Text Available Desensitization to acetyl-salicylic acid as a treatment for non-steroid anti-inflammatory drugs (NSAIDs-exacerbated respiratory disease The coexistence of hypersensitivity to acetylsalicylic acid (ASA and other NSAIDs with disease of the upper or the lower airways (rhinosinusitis/sinonasal polyposis, or asthma is defined as NSAIDs-exacerbated respiratory disease. Treatment options include the avoidance of all analgesics that inhibit COX-1 or ASA desensitization, continuing its daily consumption. The latter treatment has shown to improve quality of life, reduce the formation of sinonasal polyps, the episodes of sinus infection, the frequency of hospitalizations and surgeries for resection of polyps and the need for systemic steroid treatment. Multiple desensitization schedules have been used, trying to reduce the risk associated with the procedure and the adverse effects of chronic use of ASA. In this paper we present a review of the different methods of desensitization and two illustrative clinical cases to help understand the factors that influence the choice of treatment for these patients.

  15. Are non-steroidal anti-inflammatory drugs effective for the management of neck pain and associated disorders, whiplash-associated disorders, or non-specific low back pain? A systematic review of systematic reviews by the Ontario Protocol for Traffic Injury Management (OPTIMa) Collaboration.

    Science.gov (United States)

    Wong, Jessica J; Côté, Pierre; Ameis, Arthur; Varatharajan, Sharanya; Varatharajan, Thepikaa; Shearer, Heather M; Brison, Robert J; Sutton, Deborah; Randhawa, Kristi; Yu, Hainan; Southerst, Danielle; Goldgrub, Rachel; Mior, Silvano; Stupar, Maja; Carroll, Linda J; Taylor-Vaisey, Anne

    2016-01-01

    To evaluate the effectiveness of non-steroidal anti-inflammatory drugs (NSAIDs) for the management of neck pain and associated disorders (NAD), whiplash-associated disorders, and non-specific low back pain (LBP) with or without radiculopathy. We systematically searched six databases from 2000 to 2014. Random pairs of independent reviewers critically appraised eligible systematic reviews using the Scottish Intercollegiate Guidelines Network criteria. We included systematic reviews with a low risk of bias in our best evidence synthesis. We screened 706 citations and 14 systematic reviews were eligible for critical appraisal. Eight systematic reviews had a low risk of bias. For recent-onset NAD, evidence suggests that intramuscular NSAIDs lead to similar outcomes as combined manipulation and soft tissue therapy. For NAD (duration not specified), oral NSAIDs may be more effective than placebo. For recent-onset LBP, evidence suggests that: (1) oral NSAIDs lead to similar outcomes to placebo or a muscle relaxant; and (2) oral NSAIDs with bed rest lead to similar outcomes as placebo with bed rest. For persistent LBP, evidence suggests that: (1) oral NSAIDs are more effective than placebo; and (2) oral NSAIDs may be more effective than acetaminophen. For recent-onset LBP with radiculopathy, there is inconsistent evidence on the effectiveness of oral NSAIDs versus placebo. Finally, different oral NSAIDs lead to similar outcomes for neck and LBP with or without radiculopathy. For NAD, oral NSAIDs may be more effective than placebo. Oral NSAIDs are more effective than placebo for persistent LBP, but not for recent-onset LBP. Different oral NSAIDs lead to similar outcomes for neck pain and LBP.

  16. Non-steroidal anti- inflammatory drugs: facts and fallacies

    African Journals Online (AJOL)

    Repro

    NSAIDs), in particular aspirin, act through the inhibition of prostaglandin synthesis. The ubiquitous nature of prostaglandins and the discovery of their physiological properties led to the deci- phering of the mysteries of common symptoms such as ...

  17. Non-Steroidal Anti Inflammatory Drugs Usage In Orthopaedics And ...

    African Journals Online (AJOL)

    The abuses stem mostly from poor prescription abit by the health professionals. he poor prescription habit by the professionals and aissez-a-faire attitude to NSAID Usage informed the need this review which addresses the issues, controversies and preventive strategies to reduce the complications in Orthopedics/Trauma ...

  18. Hypersensitivities to non-steroidal anti-inflammatory drugs.

    Science.gov (United States)

    Mourad, Ahmad A; Bahna, Sami L

    2014-09-01

    NSAIDs are the most commonly used medications worldwide and are responsible for almost 25% of adverse drug reactions. Such reactions can have different manifestations and can be immunologic or non-immunologic. The diagnosis is primarily based on the medical history, which can be difficult in patients receiving multiple medications. Because skin testing and blood tests are not valid for NSAIDs reactions, confirmation requires an appropriately-designed challenge. The latter could be avoided when the history is obvious and the reaction is life-threatening. The challenge route can be oral, nasal, or bronchial. Avoidance of the causative NSAID, often associated with the avoidance of the cross-reacting preparations, is the cornerstone of management. In most cases, a safe substitute can be used. When treatment with the causative NSAID is necessary, titrated desensitization can be performed. This review discusses the classes of NSAIDs, mechanisms of their adverse reactions, manifestations, diagnosis, and management.

  19. Non-steroidal anti-inflammatory drugs for acute gout

    NARCIS (Netherlands)

    van Durme, Caroline M. P. G.; Wechalekar, Mihir D.; Buchbinder, Rachelle; Schlesinger, Naomi; van der Heijde, Désirée; Landewé, Robert B. M.

    2014-01-01

    Background Gout is an inflammatory arthritis that is characterised by the deposition of monosodium urate crystals in synovial fluid and other tissues. The natural history of articular gout is generally characterised by three periods: asymptomatic hyperuricaemia, episodes of acute gout and chronic

  20. PRODRUGS OF NON- STEROID ANTI - INFLAMMATORY AGENTS (NSAIDS)

    DEFF Research Database (Denmark)

    2013-01-01

    The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic p...

  1. Evaluation of the Effect of a Single Intra-articular Injection of Allogeneic Neonatal Mesenchymal Stromal Cells Compared to Oral Non-Steroidal Anti-inflammatory Treatment on the Postoperative Musculoskeletal Status and Gait of Dogs over a 6-Month Period after Tibial Plateau Leveling Osteotomy: A Pilot Study

    Directory of Open Access Journals (Sweden)

    Mathieu Taroni

    2017-06-01

    Full Text Available ObjectiveCompare the clinical and pressure walkway gait evolution of dogs after a tibial plateau leveling osteotomy (TPLO for a cranial cruciate ligament rupture (CrCLR and treatment with either a 1-month course of non-steroidal anti-inflammatory drugs (NSAIDs or a single postoperative intra-articular (IA injection of allogeneic neonatal mesenchymal stromal cells (MSCs.Study designProspective, double-blinded, randomized, controlled, monocentric clinical study.AnimalsSixteen client-owned dogs.Materials and methodsDogs with unilateral CrCLR confirmed by arthroscopy were included. Allogeneic neonatal canine MSCs were obtained from fetal adnexa retrieved after C-section performed on healthy pregnant bitches. The dogs were randomly allocated to either the “MSCs group,” receiving an IA injection of MSCs after TPLO, followed by placebo for 1 month, or the “NSAIDs group,” receiving IA equivalent volume of MSCs vehicle after TPLO, followed by oral NSAID for 1 month. One of the three blinded evaluators assessed the dogs in each group before and after surgery (1, 3, and 6 months. Clinical score and gait and bone healing process were assessed. The data were statistically compared between the two groups for pre- and postoperative evaluations.ResultsFourteen dogs (nine in the MSCs group, five in the NSAIDs group completed the present study. No significant difference was observed between the groups preoperatively. No local or systemic adverse effect was observed after MSCs injection at any time point considered. At 1 month after surgery, bone healing scores were significantly higher in the MSCs group. At 1, 3, and 6 months after surgery, no significant difference was observed between the two groups for clinical scores and gait evaluation.ConclusionA single IA injection of allogeneic neonatal MSCs could be a safe and valuable postoperative alternative to NSAIDs for dogs requiring TPLO surgery, particularly for dogs intolerant to this class of

  2. Non-steroidal antiinflammatory drugs fail to enhance healing of ...

    African Journals Online (AJOL)

    The effects of two non-steroidal anti-inflammatory drugs (NSAIDs), meclofenamate and diclofenac, in combination with physiotherapy modalities on the rate of healing of acute hamstring muscle tears were studied in a doubleblind, placebo-controlled trial. Forty-four of the 75 patients with this injury recruited were assessed ...

  3. PRELIMINARY PHYTOCHEMICAL AND ANTI-INFLAMMATORY ACTIVITY OF BARK OF COMMIPHORA BERRYI (ARN) ENGLOR

    Science.gov (United States)

    Mainvannan, R.; Jawahar, N.; Ganesh, E. Sai; Manivannan, C. Jothi; Judie, S.

    2004-01-01

    Various extracts (Petroleum ether, Benzene, Chloroform and Methanol) of Commiphora Berryi (Arn) Englor were subjected to preliminary phytochemical evaluation and it was shown that same extracts were evaluated for its anti-inflammatory activity against carrageenin induced rat paw oedema. Diclofenac sodium (30mg/kg), a non-steroidal anti-inflammatory agent was used as a standard drug for comparison. PMID:22557152

  4. Study of anti-inflammatory, anti-diabetic, and analgesic activity of ...

    African Journals Online (AJOL)

    The aqueous extract of the cyanobacterium Oscillatoria annae was investigated for its anti-inflammatory, anti-diabetic,analgesic and cholesterol regulating properties in different experimental standard animal models. The non-steroidal anti-inflammatory drug, indomethacin (10 mg/kg/body weight) was used as standard in ...

  5. Efeito do uso profilático do anti-inflamatório não-esteroide ibuprofeno sobre o desempenho em uma sessão de treino de força Effects of prophylactic anti-inflammatory non-steroidal ibuprofen on performance in a session of strength training

    Directory of Open Access Journals (Sweden)

    Cleiton Silva Correa

    2013-04-01

    Full Text Available INTRODUÇÃO: Medicamentos anti-inflamatórios não esteroides, como o ibuprofeno, têm sido utilizados por atletas de várias modalidades com o intuito de aumentar desempenho esportivo. OBJETIVO: Verificar o efeito do uso profilático de ibuprofeno sobre desempenho em uma sessão de treino de força. MÉTODOS: Um ensaio clínico, cruzado, randomizado, duplo-cego e placebo-controlado foi desenvolvido com 12 praticantes regulares de treino de força do sexo masculino, os quais realizaram uma sessão de treino após a ingestão de ibuprofeno (1,2 g e uma outra após a ingestão de placebo. Seis séries dos exercícios supino e agachamento foram realizadas em cada sessão de treino com uma carga constante correspondente a 65% da 1RM de cada exercício. O desempenho no treinamento foi mensurado através do número de repetições que os voluntários conseguiram realizar em cada série de exercício a cada sessão de treino de força. RESULTADOS: Não foram verificadas diferenças significativas de desempenho no treino de força com a administração prévia de placebo ou ibuprofeno (p > 0,05. CONCLUSÃO: A ingestão de ibuprofeno nos parâmetros de administração adotados pelo presente estudo não promove qualquer tipo de alteração na tolerância ao exercício em uma sessão isolada de treino de força, o que contraria a indicação dessa substância para fins ergogênicos no treino de força.INTRODUCTION: Non-steroidal anti-inflammatory drugs, such as ibuprofen, have been used by athletes of several sports modalities in order to increase athletic performance. OBJECTIVE: To verify the effect of the prophylactic use of ibuprofen on performance in a strength training session. METHODS: A crossover, randomized, double-blind and placebo-controlled clinical assay was developed with twelve male regular practitioners of strength training who performed one strength training session after ibuprofen (1.2 g ingestion and another session after placebo

  6. Cause-Specific Cardiovascular Risk Associated with Nonsteroidal Anti-Inflammatory Drugs among Myocardial Infarction Patients - A Nationwide Study

    DEFF Research Database (Denmark)

    Olsen, Anne-Marie Schjerning; Fosbøl, Emil L; Lindhardsen, Jesper

    2013-01-01

    Non steroidal anti-inflammatory drugs (NSAIDs) increase mortality and morbidity after myocardial infarction (MI). We examined cause-specific mortality and morbidity associated with NSAIDs in a nationwide cohort of MI patients.......Non steroidal anti-inflammatory drugs (NSAIDs) increase mortality and morbidity after myocardial infarction (MI). We examined cause-specific mortality and morbidity associated with NSAIDs in a nationwide cohort of MI patients....

  7. Pharmacological interactions of anti-inflammatory-analgesics in odontology

    OpenAIRE

    Gómez Moreno, Gerardo; Guardia Muñoz, Javier; Cutando Soriano, Antonio; Calvo Guirado, José Luis

    2009-01-01

    In this second article we describe the more interesting pharmacological interactions in dental practice based on the prescription of analgesic narcotics, paracetamol and non-selective non-steroid anti-inflammatory drugs (NSAI) (which inhibit cyclooxigenase 1 ?COX 1- and cyclooxigenase 2 ?COX 2-) and selective NSAIs (COX 2 inhibitors). The importance of preventing the appearance of these pharmacological interactions is because these are medicaments prescribed daily in odontology for modera...

  8. [The role of cellular mediators in the development of the phenomenon of inhibition induced by barium sulfate luminol-dependent chemiluminescence of blood under the influence of non-steroidal anti-inflammatory drugs in patients with intolerance to these drugs].

    Science.gov (United States)

    Chausova, S V; Gurevich, K G; Bondareva, G P; Filatov, O Ju; Malyshev, I Y

    2015-01-01

    We investigated contribution mediator mechanism in the development of the phenomenon of inhibition induced by barium sulfate luminol-dependent chemiluminescence (SLCHL) of blood under the influence of nonsteroidal anti-inflammatory drugs (NSAIDs) in patients with intolerance to these drugs. It was found that the phenomenon of suppression SLCHL blood under the influence of NSAIDs in patients with intolerance is mediated by the participation of mediators, and the contribution of H1--and H2--histamine receptors, 5-HT2 serotonin receptors and Cys-leukotriene receptors in the development of that phenomenon depends on the chemical nature of NSAIDs and the clinical manifestations of intolerance.

  9. Effect of non-steroidal anti-inflammatory drug etoricoxib on the hematological parameters and enzymes of colon and kidney Efecto del fármaco antiinflamatorio no esteroideo etoricoxib sobre los parámetros hematológicos y las enzimas del colon y el riñón

    OpenAIRE

    N. Behal; S. Singh Kanwar; Sharma, P.; Sanyal, S. N.

    2009-01-01

    The present study was designed to investigate the effects of a selective COX-2 inhibitor, etoricoxib in rats on the hematological and toxicity parameters in colon and kidney at two different doses of the drug, one within the therapeutic anti-inflammatory range as based on the reported ED50 value (Eto-1) while the other at ten times higher (Eto-2), relative to the toxicity studies which have not been reported so far. The results showed that the control and the drug treated animals achieved sim...

  10. Design, Synthesis, Antinociceptive and Anti-Inflammatory Activities of Novel Piroxicam Analogues

    Directory of Open Access Journals (Sweden)

    Eliezer J. Barreiro

    2012-11-01

    Full Text Available In this paper we report the design, synthesis, antinociceptive and anti-inflammatory activities of a series of benzothiazine N-acylhydrazones 14a–h, planned by structural modification of piroxicam (1, a non steroidal anti-inflammatory drug. Among the synthesized analogues, compounds 14f (LASSBio-1637 and 14g (LASSBio-1639 were identified as novel antinociceptive and anti-inflammatory prototypes, active by oral administration, acting by a mechanism of action that seems to be different from that of piroxicam, since they were inactive as an inhibitor of cyclooxygenase (COX-1 and COX-2 at concentrations of 10 mM.

  11. Incidence of non-steroidal anti-infl ammatory drugs induced gastric ...

    African Journals Online (AJOL)

    Background: Osteoarthritis is an age related degenerative disease seen predominantly in the elderly. Non-steroidal anti-inflammatory drug (NSAID) is a major therapeutic component in the management of osteoarthritis. Selective NSAID was developed to reduce the incidence of gastric irritation and erosion caused by the ...

  12. Anti-inflammatory and analgesic activity of the methanol extract of ...

    African Journals Online (AJOL)

    STORAGESEVER

    2010-02-22

    Feb 22, 2010 ... Although a defense mechanism, the complex events and mediators involved in the inflammatory reaction can induce, maintain and aggravate many disorders. The use of non-steroidal anti-inflammatory drugs (NSAIDs) in the treatment of diseases associated with inflammatory reac- tions has adverse effects ...

  13. Tolerance to alternative cyclooxygenase-2 inhibitors in nonsteroidal anti-inflammatory drug hypersensitive patients

    NARCIS (Netherlands)

    W.S.J. Malskat (Wendy S.); A.C. Knulst (André); C.A.F.M. Bruijnzeel-Koomen; Röckmann, H. (Heike)

    2013-01-01

    textabstractBackground: Non-steroidal anti-inflammatory drugs (NSAIDs) frequently cause adverse drug reactions. Many studies have shown that drugs which selectively inhibit the cyclooxygenase-2 enzyme (COX-2) are safe alternatives in the majority of patients. However, hypersensitivity reactions to

  14. A gastroenterologist and arheumatologist answer the questions on the use ofnon-steroidal anti-inflammatory drugs raised by primary care physicians

    Directory of Open Access Journals (Sweden)

    Przemysław Dyrla

    2016-03-01

    Full Text Available Non-steroidal anti-inflammatory drugs are drugs of choice for chronic pain, which is most common in chronic conditions, rheumatism in particular. According to  current recommendations, these medications should be used continuously or intermittently, and their choice should be tailored to each patient. Unfortunately, non-steroidal anti-inflammatory drugs have multiple adverse effects ranging from the most insignificant dyspepsia to severe upper gastrointestinal bleeding. Therefore, gastroscopy and, in the case of confirmed Helicobacter pylori infection, eradication is advisable for planned long-term treatment with these agents. Long-term use of proton pump inhibitors is recommended in rheumatic patients chronically receiving non-selective non-steroidal anti-inflammatory drugs, while celecoxib (a selective COX-2 inhibitor combined with proton pump inhibitor should be administered in patients at high risk of gastrointestinal complications. In rheumatic patients, the type of non-steroidal anti-inflammatory drug and the route of its administration should be tailored to each patient in terms of strength and duration of drug action, the type of disease and comorbidities as well as contraindications. Adverse gastrointestinal effects are due to the mechanism of action of non-steroidal anti-inflammatory drugs, and therefore independent of the route of administration. The use of proton pump inhibitors with cardioprotective doses of aspirin should be limited to patients with risk factors for gastrointestinal complications. High non-steroidal anti-inflammatory drug doses are limited to gout attack, acute pain and axial spondyloarthropathy showing high clinical activity. In other cases, the lowest effective non-steroidal anti-inflammatory drug dose is recommended. Advancing age is characterised by impairment in the function of all organs, therefore elderly patients should receive lower non-steroidal anti-inflammatory drug

  15. Há uma associação entre anti-inflamatórios não-esteroides e nefropatia induzida por contraste? ¿Hay una asociación entre antiinflamatorios no esteroides y nefropatía inducida por contraste? Is there an association between non-steroidal anti-inflammatory drugs and contrast nephropathy?

    Directory of Open Access Journals (Sweden)

    Luciano Passamani Diogo

    2010-12-01

    uso de AINEs y su asociación con desarrollo de NIC, a través de la alteración de los niveles de creatinina sérica o tasa de filtrado glomerular en 48 o 72 horas. RESULTADOS: En el período de julio de 2005 a julio de 2006, 236 pacientes fueron incluidos en el estudio, de los cuales 29 fueron posteriormente excluidos. La incidencia de NIC fue 10,37% (20 de 207 y 42% de los pacientes estaban recibiendo AINEs hasta el momento de la evaluación. No hubo asociación entre el uso de AINEs y el desarrollo de NIC con OR de 1,293; IC95% (0,46-4,2. El estudio detectó factores de riesgo conocidos para el desarrollo de NIC, tales como diabetes, con OR de 2,77; IC95% (1,05-7,47 e insuficiencia renal crónica con OR de 3,48; IC95% (1,1-11,07 y también sugirió una acción protectora de la hidratación con solución salina con OR de 0,166; IC95% (0,03-0,92. CONCLUSIÓN: Con base en los datos obtenidos, concluimos que no hubo asociación entre NIC y uso previo de AINEs, por lo menos con un OR > 2,85, el cual nuestra muestra detectó.BACKGROUND: The association between the use of nonsteroidal anti-inflammatory drugs (NSAIDs and acute or chronic renal failure is well documented, but evidence of such association between NSAIDs and Contrast-Induced Nephropathies (CIN is not found in the indexed literature. OBJECTIVE: To evaluate the possible association between NSAIDs and CIN. METHODS: In a cohort study, through clinical interviews of patients that underwent cardiac catheterization, we analyzed the use of NSAIDs and its association with the development of CIN, through alterations in serum creatinine or glomerular filtration rate in 48 or 72 hours. RESULTS: From July 2005 to July 2006, 236 patients were enrolled in the study, of which 29 were later excluded. The incidence of CIN was 10.37% (20 of 207 and 42% of the patients were using NSAIDs until the moment of the evaluation. There was no association between the use of NSAIDs and the development of CIN with OR of 1.293 95% CI (0

  16. Renal targeting of a non-steroidal antiinflammatory drug : effects on renal prostaglandin synthesis in the rat

    NARCIS (Netherlands)

    Haas, M; Moolenaar, F; Meijer, DKF; de Jong, PE; de Zeeuw, D

    1998-01-01

    1, Renal specific targeting of the non-steroidal anti-inflammatory drug naproxen was obtained by coupling to the low-molecular-mass protein lysozyme. A previous study showed that conjugation to lysozyme resulted in a 70-fold increase of naproxen accumulation in the kidney with a subsequent renal

  17. Fatores associados ao uso de antiinflamatórios não esteróides em população de funcionários de uma universidade no Rio de Janeiro: Estudo Pró-Saúde Factors associated with the use of non-steroidal anti-inflammatory drugs in a population of a university in Rio de Janeiro: "Pró-Saúde" Study

    Directory of Open Access Journals (Sweden)

    Tatiana Chama Borges Luz

    2006-12-01

    Full Text Available Os Antiinflamatórios Não-Esteróides (AINE estão entre os medicamentos mais utilizados no mundo. Estima-se que mais de 30 milhões de pessoas tomem AINE diariamente, apesar de sua toxicidade e de seus efeitos adversos, principalmente gastrointestinais. O presente trabalho utilizou dados seccionais da Fase 1 (1999 de um estudo de coorte (Estudo Pró-Saúde coletados entre 4.030 funcionários técnico-administrativos de uma universidade no Rio de Janeiro, nos quais foram aplicados questionários autopreenchíveis. Nesse estudo, os AINE apareceram entre os principais produtos consumidos nas duas semanas que antecederam à pesquisa, com prevalência de 7%. Verificou-se que as mulheres têm maior chance de serem usuárias (OR = 2,11; IC 95%: 1,59 - 2,79. Os dados foram submetidos a análise multivariada, tendo sido propostos modelos logísticos por sexo. A carga horária trabalhada na semana foi um importante preditor do uso de AINE (OR = 1,03; IC 95%: 1,01 - 1,04, para homens, e OR = 1,02; IC 95%: 1,00 - 1,03, para mulheres. Dor incapacitante e artrose também se mostraram relevantes, com OR = 2,89 (IC 95%: 1,77 - 4,71 e OR = 2,29 (IC 95%: 1,10 - 4,75, respectivamente, para os homens, e OR = 2,65 (IC 95%: 1,89 - 3,70 e OR = 2,00 (IC 95%: 1,37 - 2,93, respectivamente, para as mulheres. Outros preditores importantes foram a hérnia de disco (OR = 2,27; IC 95%: 0,93 - 5,54 para os homens, e LER (OR = 1,64; IC 95%: 1,15 - 2,35, cálculos vesical (OR = 1,85; IC 95%: 1,00 - 3,45 e renal (OR = 1,81; IC 95%: 1,12 - 2,91 para as mulheres. Mulheres e indivíduos com maior carga horária de trabalho semanal constituem grupos mais vulneráveis, em termos de uso irracional, e, portanto, mais sujeitos a programas de intervenção. Os resultados apontam para a importância das condições de trabalho no processo de desencadeamento de doenças.Non-steroidal Anti-inflammatory Drugs (NSAIDs are some of the most widely used drugs worldwide. It is estimated that

  18. APPLICABILITY OF THE NON STEROID ANTIINFLAMMATORY DRUGS IN FEVER THERAPY OF CHILDREN

    Directory of Open Access Journals (Sweden)

    O.A. Mubarakshina

    2008-01-01

    Full Text Available The non steroid anti-inflammatory drugs are widely applied in the pediatric practices for the fever therapy among children. While choosing the medications from this group to prescribe them to the children, it is essential to get guided towards the highly efficient medications with the least risk of the side effects. Only Paracetamol and ibuprofen are fully compliant with this requirement. They are officially recommended by who as the anti febrile medications for use in pediatrics. In the given article, the author reviews the advantages of ibuprofen over to Paracetamol based on the data from the foreign randomized research. She pays certain attention to the safety issues during the ibuprofen based treatment and to the opportunities of the combined Paracetamol and ibuprofen based therapy.Key words: fever, treatment, non steroid anti-inflammatory drugs, children.

  19. [Effect of anti-inflammatory drugs on the motility of human polymorphonuclear granulocytes].

    Science.gov (United States)

    Spisani, S; Vanzini, G; Traniello, S

    1978-11-15

    Polymorphonuclear leucocytes play an important role in the inflammatory process, and their functions are likely to be regulated by pharmacological agents. In this paper we report the "in vitro" effect of non steroidal anti-inflammatory drugs on random and chemotactic motility of human leucocytes, and demonstrate that the two forms of movement, spontaneous and directional, are differently inhibited by low concentrations of these agents. Leucocytes of patients with recurrent inflammation are unaffected by these drugs.

  20. Characterics of exposure to non-steroid anti-inflammatory drugs in European databases.

    NARCIS (Netherlands)

    Vries, F. de; Kieler, H.; Dijk, L. van; Svensson, T.; Staa, T. van

    2010-01-01

    Background: A systematic review reported that users of naproxen, ibuprofen and piroxicam did not have an increased risk of myorcardial infarction (MI), whilst users of diclofenac and indomethacin showed significantly increased risk of MI (RRs 1.4 and 1.3). While there may be biological plausible

  1. Jejunal diverticula with perforation in non steroidal anti inflammatory drug user: A case report

    Directory of Open Access Journals (Sweden)

    Shobhit Gupta

    2017-01-01

    Conclusion: Jejunal diverticula are rare lesions, and their perforation never features in the list of diagnoses for acute abdomen, especially in this part of the world. Further this unique case report opens the doors for further research to prove an assosiation between NSAID use and diverticular perforation which itself is a very rare entity.

  2. Development of poly(glycerol adipate) nanoparticles loaded with non-steroidal anti-inflammatory drugs.

    NARCIS (Netherlands)

    Wahab, A.; Favretto, M.E.; Onyeagor, N.D.; Khan, G.M.; Douroumis, D.; Casely-Hayford, M.A.; Kallinteri, P.

    2012-01-01

    The aim of this study was to assess acylated and non-acylated poly(glycerol adipate) polymers (PGA) as suitable nanoparticulate systems for encapsulation and release of ibuprofen, ibuprofen sodium salt (IBU-Na) and ketoprofen as model drugs. Drug encapsulated nanoparticles were prepared using the

  3. Effectiveness of various non-steroidal anti-inflammatory drugs in ...

    African Journals Online (AJOL)

    exclusion criteria included fractures above T7 and below L3; and other bone disorders such as disc herniation, spondylolisthesis, an infection, or a tumour. Pain intensity was assessed with the aid of a 10- point visual ... lumbar or intervertebral disc disorders for the effective management of pain and inflammation. [1,2].

  4. toxicosis of non-steroidal anti-inflammatory agents in rats

    African Journals Online (AJOL)

    ABATAN

    known for treatment of sexually transmitted infections like gonorrhoea, syphilis, and candidiasis. In this study, 48 (9.5%) of the 504 patients (male and female) were found to have T. vaginalis using the most sensitive technique for detection of the organism. A similar study carried out among couples attending fertility clinic in.

  5. toxicosis of non-steroidal anti-inflammatory agents in rats

    African Journals Online (AJOL)

    ABATAN

    This review addresses the physiologic and genetic basis for the evaluation and management of hypertension and for maximizing individual treatment needs. Genes ..... Obesity is also the cause of insulin resistance, adult – onset diabetes mellitus, left ventricular hypertrophy, hyperlipidemia, and atherosclerotic disease. A.

  6. toxicosis of non-steroidal anti-inflammatory agents in rats

    African Journals Online (AJOL)

    ABATAN

    cell (RBC) by the parasite (Lavender et al, 1989). One of the currently recommended antimalaria drug is Artemisinin (Trampuz et al, 2003), which is derived from Chinese traditional medicine and represents a totally new class of promising antimalaria agents (Klayman et al, 1985) that are active against chloroquine resistant ...

  7. toxicosis of non-steroidal anti-inflammatory agents in rats

    African Journals Online (AJOL)

    ABATAN

    rabbit jejunum and acetic acid induced pain in. Mice. Peter I Aziba. Pharmacology Unit, Swaziland Institute for ... pain relieving medicinal plant for bone fracture healing when taken as concoction, its gastrointestinal efficacy in .... either alpha or beta receptors, generally , stimulation of alpha receptor s leads to to hydrolysis of ...

  8. Non-steroidal anti-inflammatory drugs in the watercourses of Elbe basin in Czech Republic

    Czech Academy of Sciences Publication Activity Database

    Maršík, Petr; Rezek, Jan; Židková, Monika; Kramulová, Barbora; Tauchen, J.; Vaněk, Tomáš

    2017-01-01

    Roč. 171, MAR (2017), s. 97-105 ISSN 0045-6535 R&D Projects: GA ČR(CZ) GA14-22593S Grant - others:European Regional Development Fund(XE) CZ.2.16/3.1.00/24014; European Regional Development Fund(XE) CZ.2.16/3.1.00/21519 Institutional support: RVO:61389030 Keywords : chromatography-mass-spectrometry * gas-chromatography * human pharmaceuticals * waste - water * surface- water * risk-assessment * diclofenac * ibuprofen * products * plants * NSAID Surface water * Pharmaceuticals * GCxGC-TOFMS Elbe basin * Czech Republic Subject RIV: CE - Biochemistry Impact factor: 4.208, year: 2016

  9. Treatment with non-steroidal anti-inflammatory drugs in patients after myocardial infarction

    DEFF Research Database (Denmark)

    Boulakh, Lena; Gislason, G. H.

    2016-01-01

    ABSTRACT: Introduction: Studies over the past decade have shown that NSAIDs are associated with increased cardiovascular risk and may predispose to myocardial infarction in healthy individuals. Despite this knowledge patients with established cardiovascular disease are frequently treated...... with NSAIDs. The benefits versus potential harm of treatment need careful assessment. Areas covered: Observational studies and clinical trials providing information about outcome of NSAID treatment in post MI patients were retrieved; fourteen articles in total: two case-control studies, two randomized double......-blind trials and ten cohort studies. The studies had a follow-up time between 30 days and 15 years. Two studies reported of risk of atrial fibrillation, and only one addressed antithrombotic treatment. Expert opinion: The risk of death and reinfarction in this group of patients is well established. Further...

  10. Cardiovascular safety of non-steroidal anti-inflammatory drugs among healthy individuals

    DEFF Research Database (Denmark)

    Fosbøl, Emil Loldrup; Køber, Lars; Torp-Pedersen, Christian

    2010-01-01

    Studies have raised concern on the cardiovascular safety of NSAIDs. We studied safety of NSAID therapy in a nationwide cohort of healthy individuals.......Studies have raised concern on the cardiovascular safety of NSAIDs. We studied safety of NSAID therapy in a nationwide cohort of healthy individuals....

  11. toxicosis of non-steroidal anti-inflammatory agents in rats

    African Journals Online (AJOL)

    ABATAN

    Peak expiratory flow rate (PEFR) of 350 rural women aged (20-70 years) in Edo State, Nigeria who actively used wood ... The mean PEFR value for the wood exposed women (289±19.6L/mm) was significantly lower than control ..... production from earth kilns in Chisamba area, Zambia. 1-16 Stockholm Environment Institute ...

  12. toxicosis of non-steroidal anti-inflammatory agents in rats

    African Journals Online (AJOL)

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    accounting for 185,000 food borne illnesses per year (Mead et al., 1999). In Nigeria, many cases of food poisoning go unreported. In studies carried out in Ibadan (Efuntoye and Adetosoye,. 2003) and Ago-Iwoye (unpublished data) enterotoxigenic strains of S. aureus were isolated from children aged 5 years and below ...

  13. Nicolau Syndrome after intramuscular injection of non-steroidal anti-inflammatory drugs (NSAID)

    OpenAIRE

    Mehmet Dadaci; Zeynep Altuntas; Bilsev Ince; Fatma Bilgen; Osman Tufekci; Necdet Poyraz

    2015-01-01

    Nicolau syndrome is a rare complication of intramuscular injection that leads to local ischemic necrosis of the skin and adipose tissue. In this paper, we discuss etiologies, risk factors, and treatment options for gluteal Nicolau syndrome referring to patients treated in our hospital. Our study includes 17 women who visited our clinic with symptoms of gluteal necrosis secondary to intramuscular injection. The following variables were taken into account: injection site, drug administered, fre...

