Drug discoveries & therapeutics最新文献_第10页

Cetirizine more potently exerts mast cell-stabilizing property than diphenhydramine. 西替利嗪比苯海拉明更有效地发挥肥大细胞稳定特性。

IF 3.1

Drug discoveries & therapeutics Pub Date : 2022-11-20 Epub Date: 2022-10-19 DOI: 10.5582/ddt.2022.01067

Ririka Fujimura, Ayano Asada, Misato Aizawa, Itsuro Kazama

{"title":"Cetirizine more potently exerts mast cell-stabilizing property than diphenhydramine.","authors":"Ririka Fujimura, Ayano Asada, Misato Aizawa, Itsuro Kazama","doi":"10.5582/ddt.2022.01067","DOIUrl":"https://doi.org/10.5582/ddt.2022.01067","url":null,"abstract":"Cetirizine, a second-generation antihistamine, and diphenhydramine, a first-generation antihistamine, are among the most widely used anti-allergic drugs. In addition to longer duration of action and less incidence of sedative side effects, recent clinical studies also indicate a higher potency of cetirizine than diphenhydramine in the treatment or prevention of allergic disorders. In the present study, using the differential-interference contrast (DIC) microscopy, we examined the effects of cetirizine and diphenhydramine (1 μM to 1 mM) on the degranulation from rat peritoneal mast cells. Using fluorescence imaging of a water-soluble dye, lucifer yellow, we also examined their effects on the deformation of the plasma membrane. At relatively higher concentrations (100 μM, 1 mM), both cetirizine and diphenhydramine significantly reduced the numbers of degranulating mast cells. Of note, at 1 mM, cetirizine more markedly reduced the number than diphenhydramine, almost entirely suppressing the degranulation of mast cells. Additionally, 1 mM cetirizine and levocetirizine, another second-generation antihistamine, almost totally inhibited the process of exocytosis in mast cells and washed out the trapping of the lucifer yellow on the cell surface, while diphenhydramine and chlorpheniramine, another first-generation antihistamine, did not. This study provided in vitro evidence for the first time that cetirizine more potently inhibited the process of exocytosis in mast cells than diphenhydramine, indicating its higher potency as a mast cell-stabilizer. Such mast cell-stabilizing property of cetirizine could be ascribed to its counteracting effect on the plasma membrane deformation in degranulating mast cells.","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"245-250"},"PeriodicalIF":3.1,"publicationDate":"2022-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40558214","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: 2

Generic selection criteria for safety and patient benefit [XI]: Usability scores of brand-name and generic tapes containing sodium diclofenac by questionnaire survey.

IF 3.1

Drug discoveries & therapeutics Pub Date : 2022-11-20 Epub Date: 2022-10-20 DOI: 10.5582/ddt.2022.01071

Mitsuru Nozawa, Ako Gannichida, Yuko Wada, Miyuki Kumazawa, Fumiyoshi Ishii, Ken-Ichi Shimokawa

{"title":"Generic selection criteria for safety and patient benefit [XI]: Usability scores of brand-name and generic tapes containing sodium diclofenac by questionnaire survey.","authors":"Mitsuru Nozawa, Ako Gannichida, Yuko Wada, Miyuki Kumazawa, Fumiyoshi Ishii, Ken-Ichi Shimokawa","doi":"10.5582/ddt.2022.01071","DOIUrl":"https://doi.org/10.5582/ddt.2022.01071","url":null,"abstract":"The aim of this study was to evaluate patient satisfaction and usability scores of different tape treatments and examine the scores in relation to the mechanical characteristics of the tape formulation. A questionnaire for the assessment of comfort level and satisfaction with two brand-name (Naboal, Voltaren) and four generic tapes (Yutoku, Teikoku, Rakool, Towa) containing sodium diclofenac was developed and then applied to 12 healthy volunteers. Results showed that Voltaren was difficult to apply to the skin and easier to peel off the skin than Naboal (p < 0.01). Moreover, Rakool was easier to peel than Naboal (p < 0.05). The mechanically measured peeling force was associated with pain during peeling off (r = -0.65), and the measured value of bending rigidity was associated with ease of peeling off (r = -0.97). The knowledge obtained regarding the influence of pharmaceutical properties on the degree of satisfaction with and usability of different tape formulations may be useful for supporting the selection of generic tapes tailored to individual needs or pharmacist preferences, and thus improve treatment adherence and clinical outcomes.","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"210-216"},"PeriodicalIF":3.1,"publicationDate":"2022-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40374537","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

A Japanese case of melanoma of unknown origin with a rare BRAF^V600R mutation was successfully treated with BRAF/MEK inhibitors. 日本的一例未知来源的黑色素瘤，罕见的BRAFV600R突变，成功地用BRAF/MEK抑制剂治疗。

IF 3.1

Drug discoveries & therapeutics Pub Date : 2022-11-20 Epub Date: 2022-10-23 DOI: 10.5582/ddt.2022.01072

