Tìm theo
Phenoxybenzamine
Các tên gọi khác (9 ) :
  • Dibenzyline
  • Fenossibenzamina
  • Fenoxibenzamina
  • Phenoxybenzamine
  • Phenoxybenzaminum
  • POB
  • SID104171113
  • SID124879342
  • SID124879343
antihypertensive agents, vasodilator agents, adrenergic alpha antagonists
Thuốc Gốc
Small Molecule
CAS: 59-96-1
ATC: C04AX02
ĐG : Gallipot , http://www.gallipot.com
CTHH: C18H22ClNO
PTK: 303.826
An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H22ClNO
Phân tử khối
303.826
Monoisotopic mass
303.138992038
InChI
InChI=1S/C18H22ClNO/c1-16(15-21-18-10-6-3-7-11-18)20(13-12-19)14-17-8-4-2-5-9-17/h2-11,16H,12-15H2,1H3
InChI Key
InChIKey=QZVCTJOXCFMACW-UHFFFAOYSA-N
IUPAC Name
benzyl(2-chloroethyl)(1-phenoxypropan-2-yl)amine
Traditional IUPAC Name
phenoxybenzamine
SMILES
CC(COC1=CC=CC=C1)N(CCCl)CC1=CC=CC=C1
Độ tan chảy
39 °C
Độ hòa tan
1.03e-02 g/l
logP
4.7
logS
-4.5
pKa (Strongest Basic)
7.97
PSA
12.47 Å2
Refractivity
88.92 m3·mol-1
Polarizability
34.09 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Phenoxybenzamine is indicated for the control of episodes of hypertension and sweating that occur with a disease called pheochromocytoma. If tachycardia is excessive, it may be necessary to use a beta-blocking agent concomitantly. Phenoxybenzamine is a long-acting, adrenergic, alpha-receptor blocking agent which can produce and maintain "chemical sympathectomy" by oral administration. It increases blood flow to the skin, mucosa and abdominal viscera, and lowers both supine and erect blood pressures. It has no effect on the parasympathetic system. Phenoxybenzamine works by blocking alpha receptors in certain parts of the body. Alpha receptors are present in the muscle that lines the walls of blood vessels. When the receptors are blocked by Phenoxybenzamine, the muscle relaxes and the blood vessels widen. This widening of the blood vessels results in a lowering of blood pressure.
Cơ Chế Tác Dụng : An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator. [PubChem] Phenoxybenzamine produces its therapeutic actions by blocking alpha receptors, leading to a muscle relaxation and a widening of the blood vessels. This widening of the blood vessels results in a lowering of blood pressure.
Dược Động Học :
▧ Absorption :
Twenty to 30 percent of orally administered phenoxybenzamine appears to be absorbed in the active form.
▧ Half Life :
24 hours
Độc Tính : Symptoms of overdose are largely the result of block of the sympathetic nervous system and of the circulating epinephrine. They may include postural hypotension resulting in dizziness or fainting, tachycardia, particularly postural, vomiting; lethargy, and shock.
Chỉ Định : For the treatment of phaeochromocytoma (malignant), benign prostatic hypertrophy and malignant essential hypertension.
Tương Tác Thuốc :
  • Tadalafil Tadalafil may enhance the hypotensive effect of Phenoxybenzamine. Monitor for hypotension during concomitant therapy.
  • Tamsulosin Concomitant use of alpha1-adrenergic antagonists, Tamsulosin and Phenoxybenzamine, 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, Phenoxybenzamine, may occur. Monitor for hypotension during concomitant therapy.
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00925
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4768
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507191
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07435
ChemSpider
http://www.chemspider.com/Chemical-Structure.4604.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50017679
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/65197-001-01
PharmGKB
http://www.pharmgkb.org/drug/PA450919
Wikipedia
http://en.wikipedia.org/wiki/Phenoxybenzamine
RxList
http://www.rxlist.com/cgi/generic3/phenoxybenz.htm
Drugs.com
http://www.drugs.com/cdi/phenoxybenzamine.html
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