生物活性

• 描述Diltiazem hydrochloride, a benzothiazepine derivative, is antagonist of the calcium ion. Diltiazem caused a dose-dependent inhibiton of contractions as well as Ca++ influx stimulated by alpha adrenoceptor activation and high-K+ depolarization. There was a close relationship between diltiazem inhibition of Ca++ influx and inhibition of contraction when either 40 mM K+ or 10(-8) M NE (norepinephrine) was applied, but not when 10(-6) M NE was used. Also, diltiazem produced a noncompetitive inhibition of Ca++-induced contractions of depolarized rabbit aorta^[3]. In conscious and anesthetized normotensive rats, intravenous administration of diltiazem (0.1 - 3 mg/kg) produced a dose-related decrease in blood pressure. Similarly, in conscious spontaneously hypertensive rats (SHR), diltiazem dose-dependently decreased the blood pressure and increased the heart rate after intravenous administration (0.03 - 1 mg/kg). Oral administration of diltiazem (100 mg/kg) also reduced the blood pressure of SHR. In addition, the progressive increase in blood pressure in young SHR was significantly suppressed by chronic oral administration of diltiazem (30 mg/kg)^[4]. Diltiazem hydrochloride has beneficial effects on I/R (ischemia-reperfusion injury) injury, but this effect is weaker than cilostazol^[5]. Diltiazem hydrochloride-loaded microsponges dispersed in rectal gels may be useful to overcome some limitations of conventional local chronic anal fissure therapy^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02203630	Septic Shock ... more >>Sepsis Shock Tachycardia Arrhythmia Collapse <<	Phase 4	Terminated(Slow enrollment; La... more >>ck of support and equipoise) Collapse <<	-	United States, Tennessee ... more >> Vanderbilt University Medical Center Nashville, Tennessee, United States, 37232 Collapse <<
  NCT02203630	-	-	Terminated(Slow enrollment; La... more >>ck of support and equipoise) Collapse <<	-	-
  NCT00000620	Atherosclerosis ... more >> Cardiovascular Diseases Hypercholesterolemia Hypertension Diabetes Mellitus, Type 2 Diabetes Mellitus Coronary Disease Collapse <<	Phase 3	Completed	-	United States, Minnesota ... more >> Minneapolis Medical Research Foundation Minneapolis, Minnesota, United States, 55404 United States, New York Columbia University New York, New York, United States, 10027 United States, North Carolina Wake Forest University Winston-Salem, North Carolina, United States, 27106 United States, Ohio Case Western Reserve University Cleveland, Ohio, United States, 44106 United States, Tennessee Veterans Affairs Memphis, Tennessee, United States, 38104 United States, Washington University of Washington Seattle, Washington, United States, 98195 Canada, Ontario McMaster University Hamilton, Ontario, Canada Collapse <<

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• 参考文献

• [1] Freitas F, Estato V, et al. Cardiac microvascular rarefaction in hyperthyroid rats is reversed by losartan, diltiazem, and propranolol. Fundam Clin Pharmacol. 2015 Feb;29(1):31-40.

  [2] Kraus RL, Hering S, et al. Molecular mechanism of diltiazem interaction with L-type Ca2+ channels. J Biol Chem. 1998 Oct 16;273(42):27205-12.

  [3] van Breemen C, Hwang O, Meisheri KD. The mechanism of inhibitory action of diltiazem on vascular smooth muscle contractility. J Pharmacol Exp Ther. 1981; 218(2):459‐463

  [4] Sato M, Murata S, Narita H, Tomita M, Yamashita K, Yamaguchi I. Nihon Yakurigaku Zasshi. 1979;75(2):99‐106

  [5] Inan B, Sönmez Ergün S, Nurten A, et al. Effects of Cilostazol and Diltiazem Hydrochloride on Ischemia-Reperfusion Injury in a Rat Hindlimb Model. Heart Surg Forum. 2017;20(2):E058‐E065. Published 2017 Apr 29

  [6] Ivanova NA, Trapani A, Franco CD, et al. In vitro and ex vivo studies on diltiazem hydrochloride-loaded microsponges in rectal gels for chronic anal fissures treatment. Int J Pharm. 2019; 557:53‐65

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