Haruka Kuriyama, Toshihiro Kimura, Satoru Mizuhashi, Yuki Nishimura, Hisashi Kanemaru, Ikko Kajihara, Katsunari Makino, Jun Aoi, Hirotaka Matsui, Satoshi Fukushima

引用次数: 0

Potential applications of Chinese herbal medicines with hemostatic properties. 具有止血作用的中草药的潜在应用。

IF 3.1

Drug discoveries & therapeutics Pub Date : 2022-07-20 Epub Date: 2022-06-26 DOI: 10.5582/ddt.2022.01037

Naoki Ohkura

引用次数: 0

Neuroleptic malignant syndrome in a case of extra-pontine myelinolysis: On the horns of dilemma. 脑桥外髓鞘溶解一例抗精神病药恶性综合征:进退两难。

IF 3.1

Drug discoveries & therapeutics Pub Date : 2022-07-20 Epub Date: 2022-06-25 DOI: 10.5582/ddt.2021.01012

Umang Arora, Ayush Goel, Animesh Ray, Naval K Vikram

引用次数: 1

Safety of linezolid, rifampicin, and clindamycin combination therapy in patients with prosthetic joint infection. 利奈唑胺、利福平和克林霉素联合治疗假体关节感染的安全性。

IF 3.1

Drug discoveries & therapeutics Pub Date : 2022-07-20 Epub Date: 2022-06-25 DOI: 10.5582/ddt.2022.01038

Shunsuke Kobayashi, Seiji Tagawa, Takashi Ogura, Akira Kitaoka, Takeo Yasu

{"title":"Safety of linezolid, rifampicin, and clindamycin combination therapy in patients with prosthetic joint infection.","authors":"Shunsuke Kobayashi, Seiji Tagawa, Takashi Ogura, Akira Kitaoka, Takeo Yasu","doi":"10.5582/ddt.2022.01038","DOIUrl":"https://doi.org/10.5582/ddt.2022.01038","url":null,"abstract":"We investigated adverse events in patients with prosthetic joint infections receiving combination therapy with linezolid, rifampicin, and clindamycin for ≥ 7 days. Twenty-two patients were evaluated. The combination therapy was administered for 15.5 (7-29) days at dosages of 1200, 450, and 450-1200 mg/day for linezolid, rifampicin, and clindamycin, respectively. Adverse events (gastrointestinal, eye, and skin disorders; liver damage; myelosuppression; hyponatremia, and others) were recorded. The incidence rates of leukopenia, neutropenia, anemia, thrombocytopenia, and hyponatremia were 36.4%, 31.8%, 40.9%, 18.2%, and 18.2%, respectively. Common Terminology Criteria for Adverse Events version 5.0 Grade 3 neutropenia, anemia, and hyponatremia were observed. The incidence rate of myelosuppression was higher following combination therapy compared with that previously reported following single-drug administration. All patients were discharged after the infection was under control. It is important to monitor these adverse events during combination therapy with the aforementioned agents; these conditions may be relieved by discontinuing linezolid.","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"142-144"},"PeriodicalIF":3.1,"publicationDate":"2022-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40399872","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: 1

Proposal of an in vitro thrombus-growth model for evaluating anticoagulants. 一种评估抗凝剂的体外血栓生长模型的提出。

IF 3.1

Drug discoveries & therapeutics Pub Date : 2022-07-20 Epub Date: 2022-06-26 DOI: 10.5582/ddt.2022.01040

Yoshikazu Sawaguchi, Hiroyuki Yamamoto, Souma Itou, Ken Tachibana, Kentaro Ohnuma, Yusuke Kamada, Takanori Nakajima

{"title":"Proposal of an in vitro thrombus-growth model for evaluating anticoagulants.","authors":"Yoshikazu Sawaguchi, Hiroyuki Yamamoto, Souma Itou, Ken Tachibana, Kentaro Ohnuma, Yusuke Kamada, Takanori Nakajima","doi":"10.5582/ddt.2022.01040","DOIUrl":"https://doi.org/10.5582/ddt.2022.01040","url":null,"abstract":"The general anticoagulant evaluation requires high expense equipment, reagents, and space. Therefore, not all laboratories can perform research related to anticoagulant. In this study, we propose a novel simple method \"in vitro thrombus-growth model\" that can evaluate anticoagulant ability by measuring weight. The in vitro thrombus-growth model is prepared by creating a \"growth-clot\" with citrate plasma, calcium chloride, and thrombin, and then pouring new citrate plasma onto it. The prepared growth-clots were increased in volume in citrated human plasma, including surpluses calcium chloride, which was released slowly, leading to clot coagulation around the plasma. As a result of evaluating the anticoagulant ability of direct thrombin inhibitor using this in vitro thrombus-growth model, it was confirmed that clot growth was suppressed in a concentration-dependent manner. Therefore, this thrombus-growth model is useful as a primary anticoagulant test that can to discover compounds with anticoagulant activity perform in any laboratory.","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"135-138"},"PeriodicalIF":3.1,"publicationDate":"2022-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40399309","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

Urolithins and intestinal health. 尿石素和肠道健康。

IF 3.1

Drug discoveries & therapeutics Pub Date : 2022-07-20 Epub Date: 2022-06-25 DOI: 10.5582/ddt.2022.01039

