スピラプリル
- 関
- spirapril hydrochloride
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/07/26 18:15:23」(JST)
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Spirapril
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Systematic (IUPAC) name |
(8S)-7-[(2S)-2-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}propanoyl]-1,4-dithia-7-azaspiro[4.4]nonane-8-carboxylic acid
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Clinical data |
AHFS/Drugs.com |
International Drug Names |
Pregnancy
category |
|
Legal status |
|
Routes of
administration |
Oral |
Pharmacokinetic data |
Bioavailability |
50% |
Metabolism |
converted to spiraprilat |
Biological half-life |
30 to 35 hours |
Excretion |
Hepatic and renal |
Identifiers |
CAS Registry Number |
83647-97-6 Y |
ATC code |
C09AA11 |
PubChem |
CID: 5311447 |
IUPHAR/BPS |
6575 |
DrugBank |
DB01348 N |
ChemSpider |
4470933 Y |
UNII |
96U2K78I3V Y |
KEGG |
D08529 Y |
ChEMBL |
CHEMBL431 Y |
Chemical data |
Formula |
C22H30N2O5S2 |
Molecular mass |
466.616 g/mol |
SMILES
-
O=C(OCC)[C@@H](N[C@H](C(=O)N2[C@H](C(=O)O)CC1(SCCS1)C2)C)CCc3ccccc3
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InChI
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InChI=1S/C22H30N2O5S2/c1-3-29-21(28)17(10-9-16-7-5-4-6-8-16)23-15(2)19(25)24-14-22(30-11-12-31-22)13-18(24)20(26)27/h4-8,15,17-18,23H,3,9-14H2,1-2H3,(H,26,27)/t15-,17-,18-/m0/s1 Y
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Key:HRWCVUIFMSZDJS-SZMVWBNQSA-N Y
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N (what is this?) (verify) |
Spirapril hydrochloride (Renormax) is an ACE inhibitor antihypertensive drug used to treat hypertension. It belongs to dicarboxy group of ace inhibitor.
Like many ACE inhibitors, this prodrug is converted to the active metabolite spiraprilat following oral administration. Unlike other members of the group, it is eliminated both by renal and hepatic routes, which may allow for greater use in patients with renal impairment.[1] However, data on its effect upon the renal function are conflicting.[2]
References
- ^ Shohat J, Wittenberg C, Erman A, Rosenfeld J, Boner G (1999). "Acute and chronic effects of spirapril, alone or in combination with isradipine on kidney function and blood pressure in patients with reduced kidney function and hypertension.". Scand J Urol Nephrol 33 (1): 57–62. doi:10.1080/003655999750016294. PMID 10100366.
- ^ Noble S, Sorkin E (1995). "Spirapril. A preliminary review of its pharmacology and therapeutic efficacy in the treatment of hypertension.". Drugs 49 (5): 750–66. doi:10.2165/00003495-199549050-00008. PMID 7601014.
Antihypertensives: agents acting on the renin–angiotensin system (C09)
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ACE inhibitors
("-pril") |
- Sulfhydryl-containing: Captopril
- Zofenopril
- Dicarboxylate-containing: Enalapril#
- Ramipril
- Quinapril (+HCT)
- Perindopril
- Lisinopril (+HCT)
- Benazepril
- Phosphonate-containing: Fosinopril (+HCT)
- Other/ungrouped: Alacepril
- Cilazapril
- Delapril
- Enalapril
- Imidapril
- Moexipril
- Rentiapril
- Spirapril
- Temocapril
- Trandolapril
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AIIRAs/
("-sartan") |
- Azilsartan
- Candesartan
- Eprosartan
- Fimasartan
- Irbesartan
- Losartan (+HCT)
- Olmesartan (+amlodipine)
- Tasosartan§
- Telmisartan (+HCT)
- Valsartan (+HCT, +amlodipine +sacubitril)
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Renin inhibitors/
("-kiren") |
- Aliskiren (+amlodipine, +amlodipine and HCT)
- Remikiren§
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|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
Index of the circulatory system
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|
Description |
- Anatomy
- Arteries
- head and neck
- arms
- chest
- abdomen
- legs
- Veins
- head and neck
- arms
- chest
- abdomen and pelvis
- legs
- Development
- Cells
- Physiology
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|
Disease |
- Congenital
- Neoplasms and cancer
- Lymphatic vessels
- Injury
- Vasculitis
- Other
- Symptoms and signs
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|
Treatment |
- Procedures
- Drugs
- beta blockers
- channel blockers
- diuretics
- nonsympatholytic vasodilatory antihypertensives
- peripheral vasodilators
- renin–angiotensin system
- sympatholytic antihypertensives
- vasoprotectives
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|
|
UpToDate Contents
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English Journal
- Administration-time differences in effects of hypertension medications on ambulatory blood pressure regulation.
- Hermida RC1, Ayala DE, Fernández JR, Mojón A, Smolensky MH, Fabbian F, Portaluppi F.
- Chronobiology international.Chronobiol Int.2013 Mar;30(1-2):280-314. doi: 10.3109/07420528.2012.709448. Epub 2012 Oct 19.
- Specific features of the 24-h blood pressure (BP) pattern are linked to progressive injury of target tissues and risk of cardiovascular disease (CVD) events. Several studies have consistently shown an association between blunted asleep BP decline and risk of fatal and nonfatal CVD events. Thus, ther
- PMID 23077971
- Perfusion calorimetry in the characterization of solvates forming isomorphic desolvates.
- Baronsky J1, Preu M, Traeubel M, Urbanetz NA.
- European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.Eur J Pharm Sci.2011 Sep 18;44(1-2):74-82. doi: 10.1016/j.ejps.2011.06.008. Epub 2011 Jun 25.
- In this study, the potential of perfusion calorimetry in the characterization of solvates forming isomorphic desolvates was investigated. Perfusion calorimetry was used to expose different hydrates forming isomorphic desolvates (emodepside hydrates II-IV, erythromycin A dihydrate and spirapril hydro
- PMID 21726637
- Effect of angiotensin-converting enzyme inhibitor quadropril on dynamic parameters of vascular tone under conditions of NO synthesis blockade in normotensive and spontaneously hypertensive rats.
- Sonin DL1, Galagoudza MM, Syrensky AV, Tsyrlin VA.
- Bulletin of experimental biology and medicine.Bull Exp Biol Med.2011 Jul;151(3):311-3.
- The role of NO in the mechanism of quadropril modulation of the flow-dependent vasodilation was examined in normotensive (Wistar) and spontaneously hypertensive (SHR) rats. The abdominal aorta was cannulated and autoperfused at different volume rates to obtain the pressure-flow curves. In the first
- PMID 22451874
Japanese Journal
- Comparison of spirapril, isradipine, or combination in hypertensive patients with left ventricular hypertrophy. Effects on LVH regression and arrhythmogenic propensity
- Spirapril prevents left ventricular hypertrophy, decreases myocardial damage and promotes angiogenesis in spontaneously hypertensive rats
Related Links
- Shohat J, Wittenberg C, Erman A, Rosenfeld J, Boner G (1999). "Acute and chronic effects of spirapril, alone or in combination with isradipine on kidney function and blood pressure in patients with reduced kidney function and hypertension.".
- 30 Jun 2007 ... Spirapril is an ACE inhibitor antihypertensive drug used to treat hypertension. Like many ACE inhibitors, this is a prodrug which is converted to the active metabolite spiraprilat following oral administration. ACE inhibitors are ...
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