• Title/Summary/Keyword: Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

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Nonsteroidal Anti-inflammatory Drugs (비스테로이드 항염제)

  • Lee, Choong-Ki
    • Journal of Yeungnam Medical Science
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    • v.17 no.1
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    • pp.1-11
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    • 2000
  • Inhibition of cyclooxygenase(COX), and thus prevention of the formation of prostaglandins, provided a unifying explanation of the therapeutic and toxic actions of nonsteroidal anti-inflammatory drugs (NSAIDs). Recently, the discovery of the two isoforms of COX was made by molecular biologists studying neoplastic transformation in chick embryo cells. The constitutive enzyme, COX-1, is obviously responsible for the production of prostaglandins involved in housekeeping functions such as maintenance of integrity of the gastric mucosa, renal blood flow and platelet aggregation. The inducible form of COX (COX-2) is responsible for the formation of prostaglandins that pathologically affects inflammation, pain and fever. Clearly, all the experimental and clinical data support the hypothesis that the beneficial effects of NSAIDs are due to inhibition of the COX-2 enzyme, whereas the gastrotoxicity is due to inhibition of COX-1. The cox-2/COX-1 ratios of the NSAIDs in common use have been measured and compared with epidemiological data on their side effects. There is little evidence to suggest that one NSAID is clearly more effective than another, But substantial individual variability is present with respect to the pharmacology and pharmacokinetics of these drugs: therefore it is essential to adjust the dosage and choose specific drug to the patient's response.

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Nanodiamonds Conjugated with Nonsteroidal Anti-inflammatory Drugs for Transdermal Delivery

  • Rhee, Changkyu;Puzyr, Alexey P.;Burov, Andrey E.;Burova, Olga G.;Kim, Whungwhoe;Bondar, Vladimir S.
    • Journal of Powder Materials
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    • v.25 no.6
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    • pp.459-465
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    • 2018
  • Most commercially available detonation nanodiamonds (DNDs) require further processing to qualify for use in biomedical applications, as they often contain many impurities and exhibit poor dispersibility in aqueous media. In this work, DNDs are modified to improve purity and impart a high colloidal stability to the particles. The dispersive and adsorption properties of modified DNDs are evaluated in terms of the suitability of DNDs as carriers for non-steroidal anti-inflammatory drugs (NSAIDs) in transdermal delivery. The study of adsorption on strongly positively and strongly negatively charged DNDs showed their high loading capacity for NSAIDs, and a pronounced relationship between the drugs and the particles' charges. Experiments on long-term desorption carried out with DND/NSAID complexes indicate that the nanoparticles exert a sustained effect on the drug release process.

Potentiation of the Cytotoxic Effects of Imatinib and TRAIL by Nonsteroidal Anti-inflammatory Drugs on Human Cancer Cells (비스테로이드소염제(Nonsteroidal Anti-inflammatory Drug, NSAID)에 의한 인간 암세포의 imatinib 및 TRAIL의 세포 독성 증강 기전 연구)

  • Moon, Hyun-Jung;Kang, Chi-Dug;Kim, Sun-Hee
    • Journal of Life Science
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    • v.30 no.8
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    • pp.661-671
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    • 2020
  • The resistance of cancer cells to anti-cancer drugs is the leading cause of chemotherapy failure. The clinical use of nonsteroidal anti-inflammatory drugs (NSAIDs) has been gradually extended to cancer treatment through combination with anti-cancer drugs. In the current study, we investigated whether NSAIDs including celecoxib (CCB), 2,5-dimethyl celecoxib (DMC), and ibuprofen (IBU) could enhance the cytotoxic effects of imatinib and TNF-related apoptosis inducing ligand (TRAIL) on human cancer cells. We found that the NSAIDs potentiated TRAIL and imatinib cytotoxicity against human hepatocellular carcinoma (HCC) cell lines SNU-354, SNU-423, SNU-449, and SNU-475/TR and against leukemic K562 cells with high level of CD44 (CD44highK562), respectively. More specifically, CCB induced endoplasmic reticulum stress via up-regulation of ATF4/CHOP which is associated with the induction of autophagy against HCC and CD44high K562 cells. NSAID-induced autophagic activity accelerated TRAIL cytotoxicity of HCC cells through up- and down-regulation of DR5 and c-FLIP, respectively. The NSAIDs also potentiated imatinib-induced cytotoxicity and apoptosis through down-regulation of markers in CD44highK562 cells that express a stemness phenotype. Our results suggest that the ability of NSAIDs to induce autophagy could enhance the cytotoxicity of TRAIL and imatinib, leading to a reverse resistance to these drugs in the cancer cells. In conclusion, NSAIDs in combination with low-dose TRAIL or imatinib may constitute a novel clinical strategy that maximizes therapeutic efficacy of each drug and effectively reduces the toxic side effects.

