• Title/Summary/Keyword: NSAIDS

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Discovery of Epinastine-NSAID Hybrids as Potential Anti-inflammatory Agents: Synthesis and In Vitro Nitric Oxide Production Inhibitory Activity Study

  • Woo, Hyeong Ryeol;Damodar, Kongara;Lee, Yeontaek;Lim, Soon-sung;Jeon, Sung Ho;Lee, Jeong Tae
    • Journal of the Korean Chemical Society
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    • v.64 no.2
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    • pp.79-83
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    • 2020
  • A novel pharmacophore with epinastine (1) and NSAID moieties (2-5) was designed by molecular hybridization approach. The hybrid compounds 6-9 were synthesized by EDCI/HOBt or HATU-mediated coupling of 1 with salicylic acid (2), mefenamic acid (3), indomethacin (4) and naproxen (5), respectively, and were assessed for their inhibitory effect against NO production in LPS-induced RAW-264.7 macrophages in vitro. The Hybrids were found to exhibit significant NO production inhibitory effects with half-maximal inhibitory concentration (IC50) values ranging in between 15.96 ± 1.32 and 36.68 ± 2.53 μM and were non-cytotoxic to macrophages. Comparing the inhibition concentration (IC50), cytotoxicity concentration (CC50) and in vitro efficacy index (iEI), 6 (IC50 = 17.97 ± 1.92 μM; iEI = 11.13) and 9 (IC50 = 15.96 ± 1.32 μM; iEI = 12.53) were better suited than other hybrids as well as their parent compound. Our findings signify that hybrids 6 and 9 may serve as platforms for continued investigations for the development of more efficient anti-inflammatory agents.

Development of Contents for KFDA Drug Safety Information Website (식품의약품안전청의 의약품안전사용정보방 웹사이트 구축을 위한 컨텐츠 개발)

  • Ji, Eun-Hee;Park, Hyo-Yung;Noh, Hye-Jin;Lee, Dong-Eun;Han, Na-Young;Jeong, So-Hyun;Kim, In-Wha;Shin, Wan-Gyoon;Oh, Jung-Mi
    • YAKHAK HOEJI
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    • v.56 no.3
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    • pp.204-209
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    • 2012
  • The purpose of this study was to construct database for a drug safety information website to serve as an access point of up-to-date resources for a wide variety of drug-safety information helping patients and healthcare professionals make well-informed decisions about medication use. All the contents developed were confirmed by the council of advisors who were the experts in drug safety. The detailed contents of database on frequently prescribed drug including 9 NSAIDs, 19 antibiotics, 24 cardiovascular, 21 metabolic, 14 respiratory, 20 digestive, 22 hormonal, 10 genitourinary, 10 anti-allergic, 27 antifungal/antiviral, and 71 neuropsychiatric agents were developed based on the approved drug labeling of the Korean FDA. A separately searchable database of drug-specific safety information for patients and health professionals was constructed for users in need of different depth of knowledge on using medications safely. The safety information on highly prevalent chronic diseases and drug classes was also developed. Finally the most recent global drug safety news was provided. The consumer directed information was developed in layman's terms as means of proving user-friendly information. The creation of this type of website is part of the Korean FDA's ongoing initiative to address and promote the safe use of medications for the public.

The Effect of Cryotherapy on Release of Inflamation in Patient with Rheumatoid Arthritis (한랭치료가 급성 류마티스 관절염 환자의 염증완화에 미치는 효과)

  • Kim, Dong-Hwan;Park, Rae-Joon;Jun, Kyoung-Hee
    • The Journal of Korean Physical Therapy
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    • v.13 no.1
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    • pp.175-188
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    • 2001
  • The purpose of this study was to investigate the effect of the cold air application for release of inflamation and pain in patient with acute rheumatoid arthritis who had taken medication(NSAIDs, DMARDs, corticosteroids). The participants had knee joint pain and ESR score over the 30. They were randomly assigned to three groups with each 15. Control group(group I ) were applied cold air and medication, experimental group II were applied hot pack and medication. and experimental group III were applied only medication. They were evaluated from April 1, 2000 to september 1,2000 ,and it was examined by ESR and VAS(visual analoge scale) in Lee Bang Hoon rehabilitation medicine clinic in Jeju Korea. The result of this study were as follow: 1. It was found that group 1, group II and group III had the statistically significant reduction of the ESR score according to treatment time(p<.05). 2. There were not statistically significant differences in ESR change pattern of each group according to treatment time(p>.05). 3. There were not statistically significant differences in the change of ESR according to treatment time between group I and group II , group I and group III , and group II and group III (p<.05). 4. It was found that group I . group II and group III had the statistically significant reduction of the VAS(Visual Analoge Scale) score according to treatment time(p<.05). 5. There were statistically significant differences in VAS score according to treatment time between control group(group I ) and experimental groups(group II and group III)(p<.05), but there were not stsiistically significant differences between experimental groups(p>.05).

