International journal of clinical pharmacology research最新文献

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Good Clinical Practice 良好临床操作规范
International journal of clinical pharmacology research Pub Date : 2019-05-02 DOI: 10.19080/JPCR.2019.07.555706
K. Aftab
{"title":"Good Clinical Practice","authors":"K. Aftab","doi":"10.19080/JPCR.2019.07.555706","DOIUrl":"https://doi.org/10.19080/JPCR.2019.07.555706","url":null,"abstract":"Trials evaluate the safety of a Drug. This first phase of testing, which can take many months to complete, usually includes a good number of healthy volunteers (25 to 100), who are generally paid for participating in the trials. The trial is designed to determine the effect of the Drug on healthy humans including how it is behaves or act (absorbed, distributed, bio transformed and eliminated). This phase also examine the adverse effects that occur at different dosage are increased or decreased. About seventy percent of experimental drugs pass this phase of testing.","PeriodicalId":13940,"journal":{"name":"International journal of clinical pharmacology research","volume":"33 6","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72571462","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Phase II study of a novel oral formation of 5-fluorouracil in combination with low-dose cisplatin as preoperative chemotherapy of oral squamous cell carcinoma. 一种新型口服5-氟尿嘧啶制剂联合低剂量顺铂作为口腔鳞状细胞癌术前化疗的II期研究
M Nakazawa, T Ohnishi, M Ohmae, H Chisoku, S Yui, S Iwai, T Sumi, Y Fukuda, M Kishino, Y Yura
{"title":"Phase II study of a novel oral formation of 5-fluorouracil in combination with low-dose cisplatin as preoperative chemotherapy of oral squamous cell carcinoma.","authors":"M Nakazawa,&nbsp;T Ohnishi,&nbsp;M Ohmae,&nbsp;H Chisoku,&nbsp;S Yui,&nbsp;S Iwai,&nbsp;T Sumi,&nbsp;Y Fukuda,&nbsp;M Kishino,&nbsp;Y Yura","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>TS-1 is a novel oral 5-fluorouracil containing tegaful (prodrug of 5-FU) and two biochemical modulators. These modulators feature effect-enhancing and adverse reaction-reducing activity. We investigated the histological response and toxicities of combination chemotherapy with TS- 1 and low-dose cisplatin and evaluated its usefulness as preoperative chemotherapy Forty-four newly diagnosed patients with stage Il-IV oral squamous cell carcinoma were enrolled in this study from February 2002 to April 2004. Patients were administered TS-1 80 mg/m2/day (days 1-14) and cisplatin 5 mg/m2/day (days 1-5 and 8-12) followed by radical surgery within 2 weeks. The histopathological effect of chemotherapy, which was a surrogate endpoint of this trial, was evaluated with surgical or biopsy specimens. The rate of histological antitumor effect was as follows: complete response (CR) 36.4%, partial response (PR) 25.0%, minor response (MR) 18.1% and no change (NC) 20.5%. The rate of histological response (CR + PR) was 61.4%. The CR rate of effective cases was 59.3%. The main toxicities occurred in bone marrow and the digestive tract. The incidence of severe toxicity such as grade 3 or 4 was 4.5% in anemia, 9% in leukocytopenia, 11.4% in neutropenia, 4.5% in thrombocytopenia and 2.3% in anorexia, diarrhea and urticaria. Most patients showed no toxicity or mild toxicities. TS- 1 with low-dose cisplatin has highly effective antitumor activity and mild toxicities. In particular, the CR rate was very high. It is suggested that this regimen is suitable for neoadjuvant chemotherapy. We expect that this chemotherapy will contribute to avoidance of surgery for small tumors (stages I and II) and will enable function-preserving surgery for advanced tumors.</p>","PeriodicalId":13940,"journal":{"name":"International journal of clinical pharmacology research","volume":"25 3","pages":"115-22"},"PeriodicalIF":0.0,"publicationDate":"2005-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25760960","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Methotrexate-induced acute lung injury in a patient with rheumatoid arthritis. 甲氨蝶呤致类风湿关节炎患者急性肺损伤1例。