Analysis of Drug Utilization for Patients with Ankylosing Spondylitis (강직성 척추염 환자에 대한 약물사용 현황 분석)

  • Kang, Han-Bin;Je, Nam Kyung
    • Korean Journal of Clinical Pharmacy
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    • v.25 no.4
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    • pp.246-253
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    • 2015
  • Background & Object: Ankylosing spondylitis (AS) is a chronic inflammatory disease that causes ankylosis and deformation of axial joints. Since current medicine cannot cure the disease yet, alleviating pain and preventing deformation with medications are the main therapy for patients with AS. The key medications for these purposes include nonsteroidal anti-inflammatory drugs (NSAIDs), and tumor necrosis $factor-{\alpha}$ ($TNF-{\alpha}$) inhibitors. This study aims to analyze prescribing patterns of AS patients in South Korea. Method: National Patients Sample data compiled by the Health Insurance Review and Assessment Service from 2013 was analyzed. Patients with AS were identified with Korean Standard Classification of Diseases code-6, which was M45. The rates of prescription, discontinuation, and switching ingredients were calculated for each medication during 2013. Results: Total number of patients was 655, and most of them were male (n = 514, 78.5%). Of all age groups, the proportion of 30-40 year old patients was the greatest (35.1%). The most utilized drug class was NSAIDs (82.4%). Less than half of patients were prescribed $TNF-{\alpha}$ inhibitors (n = 212, 32.4%). Meloxicam, aceclofenac, and celecoxib were the most frequently prescribed NSAIDs. In case of $TNF-{\alpha}$ inhibitors, adalimumab, etanercept and infliximab were the top three most prescribed drugs. Although not recommended by the current practice guideline, significant proportions of patients were identified using disease modifying anti-rheumatic drugs (DMARDs). Conclusion: Considering the current practice guideline and previous studies about the efficacy, the use of DMARDs should be reduced and medical insurance term in South Korea should be re-examined.

Nonsteroidal Anti-inflammatory Drugs Utilization Patterns among the Elderly with Osteoarthritis at Primary Ambulatory Care Units in Busan Metropolitan City, Korea (부산지역 의원급 외래 노인 골관절염환자의 비스테로이드소염제 사용양상평가)

  • Choi, Nam-Kyong;Kim, Yoon-I;Lee, Seung-Mi;Park, Byung-Joo
    • Journal of Preventive Medicine and Public Health
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    • v.37 no.2
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    • pp.150-156
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    • 2004
  • Objectives : To investigate the utilization patterns of non-steroidal anti-inflammatory drugs (NSAIDs) among the elderly with osteoarthritis (OA) undergoing primary ambulatory care in Busan metropolitan city, Korea. Methods : OA patients, aged 65 years and over, were identified from the Korean National Health Insurance Review Agency drug prescription database. The subjects had at least one episode of claim for OA (ICD-10-CM: M15-M19) between August 1, 2000 and February 28, 2002. Trends in the determinations of NSAIDs utilization were identified using chi-squared tests for trend. Results : There were 47,711 osteoarthritic patients. The total number of visits by these patients was 177,443, with a total frequency for NSAID prescriptions of 214,952. Seventy-nine percent of the OA patients were female. NSAIDs were prescribed on 133,284 visits (75.1%) and the proportion of prescriptions was significantly increased with age. Only the proportion of visit when NSAIDs were prescribed decreased, from 65.1 to 43.5%, during the study period (p<0.001). However, the proportion of combined treatments with anti-ulcer drugs was increased. The use of NSAIDs injections was decreased. Of the individual NSAIDs, diclofenac (28.7% of total frequency of NSAID prescriptions), piroxicam (15.0%) and talniflumate (8.7%), were the most frequently prescribed. Among the NSAIDs prescribed OA visits, 45.7% used two or more NSAIDs. Conclusion : The total proportion of NSAIDs prescribed to the osteoarthritic patients was higher than in other studies. The decline in the use of NSAIDs during the study period, and the frequent selection of safer medications, such as combination therapy with anti-ulcer drug, may reflect the risk awareness of the use of NSAIDs.