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Clinical Diagnosis and Its Medical Managements from Patients with Gastrointestinal Diseases (위장관 질환자의 임상진단과 치료방법)

  • 김재웅
    • The Korean Journal of Food And Nutrition
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    • v.10 no.2
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    • pp.186-192
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    • 1997
  • Endoscopic diagnosis and medical management from K43 and C45 patients, whose sex, occupation, character and life patterns are quite different each other, were discussed. The K43 was patient with erosive gastritis, which may caused by maldietary habits and life stresses. Although the effective drugs such as H2-receptor antagonists with atacids, H+/K+-pump inhibitors, prokinetics, colloidal bismuth, and sucralfates, were administrated for long time, symptomatic relief of abdominal pain was not improved. The tests of clinical phathology and abdominal sonogram were normal, visceral hypersensitivity was appeared from barostat test of stomach. However C45 had taken headache during every day life, and endoscopically confirmed as a gastric·duodenal ulcer patiant, which may caused by chronic use of NSAIDs. The her ulceric symptoms were suppressed from active stage to healing stage by using combination therapy for H. pylori with traditional antipeptic ulcer drugs, where as amitriptyline was administrated to the K43 but not effective. Nonulcer dyspepsia and irritable bowel syndrome is pooly defined, and affect about 15% of the population annually in U. S. A. but don't seek medical care. Author would like to point out that statistics for visceral pains are absent in Korea.

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A case of Bilateral Near Blindness Secondary to Isolated Sphenoid Sinus Aspergillosis with Headache (양측성 실명을 동반한 접형동 아스페르길루스증 1 예)

  • Yoon, Jun-Pil;Lee, Se-Jin;Lee, Jun;Kim, Ju-Hyun;Noh, Hyun-Doo
    • Journal of Yeungnam Medical Science
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    • v.24 no.1
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    • pp.79-84
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    • 2007
  • Sphenoid sinus aspergillosis is notorious for its serious complications, such as permanent cranial nerve deficits and possible death. The most common associated symptoms are headache, followed by visual changes, and cranial nerve palsies. Because of an insidious onset, frequently resulting in missed and delayed diagnosis, sphenoid sinus aspergillosis is a potentially lethal medical condition. We report a case of visual loss secondary to isolated sphenoid sinus aspergillosis. A 69-year-old man presented to our hospital with the complaint of headache. The headache started one year previously and was described as severe dull pain localized bilaterally to the temporo-orbital region. The patient took daily NSAIDs for the pain. The neurological examination was normal. The MRI of the brain showed a left sphenoid sinusitis. A transnasal endoscopic superior meatal sphenoidotomy was performed. Aspergillosis was confirmed after a surgical biopsy was obtained. The patient was discharged from hospital without antifungal therapy. One month later, the patient complained of headache and loss of vision bilaterally. The orbital MRI showed a left cavernous sinus and bilateral optic nerve invasion. The loss of visions was permanent. In our case, the diagnosis was delayed; antifungal agents were not administered after surgery and the patient lost his vision as a result. Therefore, early diagnosis and proper treatment are important. Although the treatment of an invasive type of aspergillus has not been established, surgical removal of a nidus and aggressive antifungal therapy are recommended.