  14. toxicosis of non-steroidal anti-inflammatory agents in rats

    African Journals Online (AJOL)

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    During the past four decades, the Department of Health Promotion & Education,. College of Medicine, University of Ibadan, Nigeria has established a high reputation for training professional health educators and conducting research that have increased knowledge and understanding of the prevention of many public.

  15. toxicosis of non-steroidal anti-inflammatory agents in rats

    African Journals Online (AJOL)

    ABATAN

    devastating nature of this disease in the world today is unquestionable. No part of the world and no section of ... increase their chances of contacting or spreading. HIV and other sexually transmitted infections. HIV/AIDS and ... transportation networks have made HIV spread fast to rural areas and this in turn has affected the.

  16. Non-steroidal anti-inflammatory drugs and bladder cancer prevention.

    Science.gov (United States)

    Castelao, J E; Yuan, J M; Gago-Dominguez, M; Yu, M C; Ross, R K

    2000-04-01

    Inclusion of phenacetin among 'proven' human carcinogens by the IARC in 1987, raised concerns about the carcinogenic potential of acetaminophen, its major metabolite. Acetaminophen has been implicated as a possible causal agent in the development of cancer of the renal pelvis. The bladder and renal pelvis, which derive from the same embryological structure, share the same transitional type of epithelium. Past studies have been inconclusive on the possible relationship among these analgesics and bladder cancer but no large, highly detailed study of this association has been conducted. A population-based case-control study conducted in Los Angeles, California, involved 1514 incident bladder cancer cases and an equal number of controls who were matched to the index cases by sex, date of birth (within 5 years) and race. Detailed information on medication use and prior medical conditions was collected through in-person interviews. Regular use of analgesics was not associated with an increased risk of bladder cancer in either men or women. In fact, compared with non- or irregular users, regular analgesic users were at a decreased risk of bladder cancer overall (odds ratio (OR) = 0.81, 95% confidence interval (CI) = 0.68-0.96). However, there were clear differences in both the direction and strength of the associations between the different formulation classes of analgesics and bladder cancer risk. Intake of phenacetin was positively related to bladder cancer risk in a dose-dependent manner while intake of its major metabolite in humans, acetaminophen, was unrelated to risk. Intake of all classes of NSAIDs, except pyrazolon derivatives, were negatively associated with bladder cancer risk, with suggestive evidence that the protective effect varies in strength by subcategories of formulation. Acetic acids seemed to exhibit the strongest protective effect, whereas aspirin/other salicylic acids and oxicam showed the weakest protection.

  17. Inhibition of human phenol and estrogen sulfotransferase by certain non-steroidal anti-inflammatory agents

    OpenAIRE

    King, Roberta S.; Ghosh, Anasuya A.; Wu, Jinfang

    2006-01-01

    This study was initiated on the hypothesis that aryl acetic acid and aryl carboxylic acid-containing drugs would inhibit human phenol sulfotransferase (SULT1A1), and that isoform selectivity would depend on the interaction of the aryl portion of the molecule with the acceptor binding site of the sulfotransferase. This hypothesis was based on results with the rat orthologue enzyme showing that oxidation of phenolic substrates to carboxylic acid derivatives resulted in competitive inhibition of...

  18. Assessment Of Pattern Of Non-steroidal Anti-Inflammatory Drugs ...

    African Journals Online (AJOL)

    Lack of adequate knowledge in understanding written instructions on the drug information sheet was the most important reason why instructions were not followed. Level of education ... Educational status, occupation and prior knowledge of medication use contributed to inappropriate use of NSAIDs. Key words: NSAIDs ...

  19. toxicosis of non-steroidal anti-inflammatory agents in rats

    African Journals Online (AJOL)

    ABATAN

    drugs in the control of hypertension is well established. This review addresses the physiologic and genetic basis for the evaluation and management of hypertension and for maximizing individual treatment needs. Genes responsible for inherited essential hypertension can be targeted and hypertension effectively prevented.

  20. Antinociceptive and anti-inflammatory activities of a pomegranate (Punica granatum L.) extract rich in ellagitannins.

    Science.gov (United States)

    González-Trujano, María Eva; Pellicer, Francisco; Mena, Pedro; Moreno, Diego A; García-Viguera, Cristina

    2015-01-01

    Pomegranate (Punica granatum L.) has been used for centuries for the treatment of inflammatory diseases. However, there is a lack of comprehensive information focused on the properties of a certain pomegranate (poly)phenolic profile to cure pain and gastric injury induced by anti-inflammatory drugs. This study investigated the systemic effects of different doses of a HPLC-characterized pomegranate extract on the formalin-induced nociceptive behavior in mice. The effect of the extract against gastric injury caused by non-steroidal anti-inflammatory drugs and ethanol was also assessed. Pomegranate reduced nociception in both phases of the formalin test, suggesting central and peripheral activities to inhibit nociception. Indomethacin-induced gastric injury was not produced in the presence of pomegranate, which also protected against ethanol-induced gastric lesions. The present results reinforce the benefits of pomegranate (poly)phenolics in the treatment of pain as well as their anti-inflammatory properties.

  1. Pharmacological interactions of anti-inflammatory-analgesics in odontology.

    Science.gov (United States)

    Gómez-Moreno, Gerardo; Guardia, Javier; Cutando, Antonio; Calvo-Guirado, José Luis

    2009-02-01

    In this second article we describe the more interesting pharmacological interactions in dental practice based on the prescription of analgesic narcotics, paracetamol and non-selective non-steroid anti-inflammatory drugs (NSAI) (which inhibit cyclooxigenase 1 -COX 1- and cyclooxigenase 2 -COX 2-) and selective NSAIs (COX 2 inhibitors). The importance of preventing the appearance of these pharmacological interactions is because these are medicaments prescribed daily in odontology for moderate pain treatment and inflammation in the oral cavity. Paracetamol can interact with warfarin and therefore care should be taken with chronic alcoholic patients. All NSAIs reduce renal blood flow and consequently are capable of reducing the efficacy of medicaments used for treating arterial hypertension, which act via a renal mechanism. Especial attention should be taken considering the risk of interaction between the antagonists of AT1 receptors of angiostensin II (ARAII) and the NSAIs.

  2. Nonsteroidal Anti-Inflammatory Drugs and the Kidney

    Directory of Open Access Journals (Sweden)

    Walter H. Hörl

    2010-07-01

    Full Text Available Non-steroidal anti-inflammatory drugs (NSAIDs inhibit the isoenzymes COX-1 and COX-2 of cyclooxygenase (COX. Renal side effects (e.g., kidney function, fluid and urinary electrolyte excretion vary with the extent of COX-2-COX-1 selectivity and the administered dose of these compounds. While young healthy subjects will rarely experience adverse renal effects with the use of NSAIDs, elderly patients and those with co-morbibity (e.g., congestive heart failure, liver cirrhosis or chronic kidney disease and drug combinations (e.g., renin-angiotensin blockers, diuretics plus NSAIDs may develop acute renal failure. This review summarizes our present knowledge how traditional NSAIDs and selective COX-2 inhibitors may affect the kidney under various experimental and clinical conditions, and how these drugs may influence renal inflammation, water transport, sodium and potassium balance and how renal dysfunction or hypertension may result.

  3. Veterinary clinical nutrition: success stories: an overview.

    Science.gov (United States)

    Davies, Mike

    2016-08-01

    In this overview of success stories in veterinary clinical nutrition topics in cats and dogs reviewed include the dietary management of chronic kidney disease, dissolution of urinary tract uroliths by dietary modification, the recognition that taurine and L-carnitine deficiencies can cause dilated cardiomyopathy; that clinical signs associated with feline hyperthyroidism (caused by a benign adenoma) can be controlled by a low-iodine diet alone; that dietary management of canine osteoarthritis can also reduce non-steroidal anti-inflammatory drug doses; and that disease-free intervals and survival times can be statistically longer in dogs with Stage III lymphoma managed with diet. As we discover more about nutrigenetics and nutrigenomics, and as we expand our basic understanding of idiopathic diseases we are bound to identify more nutritionally related causes, and be able to develop novel dietary strategies to manage disease processes, including the formulation of diets designed to alter gene expression to obtain beneficial clinical outcomes.

  4. Pemberian Obat-Obatan Anti Inflamasi Non Steroid (AINS pada Anak

    Directory of Open Access Journals (Sweden)

    Fajriani Fajriani

    2012-10-01

    Full Text Available We know that non-steroid anti-inflammatory drugs (NSAIDs analgetic, antipirettan and anti-inflammatory effect. This drugs can decrease pain simptomaticly, the most widely prescribed drugs worldwide and being the drugs of first choice other inflammatory pain. There is many kind NSAIDs that we knaw, like aspirin, parasetamol, ibuprofen, mefenamic acid, endometasin, diklofenak, piroksikan and nemosulide. Every kind of NSAIDs has its advantage and dis advantage for that beneficial actions and side effects. That beneficial actions and harmful side effects of NSAID can be associated with its mechanism of action. Using NSAID for children must in attention. This article is expented to give information and to help the collegnes in the selecting drugs NSAID for child.DOI: 10.14693/jdi.v15i3.27

  5. Increased temperature and entropy production in cancer: the role of anti-inflammatory drugs.

    Science.gov (United States)

    Pitt, Michael A

    2015-02-01

    Some cancers have been shown to have a higher temperature than surrounding normal tissue. This higher temperature is due to heat generated internally in the cancer. The higher temperature of cancer (compared to surrounding tissue) enables a thermodynamic analysis to be carried out. Here I show that there is increased entropy production in cancer compared with surrounding tissue. This is termed excess entropy production. The excess entropy production is expressed in terms of heat flow from the cancer to surrounding tissue and enzymic reactions in the cancer and surrounding tissue. The excess entropy production in cancer drives it away from the stationary state that is characterised by minimum entropy production. Treatments that reduce inflammation (and therefore temperature) should drive a cancer towards the stationary state. Anti-inflammatory agents, such as aspirin, other non-steroidal anti-inflammatory drugs, corticosteroids and also thyroxine analogues have been shown (using various criteria) to reduce the progress of cancer.

  6. Topical ketorolac has no antinociceptive or anti-inflammatory effect in thermal injury

    DEFF Research Database (Denmark)

    Møiniche, S; Pedersen, J L; Kehlet, H

    1994-01-01

    This study investigated the antinociceptive and anti-inflammatory effect of a topical non-steroidal anti-inflammatory drug in human thermal injury. Twelve healthy unmedicated volunteers had identical burn injuries produced on the medial side of both calves with a 49 degrees C 15 x 25 mm thermode....... and MPDT, an increase in EI and development of mechanical hyperalgesia (P nociceptive or inflammatory variables studies (P > 0.2)........ Ketorolac gel or placebo were randomly applied on the right or left calf 1.5 h before burn injury, immediately after burn injury and 6 and 12 h later in a double-blind trial where every subject served as his own control. Heat pain detection thresholds (HPDT), head pain tolerance (HPT), mechanical pain...

  7. Scintiscan evaluation of rheumatoid hands for monitoring the anti-inflammatory effects of drugs

    Energy Technology Data Exchange (ETDEWEB)

    Remans, J.; Berghs, H.; Drieskens, L.; Kiebooms, L.; Polderman, J.

    1976-01-01

    In 32 patients with chronic active rheumatoid arthritis, quantitative scintiscans of the proximal interphalangeal joints were taken with /sup 99m/Tc pertechnetate before and after 20 weeks of treatment with naproxen, an anti-inflammatory non-steroidal agent. A significant decrease of the joints /sup 99m/Tc uptake was demonstrated under naproxen therapy. Simultaneously, a clinical improvement was reflected in 17 out of the 32 patients by a reduction in the composite '' disease activity index'' used to evaluate the overall status of the disease. No significant correlation was observed between the clinical evolution and the scanning evolutions of both bands. The usefulness and the possible limits of /sup 99m/Tc arthroscanning as a tool for assessing anti-inflammatory drugs are discussed, as well as some of its methodological difficulties.

  8. Rehabilitation of muscle after injury - the role of anti-inflammatory drugs

    DEFF Research Database (Denmark)

    Mackey, Abigail; Mikkelsen, U R; Magnusson, S P

    2012-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are widely consumed among athletes worldwide in relation to muscle injury and soreness. This review aims to provide an overview of studies investigating their effects on skeletal muscle, in particular the repair processes in injured muscle. Muscle...... junction, whereas contusion or overload injury can damage both myofibers and intramuscular connective tissue. The role of NSAIDs in muscle repair is complicated by differences in injury models used, variables evaluated, and time point(s) selected for evaluations. While the temporal pattern of the influence...

  9. Enhancement of anti-inflammatory property of aspirin in mice by a nano-emulsion preparation.

    Science.gov (United States)

    Subramanian, Balajikarthick; Kuo, Fonghsu; Ada, Earl; Kotyla, Tim; Wilson, Thomas; Yoganathan, Subbiah; Nicolosi, Robert

    2008-11-01

    Aspirin, a non-steroidal anti-inflammatory drug, widely used for its anti-inflammatory properties is associated with several systemic side effects including gastro-intestinal discomfort. Inflammation can be mediated by pro-inflammatory cytokines and, along with various other host factors eventually give rise to edema at the inflamed site. Because of the adverse side effects oftentimes associated with systemic exposure to aspirin, the aim of the present study was to investigate whether the anti-inflammatory property of aspirin would enhance if delivered as nano-emulsion preparation. Nano-emulsion preparations of aspirin prepared with a Microfluidizer Processor were evaluated in the croton-oil-induced ear edema CD-1 mouse model using ear lobe thickness and the accumulation of specific in situ cytokines as biomarkers of inflammation. The results showed that particle size (90 nm) populations of nano-emulsion preparations of aspirin compared to an aspirin suspension (363 nm), significantly decreased (pemulsion further reduced the auricular levels of IL-1alpha (-37%) and TNFalpha (-69%) compared to the aspirin suspension preparation (pemulsion preparation of aspirin significantly improved the anti-inflammatory properties of an aspirin suspension in a CD-1 mouse model of induced inflammation.

  10. A survey of analgesic and anti-inflammatory drug prescription for oral implant surgery

    Directory of Open Access Journals (Sweden)

    Rahul Datta

    2015-04-01

    Full Text Available Aim: This study was conducted to determine the preferred analgesic and anti-inflammatory drugs prescribed by oral implantologists in India. Methods: A structured questionnaire was distributed to 332 dentists to gather information regarding their prescription habits for analgesics and anti-inflammatory drugs. Frequency distributions were computed by type of drug being prescribed and the protocol followed. Results: Analysis of data showed that majority of dentists (85.8%, n = 285 prescribed conventional non-steroidal anti-inflammatory drugs (NSAIDs for implant surgery. The most common prescription was ibuprofen with paracetamol combination (32.2%, n = 107 followed by diclofenac (20.2%, n = 67. Most dentists reported prescribing different NSAIDs for the same procedure in different patients (64.7%, n = 215. Only, 35.5% (n = 118 followed the peri-operative protocol. Adjunctive prescription of steroids was done by only 33.7% (n = 112. Conclusion: Our study illustrates that the general trend of analgesic and anti-inflammatory drug prescription for dental implant surgery among Indian dentists is mostly in accordance with the guidelines for pain management worldwide. However, it is noteworthy that a few dentists do prescribe drugs not primarily indicated for dental pain management and use widely varying protocols for the same. Therefore, in order to avoid potential complications, it is essential to raise awareness of among the dental practitioners of the appropriate indications and dosage regimen of specific drugs.

  11. The role of chronic inflammation in the development of gastrointestinal cancers: reviewing cancer prevention with natural anti-inflammatory intervention.

    Science.gov (United States)

    Lee, Ho-Jae; Park, Jong-Min; Han, Young Min; Gil, Hong Kwon; Kim, Jinhyung; Chang, Ji Young; Jeong, Migyeong; Go, Eun-Jin; Hahm, Ki Baik

    2016-01-01

    Inflammatory mediators alter the local environment of tumors, known as the tumor microenvironment. Mechanistically, chronic inflammation induces DNA damage, but understanding this hazard may help in the search for new chemopreventive agents for gastrointestinal (GI) cancer which attenuate inflammation. In the clinic, GI cancer still remains a major cause of cancer-associated mortality, chemoprevention with anti-inflammatory agents is thought to be a realistic approach to reduce GI cancer. Proton pump inhibitors, monoclonal antibodies targeting tumor necrosis factor-alpha, anti-sense targeted smad7 and non-steroidal anti-inflammatory agents have been investigated for their potential to prevent inflammation-based GI cancer. Besides these, a wide variety of natural products have also shown potential for the prevention of GI cancer. In this review, the authors will provide insights to explain the mechanistic connection between inflammation and GI cancer, as well as describe a feasible cancer prevention strategy based on anti-inflammatory treatments.

  12. Anti-inflammatory effects of exercise

    DEFF Research Database (Denmark)

    Pedersen, Bente Klarlund

    2017-01-01

    BACKGROUND: Persistent inflammation is involved in the pathogenesis of chronic diseases such as type 2 diabetes mellitus (T2DM) and cardiovascular disease (CVD). AIMS: The aim of this review was to provide the reader with an update of the mechanisms whereby exercise-induced cytokines may impact...... and IL-10 is provoked by exercise and exerts direct anti-inflammatory effects by an inhibition of TNF-α and by stimulating IL-1ra, thereby limiting IL-1β signalling. Moreover, muscle-derived IL-6 appears to have direct anti-inflammatory effects and serves as a mechanism to improve glucose tolerance....... In addition, indirect anti-inflammatory effects of long-term exercise are mediated via improvements in body composition. CONCLUSION: Physical activity represents a natural, strong anti-inflammatory strategy with minor side effects and should be integrated in the management of patients with cardiometabolic...

  13. Tramadol plus metamizole combined or not with anti-inflammatory drugs is clinically effective for moderate to severe chronic pain treatment in cancer patients.

    Science.gov (United States)

    Flôr, Patrícia B; Yazbek, Karina V B; Ida, Keila K; Fantoni, Denise T

    2013-05-01

    To test the effectiveness and safety of tramadol plus metamizole combined or not with a non-steroidal anti-inflammatory drug (NSAID) for treating moderate to severe chronic neoplastic pain in dogs, and its impact on quality of life (QL). Prospective, uncontrolled, open-label, clinical study. Sixty nine client-owned dogs with multiple forms of cancer and visual analog scale (VAS) pain score ≥ 40 after receiving NSAIDs for at least 7 days. The MN group received metamizole + NSAID, MNT group received metamizole + NSAID + tramadol and MT group received metamizole + tramadol. Pain was scored by the 0 to 100 mm VAS (0 = no pain, 100 = worst pain) and analgesic therapy was considered effective if 25 mm differences in VAS scores were observed between day 0 and the follow ups. The QL was evaluated according to a 0 to 36 scoring method for dogs (0 = worst, 36 = best) and side effects were recorded. Data were registered at day 0 (baseline) and at the first and second follow ups (7 and 14 days after day 0, respectively). The MN group had less analgesia at day 7 (25%) and day 14 (42%) than MNT (59%, p = 0.0274; 76%, p = 0.0251, respectively) and MT groups (69%, p = 0.0151; 81%, p = 0.0341, respectively). The QL scores were lower in the MN group at the first (score 23) and second follow up (score 26) than in MNT (27, p = 0.0847; 30, p = 0.0002) and MT (28, p = 0.0384; 31, p = 0.0001) groups. Side effects were more commonly observed in the MN group (87%) than in MNT (24%, p metamizole combined or not with NSAID were well tolerated and clinically effective to treat moderate to severe pain in dogs with cancer and improved QL. © 2013 The Authors. Veterinary Anaesthesia and Analgesia © 2013 Association of Veterinary Anaesthetists and the American College of Veterinary Anesthesia and Analgesia.

  14. Endoscopical appearances of nonsteroidal anti inflammatory drug (NSAID- enteropathy

    Directory of Open Access Journals (Sweden)

    Marcellus Simadibrata

    2005-12-01

    Full Text Available Non Steroidal Anti Inflammatory Drugs (NSAID have been associated with a sudden and sustained rise in the incidence of gastrointestinal ulcer complications. The aim of the study was to reveal the endoscopical abnormalities found in the duodenum & proximal jejunum due to NSAID. Thirty eight patients taking NSAID for their arthritis or rheumatism were included in this study. Gastro-duodeno-jejunoscopy was done with Olympus PCF-10. The endoscopical appearances of NSAID entero gastropathy were evaluated with a scoring system. The NSAID-entero-gastropathy appearances were endoscopically seen as hyperemia, erosion and ulcer. From all patient recruited, 7.9% complaint of diarrhea and 71.1% complaint of dyspepsia. Endoscopically, in the duodenal bulb we found 79% cases of hyperemia, 39.5% cases of erosion and 7.9% cases of ulcer. In the second part (descending part of the duodenum we found 28.9% cases of hyperemia, 15.8% cases of erosion and 2.6% case of ulcer. In the jejunum, we found 7.9% cases of hyperemia, 2.6% case of erosion and no ulcer. It is concluded that the most frequent abnormal endoscopical appearances in NSAID- enteropathy was hyperemia. The most frequent site of NSAID-enteropathy abnormal findings was in the duodenal bulb. (Med J Indones 2005; 14: 225-9Keywords: NSAID-enteropathy, endoscopical appearances.

  15. Chamomile, a novel and selective COX-2 inhibitor with anti-inflammatory activity.

    Science.gov (United States)

    Srivastava, Janmejai K; Pandey, Mitali; Gupta, Sanjay

    2009-11-04

    Inducible cyclooxygenase (COX-2) has been implicated in the process of inflammation and carcinogenesis. Chamomile has long been used in traditional medicine for the treatment of inflammatory diseases. In this study we aimed to investigate whether chamomile interferes with the COX-2 pathway. We used lipopolysaccharide (LPS)-activated RAW 264.7 macrophages as an in vitro model for our studies. Chamomile treatment inhibited the release of LPS-induced prostaglandin E(2) in RAW 264.7 macrophages. This effect was found to be due to inhibition of COX-2 enzyme activity by chamomile. In addition, chamomile caused reduction in LPS-induced COX-2 mRNA and protein expression, without affecting COX-1 expression. The non-steroidal anti-inflammatory drug, sulindac and a specific COX-2 inhibitor, NS398, were shown to act similarly in LPS-activated RAW 264.7 cells. Our data suggest that chamomile works by a mechanism of action similar to that attributed to non-steroidal anti-inflammatory drugs. These findings add a novel aspect to the biological profile of chamomile which might be important for understanding the usefulness of aqueous chamomile extract in the form of tea in preventing inflammation and cancer.

  16. Optimization and pharmacological validation of a leukocyte migration assay in zebrafish larvae for the rapid in vivo bioactivity analysis of anti-inflammatory secondary metabolites.

    Directory of Open Access Journals (Sweden)

    María Lorena Cordero-Maldonado

    Full Text Available Over the past decade, zebrafish (Danio rerio have emerged as an attractive model for in vivo drug discovery. In this study, we explore the suitability of zebrafish larvae to rapidly evaluate the anti-inflammatory activity of natural products (NPs and medicinal plants used in traditional medicine for the treatment of inflammatory disorders. First, we optimized a zebrafish assay for leukocyte migration. Inflammation was induced in four days post-fertilization (dpf zebrafish larvae by tail transection and co-incubation with bacterial lipopolysaccharides (LPS, resulting in a robust recruitment of leukocytes to the zone of injury. Migrating zebrafish leukocytes were detected in situ by myeloperoxidase (MPO staining, and anti-inflammatory activity was semi-quantitatively scored using a standardized scale of relative leukocyte migration (RLM. Pharmacological validation of this optimized assay was performed with a panel of anti-inflammatory drugs, demonstrating a concentration-responsive inhibition of leukocyte migration for both steroidal and non-steroidal anti-inflammatory drugs (SAIDs and NSAIDs. Subsequently, we evaluated the bioactivity of structurally diverse NPs with well-documented anti-inflammatory properties. Finally, we further used this zebrafish-based assay to quantify the anti-inflammatory activity in the aqueous and methanolic extracts of several medicinal plants. Our results indicate the suitability of this LPS-enhanced leukocyte migration assay in zebrafish larvae as a front-line screening platform in NP discovery, including for the bioassay-guided isolation of anti-inflammatory secondary metabolites from complex NP extracts.

  17. Anti-Inflammatory Activity of Natural Products

    Directory of Open Access Journals (Sweden)

    Abdullatif Azab

    2016-10-01

    Full Text Available This article presents highlights of the published literature regarding the anti-inflammatory activities of natural products. Many review articles were published in this regard, however, most of them have presented this important issue from a regional, limited perspective. This paper summarizes the vast range of review and research articles that have reported on the anti-inflammatory effects of extracts and/or pure compounds derived from natural products. Moreover, this review pinpoints some interesting traditionally used medicinal plants that were not investigated yet.

  18. Anti-inflammatory and analgesic effects of ketoprofen in palm oil esters nanoemulsion.

    Science.gov (United States)

    Sakeena, M H F; Yam, M F; Elrashid, S M; Munavvar, A S; Azmin, M N

    2010-01-01

    Ketoprofen is a potent non-steroidal anti-inflammatory drug has been used in the treatment of various kinds of pains, inflammation and arthritis. However, oral administration of ketoprofen produces serious gastrointestinal adverse effects. One of the promising methods to overcome these adverse effects is to administer the drug through the skin. The aim of the present work is to evaluate the anti-inflammatory and analgesic effects from topically applied ketoprofen entrapped palm oil esters (POEs) based nanoemulsion and to compare with market ketoprofen product, Fastum(®) gel. The novelty of this study is, use of POEs for the oil phase of nanoemulsion. The anti-inflammatory and analgesic studies were performed on rats by carrageenan-induced rat hind paw edema test and carrageenan-induced hyperalgesia pain threshold test to compare the ketoprofen entrapped POEs based nanoemulsion formulation and market formulation. Results indicated that there are no significant different between ketoprofen entrapped POEs nanoemulsion and market formulation in carrageenan-induced rat hind paw edema study and carrageenan-induced hyperalgesia pain threshold study. However, it shows a significant different between POEs nanoemulsion formulation and control group in these studies at p<0.05. From these results it was concluded that the developed nanoemulsion have great potential for topical application of ketoprofen.

  19. Tomato leaves methanol extract possesses anti- inflammatory ...

    African Journals Online (AJOL)

    GREGORY

    2011-12-16

    Dec 16, 2011 ... and antioxidant (lycopene) (Junichiro, 2006). Since S. lycopersicum has long been used for the treatment of variety of disease, the present study aimed to investigate the inhibitory activity of tomato leaves against PGE2 using. RAW264.7 macrophages cells and introduce a new potential of anti-inflammatory ...

  20. Chemical Characterization, Anti inflammatory and Analgesic ...

    African Journals Online (AJOL)

    The analgesic activity was assessed by acetic acid-induced writhing in Swiss albino mice. Indomethacin (10 mg/kg) and acetyl salicylic acid (100 mg/kg) were used as standards in the anti-inflammatory and analgesic assay respectively. Phytochemical investigations reveal the presence of alkaloids, tannins, glycosides, ...

  1. Anti-inflammatory and Wound- Healing Activities

    African Journals Online (AJOL)

    Erah

    Linn (Apocynaceae) 2: Anti-inflammatory and Wound-. Healing Activities. Indranil Chanda1*, Usha Sarma2, Sanat K Basu3, Mangala Lahkar4 and. Sadhan K Dutta5. 1Girijananda Chowdhury Institute of Pharmaceutical Science, Guwahati, Assam-781017, 2Department of Pathology,. Gauhati Medical College and Hospital, ...

  2. Utilization of spray drying technique for improvement of dissolution and anti-inflammatory effect of Meloxicam.

    Science.gov (United States)

    Shazly, Gamal; Badran, Mohamed; Zoheir, Khairy; Alomrani, Abdullah

    2015-01-01

    Meloxicam (MLX) is a poorly water-soluble non steroidal anti-inflammatory drug (NSAID). The main objective of the present work was to enhance the dissolution of MLX and thus its bioavailability by the aid of additives. The novelty of this work rises from the utilization of spray drying technology to produce micro particulates solid dispersion systems containing MLX in the presence of small amount of additives. Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), and Scan Electron Microscope (SEM) were used for studying the physico-chemical and morphological properties of MLX samples. The dissolution of MLX samples was investigated in two different pH media. The morphology of MLX solid dispersion micro-particles was spherical in shape according to SEM. FT-IR profiles indicated that a complex was formed between MLX and the additives. DSC patterns of the MLX micro-particles suggested a reduction in the crystallinity of MLX and probability of presence of an interaction between MLX and the additives. The rate of dissolution of the spray-dried MLX enhanced as compared with the unprocessed MLX in both acidic and neutral media. It was found that 100% of the added MLX released within 5 min in phosphate buffer dissolution medium (pH 7.4) compared to that of the unprocessed MLX (15% in 60 min). Such increase rate in the dissolution of the spray dried MLX could be attributed to the increase in wettability of MLX particles and the hydrophilic nature of the additives. The anti-inflammatory effect of the spray dried MLX was explored using formalin induced rat paw edema model. The spray-dried samples showed an increase in the anti-inflammatory activity of MLX as compared to the unprocessed MLX. This work reveals that the spray drying technique is suitable for preparation of micro-particles with improved dissolution and anti-inflammatory effect of MLX.

  3. Synthesis and anti-angiogenic effect of conjugates between serum albumin and non-steroidal anti-inflammatory drugs

    DEFF Research Database (Denmark)

    Kjaer, B; Struve, C; Friis, T

    2010-01-01

    of investigating the anti-angiogenic efficiency of NSAID-HSA conjugates in vitro, three NSAIDs, aspirin, ibuprofen, and naproxen were conjugated to HSA using different concentrations of their N-hydroxysuccinimide esters. Conjugation ratios from 10 to 50 were achieved and the conjugates retained a growth inhibitory...

  4. Combined effects of aging and in vitro non-steroid anti-inflammatory drugs on kidney and liver mitochondrial physiology.

    Science.gov (United States)

    Rocha-Rodrigues, Sílvia; Santos-Alves, Estela; Coxito, Pedro M; Marques-Aleixo, Inês; Passos, Emanuel; Guimarães, João T; Martins, Maria J; Oliveira, Paulo J; Magalhães, José; Ascensão, António

    2013-09-03

    Aging and drug-induced side effects may contribute to deteriorate mitochondrial bioenergetics in many tissues, including kidney and liver. One possibility is that the combination of both aging and drug toxicity accelerates the process of mitochondrial degradation, leading to progressive bioenergetic disruption. We therefore analyzed in vitro kidney (KM) and liver (LM) mitochondrial response to salicylate and diclofenac in old and adult animals. Male-Wistar adult (19-wks) and aged (106-wks) rats were used. In vitro endpoints of oxygen consumption and membrane potential were evaluated in non-treated conditions (vehicle) and in the presence of salicylate (0.5mM) and diclofenac (50μM). The susceptibility to calcium-induced permeability transition pore (MPTP) was assessed. Aconitase and C, -SH and MDA contents were measured. Apoptotic signaling was followed by measuring caspase 3, 8 and 9 activities, Bax, Bcl2 and CypD expression. ANT content was semi-quantified. In general, animal age alone compromised KM state 3 and LM ADP lag phase while resulting in decreased resistance to the MPTP. Aging decreased LM CypD and increased Mn-SOD. Kidney caspase 9-like activity was lower in aged group. Salicylate and diclofenac induced KM and LM dysfunction. ADP lag phase in KM was further increased in the aged group in the presence of diclofenac. No further impairments were observed regarding drug toxicity adding to the aging process. Aging impaired KM and LM function despite no detected alterations on oxidative stress and apoptosis. However, aging did not further exacerbate KM and LM frailty induced by salicylate and diclofenac. © 2013.

  5. Patient self-reporting of potential adverse drug reactions to non-steroidal anti-inflammatory drugs in Thailand.

    Science.gov (United States)

    Jarernsiripornkul, Narumol; Chaisrisawadsuk, Sudarat; Chaiyakum, Aporanee; Krska, Janet

    2009-10-01

    To validate and pilot in Thailand a questionnaire to enable patients to identify and report symptoms perceived as potential ADRs from NSAIDs. To determine the questionnaire's usefulness in enabling Thai out-patients to report potential ADRs. To determine the frequency with which symptoms patients reported were recorded by health professionals and the frequency of ADRs to these drugs reported to the APRM Centre. To assess whether patients reported symptoms from non COX-selective inhibitors and COX-2 selective NSAIDs with different frequencies. Out-patient departments (OPD) of a University teaching hospital in North-East Thailand. A questionnaire which incorporated an extensive symptoms checklist, developed and validated in English, was translated, piloted and validated in Thai. This was distributed to patients receiving one of five NSAIDs. Causality assessment of the symptoms reported was undertaken by a pharmacist, using data on concomitant medicines and disease states from OPD records. Frequency and type of symptoms reported by patients, recording of these in OPD records, reports sent to APRM Centre. Piloting found that patients were able to understand the questionnaire, but were unaware of drug names. A response rate of 42% was obtained: 694 usable questionnaires were returned out of 1,654 distributed. Overall 73% of respondents reported at least one symptom perceived to be an ADR. Sixty percent of symptoms reported were classed as probably or possibly an ADR. Fewer symptoms per patient were reported by those taking COX-2 selective inhibitors (3.5) than those taking non-selective NSAIDs (5.5), although there were no differences in the frequency of GI symptoms reported between these two sub-classes, which may relate to other factors, such as age, previous GI problems and prescription of protective ulcer-healing therapy. Only 5% of symptoms were recorded in OPD records and reporting of ADRs to these drugs to the APRM Centre of the Thai FDA during the study was very limited. Thai out-patients were willing and able to complete questionnaires regarding potential ADRs. The questionnaire could form part of routine out-patient monitoring, aiding identification of ADRs, and may help to increase ADR reporting in Thailand.