Effect of Lower Abdomen Warmer on Primary Dysmenorrhea Patients Taking Nonsteroidal Anti-Inflammatory Drugs (비스테로이드성 소염진통제를 복용하는 원발성 월경곤란증 환자에 대한 하복부 온열찜질기의 효과)

  • Kim, Hyeong-Jun;Lee, Dong-Nyung;Ahn, Ha-Young
    • The Journal of Korean Obstetrics and Gynecology
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    • v.32 no.3
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    • pp.128-141
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    • 2019
  • Objectives: This study was performed to investigate the pain relief effect of lower abdomen warmer on primary dysmenorrhea patients taking nonsteroidal anti-inflammatory drugs and whether the using of warmer can supplement or replace the drugs. Methods: 30 women with primary dysmenorrhea were assigned to treatment group (n=15) and control group (n=15). At 1st visit, the treatment group was provided with a wirless multiuse warmer and trained to use at least three times per menstrual cycle. The control group was not provided with the warmer, and both groups were provided with a menstrual diary and instructed to record their pain intensity and dose of analgesic every menstrual period. Visual Analogue Scale (VAS) were used to assess the intensity of overall pain and the most severe pain during the menstrual period. And the total number of analgesic taken during menstruation and the average number of analgesic taken during a single dose were measured. Results: There was significant pain relief in the treatment group compared to before baseline, and there was a significant difference from the control group. In addition, there was no significant difference in the frequency of taking analgesic during the menstrual period between the treatment group and the control group, but the dose of analgesic was significantly lower in the treatment group than in the control group. Conclusions: This clinical trial showed that lower abdomen warmer would helpful in relieving primary dysmenorrhea and could help reduce the use of nonsteroidal anti-inflammatory drugs.

Changes in Toxicological Characteristics after Sales of Nonprescription Drugs in Convenience Stores (안전상비의약품 판매 이후 중독환자 특성 변화)

  • Kim, Chang Yeong;Lee, Eui Jung;Lee, Sung Woo;Kim, Su Jin;Han, Kap Su
    • Journal of The Korean Society of Clinical Toxicology
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    • v.16 no.1
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    • pp.42-48
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    • 2018
  • Purpose: On November 15, 2012, sales of OTC (Over-The-Counter) drugs began at convenience stores, which changed the accessibility of some drugs. As a result, the exposure and access patterns of these drugs could have changed. In this study, we reviewed the changes in the characteristics of drug poisoning patients because of the reposition of nonprescription drugs according to the revised Pharmaceutical Affairs Act. Methods: A retrospective study was conducted to evaluate changes in characteristics of drug poisoning patients between 2008 and 2016. A registry was developed by an emergency medical center in a local tertiary teaching hospital, and patients who visited the center were enrolled in this registry. We compared two periods, from 2008 to 2012 (Pre OTC) and from 2013 to 2016 (Post OTC), for type of intoxicant, time from poisoning to visiting the emergency center, intention, psychiatric history, previous suicidal attempt, alcohol status, and emergency room outcomes. The primary outcome was the number of patients who took acetaminophen and NSAIDs (nonsteroidal anti-inflammatory drugs). Secondary outcomes were ICU admission rate, mortality rate, and number of patients who visited the ER when the pharmacy was closed after taking acetaminophen and NSAIDs (nonsteroidal anti-inflammatory drugs). Results: Among 1,564 patients, 945 and 619 patients visited the emergency room during pre and post OTC periods. The number of patients with acetaminophen and NSAIDs poisoning decreased from 9.2% to 6.1% (p=0.016). The ICU admission rate and mortality rate in the emergency room did not show significant results in the relevant patient groups, and so was the number of patients visiting ER when the pharmacy was closed taking acetaminophen and NSAIDs. Conclusion: Despite the sales of nonprescription drugs at convenience stores, the number of acetaminophen and NSAIDs poisoning patients decreased.