K Taniguchi, Y Usui, T Matsuda, S Suzuki, K Fujiki, F Yakusiji, J Tomiyama, K Kinoshita, H Ilzuka, Y Kuga
{"title":"Methotrexate-induced acute lung injury in a patient with rheumatoid arthritis.","authors":"K Taniguchi,&nbsp;Y Usui,&nbsp;T Matsuda,&nbsp;S Suzuki,&nbsp;K Fujiki,&nbsp;F Yakusiji,&nbsp;J Tomiyama,&nbsp;K Kinoshita,&nbsp;H Ilzuka,&nbsp;Y Kuga","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Methotrexate (MTX)-induced acute lung injury developed in a female patient with rheumatoid arthritis. She was successfully treated with high-dose glucocorticoid therapy. During her hospital stay, the serum concentration of surfactant protein (SP)-D, which was markedly elevated on admission, was finally normalized and the disease resolved. However, the serum concentration of Klebs von den Lungen (KL)-6 remained high. Although the mechanisms of lung injury by MTX have not been well defined, serial measurements of serum SPD might be useful for the clinical evaluation of drug-induced acute lung injury.</p>","PeriodicalId":13940,"journal":{"name":"International journal of clinical pharmacology research","volume":"25 3","pages":"101-5"},"PeriodicalIF":0.0,"publicationDate":"2005-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25761044","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The effect of D-003 (10 mg/day) on biochemical parameters of bone remodelling in postmenopausal women: a randomized, double-blind study. D-003(10毫克/天)对绝经后妇女骨重塑生化参数的影响:一项随机、双盲研究
A Ceballos, R Mas, G Castaño, L Fernández, S Mendoza, R Menéndez, J J González, J Illnait, R Gámez, M Mesa, J Fernández
{"title":"The effect of D-003 (10 mg/day) on biochemical parameters of bone remodelling in postmenopausal women: a randomized, double-blind study.","authors":"A Ceballos,&nbsp;R Mas,&nbsp;G Castaño,&nbsp;L Fernández,&nbsp;S Mendoza,&nbsp;R Menéndez,&nbsp;J J González,&nbsp;J Illnait,&nbsp;R Gámez,&nbsp;M Mesa,&nbsp;J Fernández","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Biphosphonates, which are antiresorptive agents used to treat osteoporosis, inhibit the mevalonate pathway, preventing protein prenylation and inhibiting osteoclast activity. Statins decrease cholesterol biosynthesis by blocking the mevalonate pathway and have been reported to have beneficial effects on bone. D-003 is a mixture of high molecular weight acids purified from sugarcane wax that inhibits cholesterol biosynthesis before mevalonate production. D-003 prevents bone loss and resorption in rats with osteoporosis induced with ovariectomy or corticoids. Biochemical markers of bone turnover are used to monitor the short-term efficacy of antiosteoporotic therapy. This randomized, double-blind, placebo-controlled study was undertaken to investigate the short-term effects of D-003 (10 mg/day) on biochemical markers of bone turnover in postmenopausal women with low bone mineral density (BMD). After 4 weeks on a low-fat diet, 34 women were randomized to D-003 (10 mg/day) or placebo for 6 months. Pre- and post-treatment samples were analyzed for urinary excretion of deoxypyridinoline (DPD)/creatinine (Cr), a marker of bone resorption, and serum bone specific alkaline phosphatase (BSAP), a marker of bone formation. The effects on lipid profile and safety indicators, as well as adverse events (AE), were investigated. D-003 (10 mg/day) lowered urinary excretion of tDPD/Cr versus baseline (20.6%) (p < 0.001) and placebo (33.7%) (p < 0.01), but did not modify serum BSAP. D-003 decreased low-density lipoprotein-cholesterol (LDL-C) (32.8%), total cholesterol (TC) (16.4%) and the TC/high-density lipoprotein-cholesterol (HDL-C) ratio (34.7%), increased HDL-C (30.3%) (p < 0.001) and did not modify triglycerides. The effects on these variables were significant as early as 3 months after treatment initiation. D-003 was well tolerated. Three patients (one in the placebo group and two in the D-003 group) withdrew from the study. Two of these withdrawals were due to AE: abdominal pain (placebo) and heartburn (D-003). Five patients (four in the placebo group [22.2%] and one in the D-003 group [6.3%]) reported mild AE. In conclusion, D-003 (10 mg/day) reduced urinary excretion of tDPD/Cr, a bone resorption marker and did not change serum BSAP, a bone formation marker, while it lowered cholesterol in study patients. These preliminary results suggest that D-003 could be useful in treating postmenopausal women with low BMD. However, the potential value of D-003 in treating or preventing osteoporosis deserves further clinical investigation.