  6. Randomized trial of switching from prescribed non-selective non-steroidal anti-inflammatory drugs to prescribed celecoxib

    DEFF Research Database (Denmark)

    Macdonald, Thomas M; Hawkey, Chris J; Ford, Ian

    2017-01-01

    infarction or other biomarker positive acute coronary syndrome, non-fatal stroke or CV death analysed using a Cox model with a pre-specified non-inferiority limit of 1.4 for the hazard ratio (HR). RESULTS: In total, 7297 participants were randomized. During a median 3-year follow-up, fewer subjects than......-years with celecoxib and 1.10 per 100 patient-years with nsNSAIDs (HR = 1.04; 95% confidence interval, 0.81-1.33; P = 0.75). Pre-specified non-inferiority was achieved in the ITT analysis. The upper bound of the 95% confidence limit for the absolute increase in OT risk associated with celecoxib treatment was two......NSAIDs. There was no advantage of a strategy of switching prescribed nsNSAIDs to prescribed celecoxib. This study excluded an increased risk of the primary endpoint of more than two events per 1000 patient-years associated with switching to prescribed celecoxib....

  7. . Chronic kidney disease in patients with chronic back pain taking non-steroidal anti-inflammatory drugs

    Directory of Open Access Journals (Sweden)

    Gaydukova I.Z.

    2016-03-01

    in patients with ax-SpA, DDS and controls were comparable. The activity of pain was evaluated according to the accepted recommendations. The index of NSAID intake as calculated for the preceding year. Results. GFR in patients with ax-SpAwas 87,0 [77,25; 102,0] ml/min/1,73 m2, 11 (18% patients showed a reduction in GFR of less than 60 ml/ min/1,73m2. In patients with DDS GFR was 87,5 [65,5; 97,0] ml/min / 1,73 m 2 (p=0,27, decreased GFR of less than 60 ml/min / 1,73 m2 was detected in 3 (15% patients. The ratio of albumin / creatinine urine in patients with ax-SpA was 35,8 [25,46; 43,4] mg/g, in patients DDS —207,1 [91,66; 244,59] mg/g (p<0,0001, in healthy individuals —25,45 [17,34; 33,65] mg/g. Conclusions. Patients with chronic back pain taking NSAIDs for a long time have revealed GFR, comparable with healthy people, and increased urine albumin. Patients with degenerative diseases of the spine have a greater index of albumin in urine than patients with ax-SpA.

  8. The efficacy of non-steroidal anti-inflammatory drugs (NSAIDS) for shoulder complaints. A systematic review

    NARCIS (Netherlands)

    van der Windt, D. A.; van der Heijden, G. J.; Scholten, R. J.; Koes, B. W.; Bouter, L. M.

    1995-01-01

    The medical literature was evaluated with respect to the efficacy of NSAIDs for shoulder complaints. Nineteen randomized clinical trials met the selection criteria and were included in this review. Each publication was independently scored by two blinded reviewers, according to a standardized set of

  9. The cardiovascular safety of non-steroidal anti-inflammatory drugs (NSAIDs) among healthy people - A nationwide population study

    DEFF Research Database (Denmark)

    Fosbøl, Emil Loldrup

    2010-01-01

    -steroide anti-inflammatoriske lægemidler (NSAID) blandt raske mennesker. Ved hjælp af danskernes CPR nummer er det muligt at krydse registrene på individuelt niveau. Data dækker informationer om al anvendt receptpligtig medicin, hospitalsindlæggelser, indkomst samt overlevelsesstatus på alle danske indbyggere...... med alder på 10 år eller over den første januar 1997. Disse individer blev fulgt til slutningen af 2005. Afhandlingen bygger foruden deskriptiv statistik også på et historisk cohorte design hvor sammenhængen mellem NSAID forbrug og risiko for kardiovaskulære komplikationer analyseres ved hjælp af...... flere statistiske modeller. Tidligere studier har sat brugen af NSAID i forbindelse med øget risiko for hjertedød i forskellige grupper af patienter. Især den nye generation af lægemidlerne, de selektive cyclooxygenase (COX) 2 hæmmere, er grundigt undersøgt og den selektive COX-2 hæmmer rofecoxib (Vioxx...

  10. Non-steroidal anti-inflammatory drug use is associated with increased risk of out-of-hospital cardiac arrest

    DEFF Research Database (Denmark)

    Sondergaard, Kathrine B; Weeke, Peter; Wissenberg, Mads

    2017-01-01

    Arrest Registry, all persons with OHCA during 2001-2010 were identified. NSAID use 30 days before OHCA was categorized as follows: diclofenac, naproxen, ibuprofen, rofecoxib, celecoxib, and other. Risk of OHCA associated with use of NSAIDs was analyzed by conditional logistic regression in case.......8% of total NSAID use, respectively. Use of diclofenac (odds ratio (OR), 1.50 [95% confidence interval (CI) 1.23-1.82]) and ibuprofen (OR, 1.31 [95% CI 1.14-1.51]) was associated with a significantly increased risk of OHCA. Use of naproxen (OR, 1.29 [95% CI 0.77-2.16]), celecoxib (OR, 1.13 [95% CI 0...

  11. Analgesic And Anti-Inflammatory Activities Of Asparagus africanus ...

    African Journals Online (AJOL)

    Analgesic And Anti-Inflammatory Activities Of Asparagus africanus Root Extract. ... the roots of Asparagus africanus Lam (Liliaceae) which contains mainly saponins and ... that the extract possesses analgesic and anti-inflammatory properties.

  12. N-Acetylcysteine enhances the action of anti-inflammatory drugs as suppressors of prostaglandin production in monocytes

    Directory of Open Access Journals (Sweden)

    Erica Hoffer

    2002-01-01

    Full Text Available The anti-inflammatory effect of non-steroidal anti-inflammatory drugs (NSAIDs is associated with inhibition of cyclooxygenase (COX, the rate-limiting enzyme responsible for the synthesis of prostaglandins. Since oxygen free radicals can act as second cellular messengers, especially to modulate the metabolism of arachidonic acid and the prostaglandin tract, it seems plausible that antioxidants might affect the production of prostaglandin by activated cells. This research is focused on the effect of the antioxidant N-acetylcysteine (NAC on the inhibition of prostaglandin E2 formation in activated monocytes by specific and non-specific COX inhibitors. We found that lipopolysaccharide-induced prostaglandin E2 formation was significantly reduced by rofecoxib and by diclofenac, two NSAIDs. Addition of NAC to each of these drugs enhanced the effect of the NSAIDs. These results suggest that one might expect either a potentiation of the anti-inflammatory effect of COX inhibitors by their simultaneous administration with NAC, or obtaining the same anti-inflammatory at lower drug levels.

  13. Anti inflammatory effects of statin in COPD

    OpenAIRE

    Nasef Abdelsalam Rezk; Ahmad Elewa

    2013-01-01

    Introduction: Statins are now becoming recognized as powerful antiinflammatory agents that exert beneficial effects beyond low-density lipoprotein cholesterol reduction [1]. COPD patients receiving statins obtain a benefit from these therapeutic agents. Clearly, the best medical evidence for the association of statins with improved outcomes for COPD patients [2]. We aimed in this study to assess anti inflammatory effects of statin in COPD patients. Patients and methods: We studied 28...

  14. Anti-Inflammatory Effect of Allium ursinum

    Directory of Open Access Journals (Sweden)

    Alina Elena PÂRVU

    2014-03-01

    Full Text Available The aim of the present study was to evaluate Allium ursinum leaves and flowers extract anti-inflammatory effect. Plant extract 1:1 (w:v was prepared from A. ursinum leaves by a modified Squibb repercolation method. The in vivo anti-inflammatory effects were evaluated on a rat turpentine oil-induced inflammation (i.m. 6 mL/kg BW. The animals were randomly assigned to nine groups (n=8: negative control, inflammation, A. ursinum flower extract (AUF, A. ursinum leaves extract (AUL, indomethacin (INDO (20 mg/kg BW, aminoguanidine (AG (50 mg/kg b.w./d i.p. as a selective NOS2 inhibitor, NG-nitro L-arginine methyl ester (NAME (5 mg/kg b.w./d i.p. as a nonselective NOS inhibitor, L-arginine (ARG (100 mg/kg b.w./d i.p., NO synthesis substrate, and Trolox (20 mg/kg b.w./d i.p as an antioxidant. At 24h from inflammation induction total oxidative status (TOS, oxidative stress index (OSI, nitric oxide (NOx and in vitro phagocytosis test were reduced and the total antioxidative reactivity (TAR was increased by the testes plant extracts. AUF had a better inhibitory effect than AUL. In conclusion, we provided evidence for the hypothesis that A. ursinum leaves and flowers extract exerts anti-inflammatory activity by inhibiting the phagocytosis through the reduction of the nitro-oxidative stress.

  15. In vitro interactions between anidulafungin and nonsteroidal anti-inflammatory drugs on biofilms of Candida spp.

    Science.gov (United States)

    Rosato, Antonio; Catalano, Alessia; Carocci, Alessia; Carrieri, Antonio; Carone, Addolorata; Caggiano, Giuseppina; Franchini, Carlo; Corbo, Filomena; Montagna, Maria Teresa

    2016-03-01

    Candida spp. are responsible for many biomaterial-related infections; they give rise to infective pathologies typically associated with biofilm formation. We recently reported that the echinocandin anidulafungin (ANF) showed a strong in vitro activity against both planktonic and biofilms cells. Herein, we report the antifungal activities of ANF alone and in association with some non-steroidal anti-inflammatory drugs (NSAIDs) against nine Candida strain biofilms: four Candida albicans, two Candida glabrata and three Candida guilliermondii. The activity of ANF was assessed using an in vitro microbiological model relevant for clinical practice. ANF proved oneself to be active against biofilms cells, and a clear-cut synergism was found against Candida species biofilms when ANF was used in combination with three NSAIDs: aspirin, diclofenac, ibuprofen. The positive synergism against Candida spp. of ANF in association with aspirin or the other NSAIDs proved to be a very effective antifungal treatment (FICICandida biofilm pathologies. Copyright © 2016 Elsevier Ltd. All rights reserved.

  16. Anti-inflammatory Nanomedicine for Cardiovascular Disease

    Directory of Open Access Journals (Sweden)

    Shunsuke Katsuki

    2017-12-01

    Full Text Available Coronary artery disease, in the development of which inflammation mediated by innate immune cells plays a critical role, is one of the leading causes of death worldwide. The 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors (statins are a widely used lipid-lowering drug that has lipid-independent vasculoprotective effects, such as improvement of endothelial dysfunction, antioxidant properties, and inhibitory effects on inflammation. Despite recent advances in lipid-lowering therapy, clinical trials of statins suggest that anti-inflammatory therapy beyond lipid-lowering therapy is indispensible to further reduce cardiovascular events. One possible therapeutic option to the residual risk is to directly intervene in the inflammatory process by utilizing a nanotechnology-based drug delivery system (nano-DDS. Various nano-sized materials are currently developed as DDS, including micelles, liposomes, polymeric nanoparticles, dendrimers, carbon nanotubes, and metallic nanoparticles. The application of nano-DDS to coronary artery disease is a feasible strategy since the inflammatory milieu enhances incorporation of nano-sized materials into mononuclear phagocytic system and permeability of target lesions, which confers nano-DDS on “passive-targeting” property. Recently, we have developed a polymeric nanoparticle-incorporating statin to maximize its anti-inflammatory property. This statin nanoparticle has been tested in various disease models, including plaque destabilization and rupture, myocardial ischemia-reperfusion injury, and ventricular remodeling after acute myocardial infarction, and its clinical application is in progress. In this review, we present current development of DDS and future perspective on the application of anti-inflammatory nanomedicine to treat life-threatening cardiovascular diseases.

  17. Novel anti-inflammatory agents in COPD

    DEFF Research Database (Denmark)

    Loukides, Stelios; Bartziokas, Konstantinos; Vestbo, Jørgen

    2013-01-01

    Inflammation plays a central role in chronic obstructive pulmonary disease (COPD). COPD related inflammation is less responsive to inhaled steroids compared to asthma. There are three major novel anti-inflammatory approaches to the management of COPD. The first approach is phosphodiesterase...... on these strategies exist at the moment. A third potential approach involves novel agents whose mechanism of action is closely related to COPD mechanisms and pathophysiology. Such novel treatments are of great interest since they may treat both COPD and co-morbidities. Several novel agents are currently under...

  18. Erdosteine: antitussive and anti-inflammatory effects.

    Science.gov (United States)

    Dal Negro, Roberto W

    2008-01-01

    Erdosteine is a multifactorial drug currently used in COPD for its rheologic activity on bronchial secretions and its positive effects on bacterial adhesiveness. Erdosteine produces an active metabolite (Met 1) which was shown to produce antioxidant effects during the respiratory burst of human PMNs, due to the presence of an SH group. The substantial antitussive effects of erdosteine were first documented in clinical trials even though mucolytic agents are regarded as not consistently effective in ameliorating cough in patients with bronchitis, although they may be of benefit to this population in other ways. Actually, a mucolytic drug could exert antitussive effects if it also affects mucus consistency and enhances ciliary function. In the last decade, data from several studies on animal models pointed to the possible antitussive and anti-inflammatory properties of erdosteine and an indirect anti-inflammatory mechanism of action was suggested. Recently, data from some controlled versus placebo studies documented the antioxidant properties of erdosteine in humans and in current smokers with COPD. The mechanism of action was described as related to erdosteine's ability to inhibit some inflammatory mediators and some pro-inflammatory cytokines that are specifically involved in oxidative stress. As oxidative stress is also presumed to impair beta-adrenoceptor function and contribute to airway obstruction, specific controlled studies recently investigated the effect of antioxidant intervention on short-term airway response to salbutamol in nonreversible COPD, according to a double-blind design versus placebo and NAC. Only erdosteine consistently restored a significant short-term reversibility in COPD subjects, previously unresponsive to beta(2) adrenergics. This peculiar activity of erdosteine (to our knowledge never previously assessed) proved related to the ROS scavenging activity (which actually proved equal to that of N), and its significant inhibiting effect on

  19. Gochnatia polymorpha ssp. floccosa: bioprospecting of an anti-inflammatory phytotherapy for use during pregnancy.

    Science.gov (United States)

    David, Natan de; Mauro, Mariana de Oliveira; Gonçalves, Caroline Amélia; Pesarini, João Renato; Strapasson, Regiane Lauriano Batista; Kassuya, Cândida Aparecida Leite; Stefanello, Maria Élida Alves; Cunha-Laura, Andréa Luiza; Monreal, Antônio Carlos Duenhas; Oliveira, Rodrigo Juliano

    2014-06-11

    Gochnatia polymorpha ssp. floccosa is used in folk medicine to treat inflammation and infections. Non-steroidal anti-inflammatory drugs (NSAIDs) are the most commonly consumed medications during pregnancy in women with inflammatory diseases. However, the relationship between the use of NSAIDs and the risk of miscarriage and birth defects and/or benefits is not fully understood. Thus, an investigation regarding the use of Gochnatia polymorpha during gestation is of relevance for developing safe anti-inflammatory drugs for use during pregnancy. The pregnant females were randomly divided into 5 groups. Control group received a hydroalcoholic solution (1.2%), via gavage, for at least 15 days prior to mating and throughout the gestational period. The pre-treatment group received Gochnatia polymorpha ethanol extract (GPEE), via gavage, at a dose of 100mg/kg body weight (b.w.) for at least 15 days prior to mating and up to the appearance of the vaginal plug. The organogenesis group received GPEE at a dose of 100mg/kg (b.w.), via gavage, on the 5-15th gestacional day. The pregnancy group received GPEE at a dose of 100mg/kg (b.w.), via gavage, throughout the gestational period (from the 1st to the 18th day of pregnancy). The pre+pregnancy group received GPEE at a dose of 100mg/kg (b.w.), via gavage, for at least 15 days prior to mating and throughout the entire gestational period. The clinical signals of maternal toxicity and teratogenesis were evaluated. Additional assays to evaluate chronic inflammation, antigenotoxicity and immunomodolatory activity were performed. The results indicated that GPEE does not interfere with reproductive performance or embryo-fetal development but does correlate with reduced weight and fetal length. The extract was not teratogenic or mutagenic or an immunomodulator. However, GPEE did exhibit effective anti-inflammatory activity. Based on this study, it can be inferred that GPEE is an important, safe anti-inflammatory agent for use during

  20. Consumption and awareness of students about nonsteroidal anti-inflammatory drugs

    Directory of Open Access Journals (Sweden)

    Wawryk-Gawda Ewelina

    2014-09-01

    Full Text Available 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.

  1. Anti-inflammatory and bronchoprotective roles of endogenous prostaglandin E2

    Directory of Open Access Journals (Sweden)

    Hiroki Sakakibara

    1999-01-01

    Full Text Available Prostaglandin E2 (PGE2 is produced by resident cells in the airway, such as airway epithelial cells, airway smooth muscle cells and alveolar macrophages, and is always present in the airway. Various exogenous and endogenous stimuli cause immediate increases in PGE2 from several-fold to multiples of 10-fold. Prostaglandin E2 controls the function of cells that contribute to immune and inflammatory responses, such as lymphocytes, eosinophils, mast cells, macrophages and polymorphonuclear cells, and exhibits suppressor activity in the initial and advanced stages of allergic airway inflammation (establishment of sensitization, induction of early asthmatic response, chemotaxis of inflammatory cells and continuation of the late asthmatic response. Therefore, if the endogenous protective effects of PGE2 are weakened or absent, inflammation and hypersensitive responses readily occur in the airway. Although the effects of PGE2 remain to be clarified, the possibility of the involvement of decreased PGE2 activity in the pathogenesis of asthma exists. However, in aspirin-induced asthma the role of PGE2 as a protective factor, through an as yet undetermined mechanism, is marked. It is thought that, in this type of asthma, symptoms may be induced by the elimination of the protective action of PGE2 by non-steroidal anti-inflammatory drugs (NSAID. It is possible that PGE2 agonists that produce little airway irritation and drugs that raise the endogenous PGE2 level have potential as new types of anti-inflammatory or anti-asthma drugs.

  2. A novel pleiotropic effect of aspirin: Beneficial regulation of pro- and anti-inflammatory mechanisms in microglial cells.

    Science.gov (United States)

    Kata, Diana; Földesi, Imre; Feher, Liliana Z; Hackler, Laszlo; Puskas, Laszlo G; Gulya, Karoly

    2017-06-01

    Aspirin, one of the most widely used non-steroidal anti-inflammatory drugs, has extensively studied effects on the cardiovascular system. To reveal further pleiotropic, beneficial effects of aspirin on a number of pro- and anti-inflammatory microglial mechanisms, we performed morphometric and functional studies relating to phagocytosis, pro- and anti-inflammatory cytokine production (IL-1β, tumor necrosis factor-α (TNF-α) and IL-10, respectively) and analyzed the expression of a number of inflammation-related genes, including those related to the above functions, in pure microglial cells. We examined the effects of aspirin (0.1mM and 1mM) in unchallenged (control) and bacterial lipopolysaccharide (LPS)-challenged secondary microglial cultures. Aspirin affected microglial morphology and functions in a dose-dependent manner as it inhibited LPS-elicited microglial activation by promoting ramification and the inhibition of phagocytosis in both concentrations. Remarkably, aspirin strongly reduced the pro-inflammatory IL-1β and TNF-α production, while it increased the anti-inflammatory IL-10 level in LPS-challenged cells. Moreover, aspirin differentially regulated the expression of a number of inflammation-related genes as it downregulated such pro-inflammatory genes as Nos2, Kng1, IL1β, Ptgs2 or Ccr1, while it upregulated some anti-inflammatory genes such as IL10, Csf2, Cxcl1, Ccl5 or Tgfb1. Thus, the use of aspirin could be beneficial for the prophylaxis of certain neurodegenerative disorders as it effectively ameliorates inflammation in the brain. Copyright © 2017 Elsevier Inc. All rights reserved.

  3. Adiponectin: anti-inflammatory and cardioprotective effects.

    Science.gov (United States)

    Villarreal-Molina, M T; Antuna-Puente, B

    2012-10-01

    Adipose tissue is an endocrine organ that plays an essential role in regulating several metabolic functions through the secretion of biological mediators called "adipokines". Dysregulation of adipokines plays a crucial role in obesity-related diseases. Adiponectin (APN) is the most abundant adipokine accounting for the 0.01% of total serum protein, and is involved in a wide variety of physiological processes including energy metabolism, inflammation, and vascular physiology. APN plasma levels are reduced in individuals with obesity, type 2 diabetes and coronary artery disease, all traits with low-grade chronic inflammation. It is has been suggested that the absence of APN anti-inflammatory effects may be a contributing factor to this inflammation. APN inhibits the expression of tumor necrosis factor-α-induced endothelial adhesion molecules, macrophage-to-foam cell transformation, tumor necrosis factor-α expression in macrophages and adipose tissue, and smooth muscle cell proliferation. It also has anti-apoptotic and anti-oxidant effects, which play a role in its cardioprotective action. This review will focus on APN as an anti-inflammatory, anti-atherogenic and cardioprotective plasma protein. Copyright © 2012 Elsevier Masson SAS. All rights reserved.

  4. Biogenic antioxidative and anti-inflammatory aryl polyketides from the venerid bivalve clam Paphia malabarica.

    Science.gov (United States)

    Joy, Minju; Chakraborty, Kajal

    2017-12-15

    Chemical investigation of ethyl acetate-methanol extract of the venerid bivalve clam Paphia malabarica led to isolation of three unprecedented aryl polyketide derivatives, characterized as (E)-12-(17-ethyl-tetrahydro-16-hydroxy-15-(methyl pentanoate)-14-oxo-2H-pyran-13-yl)-9-methyl-but-11-enyl benzoate (1), isobutyl-13-(6-(benzoyloxy)-10-methylpentyl)-tetrahydro-13-methyl-2H-pyran-17-carboxylate (2) and (13-(methoxycarbonyl)-11-((E)-18-ethylhexa-16,19-dienyl)-12-propyl-cyclohex-10-enyl)-methyl-3-hydroxy benzoate (3). The structures of the polyketides were assigned by extensive spectroscopic experiments. Compound 1 displayed comparatively greater 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical quenching potential (50% inhibitory concentration, IC50 ∼0.59mg/mL) than commercially available α-tocopherol (IC50 0.63mg/mL). Potential pro-inflammatory 5-lipoxygenase (5-LOX) inhibition potential (IC50 0.76-0.92mg/mL) of the polyketides in consonant with significantly greater anti-inflammatory selectivity indices (anti-cyclooxygense-1IC50/anti-cyclooxygense-2IC50>1) than non-steroidal anti-inflammatory agent ibuprofen (0.44) described the safety profile of the title compounds. Putative biosynthetic route by means of polyketide synthatase biocatalyzed pathways unambiguously established the structural assignments of the previously undescribed polyketide analogues. The potential of hitherto undescribed polyketides from P. malabarica as natural antioxidative and anti-inflammatory functional food ingredients was demonstrated in the present study. Copyright © 2017 Elsevier Ltd. All rights reserved.

  5. Molecular docking, synthesis and biological screening of mefenamic acid derivatives as anti-inflammatory agents.

    Science.gov (United States)

    Savjani, Jignasa K; Mulamkattil, Suja; Variya, Bhavesh; Patel, Snehal

    2017-04-15

    Drug induced gastrointestinal ulceration, renal side effects and hepatotoxicity are the main causes of numerous Non-Steroidal Anti-inflammatory Drugs (NSAIDs). Cyclooxygenase-2 (COX-2) inhibitors discovered to decrease the gastrointestinal issues, but unfortunately, most of them are associated with major cardiovascular adverse effects. Along these lines, various new strategies and frameworks were developed wherein basic alterations of the present medications were accounted for. The aim of the study was to prepare derivatives of mefenamic acid to evaluate anti-inflammatory activity with fewer adverse reactions. In this study, molecular docking investigations of outlined derivatives were done utilizing Protein Data Bank (PDB ID-4PH9). Synthesis of heterocyclic compounds was carried out utilizing Dicyclohexylcarbodiimide/4-Dimethylaminopyridine (DCC/DMAP) coupling. Acute toxicity prediction was performed using free online GUSAR (General Unrestricted Structure-Activity Relationships) software. The study indicated most of the compounds under safe category. In-vitro pharmacological assessment of heterocyclic compounds was done for COX-1 and COX-2 enzymes for the determination of selectivity. In vivo pharmacological screening for anti-inflammatory activity and ED 50 value were determined utilizing carrageenan induced rat paw edema. Gastro intestinal safety study was carried out on selected compounds and found to be devoid of any gastric ulcer toxicity. Most of the compounds indicated high scores as compared to standard during molecular modelling, analysis and displayed interactions with active amino acids of a COX-2 enzyme. The pharmacological screening uncovered that compound substituted with p-bromophenyl indicated maximum potency. Copyright © 2017 Elsevier B.V. All rights reserved.

  6. Medicinal herbs as possible sources of anti-inflammatory products

    Directory of Open Access Journals (Sweden)

    Andreia Corciovă

    2017-12-01

    Full Text Available Plants constitute an inexhaustible source of bioactive compounds that can be valuable for research in the chemistry field of anti-inflammatory compounds. This review describes several plants from international and national flora that have been shown to have anti-inflammatory activity in various clinical trials. The paper includes: general aspects regarding the vegetal source, compounds responsible for anti-inflammatory activity, mechanism of action and clinical trials carried out with extracts or products containing standardized extracts.

  7. A Review on Anti-Inflammatory Activity of Monoterpenes

    Directory of Open Access Journals (Sweden)

    Damião Pergentino de Sousa

    2013-01-01

    Full Text Available Faced with the need to find new anti-inflammatory agents, great effort has been expended on the development of drugs for the treatment of inflammation. This disorder reduces the quality of life and overall average productivity, causing huge financial losses. In this review the anti-inflammatory activity of 32 bioactive monoterpenes found in essential oils is discussed. The data demonstrate the pharmacological potential of this group of natural chemicals to act as anti-inflammatory drugs.

  8. Anti-inflammatory and analgesic activities: Chemical constituents of ...

    African Journals Online (AJOL)

    Anti-inflammatory and analgesic activities: Chemical constituents of essential oils of Ocimum gratissimum , Eucalyptus citriodora and Cymbopogon giganteus inhibited lipoxygenase L-1 and cyclooxygenase of PGHS.

  9. Review of Anti-Inflammatory Herbal Medicines

    Directory of Open Access Journals (Sweden)

    Mona Ghasemian

    2016-01-01

    Full Text Available Medicinal plants and their secondary metabolites are progressively used in the treatment of diseases as a complementary medicine. Inflammation is a pathologic condition that includes a wide range of diseases such as rheumatic and immune-mediated conditions, diabetes, cardiovascular accident, and etcetera. We introduce some herbs which their anti-inflammatory effects have been evaluated in clinical and experimental studies. Curcuma longa, Zingiber officinale, Rosmarinus officinalis, Borago officinalis, evening primrose, and Devil’s claw are some of the introduced medicinal herbs in this review. Since the treatment of inflammation is not a one-dimensional remedy, this review tries to reach a multidimensional therapeutic approach to inflammation with the help of herbal medicine and modification in lifestyle.

  10. Anti-inflammatory ω-3 endocannabinoid epoxides.

    Science.gov (United States)

    McDougle, Daniel R; Watson, Josephine E; Abdeen, Amr A; Adili, Reheman; Caputo, Megan P; Krapf, John E; Johnson, Rodney W; Kilian, Kristopher A; Holinstat, Michael; Das, Aditi

    2017-07-25

    Clinical studies suggest that diets rich in ω-3 polyunsaturated fatty acids (PUFAs) provide beneficial anti-inflammatory effects, in part through their conversion to bioactive metabolites. Here we report on the endogenous production of a previously unknown class of ω-3 PUFA-derived lipid metabolites that originate from the crosstalk between endocannabinoid and cytochrome P450 (CYP) epoxygenase metabolic pathways. The ω-3 endocannabinoid epoxides are derived from docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA) to form epoxyeicosatetraenoic acid-ethanolamide (EEQ-EA) and epoxydocosapentaenoic acid-ethanolamide (EDP-EA), respectively. Both EEQ-EAs and EDP-EAs are endogenously present in rat brain and peripheral organs as determined via targeted lipidomics methods. These metabolites were directly produced by direct epoxygenation of the ω-3 endocannabinoids, docosahexanoyl ethanolamide (DHEA) and eicosapentaenoyl ethanolamide (EPEA) by activated BV-2 microglial cells, and by human CYP2J2. Neuroinflammation studies revealed that the terminal epoxides 17,18-EEQ-EA and 19,20-EDP-EA dose-dependently abated proinflammatory IL-6 cytokines while increasing anti-inflammatory IL-10 cytokines, in part through cannabinoid receptor-2 activation. Furthermore the ω-3 endocannabinoid epoxides 17,18-EEQ-EA and 19,20-EDP-EA exerted antiangiogenic effects in human microvascular endothelial cells (HMVEC) and vasodilatory actions on bovine coronary arteries and reciprocally regulated platelet aggregation in washed human platelets. Taken together, the ω-3 endocannabinoid epoxides' physiological effects are mediated through both endocannabinoid and epoxyeicosanoid signaling pathways. In summary, the ω-3 endocannabinoid epoxides are found at concentrations comparable to those of other endocannabinoids and are expected to play critical roles during inflammation in vivo; thus their identification may aid in the development of therapeutics for neuroinflammatory and

  11. Phytochemical, analgesic and anti-inflammatory studies of the ...

    African Journals Online (AJOL)

    Introduction: Commiphora mollis is used in African traditional medicine as analgesic, anti-inflammatory, antibacterial, anti-fungi, anti-oxidant as well as cytotoxic and cytostatic agent. Objective: To carry out phytochemical, analgesic and anti-inflammatory studies on the methanol leaf extract of Commiphora mollis. Methods: ...

  12. In vivo anti-inflammatory activity of Liquidambar formosana Hance ...

    African Journals Online (AJOL)

    Purpose: To evaluate the anti-inflammatory activity of Liquidambar formosana Hance infructescence (Liquidambaris fructus, ELF) in vivo, and clarify its underlying mechanisms. Methods: The in vivo anti-inflammatory activity of ELF was examined by xylene-induced ear swelling test in mice as well as carrageenan-induced ...

  13. Synthesis, Anti-inflammatory and Anti-nociceptive Evaluation of ...

    African Journals Online (AJOL)

    Synthesis, Anti-inflammatory and Anti-nociceptive Evaluation of Palmitoyl Benzamides. H Baba, CO Usifoh, PO Igbinaduwa. Abstract. Purpose: To synthesize and characterize palmitoyl amino benzamides, and to evaluate them for possible anti-inflammatory and anti-nociceptive activities. Methods: Palmitoyl amino ...

  14. Anti-inflammatory studies of yam (Dioscorea esculenta) extract on ...

    African Journals Online (AJOL)

    SERVER

    2007-08-20

    Aug 20, 2007 ... Anti-inflammatory studies of yam (Dioscorea esculenta) extract on wistar rats. J. O. Olayemi and E. O. Ajaiyeoba*. Department of Pharmacognosy, University of Ibadan, Ibadan, Nigeria. Accepted 4 July, 2007. The defatted methanol extract of Dioscorea esculenta tuber was evaluated for anti-inflammatory.

  15. Assessment of anti-inflammatory potential of Sesbania bispinosa ...

    African Journals Online (AJOL)

    Ganesh D. Boddawar

    2015-12-23

    Dec 23, 2015 ... anti-inflammatory activity in mice using acute and chronic anti-inflammatory models with aspirin as a reference drug. Materials and methods: Methanol, chloroform and hexane were used to prepare leaf extracts by soxhlet extraction method, while acetone, ethyl acetate and petroleum ether were used to ...

  16. Assessment of anti-inflammatory potential of Sesbania bispinosa ...

    African Journals Online (AJOL)

    ... S. bispinosa were evaluated for anti-inflammatory activity in mice using acute and chronic anti-inflammatory models with aspirin as a reference drug. Materials and methods: Methanol, chloroform and hexane were used to prepare leaf extracts by soxhlet extraction method, while acetone, ethyl acetate and petroleum ether ...

  17. Analgesic and anti-inflammatory effects of Crinum asiaticum leaf ...

    African Journals Online (AJOL)

    This study investigated the analgesic and anti-inflammatory effects of Crinum asiaticum (Amaryllidaceae) leaf ethanolic extract. Analgesic effect was investigated in acetic acid induced writhing model and formalin induced licking model in swiss albino mice. Anti-inflammatory effect was conducted in carrageenan-induced ...

  18. Investigation of anti-inflammatory lignans from the leaves of ...

    African Journals Online (AJOL)

    Purpose: To investigate the anti-inflammatory activity of Symplocos sumuntia Buch.-Ham. ex D. Don and identify the main secondary metabolites responsible for this effect. Methods: The in vitro anti-inflammatory activity of the plant extract and isolated compounds was determined in terms of the ability to inhibit the production ...

