Tìm theo
Doxazosin
Các tên gọi khác (8 ) :
  • 1-(4-Amino-6,7-dimethoxy-2-chinazolinyl)-4-(2,3-dihydro-1,4-benzodioxixin-2-ylcarbonyl)piperazin
  • 1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-(1,4-benzodioxan-2-ylcarbonyl)piperazin
  • Doxazosin
  • Doxazosin mesilate
  • Doxazosin mesylate
  • Doxazosina
  • Doxazosine
  • Doxazosinum
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 74191-85-8
ATC: C02CA04
ĐG : Actavis Group , http://www.actavis.com
CTHH: C23H25N5O5
PTK: 451.4751
Doxazosin is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors. It may be used to mild to moderate hypertension and in the management of symptomatic benign prostatic hyperplasia (BPH). α1-Receptors mediate contraction and hypertrophic growth of smooth muscle cells. Antagonism of these receptors leads to smooth muscle relaxation in the peripheral vasculature and prostate gland.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C23H25N5O5
Phân tử khối
451.4751
Monoisotopic mass
451.185568935
InChI
InChI=1S/C23H25N5O5/c1-30-18-11-14-15(12-19(18)31-2)25-23(26-21(14)24)28-9-7-27(8-10-28)22(29)20-13-32-16-5-3-4-6-17(16)33-20/h3-6,11-12,20H,7-10,13H2,1-2H3,(H2,24,25,26)
InChI Key
InChIKey=RUZYUOTYCVRMRZ-UHFFFAOYSA-N
IUPAC Name
2-{4-[(2,3-dihydro-1,4-benzodioxin-2-yl)carbonyl]piperazin-1-yl}-6,7-dimethoxyquinazolin-4-amine
Traditional IUPAC Name
doxazosin
SMILES
COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N1CCN(CC1)C(=O)C1COC2=CC=CC=C2O1
Độ tan chảy
289-290 °C
Độ hòa tan
24 mg/L
logP
2.1
logS
-2.8
pKa (strongest acidic)
12.67
pKa (Strongest Basic)
7.24
PSA
112.27 Å2
Refractivity
121.64 m3·mol-1
Polarizability
46.63 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
9
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Doxazosin is an alpha-adrenergic blocking agent used to treat hypertension and benign prostatic hyperplasia. Accordingly, Doxazosin is a selective inhibitor of the alpha1 subtype of alpha adrenergic receptors. In the human prostate, Doxazosin antagonizes phenylephrine (alpha1 agonist)-induced contractions, in vitro, and binds with high affinity to the alpha1c adrenoceptor, which is thought to be the predominant functional type in the prostate. Studies in normal human subjects have shown that Doxazosin competitively antagonized the pressor effects of phenylephrine (an alpha1 agonist) and the systolic pressor effect of norepinephrine. The antihypertensive effect of Doxazosin results from a decrease in systemic vascular resistance and the parent compound Doxazosin is primarily responsible for the antihypertensive activity.
Cơ Chế Tác Dụng : Doxazosin is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors. It may be used to mild to moderate hypertension and in the management of symptomatic benign prostatic hyperplasia (BPH). α1-Receptors mediate contraction and hypertrophic growth of smooth muscle cells. Antagonism of these receptors leads to smooth muscle relaxation in the peripheral vasculature and prostate gland. Doxazosin acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation.
Dược Động Học :
▧ Absorption :
65%
▧ Protein binding :
98%
▧ Metabolism :
Hepatic.
▧ Route of Elimination :
On average only 4.8% of the dose was excreted as unchanged drug in the feces and only a trace of the total radioactivity in the urine was attributed to unchanged drug.
▧ Half Life :
22 hours
Độc Tính : Symptoms of overdose include hypotension. Oral LD50 is greater than 1000 mg/kg in mice and rats.
Chỉ Định : For treatment and management of mild to moderate hypertension and urinary obstruction symptoms caused by BPH.
Tương Tác Thuốc :
  • Tadalafil Tadalafil may enhance the hypotensive effect of Doxazosin. Monitor for hypotension during concomitant therapy.
  • Tamsulosin Concomitant use of alpha1-adrenergic antagonists, Tamsulosin and Doxazosin, may result in additive antihypertensive effects. Combination therapy is not recommended.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Vardenafil Additive hypotensive effects of the PDE5 inhibitor, Vardenafil, and alpha1-blocker, Doxazosin, may occur. Monitor for hypotension during concomitant therapy.
Liều Lượng & Cách Dùng : Tablet - Oral - 1 mg
Tablet - Oral - 2 mg
Tablet - Oral - 4 mg
Tablet - Oral - 8 mg
Tablet, extended release - Oral - 4 mg
Tablet, extended release - Oral - 8 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00590
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3157
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506825
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06970
ChemSpider
http://www.chemspider.com/Chemical-Structure.3045.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-4021-01
PharmGKB
http://www.pharmgkb.org/drug/PA449407
Wikipedia
http://en.wikipedia.org/wiki/Doxazosin
RxList
http://www.rxlist.com/cgi/generic/doxazo.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/car1069.shtml
Drugs.com
http://www.drugs.com/doxazosin.html
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