Chunhua Lu, Xintong Li, Zeyuan Gao, Yuliang Song, Yuemao Shen

引用次数: 6

Efficacy and safety of sotrovimab for vaccinated or unvaccinated patients with mild-to-moderate COVID-19 in the omicron era. 单粒时代sotrovimab对轻中度COVID-19疫苗接种或未接种患者的疗效和安全性

Drug discoveries & therapeutics Pub Date : 2022-07-20 Epub Date: 2022-06-25 DOI: 10.5582/ddt.2022.01036

Takehiro Izumo, Nobuyasu Awano, Naoyuki Kuse, Keita Sakamoto, Kohei Takada, Yutaka Muto, Kazushi Fujimoto, Ayae Saiki, Yu Ito, Hiroaki Ota, Minoru Inomata

{"title":"Efficacy and safety of sotrovimab for vaccinated or unvaccinated patients with mild-to-moderate COVID-19 in the omicron era.","authors":"Takehiro Izumo, Nobuyasu Awano, Naoyuki Kuse, Keita Sakamoto, Kohei Takada, Yutaka Muto, Kazushi Fujimoto, Ayae Saiki, Yu Ito, Hiroaki Ota, Minoru Inomata","doi":"10.5582/ddt.2022.01036","DOIUrl":"10.5582/ddt.2022.01036","url":null,"abstract":"Although sotrovimab, one of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) neutralizing antibodies has been shown to be effective in patients with mild-to-moderate coronavirus disease 2019 (COVID-19) with risk factors, their efficacy in mRNA COVID-19 vaccinated patients in omicron era is unknown. To evaluate the effectiveness of sotrovimab clinical data from both COVID-19 vaccinated and unvaccinated patients who were hospitalized and receiving sotrovimab at the Japanese Red Cross Medical Center were compared. The efficacy and adverse events were evaluated. Of the total 60 patients enrolled in this study, 45 had received the mRNA COVID-19 vaccine and 15 were unvaccinated. The clinical progression with low nasal cannula or face mask was not significantly different between groups (occurring in one patient in each group; p = 0.44), with no further progression in both groups. The duration of hospitalization was eight days for both groups (p = 0.90). Two patients in each group experienced adverse events (7%, p = 0.26). The results suggested that the efficacy and safety of sotrovimab against mild-to-moderate COVID-19 with risk factors in the omicron era might not be different regardless of the vaccination status. The results of the present study are encouraging; however, further randomized clinical studies are needed.","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"124-127"},"PeriodicalIF":0.0,"publicationDate":"2022-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40399871","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

Safety verification of a new peripheral intravenous catheter placed in the upper arm vein for administration of drugs with high irritant potential. 一种新的外周静脉导管放置在上臂静脉给药具有高刺激电位的安全性验证。

Drug discoveries & therapeutics Pub Date : 2022-07-20 Epub Date: 2022-06-25 DOI: 10.5582/ddt.2022.01034

Ryoko Murayama, Hajime Oyama, Mari Abe-Doi, Yosuke Masamoto, Kosuke Kashiwabara, Hiromi Tobe, Chieko Komiyama, Hiromi Sanada, Mineo Kurokawa

{"title":"Safety verification of a new peripheral intravenous catheter placed in the upper arm vein for administration of drugs with high irritant potential.","authors":"Ryoko Murayama, Hajime Oyama, Mari Abe-Doi, Yosuke Masamoto, Kosuke Kashiwabara, Hiromi Tobe, Chieko Komiyama, Hiromi Sanada, Mineo Kurokawa","doi":"10.5582/ddt.2022.01034","DOIUrl":"10.5582/ddt.2022.01034","url":null,"abstract":"Despite the widespread use of peripheral intravenous catheters, unscheduled catheter failure before completion of treatment occurs frequently. If a large vein is selected, catheter failures may be prevented despite administering a highly irritant drug. In this study, we attempted to use a catheter that can be placed in a large upper arm vein. The new catheter was 88 mm long but had no guidewire to reduce contamination risk. This study aimed to evaluate the safety of the first-in-human trial for the new catheter with the administration of highly irritant drugs. This study was conducted at a university hospital in Tokyo, Japan. Eight Japanese adults were hospitalized adults with planned administration of non-cancer drugs with high irritant potential using a peripheral catheter. A trained nurse catheterized with the new catheter in the upper arm using ultrasonography. The catheterization site was monitored by staff and a research nurse once every 24 hours for up to 7 days. No adverse events or catheter failure occurred and the catheter placement success rate was 100%. In two patients, a temporary occlusion alarm of the infusion pump occurred, possibly due to the flexion of the catheter base. The new peripheral intravenous catheter did not interrupt medical treatments as is common after placement, but safety administered the irritant drugs. However, because this catheter may be easily affected by the contraction of the muscle at the fixation position, the position and method of catheter fixation in the upper arm need to be carefully considered.","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"128-134"},"PeriodicalIF":0.0,"publicationDate":"2022-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40399870","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