  19. Analgesic and anti-inflammatory effects of Cyphostemma vogelii (Hook

    African Journals Online (AJOL)

    Rita

    2013-04-24

    Apr 24, 2013 ... Choi E, Kwang J (2004). Anti-inflammatory, analgesic and anti-oxidant activities of the fruits of Foeniculum vulgare. Fitoterapia 75:557-565. Choi J, Jung HJ, Lee KT, Park HJ (2005). Antinociceptive and anti- inflammatory effects of saponins and sapogenins obtained from the stem of Akebia quinata. J. Med.

  20. Original Research Article In vivo Anti-Inflammatory Effect of ...

    African Journals Online (AJOL)

    Erah

    Fitoterapia. 2000; 72: 131-139. 20. Okoye FBC, Osadebe PO. Studies on the mechanisms of anti-inflammatory activity of the extracts and fractions of Alchornea floribunda leaves. Asian. Pac J Trop Med 2009; 2: 7-14. 21. Okoye FBC, Osadebe PO. A new anti-inflammatory flavonol glycoside from Alchornea floribunda leaves.

  1. Synthesis, characterization and anti-inflammatory evaluation of ...

    African Journals Online (AJOL)

    In order to explore the novel anti-inflammatory agents, some novel Trolox derivatives were synthesized and characterized by IR, 1H-NMR, 13C-NMR, mass and elemental analysis. The anti-inflammatory activities of the target compounds were evaluated via the croton oil-induced ear oedema test in Swiss mice. According to ...

  2. Comparative Anti-Inflammatory and Hepatoprotective Activities of ...

    African Journals Online (AJOL)

    The effects of AGHE and AGRE were compared with the standard drugs Phenylbutazone and silymarin, for anti-inflammatory and hepatoprotective activities respectively. Result: Both extracts showed significant anti-inflammatory activity (P< 0.001). AGRE showed comparatively more significant hepatoprotective activity (P< ...

  3. Cardiovascular effects and the use of nonsteroidal anti-inflammatory ...

    African Journals Online (AJOL)

    Nonsteroidal anti-inflammatory drugs (NSAIDs) include the nonselective and the cyclo-oxygenase-2-specific inhibitors. These agents are used for pain associated with musculoskeletal conditions. The nonselective anti-inflammatory drugs are still widely used, and are also freely available as over-the-counter analgesics.

  4. Anti-inflammatory and immunomodulatory properties of Carica papaya.

    Science.gov (United States)

    Pandey, Saurabh; Cabot, Peter J; Shaw, P Nicholas; Hewavitharana, Amitha K

    2016-07-01

    Chronic inflammation is linked with the generation and progression of various diseases such as cancer, diabetes and atherosclerosis, and anti-inflammatory drugs therefore have the potential to assist in the treatment of these conditions. Carica papaya is a tropical plant that is traditionally used in the treatment of various ailments including inflammatory conditions. A literature search was conducted by using the keywords "papaya", "anti-inflammatory and inflammation" and "immunomodulation and immune" along with cross-referencing. Both in vitro and in vivo investigation studies were included. This is a review of all studies published since 2000 on the anti-inflammatory activity of papaya extracts and their effects on various immune-inflammatory mediators. Studies on the anti-inflammatory activities of recognized phytochemicals present in papaya are also included. Although in vitro and in vivo studies have shown that papaya extracts and papaya-associated phytochemicals possess anti-inflammatory and immunomodulatory properties, clinical studies are lacking.

  5. Anti-inflammatory coumarins from Paramignya trimera.

    Science.gov (United States)

    Tuan Anh, Hoang Le; Kim, Dong-Cheol; Ko, Wonmin; Ha, Tran Minh; Nhiem, Nguyen Xuan; Yen, Pham Hai; Tai, Bui Huu; Truong, Luu Hong; Long, Vu Ngoc; Gioi, Tran; Hong Quang, Tran; Minh, Chau Van; Oh, Hyuncheol; Kim, Youn-Chul; Kiem, Phan Van

    2017-12-01

    Paramignya trimera (Oliv.) Burkill (Rutaceae) has been used to treat liver diseases and cancer. However, the anti-inflammatory effects of this medicinal plant and its components have not been elucidated. This study investigated chemical constituents of the P. trimera stems and evaluated anti-inflammatory effects of isolated compounds. Cytotoxicity of isolated compounds (5-40 μM) toward BV2 cells was tested using 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) for 24 h. Inhibitory effects of isolated compounds (5-40 μM) on nitrite and PGE2 concentrations were determined using Griess reaction and PGE2 ELISA kit, respectively (pretreated with the compounds for 3 h and then stimulated for 18 h with LPS). Inhibitory effects of compounds (5-40 μM) on iNOS and COX-2 protein expression were evaluated by Western blot analysis (pretreated with the compounds for 3 h and then stimulated for 24 h with LPS). Seven coumarins were isolated and identified as: ostruthin (1), ninhvanin (2), 8-geranyl-7-hydroxycoumarin (3), 6-(6',7'-dihydroxy-3',7'-dimethylocta-2'-enyl)-7-hydroxycoumarin (4), 6-(7-hydroperoxy-3,7-dimethylocta-2,5-dienyl)-7-hydroxycoumarin (5), 6-(2-hydroxyethyl)-2,2-dimethyl-2H-1-benzopyran (6), and luvangetin (7). Compounds 1-4 and 7 inhibited NO and PGE2 production in LPS-stimulated BV2 cells, with IC50 values ranging from 9.8 to 46.8 and from 9.4 to 52.8 μM, respectively. Ostruthin (1) and ninhvanin (2) were shown to suppress LPS-induced iNOS and COX-2 protein expression. The present study provides a scientific rationale for the use of P. trimera in the prevention and treatment of neuroinflammatory diseases. Ostruthin and ninhvanin might have potential therapeutic effects and should be considered for further development as new anti-neuroinflammatory agents.

  6. Association of terpinolene and diclofenac presents antinociceptive and anti-inflammatory synergistic effects in a model of chronic inflammation

    Directory of Open Access Journals (Sweden)

    E.M.A. Macedo

    2016-01-01

    Full Text Available Pharmacological treatment of inflammatory pain is usually done by administration of non-steroidal anti-inflammatory drugs (NSAIDs. These drugs present high efficacy, although side effects are common, especially gastrointestinal lesions. One of the pharmacological strategies to minimize such effects is the combination of drugs and natural products with synergistic analgesic effect. The monoterpene terpinolene (TPL is a chemical constituent of essential oils present in many plant species, which have pharmacological activities, such as analgesic and anti-inflammatory. The association of ineffective doses of TPL and diclofenac (DCF (3.125 and 1.25 mg/kg po, respectively presented antinociceptive and anti-inflammatory effects in the acute (0, 1, 2, 3, 4, 5 and 6 h, after treatment and chronic (10 days inflammatory hyperalgesia induced by Freund's complete adjuvant (CFA in the right hind paw of female Wistar rats (170-230 g, n=6-8. The mechanical hyperalgesia was assessed by the Randall Selitto paw pressure test, which determines the paw withdrawal thresholds. The development of edema was quantified by measuring the volume of the hind paw by plethismography. The TPL/DCF association reduced neutrophils, macrophages and lymphocytes in the histological analysis of the paw, following a standard staining protocol with hematoxylin and eosin and the counts were performed with the aid of optical microscopy after chronic oral administration of these drugs. Moreover, the TPL/DCF association did not induce macroscopic gastric lesions. A possible mechanism of action of the analgesic effect is the involvement of 5-HT2A serotonin receptors, because ketanserin completely reversed the antinociceptive effect of the TPL/DCF association. These results suggest that the TPL/DCF association had a synergistic anti-inflammatory and analgesic effect without causing apparent gastric injury, and that the serotonergic system may be involved in the antinociceptive effect of this

  7. Cutaneous reactions to analgesic-antipyretics and nonsteroidal anti-inflammatory drugs. Analysis of reports to the spontaneous reporting system of the Gruppo Italiano Studi Epidemiologici in Dermatologia.

    Science.gov (United States)

    1993-01-01

    We analyzed the cutaneous reactions to systemic analgesic-antipyretics and non-steroidal anti-inflammatory drugs reported to the spontaneous reporting system of the Gruppo Italiano Studi Epidemiologici in Dermatologia (GISED). The system has been active since 1988, with periodic intensive surveillance exercises, and 202 dermatologists have collaborated. Up to December 1991, 2,137 reactions had been collected, of which 713 were reactions to systemic analgesic-antipyretics and nonsteroidal anti-inflammatory drugs. A general profile of the reactions was identifiable. It included, in order of frequency, urticaria/angioedema, fixed eruptions, exanthemas, erythema multiforme and Stevens Johnson syndrome. Fixed eruptions and Stevens Johnson syndrome were reported with exceedingly high frequency in association with feprazone. Our system also revealed previously unreported reactions, including fixed eruption to nimesulide, fixed eruption to piroxicam and fixed eruption to flurbiprofen.

  8. No effect of anti-inflammatory medication on postprandial and postexercise muscle protein synthesis in elderly men with slightly elevated systemic inflammation

    DEFF Research Database (Denmark)

    Dideriksen, Kasper Juel; Reitelseder, Søren; Malmgaard-Clausen, Nikolai Mølkjær

    2016-01-01

    BACKGROUND: Based on circulating C-reactive protein (CRP) levels, some individuals develop slightly increased inflammation as they age. In elderly inflamed rats, the muscle response to protein feeding is impaired, whereas it can be maintained by treatment with non-steroidal anti-inflammatory drugs...... maintained in inflamed elderly compared to healthy controls (p>0.05) and so was p70S6K phosphorylation. Moreover, NSAID treatment did not significantly improve the myofibrillar and connective tissue FSR responses or reduce the plasma CRP level in inflamed, elderly individuals (p>0.05). CONCLUSION: A slight...

  9. Pharmacological interactions of anti-inflammatory-analgesics in odontology

    National Research Council Canada - National Science Library

    Gómez-Moreno, Gerardo; Guardia, Javier; Cutando, Antonio; Calvo-Guirado, José Luis

    2009-01-01

    In this second article we describe the more interesting pharmacological interactions in dental practice based on the prescription of analgesic narcotics, paracetamol and non-selective non-steroid anti...

  10. Anti-inflammatory evaluation of immature fruit and seed aqueous ...

    African Journals Online (AJOL)

    Anti-inflammatory evaluation of immature fruit and seed aqueous extracts from several populations of Tunisian Citrullus colocynthis Schrad. B Marzouk, Z Marzouk, E Haloui, M Turki, A Bouraoui, M Aouni, N Fenina ...

  11. Biochemical pharmacology of biflavonoids: implications for anti-inflammatory action.

    Science.gov (United States)

    Kim, Hyun Pyo; Park, Haeil; Son, Kun Ho; Chang, Hyeun Wook; Kang, Sam Sik

    2008-03-01

    Biflavonoids belong to a subclass of the plant flavonoid family. Distribution of biflavonoids in the plant kingdom is limited to several species. Previously, some pharmacological activities of biflavonoids were described such as inhibition of histamine release from mast cells and inhibition of lymphocyte proliferation, suggesting the anti-inflammatory/antiallergic potential of the biflavonoids. Furthermore, several natural biflavonoids including ochnaflavone and ginkgetin inhibit phospholipase A2. Most importantly, certain biflavonoids exhibit anti-inflammatory activity through the regulation of proinflammatory gene expression in vitro and in vivo. Recently, several synthetic approaches yielded new biflavonoid molecules with anti-inflammatory potential. These molecules also exhibit phospholipase A2 and cyclooxygenase-2 inhibitory activity. Although the bioavailability needs be improved, certain biflavonoids may have potential as new anti-inflammatory agents. This is the first review of biflavonoid pharmacology to date.

  12. Anti-inflammatory and analgesic activities of Melanthera scandens

    Science.gov (United States)

    Okokon, Jude E; Udoh, Anwanga E; Frank, Samuel G; Amazu, Louis U

    2012-01-01

    Objective To evaluate the anti-inflammatory and analgesic activities of leaf extract of Melanthera scandens (M. scandens). Methods The crude leaf extract (39–111 mg/kg) of M. scandens was investigated for anti-inflammatory and analgesic activities using various experimental models. The anti-inflammatory activity was investigated using carragenin, egg-albumin induced oedema models, while acetic acid, formalin-induced paw licking and thermal-induced pain models were used to evaluate the antinociceptive property. Results The extract caused a significant (P<0.05 – 0.001) dose-dependent reduction of inflammation and pains induced by different agents used. Conclusions The leaf extract possesses anti-inflammatory and analgesic effects which may be mediated through the phytochemical constituents of the plant. PMID:23569885

  13. Nonsteroidal anti-inflammatory drugs: adverse effects and their prevention.

    NARCIS (Netherlands)

    Vonkeman, Harald Erwin; van de Laar, Mart A F J

    2010-01-01

    Objectives: To discuss nonsteroidal anti-inflammatory drugs (NSAIDs), their history, development, mode of action, toxicities, strategies for the prevention of toxicity, and future developments. - Methods: Medline search for articles published up to 2007, using the keywords acetylsalicylic acid,

  14. Anti-inflammatory polymer electrodes for glial scar treatment

    National Research Council Canada - National Science Library

    Maria eAsplund; Christian eBoehler; Thomas eStieglitz

    2014-01-01

    .... A micron thick coating, deposited on the surface of a regular metallic electrode, can elute anti-inflammatory drugs for the treatment of glial scarring as well as growth factors for the support of surrounding neurons...

  15. Evaluation Of Analgesic And Anti-Inflammatory Activity Of Diospyros ...

    African Journals Online (AJOL)

    0.01) activity against all phlogistic agents used in a dose dependent manner. All these effects were compared with reference drug phenylbutazone (100 mg/kg body weight). Keywords: Diospyros cordifolia, analgesic, anti-inflammatory.

  16. Synthesis and anti-inflammatory activity of chalcone derivatives.

    Science.gov (United States)

    Herencia, F; Ferrándiz, M L; Ubeda, A; Domínguez, J N; Charris, J E; Lobo, G M; Alcaraz, M J

    1998-05-19

    Chalcones and their derivatives were synthesized and evaluated for their anti-inflammatory activity. In vitro, chalcones 2, 4, 8, 10 and 13 inhibited degranulation and 5-lipoxygenase in human neutrophils, whereas 11 behaved as scavenger of superoxide. Only four compounds (4-7) inhibited cyclo-oxygenase-2 activity. The majority of these samples showed anti-inflammatory effects in the mouse air pouch model.

  17. Multiresidue Screening of Veterinary Drugs in Meat, Milk, Egg, and Fish Using Liquid Chromatography Coupled with Ion Trap Time-of-Flight Mass Spectrometry.

    Science.gov (United States)

    Kang, JeongWoo; Park, Su-Jeong; Park, Hae-Chul; Hossain, Md Akil; Kim, Myeong-Ae; Son, Seong-Wan; Lim, Chae-Mi; Kim, Tae-Wan; Cho, Byung-Hoon

    2017-06-01

    New approaches to veterinary drug screening based on liquid chromatography-mass spectrometry (LC-MS/MS) and time-of-flight mass spectrometry (ToF/MS) are rapid and have high selectivity and sensitivity. In this study, we developed a multiresidue method for screening over 100 veterinary drug residues using ion trap (IT)-ToF/MS. The screened compounds comprised major drug classes used in veterinary practice, representing the following: amphenicols, anthelmintics, benzimidazoles, β-lactams, coccidiostats, ionophores, macrolides, non-steroidal anti-inflammatory drugs, quinolones, sulfonamides, tetracyclines, and tranquilizers. The method was developed based on chromatographic retention time, specific accurate mass, isotope distribution, and fragment data. Each compound was validated at three levels, and the mass accuracy, accuracy, and repeatability were calculated. All parameters showed acceptable values and conformed to the Commission Decision 2002/657/EC criteria. This screening method can simultaneously analyze over 100 veterinary drugs in meat, milk, eggs, and fish in a single analytical run.

  18. COX-independent mechanisms of cancer chemoprevention by anti-inflammatory drugs

    Directory of Open Access Journals (Sweden)

    Evrim eGurpinar

    2013-07-01

    Full Text Available Epidemiological and clinical studies suggest that non-steroidal anti-inflammatory drugs (NSAIDs, including cyclooxygenase (COX-2 selective inhibitors, reduce the risk of developing cancer. Experimental studies in human cancer cell lines and rodent models of carcinogenesis support these observations by providing strong evidence for the antineoplastic properties of NSAIDs. The involvement of COX-2 in tumorigenesis and its overexpression in various cancer tissues suggest that inhibition of COX-2 is responsible for the chemopreventive efficacy of these agents. However, the precise mechanisms by which NSAIDs exert their antiproliferative effects are still a matter of debate. Numerous other studies have shown that NSAIDs can act through COX-independent mechanisms. This review provides a detailed description of the major COX-independent molecular targets of NSAIDs and discusses how these targets may be involved in their anticancer effects. Toxicities resulting from COX inhibition and the suppression of prostaglandin synthesis preclude the long-term use of NSAIDs for cancer chemoprevention. Furthermore, chemopreventive efficacy is incomplete and treatment often leads to the development of resistance. Identification of alternative NSAID targets and elucidation of the biochemical processes by which they inhibit tumor growth could lead to the development of safer and more efficacious drugs for cancer chemoprevention.

  19. Effects of anti-inflammatory drugs in primary kidney cell culture of a freshwater fish.

    Science.gov (United States)

    Ribas, João Luiz Coelho; da Silva, Cesar A; de Andrade, Lucas; Galvan, Gabrieli Limberger; Cestari, Marta Margarete; Trindade, Edvaldo S; Zampronio, Aleksander R; de Assis, Helena C Silva

    2014-09-01

    The non-steroidal anti-inflammatory drugs are emerging contaminants in aquatic ecosystems. This study aimed to evaluate toxic effects of some representative drugs of this pharmaceutical group on primary culture of monocytic lineage of Hoplias malabaricus anterior kidney. The effects of diclofenac, acetaminophen and ibuprofen in cell viability, lipopolysaccharide (LPS)-induced NO production and genotoxicity were evaluated. Cytometry analysis CD11b(+) cells showed 71.5% of stem cells, 19.5% of macrophages and 9% of monocytes. Cell viability was lower in the ficoll compared to percoll separation. LPS-induced NO production by these cells was blocked after treatment with dexamethasone and NG-Methyl-L-Arginine (L-NMMA). Exposure of the cells to diclofenac (0.2-200 ng/mL), acetaminophen (0.025-250 ng/mL) ibuprofen (10-1000 ng/mL) reduced basal NO production and inhibited LPS-induced NO production at all concentrations after 24 h of exposure. Genotoxicity occurred at the highest concentration of diclofenac and at the intermediary concentration of acetaminophen. Genotoxicity was also observed by ibuprofen. In summary, the pharmaceuticals influenced NO production and caused DNA damage in monocytic cells suggesting that these drugs can induce immunosuppression and genotoxicity in fish. Copyright © 2014. Published by Elsevier Ltd.

  20. Quantitative analysis of anti-inflammatory drugs using FTIR-ATR spectrometry

    Science.gov (United States)

    Hassib, Sonia T.; Hassan, Ghaneya S.; El-Zaher, Asmaa A.; Fouad, Marwa A.; Taha, Enas A.

    2017-11-01

    Four simple, accurate, sensitive and economic Attenuated Total Reflectance-Fourier Transform Infrared Spectroscopic (ATR-FTIR) methods have been developed for the quantitative estimation of some non-steroidal anti-inflammatory drugs. The first method involves the determination of Etodolac by direct measurement of the absorbance at 1716 cm- 1. In the second method, the second derivative of the IR spectra of Tolfenamic acid and its reported degradation product (2-chlorobenzoic acid) was used and the amplitudes were measured at 1084.27 cm- 1 and 1056.02 cm- 1 for Tolfenamic acid and 2-chlorobenzoic acid, respectively. The third method used the first derivative of the IR spectra of Bumadizone and its reported degradation product, N,N-diphenylhydrazine and the amplitudes were measured at 2874.98 cm- 1 and 2160.32 cm- 1 for Bumadizone and N,N-diphenylhydrazine, respectively. The fourth method depends on measuring the amplitude of Diacerein at 1059.18 cm- 1 and of rhein, its reported degradation product, at 1079.32 cm- 1 in their first derivative spectra. The four methods were successfully applied on the pharmaceutical formulations by extracting the active constituent in chloroform and the extract was directly measured in liquid phase mode using a specific cell. Moreover, validation of these methods was carried out following International Conference of Harmonisation (ICH) guidelines.

  1. Synthesis, antinociceptive and anti-inflammatory effects of porphyrins.

    Science.gov (United States)

    Alonso-Castro, Angel Josabad; Zapata-Morales, Juan Ramón; Hernández-Munive, Abigail; Campos-Xolalpa, Nimsi; Pérez-Gutiérrez, Salud; Pérez-González, Cuauhtémoc

    2015-05-15

    Porphyrins are natural compounds with several biological activities. We report the synthesis and the evaluation of the anti-inflammatory and antinociceptive effects of 4 porphyrins: 5,10,15,20-tetraphenylporphyrin (TPP), 5,10,15,20-tetra(4'-fluorophenyl)porphyrin (TpFPP), 5,10,15,20-tetra(4'-chlorophenyl)porphyrin (TpClPP), and 5,10,15,20-tetra(4'-bromophenyl)porphyrin (TpBrPP). The in vitro anti-inflammatory effects were evaluated on heat-induced hemolysis. The antinociceptive effects were evaluated using the hot plate and formalin tests. The in vivo anti-inflammatory assays were tested on the acute and chronic TPA (12-O-tetradecanoylphorbol 13-acetate) method to induce ear edema. The anti-arthritic effects were evaluated using carrageenan kaolin induced arthritis (CKIA). All porphyrins inhibited hemolysis with similar potency than naproxen (NPX). In the antinociceptive tests, all porphyrins tested at 200mg/kg showed similar effects compared to 100mg/kg NPX. In the in vivo anti-inflammatory acute assay, only three porphyrins (TPP, TpFPP and TpBrPP) decreased inflammation with similar activity than 2mg/ear indomethacin (IND). Further anti-inflammatory experiments were carried out with TPP, TpFPP and TpBrPP. In the in vivo anti-inflammatory chronic assay, porphyrins decreased inflammation with similar activity than 8mg/kg IND. Porphyrins tested at 200mg/kg showed anti-arthritic effects. The antinociceptive, anti-inflammatory and arthritic activities of porphyrins suggest that these compounds might be a good alternative for the treatment of inflammatory diseases. Copyright © 2015 Elsevier Ltd. All rights reserved.

  2. Effect of anti-inflammatory agents on transforming growth factor beta over-expressing mouse brains: a model revised

    Directory of Open Access Journals (Sweden)

    Landreth Gary E

    2004-07-01

    Full Text Available Abstract Background The over-expression of transforming growth factor β-1(TGF-β1 has been reported to cause hydrocephalus, glia activation, and vascular amyloidβ (Aβ deposition in mouse brains. Since these phenomena partially mimic the cerebral amyloid angiopathy (CAA concomitant to Alzheimer's disease, the findings in TGF-β1 over-expressing mice prompted the hypothesis that CAA could be caused or enhanced by the abnormal production of TGF-β1. This idea was in accordance with the view that chronic inflammation contributes to Alzheimer's disease, and drew attention to the therapeutic potential of anti-inflammatory drugs for the treatment of Aβ-elicited CAA. We thus studied the effect of anti-inflammatory drug administration in TGF-β1-induced pathology. Methods Two-month-old TGF-β1 mice and littermate controls were orally administered pioglitazone, a peroxisome proliferator-activated receptor-γ agonist, or ibuprofen, a non steroidal anti-inflammatory agent, for two months. Glia activation was assessed by immunohistochemistry and western blot analysis; Aβ precursor protein (APP by western blot analysis; Aβ deposition by immunohistochemistry, thioflavin-S staining and ELISA; and hydrocephalus by measurements of ventricle size on autoradiographies of brain sections. Results are expressed as means ± SD. Data comparisons were carried with the Student's T test when two groups were compared, or ANOVA analysis when more than three groups were analyzed. Results Animals displayed glia activation, hydrocephalus and a robust thioflavin-S-positive vascular deposition. Unexpectedly, these deposits contained no Aβ or serum amyloid P component, a common constituent of amyloid deposits. The thioflavin-S-positive material thus remains to be identified. Pioglitazone decreased glia activation and basal levels of Aβ42- with no change in APP contents – while it increased hydrocephalus, and had no effect on the thioflavin-S deposits. Ibuprofen mimicked

  3. Anti-inflammatory Chitosan/Poly-γ-glutamic acid nanoparticles control inflammation while remodeling extracellular matrix in degenerated intervertebral disc.

    Science.gov (United States)

    Teixeira, Graciosa Q; Leite Pereira, Catarina; Castro, Flávia; Ferreira, Joana R; Gomez-Lazaro, Maria; Aguiar, Paulo; Barbosa, Mário A; Neidlinger-Wilke, Cornelia; Goncalves, Raquel M

    2016-09-15

    Intervertebral disc (IVD) degeneration is one of the most common causes of low back pain (LBP), the leading disorder in terms of years lived with disability. Inflammation can play a role in LPB, while impairs IVD regeneration. In spite of this, different inflammatory targets have been purposed in the context of IVD regeneration. Anti-inflammatory nanoparticles (NPs) of Chitosan and Poly-(γ-glutamic acid) with a non-steroidal anti-inflammatory drug, diclofenac (Df), were previously shown to counteract a pro-inflammatory response of human macrophages. Here, the effect of intradiscal injection of Df-NPs in degenerated IVD was evaluated. For that, Df-NPs were injected in a bovine IVD organ culture in pro-inflammatory/degenerative conditions, upon stimulation with needle-puncture and interleukin (IL)-1β. Df-NPs were internalized by IVD cells, down-regulating IL-6, IL-8, MMP1 and MMP3, and decreasing PGE2 production, compared with IL-1β-stimulated IVD punches. Interestingly, at the same time, Df-NPs promoted an up-regulation of extracellular matrix (ECM) proteins, namely collagen type II and aggrecan. Allover, this study suggests that IVD treatment with Df-NPs not only reduces inflammation, but also delays and/or decreases ECM degradation, opening perspectives to new intradiscal therapies for IVD degeneration, based on the modulation of inflammation. Degeneration of the IVD is an age-related progressive process considered to be the major cause of spine disorders. The pro-inflammatory environment and biomechanics of the degenerated IVD is a challenge for regenerative therapies. The novelty of this work is the intradiscal injection of an anti-inflammatory therapy based on Chitosan (Ch)/Poly-(γ-glutamic acid) (γ-PGA) nanoparticles (NPs) with an anti-inflammatory drug (diclofenac, Df), previously developed by us. This drug delivery system was tested in a pro-inflammatory/degenerative intervertebral disc ex vivo model. The main findings support the success of an anti-inflammatory

  4. Role of APOE and Age at Enrollment in the Alzheimer’s Disease Anti-Inflammatory Prevention Trial (ADAPT

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    Lea T. Drye

    2012-08-01

    Full Text Available Background: The Alzheimer’s Disease Anti-inflammatory Prevention Trial (ADAPT tested whether non-steroidal anti-inflammatory drugs (NSAIDs can prevent Alzheimer’s disease (AD. The results were null. We analyzed ADAPT data to examine if the effects of NSAIDs on AD risk differed depending upon APOE genotype or age as has been suggested by previous observational studies. Methods: ADAPT randomized 2,528 cognitively intact older adults to either celecoxib, naproxen sodium or placebo; 2,388 participants provided blood samples for APOE genotyping. Proportional hazards regression was used to estimate the effects of naproxen or celecoxib versus placebo on incident AD by age at enrollment and APOE genotype. Results: The proportion of subjects providing a biological sample did not differ between the treatment groups. In models of AD risk, none of the tests for 2-way interactions between either NSAID and age or APOE genotype were significant (p > 0.05. Conclusions: The data did not support the hypothesis that the association between NSAIDs and AD risk differed by age or APOE genotype.

  5. Lead Structures for Applications in Photodynamic Therapy. 6. Temoporfin Anti-Inflammatory Conjugates to Target the Tumor Microenvironment for In Vitro PDT.

    Directory of Open Access Journals (Sweden)

    Luke Rogers

    Full Text Available Due to the ongoing development of clinical photodynamic therapy (PDT, the search continues for optimized photosensitizers that can overcome some of the side effects associated with this type of treatment modality. The main protagonists being: post-treatment photosensitivity, due to only limited cellular selectivity and post-treatment tumor regrowth, due to the up-regulation of pro-inflammatory agents within the tumor microenvironment. A photosensitizer that could overcome one or both of these drawbacks would be highly attractive to those engaged in clinical PDT. Certain non-steroidal anti-inflammatory drugs (NSAIDs when used in combination with PDT have shown to increase the cytotoxicity of the treatment modality by targeting the tumor microenvironment. Temoporfin (m-THPC, the gold standard chlorin-based photosensitizer (PS since its discovery in the 1980's, has successfully been conjugated to non-steroidal anti-inflammatory compounds, in an attempt to address the issue of post-treatment tumor regrowth. Using a modified Steglich esterification reaction, a library of "iPorphyrins" was successfully synthesized and evaluated for their PDT efficacy.

  6. Anti-inflammatory treatment and risk of depression in 91,842 patients with acute coronary syndrome and 91,860 individuals without acute coronary syndrome in Denmark

    DEFF Research Database (Denmark)

    Wium-Andersen, Ida Kim; Wium-Andersen, Marie Kim; Jørgensen, Martin Balslev

    2017-01-01

    Background We examined if treatment with acetylsalicylic acid (ASA), non-steroid anti-inflammatory drugs (NSAID), or statins after acute coronary syndrome (ACS) are associated with decreased risk of depression. Method This register-based cohort study included all individuals with a first-time hos......Background We examined if treatment with acetylsalicylic acid (ASA), non-steroid anti-inflammatory drugs (NSAID), or statins after acute coronary syndrome (ACS) are associated with decreased risk of depression. Method This register-based cohort study included all individuals with a first......-time hospital admissions with an ACS diagnosis registered between January 2001 to December 2009 (N = 91,842) and a comparable reference population without ACS (N = 91,860). Information of ASA, NSAID, and statin use were retrieved from a national prescription register. The study population was followed...... for hospitalization with depression or receiving prescription of antidepressant medication for up to one year after ACS or study entry (early depression) or one to twelve years after ACS or study entry (late depression). Results ASA use after ACS was associated with decreased risk of early depression with hazard...

  7. Biogenic guaianolide-type sesquiterpene lactones with antioxidative and anti-inflammatory properties from natural mangrove hybrid Rhizophora annamalayana.

    Science.gov (United States)

    Raola, Vamshi Krishna; Chakraborty, Kajal

    2017-12-01

    Previously undescribed guaianolide-type sesquiterpene lactones were isolated from the chloroform fraction of the natural hybrid mangrove Rhizophora annamalayana, and were characterised as (Z)-3α,4,5,6-tetrahydro-5α-isobutyl-2β-(methoxymethyl)-7-methyl-3H-cyclohepta[b]carbolactone (1) and (7Z)-isopentyl 3α,4,5,6,7,8-hexahydro-2β-((E)-11-methylbut-10-enyl)-1-oxo-2H-cyclohepta[b]furan-6-carboxylate (2). Compound 2 displayed greater antioxidative activities {1, 1-diphenyl-2-picrylhydrazyl (DPPH) and 2, 2'-azino-bis-3 ethylbenzothiozoline-6-sulphonic acid diammonium salt (ABTS), IC 50 0.65 and 0.62 mg/mL, respectively)} compared to 1 (IC 50 0.83 and 1.14 mg/mL, respectively) (p < 0.05). Compound 2 recorded no significant difference in DPPH . scavenging activities (IC 50 0.65 mg/mL) compared to α-tocopherol (IC 50 0.63 mg/mL). Pro-inflammatory 5-lipoxygenase inhibitory activity of 2 was found to be comparable (IC 50 0.98 mg/mL) to that displayed by synthetic anti-inflammatory drug ibuprofen (IC 50 0.93 mg/mL). Compound 2 showed significantly greater selectivity index (anti-cyclooxygenase-1/anti-cyclooxygenase-2 = 2.15) than non-steroidal anti-inflammatory ibuprofen (<0.5) (p < 0.05), and therefore, might be used as selective cyclooxygenase-2 inhibitor. The hitherto undescribed guaianolide lactones might be used as potential anti-inflammatory and antioxidative pharmacophore leads.

  8. Anti-inflammatory activity of root of Alpinia galanga willd

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    Asim Kumar Ghosh

    2011-01-01

    Full Text Available Objective: The objective of the study is to evaluate the acute and chronic anti-inflammatory activities of root extract of Alpinia galanga in rodents. Materials and Methods: The study was carried out using albino rats of either sex (150-200 g. An extract of the root of A. galanga was prepared using absolute alcohol and distillation in a Soxhlet apparatus. The acute anti-inflammatory effects of this extract were evaluated using carrageenan-, bradykinin-, and 5-HT-induced rat paw edema. The chronic anti-inflammatory effects were evaluated using formaldehyde-induced rat paw edema. Results and Analysis: Inhibition of inflammation was seen to be 32.22% in carrageenan-induced, 37.70% in 5-HT-induced, and 35.21% in bradykinin-induced anti-inflammatory models. In chronic inflammatory model, a progressive inhibition of 34.73% (3 rd day, 37.50% (5 th day, 38.83% (7 th day, 44.66% (9 th day, 49.59% (11 th day, and 55.75% (13 th day was observed with study compound. The efficacy was comparable with the standard drugs. Conclusion: It can be thus concluded that A. galanga has anti-inflammatory properties and probably acts by blocking histaminic and serotonin pathways. It may be an effective alternative to NASAIDs and corticosteroid in inflammatory disorders.