</p>","PeriodicalId":13940,"journal":{"name":"International journal of clinical pharmacology research","volume":"25 4","pages":"175-86"},"PeriodicalIF":0.0,"publicationDate":"2005-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25792294","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Effects of D-003, a mixture of very long chain fatty acids purified from sugar cane wax, at 5 and 10 mg/day on platelet aggregation in healthy volunteers. D-003是一种从甘蔗蜡中纯化的长链脂肪酸混合物,5和10毫克/天对健康志愿者血小板聚集的影响。
M L Arruzazabala, V Molina, D Carbajal, L Fernández, R Mas, G Castaño, J Illnait, S Mendoza, J Fernańdez
{"title":"Effects of D-003, a mixture of very long chain fatty acids purified from sugar cane wax, at 5 and 10 mg/day on platelet aggregation in healthy volunteers.","authors":"M L Arruzazabala,&nbsp;V Molina,&nbsp;D Carbajal,&nbsp;L Fernández,&nbsp;R Mas,&nbsp;G Castaño,&nbsp;J Illnait,&nbsp;S Mendoza,&nbsp;J Fernańdez","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>D-003 is a mixture of high molecular weight aliphatic primary acids purified from sugar cane wax with antiplatelet and cholesterol-lowering effects. Previous studies showed that D-003 (10-20 mg/day) administered for a short time inhibits platelet aggregation, 14 days being the longest duration investigated. This study was conducted to investigate the effects of D-003 (5 and 10 mg/day) for 30 days on platelet aggregation in normocholesterolemic subjects. This report shows the effects of D-003 on platelet aggregation to arachidonic acid (AA) (1.5 mM), collagen (2 microg/ml) and adenosine 5'-diphosphate ADP (2 microM) assessed at baseline and at treatment completion. Fifty-four subjects were randomized to placebo or D-003 (5 or 10 mg/day) for 30 days. Platelet aggregation to AA, collagen and ADP were assessed. D-003 at the lowest dose (5 mg/day) significantly but modestly inhibited (p < 0.01) platelet aggregation to AA (5.0%) and (p < 0.01) to collagen (7.5%). D-003 at 10 mg/day inhibited (p < 0.001) platelet aggregation to AA and collagen (p < 0.01) by 20.3% and 14.7%, respectively. ADP-induced aggregation, however, was unchanged. D-003 at 10 mg/day, but not at 5 mg/day, lowered (p < 0.01) plasma fibrinogen. D-003 (5 and 10 mg/day) reduced low-density lipoprotein cholesterol (LDL-C) by 17.7% and 26.4%, respectively, and total cholesterol (TC) by 14.5% and 18.5%, while at 10 mg/day, but not at 5 mg/day, it increased high-density lipoprotein cholesterol (HDL-C) by 9.6%. Triglycerides, however, were unchanged with D-003. No disturbances in safety indicators were induced with D-003. One subject (D-003 5 mg/day) discontinued the study and four patients (three taking D-003 and one taking placebo) reported adverse effects (AE) (headache in two patients taking D-003 and one patient taking placebo, and polyphagia in one patient taking D-003). In conclusion, D-003 (5-10 mg/day) for 30 days inhibited platelet aggregation to AA and collagen but not to ADP Therefore, the antiplatelet effect was present with the longer treatment, even at a dose of 5 mg/day. The cholesterol-lowering effects of D-003 were consistent with those expected for such a short treatment. In addition, D-003 at 10 mg/day significantly lowered plasma fibrinogen. The treatment was well tolerated.</p>","PeriodicalId":13940,"journal":{"name":"International journal of clinical pharmacology research","volume":"25 1","pages":"29-39"},"PeriodicalIF":0.0,"publicationDate":"2005-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25263191","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Treatment with oral biphosphonates can increase the sensitivity of sestamibi radionuclide imaging in patients with primary hyperparathyroidism. 口服双膦酸盐治疗可提高原发性甲状旁腺功能亢进患者sestamibi放射性核素成像的敏感性。
