Tìm theo
Moexipril
Các tên gọi khác (4 ) :
  • Moexipril
  • Moexiprilum
  • Uniretic
  • Univasc
angiotensin converting enzyme inhibitors
Thuốc Gốc
Small Molecule
CAS: 103775-10-6
ATC: C09AA13
ĐG : Apotex Inc. , http://www.apotex.com
CTHH: C27H34N2O7
PTK: 498.5681
Moexipril is a non-sulfhydryl containing precursor of the active angiotensin-converting enzyme (ACE) inhibitor moexiprilat. It is used to treat high blood pressure (hypertension). It works by relaxing blood vessels, causing them to widen. Lowering high blood pressure helps prevent strokes, heart attacks and kidney problems.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C27H34N2O7
Phân tử khối
498.5681
Monoisotopic mass
498.236601452
InChI
InChI=1S/C27H34N2O7/c1-5-36-27(33)21(12-11-18-9-7-6-8-10-18)28-17(2)25(30)29-16-20-15-24(35-4)23(34-3)14-19(20)13-22(29)26(31)32/h6-10,14-15,17,21-22,28H,5,11-13,16H2,1-4H3,(H,31,32)/t17-,21-,22-/m0/s1
InChI Key
InChIKey=UWWDHYUMIORJTA-HSQYWUDLSA-N
IUPAC Name
(3S)-2-[(2S)-2-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}propanoyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
Traditional IUPAC Name
moexipril
SMILES
CCOC(=O)[C@H](CCC1=CC=CC=C1)N[C@@H](C)C(=O)N1CC2=CC(OC)=C(OC)C=C2C[C@H]1C(O)=O
Độ hòa tan
Soluble (about 10% weight-to-volume) in distilled water at room temperature as HCl salt.
logP
2.7
logS
-4.9
pKa (strongest acidic)
3.46
pKa (Strongest Basic)
5.2
PSA
114.4 Å2
Refractivity
132.88 m3·mol-1
Polarizability
53.55 Å3
Rotatable Bond Count
12
H Bond Acceptor Count
7
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
MDDR-Like Rule
true
Dược Lực Học : Moexipril is a non-sulfhydryl containing precursor of the active angiotensin-converting enzyme (ACE) inhibitor moexiprilat. It is used to treat high blood pressure (hypertension). It works by relaxing blood vessels, causing them to widen. Lowering high blood pressure helps prevent strokes, heart attacks and kidney problems.
Cơ Chế Tác Dụng : Moexipril is a non-sulfhydryl containing precursor of the active angiotensin-converting enzyme (ACE) inhibitor moexiprilat. It is used to treat high blood pressure (hypertension). It works by relaxing blood vessels, causing them to widen. Lowering high blood pressure helps prevent strokes, heart attacks and kidney problems. Moexipril is a prodrug for moexiprilat, which inhibits ACE in humans and animals. The mechanism through which moexiprilat lowers blood pressure is believed to be primarily inhibition of ACE activity. ACE is a peptidyl dipeptidase that catalyzes the conversion of the inactive decapeptide angiotensin I to the vasoconstrictor substance angiotensin II. Angiotensin II is a potent peripheral vasoconstrictor that also stimulates aldosterone secretion by the adrenal cortex and provides negative feedback on renin secretion. ACE is identical to kininase II, an enzyme that degrades bradykinin, an endothelium-dependent vasodilator. Moexiprilat is about 1000 times as potent as moexipril in inhibiting ACE and kininase II. Inhibition of ACE results in decreased angiotensin II formation, leading to decreased vasoconstriction, increased plasma renin activity, and decreased aldosterone secretion. The latter results in diuresis and natriuresis and a small increase in serum potassium concentration (mean increases of about 0.25 mEq/L were seen when moexipril was used alone). Whether increased levels of bradykinin, a potent vasodepressor peptide, play a role in the therapeutic effects of moexipril remains to be elucidated. Although the principal mechanism of moexipril in blood pressure reduction is believed to be through the renin-angiotensin-aldosterone system, ACE inhibitors have some effect on blood pressure even in apparent low-renin hypertension.
Dược Động Học :
▧ Absorption :
Moexipril is incompletely absorbed, with bioavailability as moexiprilat of about 13% compared to intravenous (I.V.) moexipril (both measuring the metabolite moexiprilat), and is markedly affected by food, which reduces Cmax and AUC by about 70% and 40%, respectively, after the ingestion of a low-fat breakfast or by 80% and 50%, respectively, after the ingestion of a high-fat breakfast.
▧ Volume of Distribution :
* 183 L
▧ Protein binding :
Moexiprilat is approxomately 50% protein bound.
▧ Metabolism :
Rapidly converted to moexiprilat, the active metabolite. Conversion to the active metabolite is thought to require carboxyesterases and is likely to occur in organs or tissues, other than the gastrointestinal tract, in which carboxyesterases occur. The liver is thought to be one site of conversion, but not the primary site.
▧ Route of Elimination :
Moexiprilat undergoes renal elimination.
▧ Half Life :
Moexipril elimination half-life is approximately 1 hour. Moexiprilat elimination half-life is 2 to 9 hours.
▧ Clearance :
* 441 mL/min
Độc Tính : Human overdoses of moexipril have not been reported. In case reports of overdoses with other ACE inhibitors, hypotension has been the principal adverse effect noted. Single oral doses of 2 g/kg moexipril were associated with significant lethality in mice. Rats, however, tolerated single oral doses of up to 3 g/kg. Common adverse effects include cough, dizziness, diarrhea, flu syndrome, fatigue, pharyngitis, flushing, rash, and myalgia
Chỉ Định : For the treatment of hypertension.
Tương Tác Thuốc :
  • Amiloride Increased risk of hyperkalemia
  • Azilsartan medoxomil Pharmacodynamic synergism: dual blockade of renin-angiotensin system. Increases risks of hypotension, hyperkalemia, renal impairment.
  • Icatibant Icatibant may attenuate the antihypertensive effect of ACE inhibitors by pharmacodynamic antagonism. Monitor concomitant therapy closely.
  • Lithium The ACE inhibitor increases serum levels of lithium
  • Potassium Increased risk of hyperkalemia
  • Quinupristin This combination presents an increased risk of toxicity
  • Tizanidine Tizanidine increases the risk of hypotension with the ACE inhibitor
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Triamterene Increased risk of hyperkalemia
Liều Lượng & Cách Dùng : Tablet - Oral - 15 mg
Tablet, film coated - Oral - 7.5 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Schwarz
    Sản phẩm biệt dược : Univasc
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00691
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=91270
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508441
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07704
ChemSpider
http://www.chemspider.com/Chemical-Structure.82418.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50084673
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0574-0110-01
PharmGKB
http://www.pharmgkb.org/drug/PA164769059
Wikipedia
http://en.wikipedia.org/wiki/Moexipril
RxList
http://www.rxlist.com/cgi/generic2/moexip.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/uni1468.shtml
Drugs.com
http://www.drugs.com/cdi/moexipril.html
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