  9. Anti-inflammatory activity of Bromelia hieronymi: comparison with bromelain.

    Science.gov (United States)

    Errasti, María E; Caffini, Néstor O; Pelzer, Lilian E; Rotelli, Alejandra E

    2013-03-01

    Some plant proteases (e. g., papain, bromelain, ficin) have been used as anti-inflammatory agents for some years, and especially bromelain is still being used as alternative and/or complementary therapy to glucocorticoids, nonsteroidal antirheumatics, and immunomodulators. Bromelain is an extract rich in cysteine endopeptidases obtained from Ananas comosus. In this study the anti-inflammatory action of a partially purified extract of Bromelia hieronymi fruits, whose main components are cysteine endopeptidases, is presented. Different doses of a partially purified extract of B. hieronymi were assayed on carrageenan-induced and serotonine-induced rat paw edema, as well as in cotton pellet granuloma model. Doses with equal proteolytic activity of the partially purified extract and bromelain showed significantly similar anti-inflammatory responses. Treatment of the partially purified extract and bromelain with E-64 provoked loss of anti-inflammatory activity on carrageenan-induced paw edema, a fact which is consistent with the hypothesis that the proteolytic activity would be responsible for the anti-inflammatory action. Georg Thieme Verlag KG Stuttgart · New York.

  10. Analgesic and Anti-Inflammatory Activity of Pinus roxburghii Sarg.

    Directory of Open Access Journals (Sweden)

    Dhirender Kaushik

    2012-01-01

    Full Text Available The Chir Pine, Pinus roxburghii, named after William Roxburgh, is a pine native to the Himalaya. Pinus roxburghii Sarg. (Pinaceae is traditionally used for several medicinal purposes in India. As the oil of the plant is extensively used in number of herbal preparation for curing inflammatory disorders, the present study was undertaken to assess analgesic and anti-inflammatory activities of its bark extract. Dried and crushed leaves of Pinus roxburghii Sarg. were defatted with petroleum ether and then extracted with alcohol. The alcoholic extract at the doses of 100 mg/kg, 300 mg/kg, and 500 mg/kg body weight was subjected to evaluation of analgesic and anti-inflammatory activities in experimental animal models. Analgesic activity was evaluated by acetic acid-induced writhing and tail immersion tests in Swiss albino mice; acute and chronic anti-inflammatory activity was evaluated by carrageenan-induced paw oedema and cotton pellet granuloma in Wistar albino rats. Diclofenac sodium and indomethacin were employed as reference drugs for analgesic and anti-inflammatory studies, respectively. In the present study, the alcoholic bark extract of Pinus roxburghii Sarg. demonstrated significant analgesic and anti-inflammatory activities in the tested models.

  11. Lyprinol—Is It a Useful Anti-Inflammatory Agent?

    Directory of Open Access Journals (Sweden)

    Sheila A. Doggrell

    2011-01-01

    Full Text Available The New Zealand green lipped mussel preparation Lyprinol is available without a prescription from a supermarket, pharmacy or Web. The Food and Drug Administration have recently warned Lyprinol USA about their extravagant anti-inflammatory claims for Lyprinol appearing on the web. These claims are put to thorough review. Lyprinol does have anti-inflammatory mechanisms, and has anti-inflammatory effects in some animal models of inflammation. Lyprinol may have benefits in dogs with arthritis. There are design problems with the clinical trials of Lyprinol in humans as an anti-inflammatory agent in osteoarthritis and rheumatoid arthritis, making it difficult to give a definite answer to how effective Lyprinol is in these conditions, but any benefit is small. Lyprinol also has a small benefit in atopic allergy. As anti-inflammatory agents, there is little to choose between Lyprinol and fish oil. No adverse effects have been reported with Lyprinol. Thus, although it is difficult to conclude whether Lyprinol does much good, it can be concluded that Lyprinol probably does no major harm.

  12. Analgesic and anti-inflammatory activities of Piper nigrum L.

    Science.gov (United States)

    Tasleem, Farhana; Azhar, Iqbal; Ali, Syed Nawazish; Perveen, Shaista; Mahmood, Zafar Alam

    2014-09-01

    To evaluate and compare the analgesic and anti-inflammatory activity of pure compound, piperine along with hexane and ethanol extracts of Piper nigrum L. fruit in mice and rats. The analgesic activity was determined by tail immersion method, analgesy-meter, hot plate and acetic acid induced writhing test. While the anti-inflammatory activity was evaluated by carrageenan-induced paw inflammation in rats. Piperine at a dose of 5 mg/kg and ethanol extract at a dose of 15 mg/kg after 120 min and hexane extract at a dose of 10 mg/kg after 60 min exhibited significant (PPiper nigrum L possesses potent analgesic and anti-inflammatory activities. Copyright © 2014 Hainan Medical College. Published by Elsevier B.V. All rights reserved.

  13. Modifying anti-inflammatory effect of Diclofenac with Murraya koenigii.

    Science.gov (United States)

    Kaur, Ginpreet; Daftardar, Saloni; Barve, Kalyani H

    2014-01-01

    Murraya koenigii (Curry leaves) has been widely used in Asian countries for the treatment of some ailments such as diabetes and hypertension. In the present study, leaves of Murraya koenigii were extracted with ethanol and evaluated for anti-inflammatory activity in rats using carrageenan induced paw edema method. Ethanolic extract showed a potent anti-inflammatory activity at third hour after carrageenan administration when compared with the standard drug, Diclofenac. The percent inhibition of paw volume was found to be 84.75% for 50 mg/kg of extract whereas it was found to be 80.86% for 50 mg/kg extract in combination with Diclofenac 10 mg/kg. Thus, the present study suggests that the combination therapy potentiates the anti-inflammatory effect of diclofenac and may help in reducing the dose of the synthetic drug. Some relevant patents are also outlined in this article.

  14. Hypoglycemic agents and potential anti-inflammatory activity

    Directory of Open Access Journals (Sweden)

    Kothari V

    2016-04-01

    Full Text Available Vishal Kothari,1 John A Galdo,2 Suresh T Mathews3 1Department of Nutrition and Dietetics, Boshell Diabetes and Metabolic Diseases Research Program, Auburn University, Auburn, 2Department of Pharmacy Practice, 3Department of Nutrition and Dietetics, Samford University, Birmingham, AL, USA Abstract: Current literature shows an association of diabetes and secondary complications with chronic inflammation. Evidence of these immunological changes include altered levels of cytokines and chemokines, changes in the numbers and activation states of various leukocyte populations, apoptosis, and fibrosis during diabetes. Therefore, treatment of diabetes and its complications may include pharmacological strategies to reduce inflammation. Apart from anti-inflammatory drugs, various hypoglycemic agents have also been found to reduce inflammation that could contribute to improved outcomes. Extensive studies have been carried out with thiazolidinediones (peroxisome proliferator-activated receptor- agonist, dipeptidyl peptidase-4 inhibitors, and metformin (AMP-activated protein kinase activator with each of these classes of compounds showing moderate-to-strong anti-inflammatory action. Sulfonylureas and alpha glucosidase inhibitors appeared to exert modest effects, while the injectable agents, insulin and glucagon-like peptide-1 receptor agonists, may improve secondary complications due to their anti-inflammatory potential. Currently, there is a lack of clinical data on anti-inflammatory effects of sodium–glucose cotransporter type 2 inhibitors. Nevertheless, for all these glucose-lowering agents, it is essential to distinguish between anti-inflammatory effects resulting from better glucose control and effects related to intrinsic anti-inflammatory actions of the pharmacological class of compounds. Keywords: diabetes, inflammation, insulin, metformin, thiazolidinedione, gliptin

  15. Three indigenous plants used in anti-cancer remedies, Garcinia kola Heckel (stem bark), Uvaria chamae P. Beauv. (root) and Olax subscorpioidea Oliv. (root) show analgesic and anti-inflammatory activities in animal models.

    Science.gov (United States)

    Popoola, Temidayo D; Awodele, Olufunsho; Omisanya, Adeola; Obi, Nkechinyerem; Umezinwa, Chioma; Fatokun, Amos A

    2016-12-24

    Phytochemicals with anti-oxidative and anti-inflammatory properties are known to inhibit tumour initiation, promotion and progression. Hence, there is an increasingly-convincing rationale for employing remedies containing those phytochemicals in the treatment of cancers and also as analgesic and anti-inflammatory adjuvants in therapy. The plants Garcinia kola Heckel (Clusiaceae), stem bark; Uvaria chamae P. Beauv. (Annonaceae), root; and Olax subscorpioidea Oliv. (Olacaceae), root, have been documented to be part of various indigenous anti-cancer regimens. To determine if the three plants exhibit significant anti-oxidative and anti-inflammatory properties. Using established models, the analgesic and anti-inflammatory activities of the three plants were investigated. Pre-treatment with the plant extracts at 100, 200 and 400mg/kg produced inhibition of writhes; G. kola and U. chamae showed no significant effect on formalin-induced pain, but O. subscorpioidea produced inhibition in both phases of the formalin test. Similarly, while G. kola and U. chamae did not produce any significant inhibitory effect in the xylene-induced ear oedema model, the oedema was significantly reduced by O. subscorpioidea pre-treatment. However, all the three plants significantly inhibited the time-dependent increase in paw circumference in the carrageenan- and formaldehyde-induced rat paw oedema tests, with peak effects observed at 400mg/kg, 6h after the induction of oedema, comparable in some cases to the effects of two standard drugs, the non-steroidal anti-inflammatory drug diclofenac and the anti-inflammatory antibiotic doxycycline. We conclude that the three plant extracts possess analgesic and anti-inflammatory properties, thus providing a scientific rationale for their inclusion in some traditional anti-cancer regimens. Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.

  16. Anti-inflammatory activity of Sapindus trifoliatus Linn.

    Science.gov (United States)

    Arul, B; Kothai, R; Jacob, Philip; Sangameswaran, B; Sureshkumar, K

    2004-01-01

    Anti-inflammatory activity of the ethanolic extract of the seeds of Sapindus trifoliatus Linn. was studied in wister rats using the carrageenan induced left hind paw edema, carrageenan induced pleurisy and cotton pellet induced granuloma model. The ethanolic extract (150 mg/kg, p.o.) produced the inhibition of carrageenan induced rat paw edema. It also showed an inhibitory effect on leukocyte migration and a reduction on the pleural exudates as well as reduction on the granuloma weight in the cotton pellet granuloma method. The results indicated that the ethanolic extract produced significant (P < 0.001) anti-inflammatory activity when compared with the standard and untreated control.

  17. Anti-inflammatory treatment for major depressive disorder: implications for patients with an elevated immune profile and non-responders to standard antidepressant therapy

    Science.gov (United States)

    Kopschina Feltes, Paula; Doorduin, Janine; Klein, Hans C; Juárez-Orozco, Luis Eduardo; Dierckx, Rudi AJO; Moriguchi-Jeckel, Cristina M; de Vries, Erik FJ

    2017-01-01

    Major depressive disorder (MDD) is a prevalent and disabling psychiatric disease with rates of non-responsiveness to antidepressants ranging from 30–50%. Historically, the monoamine depletion hypothesis has dominated the view on the pathophysiology of depression. However, the lack of responsiveness to antidepressants and treatment resistance suggests that additional mechanisms might play a role. Evidence has shown that a subgroup of depressive patients may have an underlying immune deregulation that could explain the lack of therapeutic benefit from antidepressants. Stimuli like inflammation and infection can trigger the activation of microglia to release pro-inflammatory cytokines, acting on two main pathways: (1) activation of the hypothalamic–pituitary adrenal axis, generating an imbalance in the serotonergic and noradrenergic circuits; (2) increased activity of the enzyme indoleamine-2,3-dioxygenase, resulting in depletion of serotonin levels and the production of quinolinic acid. If this hypothesis is proven true, the subgroup of MDD patients with increased levels of pro-inflammatory cytokines, mainly IL-6, TNF-α and IL-1β, might benefit from an anti-inflammatory intervention. Here, we discuss the pre-clinical and clinical studies that have provided support for treatment with non-steroidal anti-inflammatory drugs in depressed patients with inflammatory comorbidities or an elevated immune profile, as well as evidences for anti-inflammatory properties of standard antidepressants. PMID:28653857

  18. Bifunctional compounds eliciting anti-inflammatory and anti-cholinesterase activity as potential treatment of nerve and blister chemical agents poisoning.

    Science.gov (United States)

    Amitai, Gabi; Adani, Rachel; Fishbein, Eliezer; Meshulam, Haim; Laish, Ido; Dachir, Schlomit

    2005-12-15

    Studies cited by Cowan et al. [J. Appl. Toxicol. 23, 177 (2003)] indicate existence of inflammatory and cholinergic pathways in both nerve agents and sulfur mustard (HD) injury. Increase in AChE synthesis and neurite extension was noted after exposure to HD [K.W. Lanks et al., Exp. Cell Res. 355 (1975)]. Moreover, anti-inflammatory drugs reduce the dermal, respiratory and ocular damage caused by exposure to HD. On the other hand, recent studies have noted the involvement of neuro-inflammatory processes during exposure to the nerve agents sarin or soman [Cowan et al., 2003]. The use of various anti-inflammatory drugs in addition to the classical antidotal drugs (e.g. atropine and oximes) caused decrease in certain toxic symptoms and inflammation-induced brain damage. Our new bifunctional drugs (Scheme 1) are based on CNS-permeable molecular combination of pseudo-reversible AChE inhibitor (pyridostigmine, PYR) coupled via a hydrophobic spacer (octyl or decyl hydrocarbon chain) to a non-steroidal anti-inflammatory drug (NSAID) such as Ibuprofen or Diclofenac (Scheme 1). This study evaluates the efficacy of certain bifunctional compounds against HD and soman poisoning in mice in vivo.

  19. Anti-inflammatory and anti-oxidant properties of Curcuma longa (turmeric) versus Zingiber officinale (ginger) rhizomes in rat adjuvant-induced arthritis.

    Science.gov (United States)

    Ramadan, Gamal; Al-Kahtani, Mohammed Ali; El-Sayed, Wael Mohamed

    2011-08-01

    Turmeric (rich in curcuminoids) and ginger (rich in gingerols and shogaols) rhizomes have been widely used as dietary spices and to treat different diseases in Ayurveda/Chinese medicine since antiquity. Here, we compared the anti-inflammatory/anti-oxidant activity of these two plants in rat adjuvant-induced arthritis (AIA). Both plants (at dose 200 mg/kg body weight) significantly suppressed (but with different degrees) the incidence and severity of arthritis by increasing/decreasing the production of anti-inflammatory/pro-inflammatory cytokines, respectively, and activating the anti-oxidant defence system. The anti-arthritic activity of turmeric exceeded that of ginger and indomethacin (a non-steroidal anti-inflammatory drug), especially when the treatment started from the day of arthritis induction. The percentage of disease recovery was 4.6-8.3% and 10.2% more in turmeric compared with ginger and indomethacin (P turmeric over ginger and indomethacin, which may have beneficial effects against rheumatoid arthritis onset/progression as shown in AIA rat model.

  20. Antioxidant, anti-inflammatory and antinociceptive activities of ...

    African Journals Online (AJOL)

    Background of study: Plants used for traditional medicine contain a wide range of substances which can be used to treat various infectious diseases. Aim: The study evaluated the in vitro antioxidant, antinociceptive, and anti-inflammatory activities of the methanolic extract of Justicia secunda Vahl leaf. Methods: The acute ...

  1. Anti-inflammatory activity of Wigandia urens and Acalypha ...

    African Journals Online (AJOL)

    PRECIOUS

    2009-11-02

    Nov 2, 2009 ... Anti-inflammatory activity of Wigandia urens and. Acalypha alopecuroides. Miguel A. Zavala-Sánchez*, Cuauhtémoc Pérez-González, Lucina Arias-García and Salud. Pérez-Gutiérrez. Departamento de Sistemas Biológicos, Universidad Autónoma Metropolitana-Xochimilco. Calzada del Hueso 1100, Col.

  2. Anti-inflammatory, cytotoxic and antioxidant effects of methanolic ...

    African Journals Online (AJOL)

    The aim of this study was to investigate in vitro antioxidant, anti-inflammatory and cytotoxic activities of the petroleum ether, ethyl acetate, methanol and aqueous extracts obtained from leaves of Drypetes sepiaria (Euphorbiaceae). Total phenolic and flavonoid contents of these crude extracts were determined as gallic acid ...

  3. Anti-inflammatory and antioxidant properties of Eriobotrya japonica ...

    African Journals Online (AJOL)

    Abstract. Background: In the present work we determined phenolic and flavonoids content of Eriobotrya japonica leaves extracts and fractions and their antioxidant and anti-inflammatory properties. Objectives: To evaluate the inhibition of inflammatory PLA2 and antioxidant effects of extracts and fractions from Erio-.

  4. Evaluation of anti-inflammatory, antibacterial and cytotoxic activities ...

    African Journals Online (AJOL)

    Anti-inflammatory activity was determined using a LOX-inhibitor screening assay kit according to the manufacturer's instructions. A broth serial micro dilution method was used to determine the minimum inhibitory concentration (MIC) against, Gram-positive and Gram-negative bacteria and Mycobacterium species.

  5. Anti-inflammatory effects of kaempferol, myricetin, fisetin and ...

    African Journals Online (AJOL)

    Purpose: To investigate the anti-inflammatory effects of kaempferol, myricetin, fisetin and ibuprofen in rat pups. Methods: The expression levels of cyclooxygenase (COX)-1, COX-2 and tumour necrosis factor-α (TNF-α) were determined by western blotting; the inhibition of these proteins by plant compounds was evaluated.

  6. Phytochemical, Analgesic And Anti-Inflammatory Effects Of The ...

    African Journals Online (AJOL)

    Phytochemical screening was carried out on the ethylacetate portion of the ethanolic extract of the leaves of Pseudocedrella kotschyii and then evaluated for its analgesic (acetic acid-induced writhing) and anti-inflammatory (raw egg albumin-induced oedema) activities in mice and rats respectively. Phytochemical screening ...

  7. Cytotoxic, anti-inflammatory and antioxidant activities of four different ...

    African Journals Online (AJOL)

    Purpose: To evaluate the cytotoxic, anti-inflammatory and antioxidant activities of four different solvent extracts obtained from the aerial parts of Galega officinalis L. Methods: The hexane, DCM, methanol and water extracts of G. officinalis were successively obtained by soxhlet extraction method. The cytotoxic activity of the ...

  8. Synthesis, Analgesic, Anti-inflammatory and Antimicrobial Activities ...

    African Journals Online (AJOL)

    Purpose: Microbial infections often produce pain and inflammation. Chemotherapeutic, analgesic and anti-inflammatory drugs are prescribed simultaneously in normal practice. The compound possessing all three activities is not common.The purpose of the present study was to examine whether molecular modification ...

  9. Anti-inflammatory effects of ginsenosides from Panax ginseng and ...

    African Journals Online (AJOL)

    Ginsenosides (G) are biologically active saponin compounds found inPanax ginseng. Although these compounds are reported to possess numerous biological activities, recent issues have arisen regarding their immunosuppressive and anti-inflammatory roles in inflammatory cells. This is because 1) inflammation, ...

  10. Identification of active anti-inflammatory principles of beta- beta ...

    African Journals Online (AJOL)

    Purpose: To identify the anti-inflammatory components of beta-beta (Lunasia amara Blanco.) wood. Methods: The wood material was extracted with 96 % ethanol and fractionated with dichloromethane using a liquid-liquid continuous extraction (LLCE). The fractions were subjected to silica gel column chromatography.

  11. Anti-inflammatory effect of Zanthoxylum bungeanum -cake ...

    African Journals Online (AJOL)

    ), a kind of traditional therapy of moxibustion, has been used in China since 340 B.C. However, its mechanism remains unclear. So, this study was attempted to reveal the anti-inflammatory effect of ZBCS-moxi on rheumatoid arthritis (RA) rats.

  12. Analgesic, anti-inflammatory and antipyretic effects of the ethanol ...

    African Journals Online (AJOL)

    The leaves of Acalypha wilkesiana are commonly used for the treatment of pain, fever and ulcer by traditional medical practitioners without any scientific data to evaluate ... Different sets of rats were used for the anti-ulcer, anti-inflammatory and antipyretic studies although animal grouping for extract administration were as in ...

  13. Antipyretic, analgesic and anti-inflammatory activities of methanol ...

    African Journals Online (AJOL)

    Antipyretic, analgesic and anti-inflammatory activities of methanol extract of root bark of Acacia jacquemontii Benth (Fabaceae) in experimental animals. ... edema and dosedependent anti-pyrexia, and thus justifies the ethnomedicinal use of Acacia jacquemontii Benth. in the management of pain, fever and inflammation.

  14. Anti-Inflammatory and Analgesic Activities of Nothospondias staudtii ...

    African Journals Online (AJOL)

    Pain responses were studied in mice using the tail immersion and acetic acid induced writing while carrageenan induced paw oedema was used to access anti-inflammatory activity. The three extracts exhibited significant analgesic compared with the control (saline, 10ml/kg) as evidenced by (i) increased escape latency in ...

  15. Antinociceptive, Anti-Inflammatory and Antipyretic Activities of the ...

    African Journals Online (AJOL)

    Materials and Methods: The leaf methanol extract of Ruta graveolens was evaluated for antinociceptive activity using the acetic acid writhing and hot-plate tests in mice, also anti-inflammatory and antipyretic activities using the carrageenan-induced oedema and E. coli-induced pyrexia tests in rats, respectively. Results: R.

  16. Anti-inflammatory activity of chromatographic fractions of ...

    African Journals Online (AJOL)

    The study evaluates the anti-inflammatory activity of the vacuum liquid (A, B and C) and column (L, S and Y) chromatographic fractions of Stereospermum kunthianum stem bark. The fractions at the doses of 100, 200 and 400 mg/kg were evaluated using the carrageenan-induced paw oedema model in rats. The control rats ...

  17. Anti-inflammatory activity of Ruta graveolens Linn on carrageenan ...

    African Journals Online (AJOL)

    Aqueous, ethanolic and methanolic extracts of Ruta graveolens were investigated for anti-inflammatory activity in carrageenan induced paw edema in wistar male rats, and compared to a positive control drug, Voveran. These extracts were given (ip) in a concentration of 20 and 50 mg/kg b.w. before carrageenan injection.

  18. Phytochemical screening, safety evaluation, anti-inflammatory and ...

    African Journals Online (AJOL)

    Thereafter anti-inflammatory and analgesic studies were conducted using standard tests such as carrageenan, histamine-induced-oedema, tail flick test and acetic acid writhing test. Phytochemical screening of the powdered material showed that tannin, flavonoid and reducing sugar were present while alkaloids, cardiac ...

  19. Anti-Inflammatory Activity of N-(3-Florophenylethylcaffeamide in Mice

    Directory of Open Access Journals (Sweden)

    Yueh-Hsiung Kuo

    2013-07-01

    Full Text Available In this study, we evaluated the anti-inflammatory activity of one synthetic product, N-(3-Florophenylethylcaffeamide (abbrev. FECA, by using animal model of λ-carrageenan-induced paw edema in mice. The anti-inflammatory mechanism of FECA was determined by measuring the levels of cyclooxygenase-2 (COX-2, nitric oxide (NO, tumor necrosis factor (TNF-α, interleukin-1β (IL-1β, and malondialdehyde (MDA in the edema paw tissue, and the activities of superoxide dismutase (SOD, glutathione peroxidase (GPx, and glutathione reductase (GRd in the liver. The results showed that FECA reduced the paw edema at three, four and five hours after λ-carrageenan administration. The levels of COX-2, NO, TNF-α, and MDA in the λ-carrageenan-induced edema paws were reduced and the activities of SOD, GPx, and GRd in liver tissues were raised by FECA. These results suggested that FECA possessed anti-inflammatory activities and the anti-inflammatory mechanisms might be related to the decrease of the levels of COX-2, NO, and TNF-α in inflamed tissues and the increase in the MDA level by increasing the activities of SOD, GPx, and GRd.

  20. Anti-inflammatory Activity of the Different Parts of Nyctanthes ...

    African Journals Online (AJOL)

    The antiinflammatory activity of the extracts was estimated using different inflammatory mediators like carrageenan, arachidonic acid, histamine and serotonin to induce paw oedema in rats. WSFEE of the flowers, seeds and leaves were found to possess anti-inflammatory activity against all the inflammatory mediators in a ...

  1. Anti-Inflammatory, Antioxidant, and Selective Antibacterial Effects of ...

    African Journals Online (AJOL)

    A 70 % ethanol extract was tested for anti-inflammatory effect using the carrageenan-induced oedema in chicks. Free radical scavenging, total antioxidant and total phenol content were assessed spectrophotometrically. The extract was tested for antibacterial activity using the agar well diffusion method and micro dilution ...

  2. Hemostatic, anti-inflammatory and antibacterial effects of ...

    African Journals Online (AJOL)

    Purpose: To study the hemostatic, anti-inflammatory and antibacterial effects of Sanqixiantao dressing. Methods: Sanqixiantao dressing was prepared by mixting with sanqixiiantao extract (8 %) with membrane-forming matrix (5:4:9:2 volume ratio of polyvinyl alcohol: Na CMC: gelatin: glycerol). Rats with local surface ...

  3. Anti-inflammatory activity of Syzygium cumini seed | Kumar | African ...

    African Journals Online (AJOL)

    The Syzygium cumini (Myrtaceae) is a popular traditional medicinal plant in India. This study was intended to evaluate the anti-inflammatory activity of ethyl acetate and methanol extracts of S. cumini seed in carrageenan induced paw oedema in wistar rats at the dose level of 200 and 400 mg/kg administrated orally.

  4. Antipyretic, analgesic, anti-inflammatory and cytotoxic effects of four ...

    African Journals Online (AJOL)

    ... and 2-acetamido-5-sulfonamidobenzoic acid (AMSABA, 4) were synthesized and evaluated for their analgesic, antipyretic, anti-inflammatory and cytotoxic activities. HASBA, AASBA and AMASBA showed higher analgesic activity than aspirin (ASA) at 100 mg/kg dose, while AMSABA showed the least analgesic property.

  5. antioxidant and anti-inflammatory properties of a flavonoid fraction ...

    African Journals Online (AJOL)

    Bioline

    The extract also produced anti-nociception in the animals, as assessed by the tail flick, hot-plate and limb-withdrawal tests. These findings suggest that the leaf extract of Voacanga africana has potent anti- imfiammatory and anti-nociceptive action. Key Words: Voacanga africana; anti-inflammatory and anti-nociceptive ...

  6. Evaluation of acute toxicity and anti-inflammatory effects of ...

    African Journals Online (AJOL)

    BSE showed significant anti-inflammatory effect (62.91%) at 500 mg/kg b.w. Further the n-hexane, chloroform and methanol fractions of BSE were tested for antiinflammatory activity. The n-hexane fraction (BSH) exhibits significant activity (64.87%) at 400 mg/kg b.w. The methanol fraction (BSM) showed dose dependent ...

  7. Antioxidant, anti-inflammatory and antinociceptive activities of ...

    African Journals Online (AJOL)

    Samuel O. Onoja

    2016-07-01

    Jul 1, 2016 ... Methods: The acute toxicity was performed with up and down method and the highest dose used was. 2 g/kg. The anti-inflammatory ... loss of function, redness and heat.8 Some herbs used in eth- nomedicine in the ..... impulse transmission and/or elevation of pain threshold in the hypothalamus.42 The ...

  8. Anti-Inflammatory Effect Of Some Common Nigerian Vegetables ...

    African Journals Online (AJOL)

    Methanol extracts of four common Nigerian vegetables; A.graveoleus, C.argentia, T. triangulare and T.occidentalis were investigated for anti-inflammatory activity in rats using carrageenan. Carrageenan-induced oedema in the sub-plantar hind paw of vegetable extracts treated rats was significantly inhibited. This finding ...

  9. anti - inflammatory and analgesic activities of nothospondias staudtii ...

    African Journals Online (AJOL)

    Bioline

    Summary: The aqueous (AENS), methanolic (MENS) and chloroform (CENS) extracts of the leaves of. Nothospondias staudtii Engl (Anacardianceae) were screened for analgesic and anti-inflammatory activities in mice and rats. Pain responses were studied in mice using the tail immersion and acetic acid induced writing.

  10. Anti-Inflammatory and Antioxidant Activities of Methanol Extracts and ...

    African Journals Online (AJOL)

    Background: Methanol extracts and alkaloid fractions of different parts of four plant species belonging to Solanaceae family and used in Mexican traditional medicine were investigated for their total phenolic contents, anti-inflammatory and antioxidant properties. Materials and Methods: The total phenolic compounds of each ...

  11. Antibacterial and Anti-Inflammatory Activities of Anacardium ...

    African Journals Online (AJOL)

    ABSTRACT: Anacardium occidentale is a local medicinal plant used in ethno medicine for the treatment of diarrhea, constipation,pain and inflammation. The aqueous and ethanolic extracts of this plant parts were assessed for anti- inflammatory and antibacterial activities using experimental animal model and agar disc ...

  12. Phytochemical Analysis and Anti-Inflammatory activity of Methanol ...

    African Journals Online (AJOL)

    The present study investigated the phytochemistry and anti-inflammatory activity of methanolic root extract of Cryptolepis sanguinolenta against paw edema induced by egg albumin and carrageenan in rats. Phytochemical analysis and acute toxicity test (LD50) of the methanol extract was also carried out. Results show that ...

  13. Analgesic and anti-inflammatory activities of ethanolic extract of ...

    African Journals Online (AJOL)

    The analgesic and anti-inflammatory activities of the ethanolic extract of Rheumatic Tea Formula (RTF) a polyherbal tea consisting the leaves of Eucalyptus globulus, Albizia chevalieri and bark of Salix alba were studied in mice and rats using acetic acid induced writhing, hot plate method, formalin induced pain and ...

  14. Antinociceptive and Anti-Inflammatory Effects of Solvent Extracts of ...

    African Journals Online (AJOL)

    Erah

    SGRS College of Pharmacy, Department of Pharmacology, Pune University, Saswad, Tal-Purandar, Pune 412301,. India ... the plant material. Keywords: Tagetes erectus, Antinociceptive, Anti-inflammatory. Received: 30 December 2008. Revised accepted: 18 May 2009 ... solvent extracts of the leaves of this plant for.

  15. Anti-inflammatory, analgesic and antipyretic activities of the aqueous ...

    African Journals Online (AJOL)

    The aqueous extract of Hippobromus pauciflorus (L.f) Radlk leaves at 50, 100 and 200 mg/kg body weight were evaluated for anti-inflammatory, analgesic and antipyretic activities in male rats. Antiinflammatory activity was studied by using carrageenan and histamine induced oedema right hind paw volume while the ...

  16. Possible mechanism of anti-inflammatory activity and safety profile ...

    African Journals Online (AJOL)

    Pistia stratiotes is used extensively in inflammatory disorders in several countries including Ghana. The aim of the study was to investigate the anti-inflammatory property and possible mechanism of action of aqueous and ethanolic leaf extracts of Pistia stratiotes and to ascertain its safety for use. In separate experiments ...

  17. Anti inflammatory and antipyretic activities of the methanol leaf ...

    African Journals Online (AJOL)

    Acacia ataxacantha (Leguminosae) has been reported to be used in traditional medicine for management of pain and inflammation. The present study was designed to evaluate the anti inflammatory and antipyretic activities of methanol leaf extract of Acacia ataxacantha in rats. The acute toxicity study was carried out using ...

  18. In vitro anti-inflammatory and phytochemical properties of crude ...

    African Journals Online (AJOL)

    Baliospermum montanum (Muell – Arg) which belong to Euphorbiaceae family is a well known perennial herb in Indian medicine used to treat various disorders like asthma, bronchitis, purgative, anthelmintic, diuretic, diaphoretic, rubefacient and tonic. The anti-inflammatory activity of four different solvent extracts of B.

  19. Comparative anti-inflammatory properties of Capsaicin and ...

    African Journals Online (AJOL)

    Background: The analgesic effect of capsaicin (the active ingredient in Capsicum frutescens Linn. [Solanaceae]) had been reported in several studies. Current research is being directed at producing analgesics, anti-inflammatory agents with better side effect profile. Objectives: To investigate if either the ethyl acetate extract ...

  20. Hemostatic, anti-inflammatory and antibacterial effects of ...

    African Journals Online (AJOL)

    Hemostatic, anti-inflammatory and antibacterial effects of. Sanqixiantao dressing in vivo and in vitro. Xiaohua Qin1, Fang Hu1, Sudan Wu1 and Jie Yun2*. 1Department of General Surgery, 2Department of Nursing, Teaching Hospital of Chengdu University of Traditional Chinese. Medicine, Chengdu 610072, PR China.