P Makras, G A Kaltsas, T Athanasoulis, D Papadogias, G N Zografos, G Kontogeorgos, N Borboli, G Piaditis
{"title":"Treatment with oral biphosphonates can increase the sensitivity of sestamibi radionuclide imaging in patients with primary hyperparathyroidism.","authors":"P Makras,&nbsp;G A Kaltsas,&nbsp;T Athanasoulis,&nbsp;D Papadogias,&nbsp;G N Zografos,&nbsp;G Kontogeorgos,&nbsp;N Borboli,&nbsp;G Piaditis","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The sensitivity of 99mTc-sestamibi scan in detecting parathyroid disease in primary hyperparathyroidism (PHP) is almost 90%, and therefore facilitates successful parathyroidectomy. To enhance the diagnostic accuracy of the procedure, we repeated imaging with 99mTc-sestamibi in 15 patients with PHP and an initially negative (11 patients) or weakly positive (four patients) 99mTc-sestamibi scan after the administration of 10 mg of oral alendronate for 2 months. Serum calcium, phosphate and parathormone (PTH) measurements were obtained at presentation and after 1 and 2 months' treatment with alendronate. Eight patients with an initially negative 99mTc-sestamibi scan demonstrated at least one area of uptake in the repeated scan. Six of these patients underwent surgery and obtained a biochemical cure; a single adenoma was found in four and hyperplasia in the remaining two. In all four patients with an initially weakly positive 99mTc-sestamibi scan, the repeated scan demonstrated enhanced uptake and also revealed further areas of uptake. Two of these patients underwent surgery with a biochemical cure; an adenoma was found in one and hyperplasia in another. Compared with baseline there was a significant increase in PTH but not in calcium or phosphate levels during treatment with alendronate. We suggest that, in patients with PHP and a negative or weakly positive initial 99mTc-sestamibi scan, administration of oral alendronate may be associated with a positive repeated 99mTc-sestamibi scan and can thus enhance the sensitivity of the procedure.</p>","PeriodicalId":13940,"journal":{"name":"International journal of clinical pharmacology research","volume":"25 1","pages":"19-28"},"PeriodicalIF":0.0,"publicationDate":"2005-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25087842","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Efficacy of a novel calcium/potassium salt of (-)-hydroxycitric acid in weight control. 一种新型(-)-羟基柠檬酸钙/钾盐控制体重的效果。
H G Preuss, R I Garis, J D Bramble, D Bagchi, M Bagchi, C V S Rao, S Satyanarayana
{"title":"Efficacy of a novel calcium/potassium salt of (-)-hydroxycitric acid in weight control.","authors":"H G Preuss,&nbsp;R I Garis,&nbsp;J D Bramble,&nbsp;D Bagchi,&nbsp;M Bagchi,&nbsp;C V S Rao,&nbsp;S Satyanarayana","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The weight-loss efficacy of a novel, water-soluble, calcium-potassium salt of (-)-hydroxycitric acid (HCA-SX) was re-examined in 90 obese subjects (BMI: 30-50.8 kg/m2). We combined data from two previously reported randomized, double-blind, placebo-controlled clinical studies in order to achieve a better statistical evaluation based on a larger population. This re-examination of data also allowed us to reflect more intensely on various aspects of weight loss studies. Subjects were randomly divided into three groups: group A received a daily dose of HCA-SX 4, 667 mg (providing 2,800 mg HCA per day); group B was given a daily dose of a combination of HCA-SX 4,667 mg, niacin-bound chromium (NBC) 4 mg (providing 400 microg elemental chromium), and Gymnema sylvestre extract (GSE) 400 mg (providing 100 mg gymnemic acid); and group C received a placebo in three