Author: Mizoguchi, Makoto ; Deguchi, Nanoka ; Tanaka, Hikaru ; Hamaguchi, Shogo ; Takahashi, Yuna ; Hiiro, Haruhito ; Hashimoto, Tatsuki ; Kaneko, Mika ; Namekata, Iyuki

The negative inotropic effects of nine Vaughan Williams class I antiarrhythmic drugs were examined in guinea pig ventricular tissue preparations. The drugs decreased the contractile force of papillary muscles with different potencies: the potency order was propafenone > aprindine > cibenzoline > flecainide > ranolazine > disopyramide > pilsicainide > mexiletine > GS-458967. The potency of drugs correlated with the reported IC₅₀ values to block the L-type Ca²⁺ channel rather than the Na⁺ channel. The effects of drugs were roughly the same when examined under a high extracellular K⁺ solution, which inactivates the Na⁺ channel. Furthermore, the attenuation of the extracellular Ca²⁺-induced positive inotropy was strong with propafenone, moderate with cibenzoline, and weak with pilsicainide. These results indicate that the negative inotropic effects of class I antiarrhythmic drugs can be largely explained by their blockade of the L-type Ca²⁺ channel.

01 Aug 2022·Journal of Pharmacological Sciences

Roles of IK,ACh for perpetuating atrial fibrillation: Effects of atrial-selective K+ channel inhibitor AVE0118 and class I drugs on the persistent atrial fibrillation canine model

Article

Author: Kambayashi, Ryuichi ; Takei, Yoshinori ; Sugiyama, Atsushi ; Izumi-Nakaseko, Hiroko ; Goto, Ai ; Matsumoto, Akio ; Kawai, Shinichi

Since information is still limited whether atrial I_K,ACh may become a potential therapeutic target to terminate persistent atrial fibrillation (AF), we assessed it by using the persistent AF canine model with representative I_K,ACh inhibitor AVE0118 and class I drugs. AVE0118 (6 mg/kg, n = 7), disopyramide (3 mg/kg, n = 7) and cibenzoline (3 mg/kg, n = 6) terminated the AF in 3/7, 1/7 and 2/6 animals, respectively, whereas aprindine (3 mg/kg, n = 6) did not suppress it. These findings suggest that I_K,ACh inhibition in addition to open-state I_Na suppression with slow dissociation kinetics can synergistically exert potent antiarrhythmic action against persistent AF.

10 Jun 2021·Cureus

Delayed Ventricular Tachycardia After Prophylactic Doses of Droperidol in Patients With Mild QT Interval Prolongation Due to Preoperative Medication

Author: Shimizu, Ichiro ; Takechi, Kenichi

Prophylactic doses of droperidol are effective in preventing postoperative nausea and vomiting (PONV). However, due to concerns of QT interval prolongation and ventricular arrhythmias, the safety of droperidol for PONV prophylaxis has been debated. A 70-year-old woman was scheduled for total knee arthroplasty. She had a history of aortic valve replacement. Oral aprindine (40 mg/day) was prescribed. Preoperative electrocardiogram showed mild QT interval prolongation (QTc = 475 ms). Anesthesia was induced using propofol, remifentanil, and rocuronium, and maintained using desflurane, remifentanil, and a bolus dose of rocuronium. The surgery was uneventful. At the time of skin closure, droperidol (1.25 mg) was administered intravenously for PONV prophylaxis. Twenty-three minutes after administration of droperidol, a sudden onset of premature cardiac contraction was observed, which progressed directly to ventricular tachycardia and atrioventricular block. Arrhythmia due to droperidol-induced QT interval prolongation was strongly suspected. Intravenous magnesium sulfate (2 g) and atropine (0.5 mg) were administered immediately. The ventricular tachycardia resolved quickly after the magnesium injection. Following the resolution of the arrhythmia, the patient was extubated. The patient experienced ventricular tachycardia after a prophylactic dose of droperidol that resulted from QT interval prolongation due to the preoperative medication. It may be prudent to avoid even low-dose droperidol in the background of already present QT prolongation, especially when multiple putative QT-prolonging drugs are used.

100 Deals associated with Aprindine Hydrochloride

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KEGG	Wiki	ATC	Drug Bank
D01326	Aprindine Hydrochloride	C01BB04	DB01429

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10 top approved records.

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

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