  1. Analgesic and anti-inflammatory effects of Allium Ascalonicum ...

    African Journals Online (AJOL)

    The methanol and aqueous extract of Allium ascalonicom were investigated for analgesic and anti-inflammatory properties. Thermal and chemical models of pain assessment were used while albumin was used to induce inflammation. The extracts were administered at doses of 50, 100 and 200 mg/kg. The methanol extract ...

  2. Antinociceptive and anti-Inflammatory effects of the standardized oil ...

    African Journals Online (AJOL)

    The effect of Callistemon lanceolatus (Syn. C. citrinus curtis; Family: Myrtaceae) leaf oil was studied for the antinociceptive and anti-inflammatory activity in experimental animals. C. lanceolatus, 25 – 100 mg/kg administered orally for 3 days exhibited graded dose response equivalent to 21.95% - 89.90% protection in the tail ...

  3. Cytotoxic, anti-inflammatory and antioxidant activities of four different ...

    African Journals Online (AJOL)

    Purpose: To evaluate the cytotoxic, anti-inflammatory and antioxidant activities of four different solvent ... antioxidant activity with 2.33 ± 0.09 µmol Trolox/mg , 7.10 ± 0.9 g tannic acid equivalent (TAE), and IC50 ..... adenocarcinoma cell line. e WS1, human normal skin fibroblasts cell line. f Positive control. g An extract was.

  4. Experimental evaluation of anti-inflammatory, antinociceptive and ...

    African Journals Online (AJOL)

    Background: Clove oil of Eugenia caryophyllata (Myrtaceae) is a light yellowish fluid obtained from dried flower buds. Clove oil is used traditionally to relieve toothache. Aim: The aim of the present work was to study the anti-inflammatory, antinociceptive and antipyretic potential of clove oil in mice. Methods: Analgesic activity ...

  5. Anti-inflammatory effect of Myrtus nivellei Batt & Trab (myrtaceae ...

    African Journals Online (AJOL)

    This work aims at evaluating the anti-inflammatory activity of an endemic species of the central sahara: Myrtus nivellei Batt & Trab. The methanolic extract of this plant was extracted by Soxhlet apparatus and concentrated under reduced pressure using a rotary evaporator. In the carrageenan-induced paw edema test, five ...

  6. Synthesis, Anti-inflammatory and Anti-nociceptive Evaluation of ...

    African Journals Online (AJOL)

    rat and acetic acid-induced writhing in mice, respectively. Aspirin was used at a dose of 100mg/kg as the reference drug. Results: The compounds were obtained in high yield (70 – 90 %) and purity. The anti-inflammatory results showed a poor activity for the compounds except o-palmitoylamino N-carboxyethyl benzamide.

  7. [Hypersensitivity reactions to nonsteroidal anti-inflammatory drugs].

    Science.gov (United States)

    Chalabianloo, Fatemeh

    2012-09-18

    Nonsteroidal anti-inflammatory drugs (NSAIDs) are considered to be the second most frequent cause of adverse drug reactions, including drug hypersensitivity, after beta-lactam antibiotics. An understanding of the underlying mechanisms and clinical characteristics of hypersensitivity reactions to NSAIDs is necessary for the diagnosis and management of these undesirable reactions in the clinical setting.

  8. Anti-inflammatory activity of Eucalyptus spp. and Pistascia lentiscus ...

    African Journals Online (AJOL)

    Background: Eucalyptus spp. and Pistascia lentiscus are among the Palestinian trees that are traditionally used in folkloric medicine in treating many diseases; leaves of which are thought to have anti-inflammatory, antibacterial and antioxidant effects. The goal of this study is to evaluate the in vitro inhibitory effect of ...

  9. Investigation of the anti-inflammatory and antinociceptive activities of ...

    African Journals Online (AJOL)

    The anti-inflammatory and anti-nociceptive activities of the root extract of Elephantorrhiza elephantina (Burch.) Skeels (Fabaceae) were investigated using wistar rats. The extract was administered intraperitoneally (i.p) to rats at graded doses of 50, 100 and 200 mg/kg BWt. Carrageenan and. Histamine were injected into rat ...

  10. anti-inflammatory activity of selected nigerian medicinal plants

    African Journals Online (AJOL)

    Extracts of nineteen plant species from an inventory of Nigerian medicinal plants were screened for activity in two in vitro anti-inflammatory model test systems, inhibition of prostaglandin biosynthesis and PAF-induced elastase release from neutrophilis. Anacardium occidentale and Acalipha hispida were active in both test ...

  11. Anti-inflammatory Effects of Magnolia sieboldii Extract in ...

    African Journals Online (AJOL)

    Purpose: To investigate the effect of Magnolia sieboldii extract (MSE) on the production of proinflammatory cytokines by macrophage. Methods: The whole plant of M. sieboldii was extracted with methanol at room temperature. The in vitro anti-inflammatory activity of MSE was investigated on lipopolysaccharide ...

  12. Phytochemical screening and anti-inflammatory evaluation of ...

    African Journals Online (AJOL)

    Euphobia heterophylla is a local medicinal plant used in ethnomedicine for the treatment of constipation, bronchitis and asthma. The aqueous decoction and the methanolic extracts were subjected to anti-inflammatory activity using experimental animal model, in the presence of the positive control drugs. The inflammation ...

  13. Anti-inflammatory studies of yam ( Dioscorea esculenta ) extract on ...

    African Journals Online (AJOL)

    The defatted methanol extract of Dioscorea esculenta tuber was evaluated for anti-inflammatory properties in animal model using Wistar rats. The study was done using the cotton thread method in measuring the right hind paw oedema and granuloma tissue formation in rats. The extract was tested at doses between 100 ...

  14. Anti-inflammatory effects of kaempferol, myricetin, fisetin and ...

    African Journals Online (AJOL)

    Purpose: To investigate the anti-inflammatory effects of kaempferol, myricetin, fisetin and ibuprofen in rat pups. Methods: The expression levels of cyclooxygenase (COX)-1, COX-2 and tumour necrosis factor-α. (TNF-α) were determined by western blotting; the inhibition of these proteins by plant compounds was evaluated.

  15. Anti-Inflammatory and Analgesic Activities of Ethanolic Leaf Extract ...

    African Journals Online (AJOL)

    inflammatory action of the leaf extract is mediated both centrally and peripherally. The analgesic or anti-inflammatory effect of the extract was not attenuated by opioid antagonist, naloxone, thus ruling out the involvement of opioid receptors in the central ...

  16. Anti-inflammatory and Antinociceptive Effects of the Alcoholic Extract ...

    African Journals Online (AJOL)

    The alcoholic extract of Polygala arvensis (family Polygalaceae) was screened for antinociceptive and anti-inflammatory activities in experimental animals. The extract was administered for three consecutive days. Following an oral dose of 25 - 100 mg/kg, the extract exhibited graded dose response equivalent to 16.24% ...

  17. TOPICAL ANTI-INFLAMMATORY ACTIVITY OF COSTUS AFER ...

    African Journals Online (AJOL)

    A bioactivity-monitored extraction and chromatographic fractionation of different morphological parts of Costus afer using the croton aldehyde-induced mouse ear oedema model resulted in the location of significant anti-inflammatory activity in the chloroform-soluble fraction (CSE, 64% oedema inhibition 50 mg/200μl, ...

  18. Evaluation of the anti-inflammatory Evaluation of the Anti ...

    African Journals Online (AJOL)

    The anti-inflammatory activity of the aqueous leaf extract of Pterocarpus santalinoides was evaluated using the carrageenan-induced paw oedema and leucocyte migration in rats, and croton oil-induced ear oedema in mice. The extract (50-100mg/kg) and indomethacin (10mg/kg) produced significant (p<0.05) inhibitions of ...

  19. Evaluation of Antimicrobial and Anti-inflammatory Activities and ...

    African Journals Online (AJOL)

    Herbal therapy has been used for daily oral health care to prevent, treat or cure oral conditions from halitosis to periodontal disease. In the present study, Psidium guajava L. leaf which is used traditionally for oral diseases was evaluated for its antimicrobial and anti-inflammatory activities and then formulated with ...

  20. Evaluation of anti-inflammatory and membrane stabilizing property ...

    African Journals Online (AJOL)

    studied on rat blood cells (RBC) exposed to hypotonic solution. The results of the study revealed that the extract possesses anti-inflammatory property. MC was found to significantly (p < 0.05) reduced the oedema swellings induced by the phlogistic agents in rats in a dose-related manner. However, the extract did not exhibit ...

  1. Marine Diterpenoids as Potential Anti-Inflammatory Agents

    Science.gov (United States)

    González, Yisett; Torres-Mendoza, Daniel; Jones, Gillian E.; Fernandez, Patricia L.

    2015-01-01

    The inflammatory response is a highly regulated process, and its dysregulation can lead to the establishment of chronic inflammation and, in some cases, to death. Inflammation is the cause of several diseases, including rheumatoid arthritis, inflammatory bowel diseases, multiple sclerosis, and asthma. The search for agents inhibiting inflammation is a great challenge as the inflammatory response plays an important role in the defense of the host to infections. Marine invertebrates are exceptional sources of new natural products, and among those diterpenoids secondary metabolites exhibit notable anti-inflammatory properties. Novel anti-inflammatory diterpenoids, exclusively produced by marine organisms, have been identified and synthetic molecules based on those structures have been obtained. The anti-inflammatory activity of marine diterpenoids has been attributed to the inhibition of Nuclear Factor-κB activation and to the modulation of arachidonic acid metabolism. However, more research is necessary to describe the mechanisms of action of these secondary metabolites. This review is a compilation of marine diterpenoids, mainly isolated from corals, which have been described as potential anti-inflammatory molecules. PMID:26538822

  2. The Phytochemical Constituents, Analgesic and Anti-inflammatory ...

    African Journals Online (AJOL)

    The analgesic and anti-inflammatory effects of the methanolic extract of the leaves of Jatropha curcas were investigated in mice and rats respectively. The phytochemical screening of the extract was also carried out. The analgesic effect was determined by acetic acid – induced writhing test in mice. While the anti- ...

  3. Topical anti-inflammatory activity of yacon leaf extracts

    Directory of Open Access Journals (Sweden)

    Rejane B. Oliveira

    2013-05-01

    Full Text Available Smallanthus sonchifolius (Poepp. H. Rob. , Asteraceae, known as yacon, is an herb that is traditionally used for the treatment of diabetes in folk medicine. However, recent studies have demonstrated that this plant has other interesting properties such as anti-microbial and anti-inflammatory actions. Thus, the purpose of this study was to evaluate the topical anti-inflammatory property of different extracts prepared from yacon leaves and analyze the role of different chemical classes in this activity. Three yacon leaf extracts were obtained: aqueous extract, where chlorogenic acid derivatives and sesquiterpene lactones were detected; leaf rinse extract, rich in sesquiterpene lactones; and polar extract, rich in chlorogenic acid derivatives. All the extracts exhibited anti-edematogenic activity in vivo (aqueous extract: 25.9% edema inhibition at 0.50 mg/ear; polar extract: 42.7% inhibition at 0.25 mg/ear; and leaf rinse extract: 44.1% inhibition at 0.25 mg/ear. The leaf rinse extract furnished the best results regarding neutrophil migration inhibition, and NO, TNF-α and PGE2 inhibition. These data indicate that both sesquiterpene lactones and chlorogenic acid derivatives contribute to the anti-inflammatory action, although sesquiterpene lactones seem to have more pronounced effects. In conclusion, yacon leaf extracts, particularly the sesquiterpene lactone-rich extract, has potential use as topical anti-inflammatory agent.

  4. The effects of corticosteroids and nonsteroidal anti-inflammatory ...

    African Journals Online (AJOL)

    conversion of arachidonic acid to prostaglandins by COX. Corticosteroids reduce the availability of ... use of nonsteroidal anti-inflammatory drugs. NSAIDs are an essential component of multimodal pain therapy,10 .... reduces the therapeutic effect of aspirin for CV disease, but also amplifies the gastrointestinal side-effects of ...

  5. Anti-inflammatory activity of bark of Xeromphis spinosa

    Directory of Open Access Journals (Sweden)

    Biswa Nath Das

    2009-06-01

    Full Text Available The bark of Xeromphis spinosa extracted by a mixture of equal proportions of petroleum ether, ethyl acetate and methanol at an oral dose of 200 and 400 mg/kg body weight exhibited significant anti-inflammatory activity when compared with control.

  6. antioxidant and anti-inflammatory activities of acalypha fruticosa

    African Journals Online (AJOL)

    In the chronic model (cotton pellet induced granuloma), the MEAF (500 mg/kg) and standard drug showed decreased formation of granuloma tissue at 52.4% and 57.3% (p<0.001) respectively. Thus, the present study revealed that the MEAF exhibited antioxidant and anti-inflammatory activity in the tested models.

  7. Evaluation of analgesic and anti-inflammatory activities of ...

    African Journals Online (AJOL)

    Materials and Methods: The analgesic and anti-inflammatory activities of PYS were determined using acetic acid-induced writhing response, hot plate test, xylene-induced ear swelling test, carrageenan-induced paw edema test, and acetic acid-induced capillary permeability and leukocyte infiltration test with oral doses of ...

  8. Antinociceptive and anti-inflammatory activities of Bowdichia virgilioides (sucupira).

    Science.gov (United States)

    Thomazzi, S M; Silva, C B; Silveira, D C R; Vasconcellos, C L C; Lira, A F; Cambui, E V F; Estevam, C S; Antoniolli, A R

    2010-02-03

    Bowdichia virgilioides Kunth (Leguminosae Papilonoideae) is a plant with anti-inflammatory activity used in folk medicine. The importance of this plant promoted its inclusion in Brazilian Pharmacopoeia. In order to evaluate the actions of this plant, studies were performed on antinociceptive and anti-inflammatory activities. The aqueous extracts (AE) of Bowdichia virgilioides inner bark and leaves were used at 100, 200, and 400mg/kg. Antinociceptive activity of plant extract was evaluated by writhing, hot-plate and formalin tests. Anti-inflammatory activity was evaluated using paw oedema and peritonitis methods. Oral treatment with the AE of inner bark or leaves elicited inhibitory activity (P400mg/kg, and reduced the formalin effect at the second-phase (200 and 400mg/kg, P400mg/kg (P<0.05), and by the reference compounds aspirin (P<0.001) and dexamethasone (P<0.001), respectively. The AE of Bowdichia virgilioides shows antinociceptive and anti-inflammatory activities, supporting the folkloric usage of the plant to treat various inflammatory diseases. Copyright 2009 Elsevier Ireland Ltd. All rights reserved.

  9. Antinociceptive and Anti-Inflammatory Activities of Methanol Root ...

    African Journals Online (AJOL)

    The inflammatory activity of the extract was assayed by egg-albumen induced paw oedema and formalin paw lick test in rats whereas its analgesic activity was ... from this study showed that extract of T. potatoria possess anti-inflammatory and analgesic potencies most probably via the central and peripheral mechanisms.

  10. Antinociceptive and Anti-Inflammatory Effects of Solvent Extracts of ...

    African Journals Online (AJOL)

    (phenylbutazone). It also increased pain threshold in the oedematous right hind limb paw of the rats. Conclusion: The results obtained show that the extracts of Tagetes erectus L. (Asteraceae) has antinociceptive and anti-inflammatory properties. This finding provides a basis for the traditional use of the plant material.

  11. Anti-inflammatory medicinal plants and the molecular mechanisms ...

    African Journals Online (AJOL)

    Background: Medicinal plant and plant products have shown tremendous potentials and are used beneficially in the treatment of inflammation and in the management of diseases with significant inflammatory components. Many medicinal plants employed as anti-inflammatory and antiphlogistic remedies lack the ...

  12. In vitro anti-inflammatory and phytochemical properties of crude ...

    African Journals Online (AJOL)

    pc owner

    2013-09-25

    Sep 25, 2013 ... methanol and the preliminary screening of phytochemical test was investigated. ... Key words: Baliospermum montanum, anti-inflammatory, MTT assay, phytochemical. .... Three methods were used to determine the presence of flavonoids ... were tested with in vitro model for studying its anti-inflam-.

  13. Saponins are involved in the analgesic and anti-inflammatory ...

    African Journals Online (AJOL)

    Our results provided evidence that saponins are implicated in the analgesic and anti-inflammatory effects observed in our earlier studies on the crude methanol extract of Ficus platyphylla stem bark, thus supporting the isolation and development of the saponin components of this medicinal plant as analgesics and ...

  14. Anti-inflammatory activity of Wigandia urens and Acalypha ...

    African Journals Online (AJOL)

    PRECIOUS

    2009-11-02

    Xochimilco. Calzada del Hueso 1100, Col. Villa Quietud C.P. 04960, Coyoacán, México D.F. México. Accepted 2 January, 2009. The anti-inflammatory activity of the chloroform, methanol and aqueous extracts of Wigandia urens ...

  15. Anti-Inflammatory Activity of Compounds Isolated from Plants

    Directory of Open Access Journals (Sweden)

    R.M. Perez G.

    2001-01-01

    Full Text Available This review shows over 300 compounds isolated and identified from plants that previously demonstrated anti-inflammatory activity. They have been classified in appropriate chemical groups and data are reported on their pharmacological effects, mechanisms of action, and other properties.

  16. Identification of active anti-inflammatory principles of betabeta wood ...

    African Journals Online (AJOL)

    Purpose: To identify the anti-inflammatory components of beta-beta (Lunasia amara Blanco.) wood. Methods: The wood material was extracted with 96 % ethanol and fractionated with dichloromethane using a liquid-liquid continuous extraction (LLCE). The fractions were subjected to silica gel column chromatography.

  17. [Allergy to non-steroidal antiinflammatory drugs: recommendations of the Israeli allergy and clinical immunology association].

    Science.gov (United States)

    Tal, Yuval; Hersheko, Alon; Broides, Arnon; Asher, Iran; Staubers, Tali; Confino-Cohen, Ronit; Agmon-Levin, Nancy

    2014-10-01

    Drug hypersensitivity is an adverse reaction that was brought-about by a specific immunologic response. Some of these reactions are Linked with significant morbidity and mortality. Nowadays, hypersensitivity reactions to most drugs can be well defined and the risk of re-exposure to the culprit drug and/or related drugs can be properly assessed. Medical history, skin, blood and challenge tests, conducted in an allergy clinic, enable the prediction and prevention of repeated events as well as unnecessary avoidance of needed compounds. Non-steroidal anti-inflammatory drugs [NSAID] are the second most prevalent group of drugs that provoke hypersensitivity responses occurring either immediately or later. Immediate type responses to NSAID could be divided into 2 groups, each related to a different mechanism. The most common reaction is not allergic but rather it is mediated by the inhibition of the cyclooxygenase I enzyme pathway. Accordingly, this reaction is not selective to a single chemical compound but rather cross-reacts with other members of this "family" of drugs, depending on their biochemical properties. The clinical distinction between those two subtypes of immediate reaction is hard and sometimes utterly impossible. Moreover, the clinical appearance of an immediate reaction may vary from rhinitis, asthma, new appearance or augmentation of chronic urticaria and up to overt anaphylaxis and death. Furthermore, delayed type reactions may also be life-threatening and typically appear 24 hours and up to days following initiation of therapy. In the current review, we present the recommendations of the Israel Association for Allergy and Clinical Immunology for the evaluation and treatment of patients suspected to suffer from hypersensitivity to NSAIDs.

  18. Anti-inflammatory effects of Zea mays L. husk extracts.

    Science.gov (United States)

    Roh, Kyung-Baeg; Kim, Hyoyoung; Shin, Seungwoo; Kim, Young-Soo; Lee, Jung-A; Kim, Mi Ok; Jung, Eunsun; Lee, Jongsung; Park, Deokhoon

    2016-08-19

    Zea mays L. (Z. mays) has been used for human consumption in the various forms of meal, cooking oil, thickener in sauces and puddings, sweetener in processed food and beverage products, bio-disel. However, especially, in case of husk extract of Z. mays, little is known about its anti-inflammatory effects. Therefore, in this study, the anti-inflammatory effects of Z. mays husk extract (ZMHE) and its mechanisms of action were investigated. The husks of Z. Mays were harvested in kangwondo, Korea. To assess the anti-inflammatory activities of ZMHE, we examined effects of ZMHE on nitric oxide (NO) production, and release of soluble intercellular adhesion molecule-1 (sICAM-1) and eotaxin-1. The expression level of inducible nitric oxide synthase (iNOS) gene was also determined by Western blot and luciferase reporter assays. To determine its mechanisms of action, a luciferase reporter assay for nuclear factor kappa B (NF-kB) and activator protein-1 (AP-1) was introduced. ZMHE inhibited lipopolysaccharide (LPS)-induced production of NO in RAW264.7 cells. In addition, expression of iNOS gene was reduced, as confirmed by Western blot and luciferase reporter assays. Effects of ZMHE on the AP-1 and NF-kB promoters were examined to elucidate the mechanism of its anti-inflammatory activity. Activation of AP-1 and NF-kB promoters induced by LPS was significantly reduced by ZMHE treatment. In addition, LPS-induced production of sICAM-1 and IL-4-induced production of eotaxin-1 were all reduced by ZMHE. Our results indicate that ZMHE has anti-inflammatory effects by downregulating the expression of iNOS gene and its downregulation is mediated by inhibiting NF-kB and AP-1 signaling.

  19. New anti-inflammatory formulation containing Synurus deltoides extract.

    Science.gov (United States)

    Choi, Yong Hwan; Son, Kun Ho; Chang, Hyeun Wook; Bae, KiHwan; Kang, Sam Sik; Kim, Hyun Pyo

    2005-07-01

    Synurus deltoides was previously found to possess significant anti-inflammatory activity especially against chronic inflammation, and strong analgesic activity in vivo. In this study, new anti-inflammatory formulation containing S. deltoides extract as a major ingredient was prepared and in vivo activity was evaluated. The plausible action mechanism was also investigated. The new formulation (SAG) contains 1 part of S. deltoides extract, 0.9 part of Angelica gigas extract and 0.9 part of glucosamine sulfate (w/w). SAG inhibited dose-dependently edematic response of arachidonic acid (AA)- and 12-O-tetradecanoyl 13-acetate (TPA)-induced ear edema in mice, which is an animal model of acute inflammation. SAG showed 44.1% inhibition of AA-induced ear edema at an oral dose of 50 mg/kg. In an animal model of chronic inflammation, SAG clearly reduced the edematic response of 7-day model of multiple treatment of TPA (38.1% inhibition at 200 mg/kg/day). Furthermore, SAG (50-800 mg/kg/day) as well as S. deltoides extract (285 mg/kg/day) significantly inhibited prostaglandin E2 production from the skin lesion of the animals of 7-day model. These results were well correlated with in vitro finding that SAG as well as S. deltoides extract reduced cyclooxygenase (COX)-1- and COX-2-induced prostanoid production, measured in mouse bone marrow-derived mast cells. Therefore, these results suggest that SAG possesses anti-inflammatory activity in vivo against acute as well as chronic inflammatory animal models at least in part by inhibition of prostaglandin production through COX-1/COX-2 inhibition. And COX inhibition of SAG is possibly contributed by S. deltoides extract among the ingredients. Although the anti-inflammatory potencies of SAG were less than those of currently used anti-inflammatory drugs, this formulation may have beneficial effect on inflammatory disorders as a neutraceutical.

  20. Effectiveness of action in India to reduce exposure of Gyps vultures to the toxic veterinary drug diclofenac.

    Directory of Open Access Journals (Sweden)

    Richard Cuthbert

    Full Text Available Contamination of their carrion food supply with the non-steroidal anti-inflammatory drug diclofenac has caused rapid population declines across the Indian subcontinent of three species of Gyps vultures endemic to South Asia. The governments of India, Pakistan and Nepal took action in 2006 to prevent the veterinary use of diclofenac on domesticated livestock, the route by which contamination occurs. We analyse data from three surveys of the prevalence and concentration of diclofenac residues in carcasses of domesticated ungulates in India, carried out before and after the implementation of a ban on veterinary use. There was little change in the prevalence and concentration of diclofenac between a survey before the ban and one conducted soon after its implementation, with the percentage of carcasses containing diclofenac in these surveys estimated at 10.8 and 10.7%, respectively. However, both the prevalence and concentration of diclofenac had fallen markedly 7-31 months after the implementation of the ban, with the true prevalence in this third survey estimated at 6.5%. Modelling of the impact of this reduction in diclofenac on the expected rate of decline of the oriental white-backed vulture (Gyps bengalensis in India indicates that the decline rate has decreased to 40% of the rate before the ban, but is still likely to be rapid (about 18% year(-1. Hence, further efforts to remove diclofenac from vulture food are still needed if the future recovery or successful reintroduction of vultures is to be feasible.

  1. Anti-inflammatory drugs: new multitarget compounds to face an old problem. The dual inhibition concept.

    Science.gov (United States)

    Celotti, F; Laufer, S

    2001-05-01

    In this short review we have tried to focus on some new relevant aspects of the pharmacological control of inflammation. The clinical availability of new drugs able to produce a selective inhibition of type 2 cyclooxygenase (COX-2), the enzyme thought to be mainly responsible for generating arachidonic-acid-derived inflammatory mediators, has been the origin of much hope. However, expectations of having an effective and completely safe non-steroidal anti-inflammatory drug (NSAID) have been only partially fulfilled. Emerging information has challenged some aspects of the original hypothesis indicating COX-2 as devoid of 'housekeeping' physiological functions. Moreover, the recently available clinical studies have indicated only a relatively small improvement in the tolerability of the newer 'selective' COX-2 inhibitors over the classical COX-1/COX-2 mixed type NSAIDs. The new appreciation of the role of other arachidonic acid derivatives, the leukotrienes (LTS), in producing and maintaining inflammation has generated considerable interest in drugs able to block LTS receptors or to produce a selective inhibition of 5-lipoxygenase (5-LO), the initial key enzyme of the leukotriene pathway. These drugs are now included among the effective therapies of asthma but appear, in the few clinical studies performed, to be an insufficient single therapeutic approach in other inflammatory diseases. Drugs able to block equally well both COX and 5-LO metabolic pathways (dual inhibitors) have been developed and experimentally evaluated in the last few years, but none are available on the market yet. The pharmacological rationale at the basis of their development is strong, and animal studies are indicative of a wide range of anti-inflammatory activity. What appears most impressive from the available studies on dual inhibitors is their almost complete lack of gastric toxicity, the most troublesome side effect of NSAIDs. The mechanism of the gastric-sparing properties of these drugs

  2. Anti-inflammatory and cytotoxic activities of Bursera copallifera.

    Science.gov (United States)

    Columba-Palomares, M F María C; Villareal, Dra María L; Acevedo Quiroz, M C Macdiel E; Marquina Bahena, M C Silvia; Álvarez Berber, Dra Laura P; Rodríguez-López, Dra Verónica

    2015-10-01

    The plant species Bursera copallifera (DC) bullock is used in traditional medicine to treat inflammation. The leaves of this plant can be prepared as an infusion to treat migraines, bronchitis, and dental pain. The purpose of this study was to determine the anti-inflammatory and cytotoxic activities of organic extracts from the stems, stem bark, and leaves of B. copallifera, which was selected based on the knowledge of its traditional use. We evaluated the ability of extracts to inhibit mouse ear inflammation in response to topical application of 12-O tetradecanoylphorbol-13-acetate. The extracts with anti-inflammatory activity were evaluated for their inhibition of pro-inflammatory enzymes. In addition, the in vitro cytotoxic activities of the organic extracts were evaluated using the sulforhodamine B assay. The hydroalcoholic extract of the stems (HAS) exhibited an anti-inflammatory activity of 54.3% (0.5 mg/ear), whereas the anti-inflammatory activity of the dichloromethane-methanol extract from the leaves (DMeL) was 55.4% at a dose of 0.1 mg/ear. Methanol extract from the leaves (MeL) showed the highest anti-inflammatory activity (IC50 = 4.4 μg/mL), hydroalcoholic extract of leaves, and DMeL also reduce the enzyme activity, (IC50 = 6.5 μg/mL, IC50 = 5.7 μg/mL), respectively, from stems HAS exhibit activity at the evaluated concentrations (IC50 =6.4 μg/mL). The hydroalcoholic extract of the stems exhibited the highest cytotoxic activity against a breast adenocarcinoma cell line (MCF7, IC50 = 0.90 μg/mL), whereas DMeL exhibited an IC50 value of 19.9 μg/mL. In conclusion, extracts from leaves and stems inhibited cyclooxygenase-1, which is the target enzyme for nonsteroidal anti inflammatory drugs, and some of these extracts demonstrated substantial antiproliferative effects against the MCF7 cell line. These results validate the traditional use of B. copallifera.

  3. The substituent effect from the perspective of local hyper-softness. An example applied on normeloxicam, meloxicam and 4-meloxicam: Non-steroidal anti-inflammatory drugs

    Science.gov (United States)

    Martínez-Araya, Jorge Ignacio; Glossman-Mitnik, Daniel

    2015-01-01

    Normeloxicam, meloxicam and 4-meloxicam were analyzed from the perspective of the conceptual density functional theory perspective to determine the substituent effect exerted by the methyl group that is located at the thiazole ring. This analysis was performed in absence and presence of water. The position of the methyl group suggests that differences that have been experimentally reported in a previous paper can be mainly attributable to electronic effects exerted by the substituent aforementioned group. Finally, the use of total electronic densities is encouraged in future calculations instead of densities of frontier molecular orbitals to obtain more accurate results.

  4. Effects of kinesiotaping versus non-steroidal anti-inflammatory drugs and physical therapy for treatment of pes anserinus tendino-bursitis: A randomized comparative clinical trial.

    Science.gov (United States)

    Homayouni, Kaynoosh; Foruzi, Shima; Kalhori, Fereshte

    2016-09-01

    Pes anserinus tendino-bursitis is a condition caused by repetitive friction over the bursa or direct trauma to knee joint and it presents with proximal medial tibial pain and swelling. The aim of this study is to determine the effects of kinesiotaping in comparison with naproxen and physical therapy in treatment of pes anserinus tendino-bursitis. In a randomized comparative clinical trial 56 patients with clinical diagnosis of pes anserinus tendino-bursitis were randomly assigned to kinesiotaping and naproxen/physical therapy (28 patients in each group). Kinesiotaping on the tender area in the form of space-correction (lifting) technique was used and repeated for three times with a one-week interval. Another group received naproxen (250mg TID for 10 days) and ten sessions of daily physical therapy. The visual analog scale (VAS) was used for evaluation of pain. The depth of swelling of the area was measured with sonography before and after treatment. Wilcoxon signed ranks test has been used for determining the influence of interventions on pain (VAS) and swelling scores in each group. The ANCOVA (Analysis of covariance) test was applied for comparing the influence of interventions on VAS and swelling scores after adjustment for co-variables. At end of the study, 27 patients remained in the kinesiotaping group and 19 patients in naproxen/physical therapy group. Treatment with kinesiotaping significantly decreased the pain (P=0.0001) and swelling scores (P=0.0001) in comparison with naproxen/physical therapy after adjustment for baseline characteristics. Kinesiotaping was safe without any complications except for a mild local skin irritation in one patient. Kinesiotaping is more effective than naproxen plus physical therapy in reduction of pain and swelling in patients with pes anserinus tendino-bursitis. www.ClinicalTrials.gov identifier is NCT01680263.

  5. Paracetamol (acetaminophen) or non-steroidal anti-inflammatory drugs, alone or combined, for pain relief in acute otitis media in children

    NARCIS (Netherlands)

    Sjoukes, Alies|info:eu-repo/dai/nl/413981436; Venekamp, Roderick P|info:eu-repo/dai/nl/343020211; van de Pol, Alma C|info:eu-repo/dai/nl/304816736; Hay, Alastair D; Little, Paul; Schilder, Anne GM|info:eu-repo/dai/nl/09110906X; Damoiseaux, Roger Amj|info:eu-repo/dai/nl/183925858

    2016-01-01

    BACKGROUND: Acute otitis media (AOM) is one of the most common childhood infectious diseases and a significant reason for antibiotic prescriptions in children worldwide. Pain from middle ear infection and pressure behind the eardrum is the key symptom of AOM. Ear pain is central to children's and

  6. Rapid confirmatory analysis of non-steroidal anti-inflammatory drugs in bovine milk by rapid resolution liquid chromatography tandem mass spectrometry.

    Science.gov (United States)

    Dowling, Geraldine; Gallo, Pasquale; Malone, Edward; Regan, Liam

    2009-11-13

    A rapid method has been developed to analyse carprofen (CPF), diclofenac (DCF), mefenamic acid (MFN), niflumic acid (NIFLU), naproxen (NAP), oxyphenylbutazone (OXYPHEN), phenylbutazone (PBZ) and suxibuzone (SUXI) residues in bovine milk. Milk samples are extracted with acetonitrile and sample extracts were purified on Evolute ABN solid phase extraction cartridges. Aliquots were analysed by rapid resolution liquid chromatography tandem mass spectrometry (RRLC-MS/MS) with a runtime of 6.5 min. The method was validated in bovine milk, according to the criteria defined in Commission Decision 2002/657/EC. CCalpha values of 0.46, 1.08, 0.92, 1.26, 1.29, 2.12, 0.55 and 2.86 ng mL(-1) were determined for CPF, DCF, MFN, NIFLU, NAP, OXYPHEN, PBZ and SUXI, respectively. CCbeta values of 0.79, 1.85, 1.56, 2.15, 2.19, 3.62, 0.94 and 4.87 ng mL(-1) were determined for CPF, DCF, MFN, NIFLU, NAP, OXYPHEN, PBZ and SUXI, respectively. The measurement uncertainty of the method was estimated at 9, 28, 28, 45, 46, 45, 10 and 39% for CPF, DCF, MFN, NIFLU, NAP, OXYPHEN, PBZ and SUXI. Fortifying bovine milk samples (n=18) in three separate assays, show the accuracy of the method to be between 82 and 108%. The precision of the method, expressed as RSD values for the within-lab reproducibility at the three levels of fortification (5, 7.5 and 10 ng mL(-1)) was less than 16%, respectively. The advantage of the method is that low ng mL(-1) levels can be detected and quantitatively confirmed rapidly in milk and that 3 batches of samples can be analysed within a single day using RRLC-MS/MS with a runtime of 6.5 min.

