<i>α</i><sub>1</sub>-Adrenoceptor Blockade by Class I Antiarrhythmic Drugs in Guinea Pig Thoracic Aorta as Revealed by Mechanical and Fluorescence Displacement Analysis

Article

Author: Tanaka, Hikaru ; Igarashi, Hiro ; Namekata, Iyuki ; Shirai, Kuniaki ; Kawazoe, Ayaka ; Tsukada, Kohei ; Seki, Maika ; Hamaguchi, Shogo ; Miyahara, Marina

The effects of thirteen Vaughn Williams class I antiarrhythmic drugs on the α₁-adrenergic receptor-mediated contraction were examined in thoracic aorta tissue preparations isolated from the guinea pig. Cibenzoline, quinidine, aprindine, and ranolazine, as well as prazosin, inhibited the phenylephrine-induced contraction with pA₂ values of 5.64, 5.59, 5.61, 5.08, and 8.50, respectively, but not prostaglandin F_2α-induced. These drugs reduced the staining of the smooth muscle layer by fluorescent prazosin. Propafenone inhibited the phenylephrine-induced contraction with an apparent pA₂ value of 5.31 and reduced the staining by fluorescent prazosin, but also inhibited the prostaglandin F_2α-induced contraction. Other class I antiarrhythmic drugs, disopyramide, pirmenol, procainamide, lidocaine, mexiletine, flecainide, pilsicainide, and GS-458967, affected neither the contraction by phenylephrine nor the fluorescent staining by prazosin. These results indicate that among the class I antiarrhythmic drugs, cibenzoline, aprindine, and propafenone, as well as quinidine and ranolazine, have α₁-adrenoceptor-blocking activity at therapeutically relevant concentrations.

31 Dec 2024·Journal of Dermatological Treatment

Risk of neutropenia in psoriasis patients prescribed anti-IL-23 antibody in comparison with anti-IL-17 antibody or adalimumab based on real-world data from the MID-NET ^® in Japan

Article

Author: Okada, Yusuke ; Komiyama, Noriyuki ; Uyama, Yoshiaki ; Horiuchi, Naoya ; Ishiguro, Chieko ; Kuga, Wataru ; Komaki, Tomomi ; Nonaka, Takahiro ; Kajiyama, Kazuhiro ; Iguchi, Toyotaka

BACKGROUNDTo evaluate the risk of neutropenia during treatment with anti-IL-23 antibodies in patients with psoriasis.METHODWe conducted an observational study with cohort design using MID-NET^® in Japan. We identified patients with psoriasis who were newly prescribed anti-IL-23 antibodies, anti-IL-17-antibodies, adalimumab, or apremilast between January 1, 2009, and March 31, 2021. We estimated the adjusted hazard ratio (aHR) of anti-IL-23 antibodies compared to that of anti-IL-17 antibodies, adalimumab, or apremilast, for the risk of grade 2 (neutrophil count < 1,500/μL) or grade 3 (neutrophil count < 1,000/μL) neutropenia.RESULTSOverall, 287 patients on anti-IL-23 antibodies, 189 patients on anti-IL-17 antibodies, 293 patients on adalimumab, and 540 patients on apremilast were included. Compared with anti-IL-17 antibodies, the aHR (95% confidence interval (CI)) of anti-IL-23 antibodies was 0.83 (0.27-2.51) for grade 2 and 0.40 (0.02-7.60) for grade 3 neutropenia; that when compared with adalimumab was 0.76 (0.28-2.06) for grade 2 but was not calculated for grade 3 as no cases were found; and that compared with apremilast was 3.88 (0.62-24.48) for grade 2 and 0.43 (0.02-11.63) for grade 3 neutropenia.CONCLUSIONNo clear increase in the risk of neutropenia with anti-IL-23 antibodies was observed.

01 Dec 2024·Monatshefte für Chemie - Chemical Monthly

The synthesis of indane derivatives and antioxidant effects

Author: Tiras, Canan ; Bilici, Elif Gokcay ; Kus, Nermin Simsek

In this article, the synthesis and antioxidant properties of indane derivatives with high biol. activity were examinedWhile some of the examined indane derivatives were synthesized, some were purchased.Addnl., two new indane derivatives were introduced to the literature.As a result of the study, it was observed that indane derivatives could be used as antioxidants.

100 Deals associated with Aprindine Hydrochloride

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KEGG	Wiki	ATC	Drug Bank
D01326	Aprindine Hydrochloride	C01BB04	DB01429

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Indication	Country/Location	Organization	Date
Tachycardia	Japan	Bayer AG	01 Mar 1987
Arrhythmias, Cardiac	China	Tianjin Pharm Research Inst Pharm Co Ltd.	01 Jan 1981

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