生物活性

• 描述Angiotensin-converting enzyme (ACE) is responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII), which regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS) ^[4]. Imidapril hydrochloride (imidapril) is a long-acting, non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor, which has been used clinically in the treatment of hypertension, chronic congestive heart failure (CHF), acute myocardial infarction (AMI), and diabetic nephropathy ^[5]. After oral administration, imidapril is rapidly converted in the liver to its active metabolite imidaprilat. The plasma levels of imidaprilat gradually increase in proportion to the dose, and decline slowly. The time to reach the maximum plasma concentration (T_max) is 2.0 h for imidapril and 9.3 h for imidaprilat. The elimination half-lives (t_1/2) of imidapril and imidaprilat is 1.7 and 14.8 h, respectively ^[5]. In patients with hypertension, blood pressure was still decreased at 24 h after imidapril administration. The antihypertensive effect of imidapril was dose-dependent ^[5]. The maximal reduction of blood pressure and plasma ACE was achieved with imidapril, 10 mg once daily, and the additional effect was not prominent with higher doses. When administered to patients with AMI, imidapril improved left ventricular ejection fraction and reduced plasma brain natriuretic peptide (BNP) levels ^[5]. In patients with mild-to-moderate CHF [New York Heart Association (NYHA) functional class II–III], imidapril increased exercise time and physical working capacity and decreased plasma atrial natriuretic peptide (ANP) and BNP levels in a dose-related manner. In patients with diabetic nephropathy, imidapril decreased urinary albumin excretion ^[5].

• 动物研究
  剂量	Cat: 0.5 mg/kg - 5 mg/kg[2] (p.o.) Dog: 0.25 mg/kg[2] (p.o.)
  给药途径	p.o.
  动物药代数据	Animal Rats[3] Dose 2.5 mg per rat Administration p.o. s.c. Cmax 1840 ± 280 ng/ml (p.o.) 24.1 ± 1.3 ng/ml (s.c.) ΔSBPmax (Systolic blood pressure) 25.2 ± 1.8% (p.o.) 30.8 ± 3.7% (s.c.) AUC 210.7 ± 23.8 ng·day/ml (p.o.) 447.3 ± 45.5 ng·day/ml (s.c.)

• 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
  NCT01715584	Hypertension	Phase 4	Recruiting	December 31, 2019	Canada, Ontario ... more >> London Health Sciences Centre - Victoria Campus Recruiting London, Ontario, Canada, N6A 5W9 Contact: Craig J Railton, MD, PhD    519 685 8500 ext 58525    Craig.Railton@lhsc.on.ca    Principal Investigator: Craig J Railton, MD, PhD          Sub-Investigator: Jonathan Fairbairn, BSc          Sub-Investigator: George Nicoloau, MD          Sub-Investigator: Robert Gros, PhD          Sub-Investigator: Jason Franklin, MD          Sub-Investigator: John Yoo, MD          Sub-Investigator: Kevin Fung, MD          Sub-Investigator: Anthony Nichols, MD          Sub-Investigator: Danielle McNeil, MD Collapse <<
  NCT00360763	Hypertension	Phase 4	Unknown	-	China, Hubei ... more >> Department of Cardiology, Wuhan Union Hospital Recruiting Wuhan, Hubei, China, 430022 Contact: Yu-Hua Liao, Doctor    00862785726376    yumiaowei@vip.sina.com Collapse <<
  NCT00890279	Kidney, Polycystic, Autosomal ... more >>Dominant Collapse <<	Phase 2	Unknown	November 2012	Japan ... more >> Department of Medicine II, Hokkaido Univserity School of Medicine Recruiting Sapporo, Hokkaido, Japan, 0608638 Contact: Toshio Mochizuki, MD    +81117065915    mtoshi@med.hokudai.ac.jp    Principal Investigator: Toshio Mochizuki, MD          Toranomon Hospital Kajigaya, Kidney center Not yet recruiting Kawasaki, Kanagawa, Japan, 2138587 Contact: Yoshihumi Ubara, MD    +81448775111 ext 6064    ubara@toranomon.gr.jp    Principal Investigator: Yoshihumi Ubara, MD          Department of Medicine II, Nippon Medical School Not yet recruiting Bunkyo-ku, Tokyo, Japan, 1138602 Contact: Yasuhiko Iino, MD    +81338222131    iinoyasuhiko@nms.ac.jp    Principal Investigator: Yasuhiko Iino, MD          Department of Urology, Teikyo University School of Medicine Recruiting Itabashi-ku, Tokyo, Japan, 1738605 Contact: Shigeo Horie, MD    +81339642497    shorie@med.teikyo-u.ac.jp    Contact: Satoru Muto, MD    +81339642497    muto@med.teikyo-u.ac.jp    Principal Investigator: Shigeo Horie, MD          Toranomon Hospital, Kidney center Not yet recruiting Minato-ku, Tokyo, Japan, 1058470 Contact: Kenmei Takaichi, MD    +81335881111 ext 7065    takaichi@toranomon.gr.jp    Principal Investigator: Kenmei Takaichi, MD          Division of Kidney and Hypertension, Department of Internal Medicine, Jikei University School of Medicine Active, not recruiting Minato-ku, Tokyo, Japan, 1058471 Department of Urology, Kyorin University School of Medicine Not yet recruiting Mitaka, Tokyo, Japan, 1818611 Contact: Eiji HIgashihara, MD    81422475511    ehigashi@kyorin-u.ac.jp    Contact: Kikuo Nutahara, MD    81422475511    kinuta@kyorin-u.ac.jp    Principal Investigator: Eiji Higashihara, MD          Sub-Investigator: Kikuo Nutahara, MD          Department of Urology, National Hospital Organaization Chiba-East Hospital Not yet recruiting Chiba, Japan, 2608712 Contact: Koichi Kamura, MD    +81432615171 ext 7607    kamura@cehpnet.com    Principal Investigator: Koichi Kamura, MD          Division of Clinical Nephrology and Rheumatology, Niigata University Graduate School of Medical and Dental Sciences Not yet recruiting Niigata, Japan, 9518510 Contact: Ichiei Narita, MD    +813252272193    naritai@med.niigata-u.ac.jp    Principal Investigator: Ichiei Narita, MD Collapse <<

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• 参考文献

• [1] Hosoya K, Ishimitsu T. Protection of the cardiovascular system by imidapril, a versatile angiotensin-converting enzyme inhibitor. Cardiovasc Drug Rev. 2002 Summer;20(2):93-110.

  [2] Thoulon F, Woehrlé F, et al. Long-term tolerance of imidapril in the cat. J Vet Cardiol. 2003 May;5(1):29-34.

  [3] Yamanaka K, Takehara N, et al. Pharmacokinetic and pharmacodynamic study of imidaprilat, an active metabolite of imidapril, a new angiotensin-converting enzyme inhibitor, in spontaneously hypertensive rats. J Pharm Biomed Anal. 1997 Aug;15(12):1851-9.

  [4] Song JC. Clinical pharmacokinetics and selective pharmacodynamics of new angiotensin converting enzyme inhibitors: an update. Clin Pharmacokinet. 2002;41(3):207-24.

  [5] Hosoya K, Ishimitsu T. Protection of the cardiovascular system by imidapril, a versatile angiotensin-converting enzyme inhibitor. Cardiovasc Drug Rev. 2002 Summer;20(2):93-110.

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