Tìm theo
Spirapril
Các tên gọi khác (2) :
  • Renormax
  • Spirapril
Thuốc Gốc
Small Molecule
CAS: 83647-97-6
ATC: C09AA11
CTHH: C22H30N2O5S2
PTK: 466.614
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 used primarily in treatment of hypertension and congestive heart failure.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H30N2O5S2
Phân tử khối
466.614
Monoisotopic mass
466.15961346
InChI
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
InChI Key
InChIKey=HRWCVUIFMSZDJS-SZMVWBNQSA-N
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
Traditional IUPAC Name
spirapril
SMILES
CCOC(=O)[C@H](CCC1=CC=CC=C1)N[C@@H](C)C(=O)N1CC2(C[C@H]1C(O)=O)SCCS2
Độ hòa tan
2.93e-02 g/l
logP
1.6
logS
-4.2
pKa (strongest acidic)
3.62
pKa (Strongest Basic)
5.2
PSA
95.94 Å2
Refractivity
121.94 m3·mol-1
Polarizability
48.74 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Spirapril is an angiotensin-converting enzyme (ACE) inhibitor. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. By blocking ACE, spirapril decreases angiotensin II which is a vasoconstrictor and inducer of aldosterone. So by inhibiting the enzymes, aldosterone secreation is decreased (so less sodium is reabsorbed) and there is a decrease in vasoconstriction. Combined, this leades to a decrease in blood pressure.
Cơ Chế Tác Dụng : 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 used primarily in treatment of hypertension and congestive heart failure. Spiraprilat, the active metabolite of spirapril, competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. Inhibition of ACE results in decreased plasma angiotensin II. As angiotensin II is a vasoconstrictor and a negative-feedback mediator for renin activity, lower concentrations result in a decrease in blood pressure and stimulation of baroreceptor reflex mechanisms, which leads to decreased vasopressor activity and to decreased aldosterone secretion. Spiraprilat may also act on kininase II, an enzyme identical to ACE that degrades the vasodilator bradykinin.
Dược Động Học :
▧ Absorption :
Bioavailability is 50% following oral administration.
▧ Metabolism :
Hepatic. Converted to spiraprilat following oral administration.
▧ Half Life :
30 to 35 hours
Chỉ Định : Spirapril is an ACE inhibitor class drug used to treat hypertension.
Tương Tác Thuốc :
  • Amiloride Increased risk of hyperkalemia
  • Lithium The ACE inhibitor increases serum levels of lithium
  • Potassium Increased risk of hyperkalemia
  • Tizanidine Tizanidine increases the risk of hypotension with the ACE inhibitor
  • Triamterene Increased risk of hyperkalemia
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Renormax
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01348
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5311447
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506126
ChemSpider
http://www.chemspider.com/Chemical-Structure.4470933.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50017124
PharmGKB
http://www.pharmgkb.org/drug/PA164776913
Wikipedia
http://en.wikipedia.org/wiki/Spirapril
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