Maria Steffi A, Kumar Aniket, Wilfred Premila M, Shanthi Margaret, Peedicayil Jacob
Department of Pharmacology & Clinical Pharmacology, Christian Medical College, Vellore, India.
Curr Ther Res Clin Exp. 2023 Sep 30;99:100717. doi: 10.1016/j.curtheres.2023.100717. eCollection 2023.
Cilnidipine is a fourth-generation calcium channel blocker that is clinically used to treat hypertension. It is a dihydropyridine that blocks L- and N-type calcium channels. The inhibitory effect of cilnidipine on isolated detrusor muscle contractility has not been studied. This study investigated the inhibitory effect of cilnidipine on isolated caprine (goat) detrusor muscle contractility and the reversal of the inhibition by calcium channel openers.
Fourteen caprine detrusor strips were made to contract using 80 mM potassium chloride before and after addition of three concentrations (20, 40, and 60 µM) of cilnidipine. Two reversal agents, the L-type calcium channel opener FPL64716, and the N-type calcium channel opener GV-58, were investigated for their ability to reverse the inhibitory effect of 40 µΜ cilnidipine on potassium chloride-induced detrusor contractility.
Cilnidipine caused a dose-dependent and statistically significant inhibition of detrusor contractility at all concentrations of cilnidipine used (20, 40, and 60 µΜ). The inhibitory effect of 40 µM cilnidipine on detrusor contractility was significantly reversed by the addition of FPL64716 and GV-58.
Cilnidipine inhibits the contractility of the isolated detrusor by blocking L- and N-type calcium channels. Cilnidipine could be evaluated for treating clinical conditions requiring relaxation of the detrusor such as overactive bladder.
西尼地平是一种第四代钙通道阻滞剂，临床上用于治疗高血压。它是一种二氢吡啶类药物，可阻断L型和N型钙通道。西尼地平对离体逼尿肌收缩力的抑制作用尚未得到研究。本研究调查了西尼地平对离体山羊逼尿肌收缩力的抑制作用以及钙通道开放剂对该抑制作用的逆转情况。
在添加三种浓度（20、40和60μM）的西尼地平之前和之后，使用80mM氯化钾使14条山羊逼尿肌条收缩。研究了两种逆转剂，即L型钙通道开放剂FPL64716和N型钙通道开放剂GV-58，对40μM西尼地平抑制氯化钾诱导的逼尿肌收缩作用的逆转能力。
在所使用的所有西尼地平浓度（20、40和60μM）下，西尼地平均引起逼尿肌收缩力呈剂量依赖性且具有统计学意义的抑制。添加FPL64716和GV-58可显著逆转40μM西尼地平对逼尿肌收缩力的抑制作用。
西尼地平通过阻断L型和N型钙通道抑制离体逼尿肌的收缩力。对于治疗需要逼尿肌松弛的临床病症，如膀胱过度活动症，可对西尼地平进行评估。