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Herpes Zoster Ophthalmicus in Minor Facial Burn (눈대상포진이 병발된 경미한 얼굴의 화상)

  • Han, Jung Kyu;Kim, Sun Goo;Kim, Yu Jin
    • Archives of Plastic Surgery
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    • v.36 no.6
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    • pp.803-805
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    • 2009
  • Purpose: Many conditions can mimic the presentation of burns. Herpes zoster is one of them. The characteristic features of herpes zoster such as vesicles, pustular lesions and crusts can also be found in burns. Herpes zoster ophthalmicus is a disease caused by recurrent infection of varicella - zoster virus in the ophthalmic division of the trigeminal nerve. This virus frequently affects nasociliary branch and serious ocular complications can occur. Thus, early diagnosis and proper treatment of this disease is important to prevent further ocular manifestations. We report a man who sustained minor facial burn injury that was complicated with herpes zoster ophthalmicus. Methods: A 66 - year - old man visited emergency room with multiple whitish vesicles with serous discharge on right forehead, right medial canthal area and nose. At first he was thought to have a secondary infection of facial burn injury. The vesicles on his face began to form crusts on the next day. Since his skin lesion was located on the ophthalmic division of trigeminal nerve, we also suspected herpes zoster ophthalmicus. He was referred to dermatologist and ophthalmologist. Results: We used antiviral agent (Acyclovir) and NSAIDs for treatment. The patient had no ocular complications. His skin lesion was almost healed after 1 month and remained scars. We treated a patient with minor facial burn complicated with herpes zoster ophthalmicus with antiviral agent. Conclusion: In this work, we describe a case of old patient with herpetic infection and emphasize the need for careful examination to diagnose accurately.

Effect of Other Medications on the Stability of Omeprazole in Aqueous Solution for the Peptic Ulcer Disease (소화성궤양시 병용약물이 수용액 중의 오메프라졸 안정성에 미치는 영향)

  • Lee, Young-Jae;Whang, Wan-Kyunn;Cho, Seong-Wan
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.10 no.11
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    • pp.3494-3499
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    • 2009
  • The stability of omeprazole in the aqueous solutions containing loxoprofen or Sodium bicarbonate was examined at room temperature. Loxoprofen or Sodium bicarbonate (60 mg) was added to omeprazole (600 ${\mu}g$/ml) solution to check the stability profile. Then, the solution was kept at room temperature for 80 hours. The concentration was assayed at each concentration by stability-indicating High performance liquid chromatography (HPLC) method. Aliquots of the solution were withdrawn at specified time intervals and assayed by chromatographic analysis for intact omeprazole. The relation between omeprazole concentration and peak area was linear from 5 to 160 ${\mu}g$/ml. The analysis method was precise with relative standard deviation (% RSD) no greater than 3.05 %. The remaining percentage-time curves revealed that omeprazole was degraded rapidly as functions of time and temperature following pseudo first-order kinetics. In conclusion, the stability of omeprazole was significantly affected by liquid solutions mixed with alkalizer (Sodium carbonate) or the NSAIDs (loxoprofen).

Activation of SAPK and Increase in Bak Levels during Ceramide and Indomethacin-Induced Apoptosis in HT29 Cells

  • Kim, Ju-Ho;Oh, Sae-Ock;Jun, Sung-Sook;Jung, Jin-Sup;Woo, Jae-Suk;Kim, Yong-Keun;Lee, Sang-Ho
    • The Korean Journal of Physiology and Pharmacology
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    • v.3 no.1
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    • pp.75-82
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    • 1999
  • It has been reported that activation of sphingomyelin pathway and nonsteroidal anti-inflammatory drugs (NSAIDS) inhibit the promotion of colon carcinoma. Ceramide, a metabolite of sphingomyelin, and indomethacin were shown to induce apoptosis in colon carcinoma cells. However, the mechanisms of ceramide- and indomethacin-induced apoptosis in the colon carcinoma cells are not clearly elucidated. Recent studys showed that indomethacin-induced apoptosis in colon cancer cells through the cyclooxygenase-independent pathways, and that may be mediated by generation of ceramide. In this study, we compared effects of ceramide and indomethacin on important modulators of apoptotic processes in HT29 cells, a human colon cancer cell line. Ceramide and indomethacin induced apoptosis dose- and time- dependently. Ceramide and indomethacin increased stress-activated protein kinase (SAPK) activity, and decreased mitogen-activated protein kinase (MAPK) activity. The expression of Bak was increased by the treatment of ceramide and indomethacin. The expression of other Bcl-2 related proteins (Mcl-1, $Bcl-X_L,$ Bax) which were known to be expressed in colon epithelial cells was not changed during the ceramide- and indomethacin-induced apoptosis. Our results suggest that ceramide and indomethacin share common mechanisms for induction of apoptosis in HT29 cells.