equally divided doses 30-60 min before each meal. All subjects were provided a 2,000 kcal diet/day and participated in a supervised walking program for 30 min/day, 5 days/week. Eighty-two subjects completed the study. At the end of 8 weeks, in group A, both body weight and BMI decreased by 5.4%, low-density lipoprotein and triglycerides levels were reduced by 12.9% and 6.9%, respectively, while high-density lipoprotein levels increased by 8.9%, serum leptin levels decreased by 38%, serotonin levels increased by 44.5% and urinary excretion of fat metabolites increased by 32-109%. Group B demonstrated similar beneficial changes, but generally to a greater extent. No significant adverse effects were observed. The combined results confirm that HCA-SX and, to a greater degree, the combination of HCA-SX plus NBC and GSE reduce body weight and BMI, suppress appetite, improve blood lipid profiles, increase serum leptin and serotonin levels and increase fat oxidation more than placebo. We conclude that dosage levels, timing of administration, subject compliance and bioavailability of HCA-SX significantly affect results and that when taken as directed, HCA-SX is a highly effective adjunct to healthy weight control.</p>","PeriodicalId":13940,"journal":{"name":"International journal of clinical pharmacology research","volume":"25 3","pages":"133-44"},"PeriodicalIF":0.0,"publicationDate":"2005-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25760963","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Identification of human papillomavirus DNA in melanoma biopsy specimens of Greek population. 希腊人群黑色素瘤活检标本中人乳头瘤病毒DNA的鉴定。
A V Roussaki-Schulze, C Kouskoukis, C Rammos, E Rallis, F Kontos, E Zafiriou, G Gross
{"title":"Identification of human papillomavirus DNA in melanoma biopsy specimens of Greek population.","authors":"A V Roussaki-Schulze,&nbsp;C Kouskoukis,&nbsp;C Rammos,&nbsp;E Rallis,&nbsp;F Kontos,&nbsp;E Zafiriou,&nbsp;G Gross","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The aim of this retrospective study was to evaluate melanoma biopsy specimens from the Greek population living in the prefecture of Larissa for the presence of human papillomavirus (HPV) DNA and to determine the possible relationship between HPV and clinical outcome in these patients. Twenty-eight melanoma biopsy specimens, 20 from primary cutaneous melanoma and eight from melanoma metastasis were obtained from 28 patients. The biopsy samples were formalin-fixed and paraffin wax-embedded. The control group consisted of three junctional melanocytic nevi, histologically confirmed, and three punch biopsies from normal skin that were obtained from six healthy individuals. The presence and types of HPV DNA were assessed by the amplification of a fragment of the LI region by consensus primer polymerase chain reaction (PCR) combined with restriction fragment length polymorphism analysis (RFLPA). In each biopsy specimen that was evaluated, HPV 6, HPV 11, HPV 16 and HPV 18 positive controls from genital HPV lesions were included. Five of 28 (17.85%) biopsy melanoma specimens were positive for HPV DNA. Conversely, HPV was not detected in any of the biopsy specimens of the control group (0/6). HPV viral type 16 was found in two samples and HPV 6 DNA in three. Our results regarding the possible relationship between melanoma and HPV DNA were not statistically significant (p > 0.05). These findings suggest that ultraviolet sun exposure remains the main cause of melanoma in our region. The role of cutaneous HPV infection in the pathogenesis of melanoma remains elusive.</p>","PeriodicalId":13940,"journal":{"name":"International journal of clinical pharmacology research","volume":"25 3","pages":"145-50"},"PeriodicalIF":0.0,"publicationDate":"2005-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25760964","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Multicenter study of hyaluronic acid obtained by biotechnology to evaluate clinical efficacy and safety in knee osteoarthritis. 生物技术获得透明质酸的多中心研究评估膝关节骨关节炎的临床疗效和安全性。