  7. Lactobacillus plantarum Strains Can Enhance Human Mucosal and Systemic Immunity and Prevent Non-steroidal Anti-inflammatory Drug Induced Reduction in T Regulatory Cells

    NARCIS (Netherlands)

    de Vos, Paul; Mujagic, Zlatan; de Haan, Bart J.; Siezen, Roland J.; Bron, Peter A.; Meijerink, Marjolein; Wells, Jerry M.; Masclee, Ad A. M.; Boekschoten, Mark V.; Faas, Marijke M.; Troost, Freddy J.

    2017-01-01

    Orally ingested bacteria interact with intestinal mucosa and may impact immunity. However, insights in mechanisms involved are limited. In this randomized placebo-controlled cross-over trial, healthy human subjects were given Lactobacillus plantarum supplementation (strain TIFN101, CIP104448, or

  8. Optimization of the Ion Source-Mass Spectrometry Parameters in Non-Steroidal Anti-Inflammatory and Analgesic Pharmaceuticals Analysis by a Design of Experiments Approach

    Science.gov (United States)

    Paíga, Paula; Silva, Luís M. S.; Delerue-Matos, Cristina

    2016-10-01

    The flow rates of drying and nebulizing gas, heat block and desolvation line temperatures and interface voltage are potential electrospray ionization parameters as they may enhance sensitivity of the mass spectrometer. The conditions that give higher sensitivity of 13 pharmaceuticals were explored. First, Plackett-Burman design was implemented to screen significant factors, and it was concluded that interface voltage and nebulizing gas flow were the only factors that influence the intensity signal for all pharmaceuticals. This fractionated factorial design was projected to set a full 22 factorial design with center points. The lack-of-fit test proved to be significant. Then, a central composite face-centered design was conducted. Finally, a stepwise multiple linear regression and subsequently an optimization problem solving were carried out. Two main drug clusters were found concerning the signal intensities of all runs of the augmented factorial design. p-Aminophenol, salicylic acid, and nimesulide constitute one cluster as a result of showing much higher sensitivity than the remaining drugs. The other cluster is more homogeneous with some sub-clusters comprising one pharmaceutical and its respective metabolite. It was observed that instrumental signal increased when both significant factors increased with maximum signal occurring when both codified factors are set at level +1. It was also found that, for most of the pharmaceuticals, interface voltage influences the intensity of the instrument more than the nebulizing gas flowrate. The only exceptions refer to nimesulide where the relative importance of the factors is reversed and still salicylic acid where both factors equally influence the instrumental signal.

  9. Validated RP-HPLC Method for the Assay of Etoricoxib (A Non-Steroidal Anti-Inflammatory Drug in Pharmaceutical Dosage Forms

    Directory of Open Access Journals (Sweden)

    Srinivasu Topalli

    2012-01-01

    Full Text Available A simple, accurate, sensitive and reproducible reverse phase high performance liquid chromatographic method has been developed for the quantitative determination of Etoricoxib in pharmaceutical dosage forms. The assay was performed on Hypersil ODS C-18 (250 x 4.6 mm., 5µm particle size column using acetonitrile and potassium dihydrogen phosphate buffer (pH 4.2 (46:54 % v/v as mobile phase with UV detection at 280 nm (flow rate 1.2 ml/min. Bromhexine was used as an internal standard. Quantization was achieved by measurement of the peak area ratio of the drug to the internal standard. The limit of detection (LOD and the limit of quantification (LOQ were 0.0704 µg ml-1 and 0.2134 µg ml-1 respectively. Each analysis required no longer than 10 minutes. The calibration curve was linear over the concentration range from 0.5-85.0 µg ml-1. The retention times of Etoricoxib and Bromhexine were found to be 3.083 and 7.631 minutes respectively. The proposed method was validated according to the ICH guidelines and can be used successfully to analyse marketed formulations.

  10. INFLUENCE OF NON-STEROIDAL ANTI-INFLAMMATORY EYE DROPS ON THE EPITHELIUM CELLS OF THE CORNEA AND CONJUNCTIVA IN VITRO

    Directory of Open Access Journals (Sweden)

    O. I. Aleksandrova

    2017-01-01

    Full Text Available Objective: to evaluate the effect of NSAIDs eye drops with different preservatives on the viability of epithelial cells of human eyes in vitro. Materials and methods. The object of the study was four of the drug Broxinac®, Acular LS®, Diclo-F ®, Indocollyre®. As test-systems were used permanent cell lines of transformed conjunctival (Chang Conjunctiva, Clone 1-5c-4 and corneal (HCEC. The cytotoxicity of NSAID drops were assessed by the morphology and functional cells activity by the methods of phase contrast microscopy (PCM, MTT test and cell analysis in real time using the xCELLigence system. Results. It was found with MTT-test that cell lines HCEC are more sensitive to the cytotoxic action of the studied drugs than cell lines of Chang Conjunctiva, Clone 1-5C-4. The metabolic activity of conjunctiva cells in the presence of drugs, Acular LS® and Broxinac® was three times lower than in control; in the presence of drugs Indocollyre® and Diclo-F® — 20 times lower vs. the control. The metabolic activity of the cornea cells e in the presence of drugs, Acular LS® and Broxinac® was four times lower than in control; in the presence of drugs Indocollyre® and Diclo-F® viable cells were not identified. Drugs Indocollyre® and Diclo-F® has had a very high toxic effect on both cell types. The results of cell analysis xCELLIgence for both types of cells are consistent with the results of MTT test and in vivo observation of cells. Conclusion. Based on these data, there is the following gradation of NSAID eye drop’s cytotoxic potential: (reduce toxicity: Indocollyre® = Diclo-F® > Acular LS® = Broxinac®.

  11. GUIDELINES FOR PREVENTION AND MANAGEMENT OF GASTROINTESTINAL ADVERSE EFFECTS IN PATIENTS RECEIVING NON-STEROIDAL ANTI-INFLAMMATORY AND ANTIAGGREGANT THERAPY

    Directory of Open Access Journals (Sweden)

    Borut Štabuc

    2015-03-01

    Full Text Available Adverse effects of nonsteroidal antiinflammatory drugs and antiaggregants on gastrointestinal tract can be prevented or reduced by rational prescribing, use of proton pump inhibitors and Helicobacter pylori eradication.Nonsteroidal antiinflammatory drugs should not be used to treat patients with high risk for serious adverse effects on either upper gastrointestinal or cardiovascular system. Proton pump inhibitors in standard oral dosages are used for treatment of dyspepsia or gastric and duodenal erosions and ulcers, caused by nonsteroidal antiinflammatory drug or antiaggregant use. Peptic ulcer hemorrhage is treated with endoscopic hemostasis and proton pump inhibitors (72-hour continuous infusion followed by 4 – 8 week standard dose oral treatment.Patients can be stratified into three groups based on risk for upper gastrointestinal system adverse effects associated with nonsteroidal antiinflammatory drugs or antiaggregants use. Absence of risk factors denotes low-risk patient population, one or two risk factors are associated with medium risk; high-risk patients harbor either three or more risk factors or history of complicated peptic ulcer disease.  Helicobacter pylori should be eradicated (if present in all medium and high-risk patients prior to introduction of nonsteroidal antiinflammatory drugs or antiaggregants and proton pump inhibitors in standard daily dose should be prescribed for the duration of the treatment.Risk of gastrointestinal hemorrhage should be considered when planning invasive cardiovascular procedures or introduction of antiaggregant or anticoagulant treatment. In the context of acute gastrointestinal hemorrhage, antiaggregants should not be discontinued for longer than 7 days and oral anticoagulant therapy should be stopped and converted to low-molecular-weight heparin after complete hemostasis.

  12. The pattern of use of non-steroidal anti-inflammatory drugs (NSAIDs) from 1997 to 2005: a nationwide study on 4.6 million people

    DEFF Research Database (Denmark)

    Fosbøl, Emil Loldrup; Gislason, Gunnar H; Jacobsen, Søren

    2008-01-01

    and increasing age was associated with increased use of NSAID. Factors predicting extensive NSAID use were: rheumatic disease (odds ratio (OR) = 1.79, 95% confidence interval (CI): 1.69-1.90), gout agents (allopurinol) (OR = 2.54, CI: 2.44-2.64) and other pain medication (OR = 3.27, CI: 3.23-3.31). NSAIDs were...

  13. Detecting drug-drug interactions using a database for spontaneous adverse drug reactions : an example with diuretics and non-steroidal anti-inflammatory drugs

    NARCIS (Netherlands)

    van Puijenbroek, E P; Egberts, A C; Heerdink, E R; Leufkens, H G

    2000-01-01

    OBJECTIVE: Drug-drug interactions are relatively rarely reported to spontaneous reporting systems (SRSs) for adverse drug reactions. For this reason, the traditional approach for analysing SRS has major limitations for the detection of drug-drug interactions. We developed a method that may enable

  14. The impact of selective and non-selective non-steroid anti-inflammatory drugs on secondary hemostasis in healthy volunteers

    DEFF Research Database (Denmark)

    Schjerning, Ole; Larsen, Torben B; Damkier, Per

    2009-01-01

    celecoxib 100 mg b.i.d. or naproxen 250 mg b.i.d. Treatment periods were separated by a washout period of 28 days. Blood samples were obtained before the first medication period, and at the end of each medication period. Primary effect parameter was FXII level. Secondary effect parameters included a wide...... range of coagulation factors involved in secondary hemostasis. RESULTS: There was no statistically significant effect of celecoxib or naproxen on the primary effect parameter. Protein C activity was significantly decreased after treatment with naproxen (P..., demonstrated as closure time (CT), was at baseline 118+/-24 sec. (mean+/-SD). Naproxen prolonged CT to 171+/-50 sec. (Pnaproxen caused any change...

  15. Ongoing treatment with non-steroidal anti-inflammatory drugs at time of admission is associated with poorer prognosis in patients with first-time acute myocardial infarction

    DEFF Research Database (Denmark)

    Lamberts, M.; Fosbol, E. L.; Olsen, A. M. S.

    2013-01-01

    was significantly increased in patients receiving rofecoxib (hazard ratio [HR] 1.15; CI 1.04-1.27), celecoxib (HR 1.13; CI 1.01-1.26), diclofenac (HR 1.12; CI 1.04-1.20) or any NSAID use (HR 1.05; CI 1.02-1.09). No association was found for naproxen or ibuprofen. Conclusion: Ongoing treatment with NSAIDs...

  16. Automated evaluation of protein binding affinity of anti-inflammatory choline based ionic liquids.

    Science.gov (United States)

    Ribeiro, Rosa; Pinto, Paula C A G; Azevedo, Ana M O; Bica, Katharina; Ressmann, Anna K; Reis, Salette; Saraiva, M Lúcia M F S

    2016-04-01

    In this work, an automated system for the study of the interaction of drugs with human serum albumin (HSA) was developed. The methodology was based on the quenching of the intrinsic fluorescence of HSA by binding of the drug to one of its binding sites. The fluorescence quenching assay was implemented in a sequential injection analysis (SIA) system and the optimized assay was applied to ionic liquids based on the association of non-steroidal anti-inflammatory drugs with choline (IL-API). In each cycle, 100 µL of HSA and 100 µL of IL-API (variable concentration) were aspirated at a flow rate of 1 mL min(-1) and then sent through the reaction coil to the detector where the fluorescence intensity was measured. In the optimized conditions the effect of increasing concentrations of choline ketoprofenate and choline naproxenate (and respective starting materials: ketoprofen and naproxen) on the intrinsic fluorescence of HSA was studied and the dissociation constants (Kd) were calculated by means of models of drug-protein binding in the equilibrium. The calculated Kd showed that all the compounds bind strongly to HSA (Kd<100 µmol L(-1)) and that the use of the drugs in the IL format does not affect or can even improve their HSA binding. The obtained results were compared with those provided by a conventional batch assay and the relative errors were lower than 4.5%. The developed SIA methodology showed to be robust and exhibited good repeatability in all the assay conditions (rsd<6.5%). Copyright © 2015 Elsevier B.V. All rights reserved.

  17. Fetal exposure to nonsteroidal anti-inflammatory drugs and spontaneous abortions

    Science.gov (United States)

    Daniel, Sharon; Koren, Gideon; Lunenfeld, Eitan; Bilenko, Natalya; Ratzon, Ronit; Levy, Amalia

    2014-01-01

    Background: Spontaneous abortion is the most common complication of pregnancy. Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used during pregnancy. Published data are inconsistent regarding the risk of spontaneous abortion following exposure to NSAIDs. Methods: We performed a historical cohort study involving all women who conceived between January 2003 and December 2009 and who were admitted for delivery or spontaneous abortion at Soroka Medical Center, Clalit Health Services, Israel. A computerized database of medication dispensation was linked with 2 computerized databases containing information on births and spontaneous abortions. We constructed time-varying Cox regression models and adjusted for maternal age, diabetes mellitus, hypothyroidism, obesity, hypercoagulation or inflammatory conditions, recurrent miscarriage, in vitro fertilization of the current pregnancy, intrauterine contraceptive device, ethnic background, tobacco use and year of admission. Results: The cohort included 65 457 women who conceived during the study period; of these, 58 949 (90.1%) were admitted for a birth and 6508 (9.9%) for spontaneous abortion. A total of 4495 (6.9%) pregnant women were exposed to NSAIDs during the study period. Exposure to NSAIDs was not an independent risk factor for spontaneous abortion (nonselective cyclooxygenase [COX] inhibitors: adjusted hazard ratio [HR] 1.10, 95% confidence interval [CI] 0.99–1.22; selective COX-2 inhibitors: adjusted HR 1.43, 95% CI 0.79–2.59). There was no increased risk for specific NSAID drugs, except for a significantly increased risk with exposure to indomethacin (adjusted HR 2.8, 95% CI 1.70–4.69). We found no dose–response effect. Interpretation: We found no increased risk of spontaneous abortion following exposure to NSAIDs. Further research is needed to assess the risk following exposure to selective COX-2 inhibitors. PMID:24491470

  18. Fetal exposure to nonsteroidal anti-inflammatory drugs and spontaneous abortions.

    Science.gov (United States)

    Daniel, Sharon; Koren, Gideon; Lunenfeld, Eitan; Bilenko, Natalya; Ratzon, Ronit; Levy, Amalia

    2014-03-18

    Spontaneous abortion is the most common complication of pregnancy. Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used during pregnancy. Published data are inconsistent regarding the risk of spontaneous abortion following exposure to NSAIDs. We performed a historical cohort study involving all women who conceived between January 2003 and December 2009 and who were admitted for delivery or spontaneous abortion at Soroka Medical Center, Clalit Health Services, Israel. A computerized database of medication dispensation was linked with 2 computerized databases containing information on births and spontaneous abortions. We constructed time-varying Cox regression models and adjusted for maternal age, diabetes mellitus, hypothyroidism, obesity, hypercoagulation or inflammatory conditions, recurrent miscarriage, in vitro fertilization of the current pregnancy, intrauterine contraceptive device, ethnic background, tobacco use and year of admission. The cohort included 65,457 women who conceived during the study period; of these, 58,949 (90.1%) were admitted for a birth and 6508 (9.9%) for spontaneous abortion. A total of 4495 (6.9%) pregnant women were exposed to NSAIDs during the study period. Exposure to NSAIDs was not an independent risk factor for spontaneous abortion (nonselective cyclooxygenase [COX] inhibitors: adjusted hazard ratio [HR] 1.10, 95% confidence interval [CI] 0.99-1.22; selective COX-2 inhibitors: adjusted HR 1.43, 95% CI 0.79-2.59). There was no increased risk for specific NSAID drugs, except for a significantly increased risk with exposure to indomethacin (adjusted HR 2.8, 95% CI 1.70-4.69). We found no dose-response effect. We found no increased risk of spontaneous abortion following exposure to NSAIDs. Further research is needed to assess the risk following exposure to selective COX-2 inhibitors.

  19. Biochemical pharmacology of nonsteroidal anti-inflammatory drugs.

    Science.gov (United States)

    Wu, K K

    1998-03-01

    Aspirin and conventional nonsteroidal anti-inflammatory drugs are nonselective inhibitors of cyclooxygenase-1 (COX-1) and COX-2 enzymes. Two classes of selective COX-2 inhibitors: (1) sulfonamides, such as L-745,337, and (2) tricyclic methyl sulfone derivatives, such as SC58125, have been developed. X-ray crystal structures of COX-1 and COX-2 have provided valuable information regarding the structural basis for their COX-2 selectivity. These compounds have less gastrointestinal complications in animal experiments. Their clinical efficacy and side-effects are being evaluated. Salicylate has very weak activity against either COX isoform and yet possesses anti-inflammatory actions. Recent studies indicate that it suppresses the expression of genes involved in inflammation. These activities may provide a plausible explanation for the pharmacological dilemma and, furthermore, may represent novel mechanisms for controlling inflammation.

  20. Anti-Inflammatory Properties of Dendrimers per se

    Directory of Open Access Journals (Sweden)

    Myriam Hayder

    2011-01-01

    Full Text Available Dendrimers are polybranched and polyfunctionalized tree-like polymers. Unlike linear polymers, they have perfectly defined structure and molecular weight, due to their iterative step-by-step synthesis. Their multivalent structure and supramolecular properties have made them attractive nanotools for applications, particularly in biology and medicine. Among the different biological and medical properties of dendrimers that have been developed over the past decades, the anti-inflammatory properties of several groups of dendrimers are the most recently discovered. Thereof, dendrimers emerge as promising, although heretical, drug candidates for the treatment of still-uncured chronic inflammatory disorders. This mini-review is based on the five main scientific articles giving an overview of what can be the spectrum of anti-inflammatory characteristics displayed by dendrimers.

  1. Anti-inflammatory flavanol glycosides from Saraca asoca bark.

    Science.gov (United States)

    Ahmad, Furkan; Misra, Laxminarain; Tewari, Rashi; Gupta, Preeti; Mishra, Pratikshita; Shukla, Rakesh

    2016-01-01

    Saraca asoca (Roxb.) de Wilde, a common tree of India, is popularly used in the Ayurvedic and modern herbal systems of medicine for genito-urinary problems of women. Considering the reported antimicrobial or anti-inflammatory effect of S. asoca bark against such infections, we studied the anti-inflammatory activity-guided isolation of active compounds from methanol extract. The methanol extract of bark has yielded 10 compounds out of which 3'-deoxyepicatechin-3-O-β-D-glucopyranoside (6) and 3'-deoxycatechin-3-O-α-L-rhamnopyranoside (8) have been found to be in vitro and in vivo active. 3',5-Dimethoxy epicatechin (3), 3'-deoxyepicatechin-3-O-β-D-glucopyranoside (6), 3'-deoxycatechin-3-O-α-L-rhamnopyranoside (8) and epigallocatechin (9) are being reported for the first time from S. asoca.

  2. Anti-inflammatory and analgesic activity of r.a.p . ( Radix Angelicae ...

    African Journals Online (AJOL)

    The objective of this paper was to study the anti-inflammatory and analgesic effects of Radix Angelicae Pubescentis (R.A.P) ethanol extracts. Three classic anti-inflammatory models and two analgesic models were used in this research. In anti-inflammatory tests, all the extracts have a certain inhibition on the acute ...

  3. Immunomodulatory and anti-inflammatory activity of Picrorhiza scrophulariiflora.

    Science.gov (United States)

    Smit, H F; Kroes, B H; van den Berg, A J; van der Wal, D; van den Worm, E; Beukelman, C J; van Dijk, H; Labadie, R P

    2000-11-01

    Extracts of the rhizomes of Picrorhiza scrophulariiflora Pennell (Scrophulariaceae) were investigated for their in vitro and in vivo immunomodulatory properties. Diethyl ether extracts showed potent inhibitory activity towards the classical pathway of the complement system, the respiratory burst of activated polymorphonuclear leukocytes, and mitogen-induced proliferation of T-lymphocytes. Furthermore, such extracts showed anti-inflammatory activity towards carrageenan-induced paw edema. No effects were observed in experimentally induced arthritis in mice.

  4. Anti-inflammatory and Antinociceptive Effects of the Alcoholic Extract ...

    African Journals Online (AJOL)

    Anti-inflammatory and Antinociceptive Effects of the Alcoholic Extract of Indian Polygala arvensis in Experimental Animals. ... time in the hot plate method by 69.55% (p < 0.01) and 107.13% (p < 0.001) respectively as well as in analgesymeter-induced mechanical pain by 28.84% (p < 0.5) and 55.71% (p < 0.05) respectively.

  5. Two Anti-inflammatory Steroidal Saponins from Dracaena angustifolia Roxb.

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    Yueh-Hsiung Kuo

    2013-07-01

    Full Text Available Two new steroidal saponins, named drangustosides A–B (1–2, together with eight known compounds 3–10 were isolated and characterized from the MeOH extract of Dracaena angustifolia Roxb. The structures of compounds were assigned based on 1D and 2D NMR spectroscopic analyses, including HMQC, HMBC, and NOESY. Compounds 1 and 2 showed anti-inflammatory activity by superoxide generation and elastase release by human neutrophils in response to fMLP/CB.

  6. ANTI-INFLAMMATORY EFFECTS OF CHAMOMILE ESSENTIAL OIL IN MICE

    OpenAIRE

    Fabian, D.; Juhás, Š. (Štefan); Bukovska, A.; Bujňáková, D.; Grešáková, L.; Koppel, J.

    2011-01-01

    Essential oils are plant secondary metabolites with positive pharmacological properties, e.g. anti-oxidative, antimicrobial or immunomodulative, but they can have toxic and allergic effects as well. The aim of this study was to analyze anti-inflammatory effects of chamomile essential oil dietary administration in carrageenan paw oedema and trinitrobenzene sulfonic acid (TNBS) colitis. Mice received chamomile essential oil in three concentrations (5000, 2500 and 1250 ppm) in the standard roden...

  7. Synthesis, in vitro anti-inflammatory activity and molecular docking ...

    Indian Academy of Sciences (India)

    Synthesis, in vitro anti-inflammatory activity and molecular docking .... 2.2 Synthesis. 2.2a Synthesis of 2,3-bis (4-methoxy phenyl)-3-chloro-2- prop-2-ene aldehyde (2): 0.05 mol (7.66 g) of phosphorous oxychloride (POCl3) was added drop wise over a period of ...... a mechanism of action for aspirin-like drugs Nature 231.

  8. Current status of anti-inflammatory therapy for posttraumatic osteoarthritis.

    Science.gov (United States)

    Schmal, H; Marintschev, I; Salzmann, G M

    2016-09-01

    Although there is ample evidence that intra-articular injuries are associated with the up-regulation of pro-inflammatory cytokines, the success of anti-inflammatory, disease-modifying treatments to prevent posttraumatic osteoarthritis (PTOA) remain uncertain. To summarize the current status of anti-inflammatory therapy for PTOA, we conducted a systematic review. 9 clinical studies in humans were identified applying anti-inflammatory agents to prevent or treat PTOA. A total of 347 patients aged an average 41 ± 14 years were included in this review. 5 studies had comparable designs with randomized allocation. Those studies of course had a statistically significant higher Coleman Methodology Score (65 ± 6) than the case-control studies (39 ± 13, p = 0.013). The most frequently reported main outcome parameter was pain assessed by different scales (n = 7), the most examined joint the knee (n = 7). The majority of the analyses (n = 6) focused on the intra-articular (IA) application of hyaluronic acid (HA) reporting mainly positive effects. One study stated positive results following IA administration of Interleukin 1 receptor antagonist in -patients presenting rupture of the anterior cruciate ligament. Platelet-rich plasma was also used to relieve symptoms following acute injury, but the study quality was too low to conclude any effects. Although the initial data, especially regarding IA HA injection, are encouraging, study designs differ substantially. Therefore, current data does not allow us to conclude that anti-inflammatory therapy following acute injuries has beneficial effects on short- or long-term outcomes.

  9. Anti-inflammatory activity of traditional Chinese medicinal herbs

    Directory of Open Access Journals (Sweden)

    Min-Hsiung Pan

    2011-10-01

    Full Text Available Accumulating epidemiological and clinical evidence shows that inflammation is an important risk factor for various human diseases. Thus, suppressing chronic inflammation has the potential to delay, prevent, and control various chronic diseases, including cerebrovascular, cardiovascular, joint, skin, pulmonary, blood, lymph, liver, pancreatic, and intestinal diseases. Various natural products from traditional Chinese medicine (TCM have been shown to safely suppress proinflammatory pathways and control inflammation-associated disease. In vivo and/or in vitro studies have demonstrated that anti-inflammatory effects of TCM occur by inhibition of the expression of master transcription factors (for example, nuclear factor-κB (NF-κB, pro-inflammatory cytokines (for example, tumor necrosis factor-α (TNF-α, chemokines (for example, chemokine (C-C motif ligand (CCL-24, intercellular adhesion molecule expression and pro-inflammatory mediators (for example, inducible nitric oxide synthase (iNOS and cyclooxygenase 2 (COX2. However, a handful of review articles have focused on the anti-inflammatory activities of TCM and explore their possible mechanisms of action. In this review, we summarize recent research attempting to identify the anti-inflammatory constituents of TCM and their molecular targets that may create new opportunities for innovation in modern pharmacology.

  10. Anti-Inflammatory Cembranoids from the Soft Coral Lobophytum crassum

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    Kuei-Hung Lai

    2017-10-01

    Full Text Available Abstract: Cembrane-type diterpenoids are among the most frequently encountered natural products from the soft corals of the genus Lobophytum. In the course of our investigation to identify anti-inflammatory constituents from a wild-type soft coral Lobophytum crassum, two new cembranoids, lobophyolide A (1 and B (2, along with five known compounds (3–7, were isolated. The structures of these natural products were identified using NMR and MS spectroscopic analyses. Compound 1 was found to possess the first identified α-epoxylactone group among all cembrane-type diterpenoids. The in vitro anti-inflammatory effect of compounds 1–5 was evaluated. The results showed that compounds 1–5 not only reduced IL-12 release, but also attenuated NO production in LPS-activated dendritic cells. Our data indicated that the isolated series of cembrane-type diterpenoids demonstrated interesting structural features and anti-inflammatory activity which could be further developed into therapeutic entities.

  11. Anti-inflammatory activity of polysaccharide from Pholiota nameko.

    Science.gov (United States)

    Li, Haiping; Lu, Xiaoxiang; Zhang, Shuhai; Lu, Meijun; Liu, Hongmei

    2008-06-01

    Pholiota nameko polysaccharide (PNPS-1) has been isolated and purified by enzymatic hydrolysis, hot water extraction, ethanol precipitation, and ion-exchange and gel-filtration chromatography. The anti-inflammatory activity of PNPS-1 was evaluated in rodents using xylene-induced ear edema, egg albumin-, carrageenin-, and formaldehyde-induced paw edema, cotton pellet granuloma test, adhesion of peritoneal leukocytes in vitro, and ulcerogenic activity. The results showed that PNPS-1 (5 mg/ear) inhibited topical edema in the mouse ear and at 100, 200, and 400 mg/kg (intraperitoneally) it significantly suppressed the development of egg albumin-, carrageenin-, and formaldehyde-induced paw edema in the animals. PNPS-1 (100, 200, and 400 mg/kg, per oral) significantly inhibited the growth of granuloma tissues induced by subcutaneously implanted cotton pellets in rats by 10.96, 18.07, and 43.75%, respectively. PNPS-1 also inhibited spontaneous and phorbol-12-myristate-13-acetate-activated adhesion of peritoneal leukocytes in vitro. Further, both acute as well as chronic administration of PNPS-1 (100, 200, and 400 mg/kg, per oral) did not produce any gastric lesion in rats. In conclusion, these data indicated that PNPS-1 possesses significant anti-inflammatory activity suggesting its potential as an anti-inflammatory agent for use in the treatment of various inflammatory-related diseases.

  12. Anti-inflammatory activity in selected Antarctic benthic organisms

    Directory of Open Access Journals (Sweden)

    Juan eMoles

    2014-07-01

    Full Text Available Antarctic benthos was prospected in search for anti-inflammatory activity in polar benthic invertebrates, in two different geographical areas: deep-bottoms of the Eastern Weddell Sea and shallow-waters of the South Shetland Islands. A total of 36 benthic algae and invertebrate species were selected to perform solubility tests in order to test them for anti-inflammatory activity. From these, ethanol extracts of ten species from five different phyla resulted suitable to be studied in cell macrophage cultures (RAW 264.7. Cytotoxicity (MTT method and production of inflammatory mediators (prostaglandin E2, leukotriene B4, interleukin-1 were determined at three extract concentrations (50, 125, 250 g/mL. Bioassays resulted in four different species showing anti-inflammatory activity corresponding to three sponges: Mycale (Oxymycale acerata, Isodictya erinacea, and I. toxophila; and one hemichordate: Cephalodiscus sp. These results show that Antarctic sessile invertebrates may have great value as a source of lead compounds with potential pharmaceutical applications.

  13. Anti-inflammatory properties of pterocarpanquinone LQB-118 in mice.

    Science.gov (United States)

    Riça, Ingred G; Netto, Chaquip D; Rennó, Magdalena N; Abreu, Paula A; Costa, Paulo R R; da Silva, Alcides J M; Cavalcante, Moisés C M

    2016-09-15

    Pterocarpanquinone (+/-)-LQB-118 presents antineoplastic and antiparasitic properties and also shows great inhibitory effect on TNF-α release in vitro. Here, its anti-inflammatory activity was evaluated in a lipopolysaccharide (LPS)-induced lung inflammation model in C57BL/6 mice. LPS inhalation induced a marked neutrophil infiltration to the lungs which was reduced by intraperitoneal treatment with (+/-)-LQB-118 in a similar manner to that of dexamethasone and even better than that of acetylsalicylic acid. Moreover, (+/-)-LQB-118 administration resulted in decrease of NF-κB activation and KC level in lungs, with a pronounced inhibitory effect on TNF-α release, measured in bronchoalveolar lavage fluid. Trying to understand the anti-inflammatory mechanism by which (+/-)-LQB-118 acts, we performed a molecular modeling analysis, including docking to estrogen receptors α and β. Results suggested that (+/-)-LQB-118 may bind to both receptors, with a similar orientation to 17-β-estradiol. Together, these results showed that (+/-)-LQB-118 exhibits an anti-inflammatory effect, most likely by inhibiting TNF-α release and NF-κB activation, which may be related to the estrogen receptor binding. Copyright © 2016 Elsevier Ltd. All rights reserved.

  14. UV filters, ingredients with a recognized anti-inflammatory effect.

    Directory of Open Access Journals (Sweden)

    Céline Couteau

    Full Text Available BACKGROUND: To explain observed differences during SPF determination using either an in vivo or in vitro method, we hypothesized on the presence of ingredients having anti-inflammatory properties. METHODOLOGY/PRINCIPAL FINDINGS: To research our hypothesis, we studied the 21 UV filters both available on the market and authorized by European regulations and subjected these filters to the phorbol-myristate-acetate test using mice. We then catalogued the 13 filters demonstrating a significant anti-inflammatory effect with edema inhibition percentages of more than 70%. The filters are: diethylhexyl butamido triazone (92%, benzophenone-5 and titanium dioxide (90%, benzophenone-3 (83%, octocrylène and isoamyl p-methoxycinnamate (82%, PEG-25 PABA and homosalate (80%, octyl triazone and phenylbenzimidazole sulfonic acid (78%, octyl dimethyl PABA (75%, bis-ethylhexyloxyphenol methoxyphenyl triazine and diethylamino hydroxybenzoyl hexylbenzoate (70%. These filters were tested at various concentrations, including their maximum authorized dose. We detected a dose-response relationship. CONCLUSIONS/SIGNIFICANCE: The anti-inflammatory effect of a sunscreen ingredient may affect the in vivo SPF value.