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Assessment of Potentially Inappropriate Medication Use in Korean Elderly Patients with Chronic Heart Failure (국내 노인 심부전 환자에서의 잠재적으로 부적절한 약물사용 현황에 대한 연구)

  • Bae, Min Kyung;Lee, Iyn-Hyang;Yoon, Jeong-Hyun
    • Korean Journal of Clinical Pharmacy
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    • v.24 no.2
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    • pp.115-125
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    • 2014
  • Purpose: The purpose of the present study was to assess the incidence of the potentially inappropriate medication (PIM) use in Korean elderly patients with heart failure, and to evaluate factors that influence PIM use. Method: Korean National Health Insurance claims database between January 2009 and December 2009 was used. Using 2012 updated Beers criteria, PIM use in heart failure patients aged 65 years or older was examined. Result: The incidence of PIM use in elderly heart failure patients was higher than in overall elderly patients. Among the 12,759 elderly patients with heart failure, 46.2% of study subjects were prescribed PIM(s) at least once. The number of PIM per 10 medications that patients received per patient was 1.53. The most commonly used PIMs in elderly heart failure patients were benzodiazepines (30.9%), non-steroidal anti-inflammatory drugs (NSAIDs) including COX-2 inhibitors (16.3%), digoxin (9.9%), and spironolactone (9.0%). Women (odds ratio, 1.20; 95% CI, 1.17-1.24), medical aid (odds ratio, 1.11; 95% CI, 1.08-1.13), and long-term facilities (odds ratio, 2.69; 95% CI, 2.44-2.96) were revealed to be important factors associated with PIM use. In addition, patient's age also seems to influence PIM use. Conclusion: Elderly heart failure patients are at a greater risk for adverse drug events attributed by inappropriate medication use. Efforts to increase awareness of PIM use in elderly heart failure patients are needed. In addition, various comprehensive strategies and policies to identify and prevent PIM use should be established nationwide.

Rotator Cuff Tears Syndrome (회전근개 파열 증후군)

  • Kang, Jeom-Deok;Kim, Hyun-Joo
    • The Journal of Korean Academy of Orthopedic Manual Physical Therapy
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    • v.13 no.1
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    • pp.67-72
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    • 2007
  • Anatomy: The rotator cuff comprises four muscles-the subscapularis, the supraspinatus, the infraspinatus and the teres minor-and their musculotendinous attachments. The subscapularis muscle is innervated by the subscapular nerve and originates on the scapula. It inserts on the lesser tuberosity of the humerus. The supraspinatus and infraspinatus are both innervated by the suprascapular nerve, originate in the scapula and insert on the greater tuberosity. The teres minor is innervated by the axillary nerve, originates on the scapula and inserts on the greater tuberosity. The subacromial space lies underneath the acromion, the coracoid process, the acromioclavicular joint and the coracoacromial ligament. A bursa in the subacromial space provides lubrication for the rotator cuff. Etiology: The space between the undersurface of the acromion and the superior aspect of the humeral head is called the impingement interval. This space is normally narrow and is maximally narrow when the arm is abducted. Any condition that further narrows this space can cause impingement. Impingement can result from extrinsic compression or from loss of competency of the rotator cuff. Syndrome: Neer divided impingement syndrome into three stages. Stage I involves edema and/or hemorrhage. This stage generally occurs in patients less than 25 years of age and is frequently associated with an overuse injury. Generally, at this stage the syndrome is reversible. Stage II is more advanced and tends to occur in patients 25 to 40 years of age. The pathologic changes that are now evident show fibrosis as well as irreversible tendon changes. Stage III generally occurs in patients over 50 years of age and frequently involves a tendon rupture or tear. Stage III is largely a process of attrition and the culmination of fibrosis and tendinosis that have been present for many years. Treatment: In patients with stage I impingement, conservative treatment is often sufficient. Conservative treatment involves resting and stopping the offending activity. It may also involve prolonged physical therapy. Sport and job modifications may be beneficial. Nonsteroidal anti - inflammatory drugs(NSAIDS) and ice treatments can relieve pain. Ice packs applied for 20 minutes three times a day may help. A sling is never used, because adhesive capsulitis can result from immobilization.

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