A C Novaes, P Schaiquevich, G Nasswetter
{"title":"Multicenter study of hyaluronic acid obtained by biotechnology to evaluate clinical efficacy and safety in knee osteoarthritis.","authors":"A C Novaes,&nbsp;P Schaiquevich,&nbsp;G Nasswetter","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Viscosuppplementation with intra-articular hyaluronic acid (hyaluronan [HA]) is a relatively new option for improving pain and articular function in patients with symptomatic knee osteoarthritis. An open multi-center study was performed in 365 patients with definite and symptomatic knee osteoarthritis from seven Latin American countries. Five doses of HA were administered once a week. The parameters studied were pain (six items), stiffness (two items) and functional capacity (17 items). The parameters were evaluated 1 week after the corresponding injection. Statistical differences were found when basal determinations of the three parameters were compared with the results of the first and fourth administration (p < 0.05). Intra-articular HA administration was well tolerated. Treatment-related nonserious adverse events were registered in 2.5% of administrations. Based on the results obtained, HA is a useful and well-tolerated symptomatic treatment for knee osteoarthritis with a rapid onset of action.</p>","PeriodicalId":13940,"journal":{"name":"International journal of clinical pharmacology research","volume":"25 1","pages":"1-7"},"PeriodicalIF":0.0,"publicationDate":"2005-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25087840","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Telmisartan has the strongest binding affinity to angiotensin II type 1 receptor: comparison with other angiotensin II type 1 receptor blockers. 替米沙坦与血管紧张素II型1受体结合亲和力最强:与其他血管紧张素II型1受体阻滞剂比较。
H Kakuta, K Sudoh, M Sasamata, S Yamagishi
{"title":"Telmisartan has the strongest binding affinity to angiotensin II type 1 receptor: comparison with other angiotensin II type 1 receptor blockers.","authors":"H Kakuta,&nbsp;K Sudoh,&nbsp;M Sasamata,&nbsp;S Yamagishi","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>There is a growing body of evidence that the renin-angiotensin system (RAS) plays a pivotal role in the pathogenesis of cardiovascular diseases. Indeed, large clinical trials have demonstrated a substantial benefit of the blockade of this system for cardiovascular-organ protection. Although several types of angiotensin II type 1 (AT1) receptor blockers (ARBs) are commercially available for the treatment of patients with hypertension, comparisons of the binding affinity to AT1 receptor among them remain to be elucidated. In this study, we examined the dissociation rate of several ARBs from AT1 receptor in vitro. Angiotensin II time-dependently dissociated telmisartan, olmesartan, candesartan, valsartan, losartan and an active metabolite of losartan, EXP3174, from membrane components containing human AT1 receptor The dissociation rate constant of each ARB was 0.003248, 0.004171, 0.005203, 0.009946, 0.01027 and 0.008561 min(-1), with corresponding half-lives of 213, 166, 133, 70, 67 and 81 min, respectively. These results demonstrate that telmisartan has the strongest binding affinity to AT1 receptor among various ARBs examined herein. The rank order of affinity was telmisartan > olmesartan > candesartan > EXP3174 > or = valsartan > or = losartan. The present findings suggest that telmisartan (Micardis) may have long-lasting blood pressure-lowering effects and superior cardioprotective properties in patients with hypertension due to its strongest AT1 receptor antagonistic ability.</p>","PeriodicalId":13940,"journal":{"name":"International journal of clinical pharmacology research","volume":"25 1","pages":"41-6"},"PeriodicalIF":0.0,"publicationDate":"2005-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25087843","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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