  15. Anti-inflammatory effect of thalidomide dithiocarbamate and dithioate analogs.

    Science.gov (United States)

    Talaat, Roba; El-Sayed, Waheba; Agwa, Hussein S; Gamal-Eldeen, Amira M; Moawia, Shaden; Zahran, Magdy A H

    2015-08-05

    Thalidomide has anti-inflammatory, immunomodulatory, and anti-angiogenic properties. It has been used to treat a variety of cancers and autoimmune diseases. This study aimed to characterize anti-inflammatory activities of novel thalidomide analogs by exploring their effects on splenocytes proliferation and macrophage functions and their antioxidant activity. MTT assay was used to assess the cytotoxic effect of thalidomide analogs against splenocytes. Tumor necrosis factor (TNF-α) and nuclear factor kappa B (NF-κB-P65) were determined by enzyme-linked immunosorbent assay (ELISA). Nitric oxide (NO) was estimated by colorimetric assay. Antioxidant activity was examined by ORAC assay. Our results demonstrated that thalidomide dithioate analog 2 and thalidomide dithiocarbamate analog 4 produced a slight increase in splenocyte proliferation compared with thalidomide. Thalidomide dithiocarbamate analog 1 is a potent inhibitor of TNF-α production, whereas thalidomide dithiocarbamate analog 5 is a potent inhibitor of both TNF-α and NO. Analog 2 has a pronounced inhibitory effect on NF-κB-P65 production level. All thalidomide analogs showed prooxidant activity against hydroxyl (OH) radical. Analog 1 and thalidomide dithioate analog 3 have prooxidant activity against peroxyl (ROO) radical in relation to thalidomide. On the other hand, analog 4 has a potent scavenging capacity against peroxyl (ROO) radical compared with thalidomide. Taken together, the results of this study suggest that thalidomide analogs might have valuable anti-inflammatory activities with more pronounced effect than thalidomide itself. Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.

  16. Anti-Inflammatory Activity and Composition of Senecio salignus Kunth

    Science.gov (United States)

    Pérez González, Cuauhtemoc; Serrano Vega, Roberto; González-Chávez, Marco; Zavala Sánchez, Miguel Angel; Pérez Gutiérrez, Salud

    2013-01-01

    We investigated the anti-inflammatory activity of Senecio salignus. This medicinal plant is often used in Mexico for the treatment of fever and rheumatism. Chloroform and methanol extracts of the plant were tested on 12-O-tetradecanoylphorbol-13-acetate- (TPA-) induced edema in mice ears. The methanol extract of the plant inhibited edema by 36 ± 4.4% compared with the control, while the chloroform extract exhibited an even greater level of inhibition (64.1%). The chloroform extract was then fractionated, and the composition of the active fraction was determined by GC-MS. The anti-inflammatory activity of this fraction was then tested on TPA-induced ear edema in mice, and we found that the active fraction could inhibit edema by 46.9%. The anti-inflammatory effect of the fraction was also tested on carrageenan-induced paw edema in rats at doses of 100 mg/kg; a 58.9 ± 2.8% reduction of the edema was observed 4 h after administration of carrageenan, and the effect was maintained for 5 h. PMID:23691512

  17. Characterization of a novel non-steroidal glucocorticoid receptor antagonist

    Energy Technology Data Exchange (ETDEWEB)

    Li, Qun-Yi; Zhang, Meng [The National Center for Drug Screening, Shanghai (China); State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai (China); Hallis, Tina M.; DeRosier, Therese A. [Cell Systems Division, Invitrogen, Madison, WI (United States); Yue, Jian-Min; Ye, Yang [State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai (China); Mais, Dale E. [The National Center for Drug Screening, Shanghai (China); MPI Research, Mattawan, MI (United States); Wang, Ming-Wei, E-mail: wangmw@mail.shcnc.ac.cn [The National Center for Drug Screening, Shanghai (China); State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai (China)

    2010-01-15

    Selective antagonists of the glucocorticoid receptor (GR) are desirable for the treatment of hypercortisolemia associated with Cushing's syndrome, psychic depression, obesity, diabetes, neurodegenerative diseases, and glaucoma. NC3327, a non-steroidal small molecule with potent binding affinity to GR (K{sub i} = 13.2 nM), was identified in a high-throughput screening effort. As a full GR antagonist, NC3327 greatly inhibits the dexamethasone (Dex) induction of marker genes involved in hepatic gluconeogenesis, but has a minimal effect on matrix metalloproteinase 9 (MMP-9), a GR responsive pro-inflammatory gene. Interestingly, the compound recruits neither coactivators nor corepressors to the GR complex but competes with glucocorticoids for the interaction between GR and a coactivator peptide. Moreover, NC3327 does not trigger GR nuclear translocation, but significantly blocks Dex-induced GR transportation to the nucleus, and thus appears to be a 'competitive' GR antagonist. Therefore, the non-steroidal compound, NC3327, may represent a new class of GR antagonists as potential therapeutics for a variety of cortisol-related endocrine disorders.

  18. Amamentação e uso de antiinflamatórios não esteróides pela nutriz: informações científicas versus conteúdo em bulas de medicamentos comercializados no Brasil Breastfeeding and use of nonsteroidal anti-inflammatory drugs by lactating women: scientific information versus patient information leaflets in medication available in the Brazilian market

    Directory of Open Access Journals (Sweden)

    Roberto Gomes Chaves

    2006-09-01

    Full Text Available OBJETIVOS: confrontar as informações contidas nas bulas de medicamentos antiinflamatórios não esteróides com as evidências científicas do uso desses fármacos durante a amamentação. MÉTODOS: foi realizada revisão bibliográfica nas bases de dados LILACS e MEDLINE, utilizando os termos: "amamentação", "lactação", "drogas", "medicamentos", "antiinflamatórios não esteróides" e "bulas". As informações obtidas em artigos e livros foram confrontadas com o conteúdo das bulas sobre o uso dos AINEs durante a lactação. RESULTADOS: dentre os 27 antinflamatórios não esteróides comercializados no Brasil foram encontradas referências sobre segurança para uso durante a amamentação em apenas 14 (51,9%. Dos dez antinflamatórios não esteróides considerados como seguros para uso durante a lactação, nove (90% continham informação em bula para evitar uso nesse período ou suspender a amamentação. Na bula de 11 aos 13 (84,6% antinflamatórios não esteróides carentes de informações sobre uso pelas nutrizes foi sugerido evitar seu uso ou suspender a amamentação. CONCLUSÕES: as informações contidas nas bulas são discordantes das evidências científicas a respeito da compatibilidade dos antinflamatórios não esteróides com a amamentação. Há necessidade de maior conhecimento acerca da segurança desses medicamentos durante a amamentação.OBJECTIVES: confront information contained in non-steroidal anti-inflammatory drugs labels and information leaflets with the scientific data on their use during lactation. METHODS: a bibliographic review was performed using the terms: "breastfeeding", "lactating", "drugs", "medication", "non-steroidal anti-inflammatory drugs" and "information leaflets". The information obtained in articles and books were compared with the information in leaflets and labels on the use of non-steroidal anti-inflammatory drugs during the breastfeeding period. RESULTS: among the 27 non-steroidal anti-inflammatory

  19. Antinociceptive and anti-inflammatory potential of Rhododendron arboreum bark.

    Science.gov (United States)

    Nisar, Muhammad; Ali, Sajid; Muhammad, Naveed; Gillani, Syed N; Shah, Muhmmad R; Khan, Haroon; Maione, Francesco

    2016-07-01

    Rhododendron arboreum Smith. (Ericaceae), an evergreen small tree, is one of the 1000 species that belongs to genus Rhododendron distributed worldwide. In folk medicine, as various parts of this plant exhibit medicinal properties, it is used in the treatment of different ailments.The present study was designed to evaluate the potential anti-inflammatory and antinociceptive effects of methanolic extract of R. arboreum bark, followed by activity-guided fractionation of n-hexane, n-butanol, chloroform, ethyl acetate and aqueous fractions.The ethyl acetate fraction (200 mg/kg i.p.) showed the maximum analgesic effect (82%) in acetic acid-induced writhing, followed, to a less extent, by crude extract and chloroform fraction both at a dose of 200 mg/kg i.p. (65.09% and 67.89%, respectively). In carrageenan-induced mouse paw oedema, the crude extract and its related fractions displayed in a dose-dependent manner (50-200 mg/kg i.p.) an anti-inflammatory activity for all time-courses (1-5 hrs). For the active extract/fractions (200 mg/kg i.p.), the maximum effect was observed 5 h after carrageenan injection. These evidences were also supported by in vitro lipoxygenase inhibitory properties. In conclusion, R. arboreum crude methanolic extract and its fractions exhibited anti-inflammatory and antinociceptive effects. For these reasons, this plant could be a promising source of new compounds for the management of pain and inflammatory diseases. © The Author(s) 2014.

  20. Anti-inflammatory profile of paricalcitol in kidney transplant recipients.

    Science.gov (United States)

    Donate-Correa, Javier; Henríquez-Palop, Fernando; Martín-Núñez, Ernesto; Hernández-Carballo, Carolina; Ferri, Carla; Pérez-Delgado, Nayra; Muros-de-Fuentes, Mercedes; Mora-Fernández, Carmen; Navarro-González, Juan F

    Paricalcitol, a selective vitamin D receptor activator, is used to treat secondary hyperparathyroidism in kidney transplant patients. Experimental and clinical studies in non-transplant kidney disease patients have found this molecule to have anti-inflammatory properties. In this exploratory study, we evaluated the anti-inflammatory profile of paricalcitol in kidney-transplant recipients. Thirty one kidney transplant recipients with secondary hyperparathyroidism completed 3 months of treatment with oral paricalcitol (1μg/day). Serum concentrations and gene expression levels of inflammatory cytokines in peripheral blood mononuclear cells were analysed at the beginning and end of the study. Paricalcitol significantly decreased parathyroid hormone levels with no changes in calcium and phosphorous. It also reduced serum concentrations of interleukin (IL)-6 and tumour necrosis factor-alpha (TNF-α) by 29% (P<0.05) and 9.5% (P<0.05) compared to baseline, respectively. Furthermore, gene expression levels of IL-6 and TNF-α in peripheral blood mononuclear cells decreased by 14.1% (P<0.001) and 34.1% (P<0.001), respectively. The ratios between pro-inflammatory cytokines (TNF-α and IL-6) and anti-inflammatory cytokines (IL-10), both regarding serum concentrations and gene expression, also experienced a significant reduction. Paricalcitol administration to kidney transplant recipients has been found to have beneficial effects on inflammation, which may be associated with potential clinical benefits. Copyright © 2017 Sociedad Española de Nefrología. Published by Elsevier España, S.L.U. All rights reserved.

  1. Anti-inflammatory activity of Euphorbia aegyptiaca extract in rats

    Science.gov (United States)

    Abo-dola, Marium A.; Lutfi, Mohamed F.

    2016-01-01

    Background There were no studies on the anti-inflammatory activity of Euphorbia aegyptiaca, though it is commonly used by Sudanese herbalists in the treatment of rheumatoid arthritis. Objectives To determine phytochemical constituents of Euphorbia aegyptiaca To investigate the anti-inflammatory activity of Euphorbia aegyptiaca in rats. Methodology Plant material was extracted by ethanol and phytochemical screening was done according to standard methods. The thickness of Albino rats’ paws were measured before injection of 0.1 ml of 1% formalin in the sub planter region and then, 1, 2, 3, 4 and 24 hours after oral dose of ethanolic extract of Euphorbia aegyptiaca at a rate of 400mg/kg, 800mg/kg, indomethacin (5mg/kg) and normal saline (5ml/kg). Edema inhibition percentage (EI%) and mean paw thickness (MPT) were measured in the different groups and compared using appropriate statistical methods. Results The phytochemical screening revealed the presence of saponins, cumarins, flavonoids, tannins, sterols, triterpenes, and absence of alkaloids, anthraquinones glycosides and cyanogenic glycosides. The mean of EI% of rats treated with indomethacin at a dose of 5 mg/kg over different time intervals (64.0%) was significantly lower compared to those treated with Euphorbia aegyptiaca at a dose of 800 mg/kg (75.0%, P< 0.001), but higher compared to rats treated at higher dose of 400 mg/kg (57.4%, P< 0.001). In contrast, MPT of rats treated with indomethacin at a dose of 5 mg/kg (6.5±1.1 mm) was significantly higher compared to those treated with Euphorbia aegyptiaca at a dose of 800 mg/kg (6.1±.7 mm, P< 0.001) as well as 400 mg/kg (5.9±.5, P< 0.001). Conclusion Euphorbia aegyptiaca ethanolic extract has a sustained dose-dependent anti-inflammatory activity. PMID:27004059

  2. Hepatotoxicity of anti-inflammatory and analgesic drugs: ultrastructural aspects.

    Science.gov (United States)

    Manov, Irena; Motanis, Helen; Frumin, Idan; Iancu, Theodore C

    2006-03-01

    With the increasing incidence of drug-induced liver disease, attempts are being made to better understand the mechanisms behind these frequently life-endangering reactions. Analgesics and anti-inflammatory drugs are a major group exhibiting hepatotoxicity. We review research relating to these reactions, focusing on ultrastructural findings, which may contribute to the comprehension and possible avoidance of drug-induced liver disease. We also present some original observations on clinical material and cultured cells exposed to acetaminophen alone or in combination with the antioxidant N-acetylcysteine or the P-glycoprotein inhibitor verapamil.

  3. [Anti-inflammatory drugs and community-acquired pneumonia].

    Science.gov (United States)

    Dirou, S; Voiriot, G

    2015-10-01

    Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used in ambulatory medicine for their analgesic and antipyretic properties and are often used as self-medication. Their use in community-acquired pneumonia is associated with an increased risk of loco-regional complications, especially pleural empyema. Appropriate therapeutic care and hospital admissions are often delayed because of initial improvement of symptoms with NSAIDs. Despite worrying observational data, a causal link remains to be established. Currently, there is no recommendation cautioning against the use of NSAIDs in the management of community-acquired pneumonia. Copyright © 2015 SPLF. Published by Elsevier Masson SAS. All rights reserved.

  4. Topical Nonsteroidal Anti-Inflammatory Drugs for Macular Edema

    Directory of Open Access Journals (Sweden)

    Andrea Russo

    2013-01-01

    Full Text Available Nonsteroidal anti-inflammatory drugs (NSAIDs are nowadays widely used in ophthalmology to reduce eye inflammation, pain, and cystoid macular edema associated with cataract surgery. Recently, new topical NSAIDs have been approved for topical ophthalmic use, allowing for greater drug penetration into the vitreous. Hence, new therapeutic effects can be achieved, such as reduction of exudation secondary to age-related macular degeneration or diabetic maculopathy. We provide an updated review on the clinical use of NSAIDs for retinal diseases, with a focus on the potential future applications.

  5. Anti-inflammatory agents in the treatment of bipolar depression

    DEFF Research Database (Denmark)

    Rosenblat, Joshua D; Kakar, Ron; Berk, Michael

    2016-01-01

    OBJECTIVE: Inflammation has been implicated in the risk, pathophysiology, and progression of mood disorders and, as such, has become a target of interest in the treatment of bipolar disorder (BD). Therefore, the objective of the current qualitative and quantitative review was to determine...... of adjunctive anti-inflammatory agents on depressive symptoms was -0.40 (95% confidence interval -0.14 to -0.65, p = 0.002), indicative of a moderate and statistically significant antidepressant effect. The heterogeneity of the pooled sample was low (I² = 14%, p = 0.32). No manic/hypomanic induction...

  6. Terpenoids with anti-inflammatory activity from Abies chensiensis.

    Science.gov (United States)

    Zhao, Qian-Qian; Wang, Shu-Fang; Li, Ya; Song, Qiu-Yan; Gao, Kun

    2016-06-01

    The phytochemical investigation of Abies chensiensis led to the isolation and identification of nine new compounds including eight triterpenoids (1-8) and a new abietane-type diterpene (9), along with three known compounds (10-12). The absolute configuration of 9 was assigned by X-ray diffraction analysis. Compounds 1-11 were evaluated for the anti-inflammatory activity. Among the tested compounds, 1, 2, 5 and 6 exhibited potent inhibitory activity with IC50 values of 15.97, 18.73, 20.18 and 10.97μM, respectively. Copyright © 2016 Elsevier B.V. All rights reserved.

  7. Nonsteroidal Anti-Inflammatory Drugs for Retinal Disease

    Directory of Open Access Journals (Sweden)

    Scott D. Schoenberger

    2013-01-01

    Full Text Available Nonsteroidal anti-inflammatory drugs (NSAIDs are used extensively in ophthalmology for pain and photophobia after photorefractive surgery and to reduce miosis, inflammation, and cystoid macular edema following cataract surgery. In recent years, the US Food and Drug Administration has approved new topical NSAIDs and previously approved NSAIDs have been reformulated. These changes may allow for greater drug penetration into the retina and thereby offer additional therapeutic advantages. For example, therapeutic effects on diabetic retinopathy and age-related macular degeneration may now be achievable. We provide an updated review on the scientific rationale and clinical use of NSAIDs for retinal disease.

  8. Isolation, Characterization and Anti-Inflammatory Property of Thevetia Peruviana

    Directory of Open Access Journals (Sweden)

    R. Thilagavathi

    2010-01-01

    Full Text Available Thevetia peruviana seeds contain glucosides of neriifolin, acetylneriifolin and thevetin. Seed oil distillates of Thevetia peruviana have been found to contain anti-bacterial activity. In the persent work, the fresh flowers of Thevetia peruviana was subjected to phytochemical studies. The results of the study showed that the flowers contain quercetin, kaempferol and quercetin-7-o-galactoside. The structure of the isolated compound was characterized by UV, 1H NMR and 13C NMR spectra. The anti-inflammatory character of the isolated compound was tested by in vitro method and the results of the study revealed that the isolated compound showed a biphasic property.

  9. Use of low-dose aspirin and non-aspirin nonsteroidal anti-inflammatory drugs and risk of glioma

    DEFF Research Database (Denmark)

    Gaist, David; García-Rodríguez, L A; Sørensen, H T

    2013-01-01

    Background:Few studies have examined the association between use of aspirin or other non-steroidal anti-inflammatory drugs (NSAIDs) and risk of glioma and the results have been equivocal. We therefore investigated the influence of NSAID use on glioma risk in a nationwide setting.Methods:We used...... exposure to low-dose aspirin or non-aspirin (NA) NSAIDs into ever use or long-term use, defined as continuous use for 5 years. Conditional logistic regression was used to compute odds ratios (ORs), with 95% confidence intervals (CIs), for glioma associated with NSAID use, adjusted for potential...... confounders.Results:A total of 2688 glioma cases and 18 848 population controls were included in the study. Ever use of low-dose aspirin (OR=0.90; 95% CI: 0.77-1.04) or NA-NSAIDs (OR=1.05; 95% CI: 0.96-1.14) was not associated with glioma risk. Compared with never use, long-term use of low-dose aspirin...

  10. Skeletal muscle adaptation to immobilization and subsequent retraining in elderly men: No effect of anti-inflammatory medication.

    Science.gov (United States)

    Dideriksen, K; Boesen, A P; Kristiansen, J F; Magnusson, S P; Schjerling, P; Holm, L; Kjaer, M

    2016-09-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) may enhance resistance training induced gain in skeletal muscle mass and strength, but it is unknown if NSAIDs affects muscle loss during periods of inactivity in elderly individuals. Thus, we studied the influence of NSAID treatment on human skeletal muscle during immobilization and rehabilitation resistance training (retraining). 19 men (60-80yrs, range) were randomly assigned to ibuprofen (1200mg/d, Ibu) or placebo (Plc). One lower limb was immobilized in a cast for 2weeks and retrained for 6weeks. Moreover, whey protein isolate was ingested (2×20g/d) throughout the whole study period. Plasma inflammatory markers, quadriceps muscle mass and strength, and muscle gene expression were investigated. Muscle mass and strength decreased after 2weeks of immobilization (Pmuscle mass and strength reached beyond baseline levels after 6weeks of retraining (p0.05). No group-differences, but differences over time, were observed for muscle gene expression of proteolytic and anabolic factors. Plasma inflammatory markers were unaffected by the study intervention and NSAID treatment. Two weeks of lower limb immobilization lead to a reduction in muscle mass and strength, but these parameters were restored already after2 weeks of retraining and whey protein supplementation. After 6weeks of retraining and whey protein supplementation, muscle mass and strength increased beyond baseline levels, and NSAID treatment did not significantly influence this in elderly. Copyright © 2016 Elsevier Inc. All rights reserved.

  11. Anti-inflammatory activity of Seabuckthorn (Hippophae rhamnoides) leaves.

    Science.gov (United States)

    Ganju, Lilly; Padwad, Yogendra; Singh, Richa; Karan, Dev; Chanda, Sudipta; Chopra, Mohinder Kumar; Bhatnagar, Parul; Kashyap, Ravi; Sawhney, Ramesh Chandra

    2005-11-01

    Immunomodulatory activity of Seabuckthorn (SBT) leaf extract was evaluated in adjuvant induced arthritis (AIA) rat model. Inflammation was induced by injecting Complete Freund's Adjuvant (CFA) in the right hind paw of rats. SBT extract was administered intraperitoneally to treat the inflammation. The extent of inflammation and treatment response was evaluated by clinical analysis, scintigraphic visualization using technitium-99m-glutathione (Tc99m-GSH) and lymphocyte proliferation. Serial evaluation was carried out on days 1, 7, 14, 21 and 28 after creation of inflammation. The Tc99m-GSH uptake in the inflamed leg was compared with the normal contralateral leg of the same animal. The measurements were done by obtaining scintigraphic images using gamma camera and an online computer. Both qualitative and quantitative evaluation of radiotracer accumulation was considered to evaluate the anti-inflammatory response. The lymphocyte proliferation study revealed cellular immunosuppression during the early phase of the disease. Administration of SBT extract on the same day or 5 days prior to inflammatory insult into the joint, significantly reduced the inflammation as compared to the untreated animals in a dose dependent manner. These observations suggest that the SBT leaf extract has a significant anti-inflammatory activity and has the potential for the treatment of arthritis.

  12. Develop Anti-Inflammatory Nanotherapies to Treat Cardiovascular Disease

    Science.gov (United States)

    Tang, Jun

    Cardiovascular disease (CVD) is the leading cause of disease-related death in the world, accounting for 30 % global mortality. The majority of CVD is caused by atherosclerosis, a chronic inflammatory disease of major arteries featured by the deposition of lipids and cholesterol. Inflammation of atherosclerosis is mainly promoted by the pathological macrophages and monocytes, and modulating their functions has been proposed as a promising therapeutic target. This dissertation first presents the development of a novel simvastatin-loaded high-density lipoprotein (HDL) based nanoparticle ([S]-rHDL), which was able to deliver anti-inflammatory simvastatin preferentially to inflammatory monocytes in the blood and to macrophages in advanced atherosclerotic plaques, leading to the reduced inflammation in the tissue. Second, extensive in vivo characterization of [S]-rHDL in a mouse atherosclerosis model revealed that the anti-inflammatory capability of [S]-rHDL derived from its effects on blood monocytes, endothelial layer, monocyte recruitment, and plaque macrophage function. Third, a translational study that integrated the use of [S]-rHDL into oral statin treatment demonstrated a great potential for this nanomedicine as an attractive addition to the current high-dose oral statin standard-of-care for acute coronary syndrome. Finally, preliminary results suggested potential applications of the rHDL platform to other macrophage-implicated diseases.

  13. Anti-inflammatory and analgesic potential of Caesalpinia ferrea

    Directory of Open Access Journals (Sweden)

    Sandrine Maria A. Lima

    2012-02-01

    Full Text Available Caesalpinia ferrea Mart. belongs to the family Fabaceae. Known as pau-ferro and jucá, it is used in folk medicine to treat diabetes, as antipyretic and antirheumatic. This study aimed to evaluate the anti-inflammatory and antinociceptive activities of the ethanol extract of the fruits of C. ferrea (EECf. In the evaluation of anti-inflammatory activity, EECf (50 mg/kg produced significantly inhibition of ear edema by 66.6% compared to control. Indomethacin (10 mg/kg showed inhibition of 83.9% compared to control. EECf (50 mg/kg inhibited of vascular permeability induced by acetic acid and was also able to reduce of cell migration to the peritoneal cavity induced by thioglycolate. In the writhing test induced by acid acetic, EECf (12.5, 25 and 50 mg/kg significantly reduced the number of contortions by 24.9, 46.9 and 74.2%, respectively. In the formalin test, EECf presented effects only in the second phase. The results provided experimental evidence for the effectiveness of the traditional use of C. ferrea in treating various diseases associated with inflammation and pain.

  14. A Novel Anti-Inflammatory Effect for High Density Lipoprotein.

    Directory of Open Access Journals (Sweden)

    Scott J Cameron

    Full Text Available High density lipoprotein has anti-inflammatory effects in addition to mediating reverse cholesterol transport. While many of the chronic anti-inflammatory effects of high density lipoprotein (HDL are attributed to changes in cell adhesion molecules, little is known about acute signal transduction events elicited by HDL in endothelial cells. We now show that high density lipoprotein decreases endothelial cell exocytosis, the first step in leukocyte trafficking. ApoA-I, a major apolipoprotein of HDL, mediates inhibition of endothelial cell exocytosis by interacting with endothelial scavenger receptor-BI which triggers an intracellular protective signaling cascade involving protein kinase C (PKC. Other apolipoproteins within the HDL particle have only modest effects upon endothelial exocytosis. Using a human primary culture of endothelial cells and murine apo-AI knockout mice, we show that apo-AI prevents endothelial cell exocytosis which limits leukocyte recruitment. These data suggest that high density lipoprotein may inhibit diseases associated with vascular inflammation in part by blocking endothelial exocytosis.

  15. Melatonin as an Anti-Inflammatory Agent Modulating Inflammasome Activation

    Directory of Open Access Journals (Sweden)

    Gaia Favero

    2017-01-01

    Full Text Available Inflammation may be defined as the innate response to harmful stimuli such as pathogens, injury, and metabolic stress; its ultimate function is to restore the physiological homeostatic state. The exact aetiology leading to the development of inflammation is not known, but a combination of genetic, epigenetic, and environmental factors seems to play an important role in the pathogenesis of many inflammation-related clinical conditions. Recent studies suggest that the pathogenesis of different inflammatory diseases also involves the inflammasomes, intracellular multiprotein complexes that mediate activation of inflammatory caspases thereby inducing the secretion of proinflammatory cytokines. Melatonin, an endogenous indoleamine, is considered an important multitasking molecule with fundamental clinical applications. It is involved in mood modulation, sexual behavior, vasomotor control, and immunomodulation and influences energy metabolism; moreover, it acts as an oncostatic and antiaging molecule. Melatonin is an important antioxidant and also a widespread anti-inflammatory molecule, modulating both pro- and anti-inflammatory cytokines in different pathophysiological conditions. This review, first, gives an overview concerning the growing importance of melatonin in the inflammatory-mediated pathological conditions and, then, focuses on its roles and its protective effects against the activation of the inflammasomes and, in particular, of the NLRP3 inflammasome.

  16. Novel anti-inflammatory therapies for the treatment of atherosclerosis.

    Science.gov (United States)

    Khan, Razi; Spagnoli, Vincent; Tardif, Jean-Claude; L'Allier, Philippe L

    2015-06-01

    The underlying role of inflammation in atherosclerosis has been characterized. However, current treatment of coronary artery disease (CAD) predominantly consists of targeted reductions in serum lipoprotein levels rather than combating the deleterious effects of acute and chronic inflammation. Vascular inflammation acts by a number of different molecular and cellular pathways to contribute to atherogenesis. Over the last decades, both basic studies and clinical trials have provided evidence for the potential benefits of treatment of inflammation in CAD. During this period, development of pharmacotherapies directed towards inflammation in atherosclerosis has accelerated quickly. This review will highlight specific therapies targeting interleukin-1β (IL-1β), P-selectin and 5-lipoxygenase (5-LO). It will also aim to examine the anti-inflammatory effects of serpin administration, colchicine and intravenous HDL-directed treatment of CAD. We summarize the mechanistic rationale and evidence for these novel anti-inflammatory treatments at both the experimental and clinical levels. Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.

  17. Melatonin as an Anti-Inflammatory Agent Modulating Inflammasome Activation.

    Science.gov (United States)

    Favero, Gaia; Franceschetti, Lorenzo; Bonomini, Francesca; Rodella, Luigi Fabrizio; Rezzani, Rita

    2017-01-01

    Inflammation may be defined as the innate response to harmful stimuli such as pathogens, injury, and metabolic stress; its ultimate function is to restore the physiological homeostatic state. The exact aetiology leading to the development of inflammation is not known, but a combination of genetic, epigenetic, and environmental factors seems to play an important role in the pathogenesis of many inflammation-related clinical conditions. Recent studies suggest that the pathogenesis of different inflammatory diseases also involves the inflammasomes, intracellular multiprotein complexes that mediate activation of inflammatory caspases thereby inducing the secretion of proinflammatory cytokines. Melatonin, an endogenous indoleamine, is considered an important multitasking molecule with fundamental clinical applications. It is involved in mood modulation, sexual behavior, vasomotor control, and immunomodulation and influences energy metabolism; moreover, it acts as an oncostatic and antiaging molecule. Melatonin is an important antioxidant and also a widespread anti-inflammatory molecule, modulating both pro- and anti-inflammatory cytokines in different pathophysiological conditions. This review, first, gives an overview concerning the growing importance of melatonin in the inflammatory-mediated pathological conditions and, then, focuses on its roles and its protective effects against the activation of the inflammasomes and, in particular, of the NLRP3 inflammasome.

  18. Synergistic analgesic, anti-pyretic and anti-inflammatory effects of extra virgin olive oil and ibuprofen in different experimental models of albino mice.

    Science.gov (United States)

    Osman, Walla'a A; Labib, Dina A; Abdelhalim, Mona O; Elrokh, Elsayed M

    2017-10-01

    Olive oil was used in the past as a remedy for many diseases due to its unlimited benefits in health. This study was carried out to assess the analgesic, anti-pyretic and anti-inflammatory activities of extra virgin olive oil (EVOO) at a dose of 8 mL/kg body weight and to compare it with ibuprofen (IBU) as an individual drug therapy and in combination with two different doses of IBU (therapeutic dose 100 mg/kg and low dose 40 mg/kg), on different animal models in albino mice. A total of 132 adult healthy male Swiss albino mice were used in this study. The analgesic effect was assessed using acetic acid-induced writhing test. The antipyretic effect was evaluated by brewer's yeast-induced pyrexia, while the anti-inflammatory activity was assessed by two different models; the carrageenan-induced paw edema and the carrageenan-induced peritonitis in which the levels of total leukocyte count (TLC), neutrophil count, prostaglandin E2 (PGE2) and interferon gamma (INF-γ) were measured in the peritoneal exudates. The results revealed significant protection in all the treated groups; however, the combination of EVOO with IBU at its therapeutic dose showed superiority over the two compounds when used separately. Using EVOO with the therapeutic dose of IBU showed synergistic effect in controlling the cardinal signs of acute inflammation rather than using non-steroidal anti-inflammatory drugs alone. © 2017 Asia Pacific League of Associations for Rheumatology and John Wiley & Sons Australia, Ltd.

  19. Anti-Inflammatory Effects of Metformin Irrespective of Diabetes Status

    Science.gov (United States)

    Cameron, Amy R.; Morrison, Vicky L.; Levin, Daniel; Mohan, Mohapradeep; Forteath, Calum; Beall, Craig; McNeilly, Alison D.; Balfour, David J.K.; Savinko, Terhi; Wong, Aaron K.F.; Viollet, Benoit; Sakamoto, Kei; Fagerholm, Susanna C.; Foretz, Marc

    2016-01-01

    Rationale: The diabetes mellitus drug metformin is under investigation in cardiovascular disease, but the molecular mechanisms underlying possible benefits are poorly understood. Objective: Here, we have studied anti-inflammatory effects of the drug and their relationship to antihyperglycemic properties. Methods and Results: In primary hepatocytes from healthy animals, metformin and the IKKβ (inhibitor of kappa B kinase) inhibitor BI605906 both inhibited tumor necrosis factor-α–dependent IκB degradation and expression of proinflammatory mediators interleukin-6, interleukin-1β, and CXCL1/2 (C-X-C motif ligand 1/2). Metformin suppressed IKKα/β activation, an effect that could be separated from some metabolic actions, in that BI605906 did not mimic effects of metformin on lipogenic gene expression, glucose production, and AMP-activated protein kinase activation. Equally AMP-activated protein kinase was not required either for mitochondrial suppression of IκB degradation. Consistent with discrete anti-inflammatory actions, in macrophages, metformin specifically blunted secretion of proinflammatory cytokines, without inhibiting M1/M2 differentiation or activation. In a large treatment naive diabetes mellitus population cohort, we observed differences in the systemic inflammation marker, neutrophil to lymphocyte ratio, after incident treatment with either metformin or sulfonylurea monotherapy. Compared with sulfonylurea exposure, metformin reduced the mean log-transformed neutrophil to lymphocyte ratio after 8 to 16 months by 0.09 U (95% confidence interval, 0.02–0.17; P=0.013) and increased the likelihood that neutrophil to lymphocyte ratio would be lower than baseline after 8 to 16 months (odds ratio, 1.83; 95% confidence interval, 1.22–2.75; P=0.00364). Following up these findings in a double-blind placebo controlled trial in nondiabetic heart failure (trial registration: NCT00473876), metformin suppressed plasma cytokines including the aging

  20. Molecular mechanism of protopanaxadiol saponin fraction-mediated anti-inflammatory actions

    National Research Council Canada - National Science Library

    Yang, Yanyan; Lee, Jongsung; Rhee, Man Hee; Yu, Tao; Baek, Kwang-Soo; Sung, Nak Yoon; Kim, Yong; Yoon, Keejung; Kim, Ji Hye; Kwak, Yi-Seong; Hong, Sungyoul; Kim, Jong-Hoon; Cho, Jae Youl

    Korean Red Ginseng (KRG) is a representative traditional herbal medicine with many different pharmacological properties including anticancer, anti-atherosclerosis, anti-diabetes, and anti-inflammatory activities...