Treatment of juvenile rheumatoid arthritis

  • Kim, Kwang-Nam
    • Clinical and Experimental Pediatrics
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    • v.53 no.11
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    • pp.936-941
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    • 2010
  • The systematic approach to pharmacologic treatment is typically to begin with the safest, simplest, and most conservative measures. It has been realized that the more rapidly inflammation is under control, the less likely it is that there will be permanent sequelae. Nonsteroidal anti-inflammatory drugs (NSAIDs) are the mainstay of initial treatment for inflammation. In addition, the slow-acting antirheumatic drugs (SAARDs) and disease-modifying antirheumatic drugs (DMARDs) have efficacy of anti-inflammatory action in children with chronic arthritis. New therapeutic modalities for inflammation, such as etanercept and infliximab, promise even further improvements in the risk/benefit ratio of treatment. It is not typically possible at the onset of the disease to predict which children will recover and which will go on to have unremitting disease with lingering disability or enter adulthood with serious functional impairment. Therefore, the initial therapeutic approach must be vigorous in all children.

Effect of Auricular Acupuncture on Nonsteroidal Antiinflammatory Drug Dose in Primary Dysmenorrhea : A Randomized Controlled Trials (비스테로이드성 소염진통제를 복용하는 원발성 월경곤란증 환자에 대한 이침치료의 무작위대조군임상시험)

  • Hur, Da-Hee;Kang, So-Hyeon;Kwon, Han-Seul;Ahn, Ha-Young;Baek, Hyung-Chan;Kim, Hyeong-Jun
    • The Journal of Korean Obstetrics and Gynecology
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    • v.35 no.4
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    • pp.161-173
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    • 2022
  • Objectives: This study was conducted to evaluate the effectiveness of acupuncture in patients with primary menstrual difficulties taking NSAIDs. Methods: 30 women with primary menstrual difficulties with NSAIDs were assigned to treatment groups (n=15) and control groups (n=15). On their first visit, both groups were provided with a menstrual diary and were required to record the intensity of pain and the dosage of painkillers during each menstrual cycle. The treatment group received two acupuncture treatments per cycle during two cycles, and the control group did not receive acupuncture. Pain strength during menstruation was evaluated using Visual Analogue Scale (VAS), and the total number of painkillers taken during menstruation and the average number of painkillers taken during a single dose was measured. Results: The treatment group had significant pain relief compared to the pre-test group and significant differences from the control group. In addition, there was a significant difference between the treatment group and the control group in the frequency of taking painkillers during the menstrual period and the dose in the test group was significantly lower than before treatment. Conclusions: This clinical trial showed that this acupuncture can help alleviate primary menstruation and reduce the use of nonsteroidal anti-inflammatory drugs.

Inhibition of Heat-induced Denaturation of Albumin by Nonsteroidal Antiinflammatory Drugs (NSAIDs): Pharmacological Implications

  • Luciano-Saso;Giovanni-Valentini;Casini, Maria-Luisa;Eleonora-Grippa;Gatto, Maria-Teresa;Leone, Maria-Grazia;Bruno-Silvestrini
    • Archives of Pharmacal Research
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    • v.24 no.2
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    • pp.150-158
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    • 2001
  • The activity of nonsteroidal antiinflammatory drugs (NSAIDs) in rheumatoid arthritis is not only due to the inhibition of the production of prostaglandins, which can even have beneficial immunosuppressive effects in chronic inflammatory processes. Since we speculated that these drugs could also act by protecting endogenous proteins against denaturation, we evaluated their effect on heat-induced denaturation human serum albumin (HSA) in comparison with several fatty acids which are known to be potent stabilizers of this protein. By the Mizushimas assay and a recently developed HPLC assays we observed that NSAIDs were slightly less active [$EC_{50}~10^{-5}-10^{-4}$ M] than FA and that the HPLC method was less sensitive but more selective than the turbidimetric assay, i.e. it was capable of distinguishing true antiaggregant agents like FA and NSAIDs from substances capable of inhibiting the precipitation of denatured protein aggregates. In conclusion, this survey could be useful for the development of more effective agents in protein condensation diseases like rheumatic disorders, cataract and Alzheimers disease.

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