Tìm theo
Prazosin
Các tên gọi khác (5 ) :
  • 1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-furanylcarbonyl)piperazine
  • 2-(4-(2-Furoyl)piperazin-1-yl)-4-amino-6,7-dimethoxyquinazoline
  • Prazosina
  • Prazosine
  • Prazosinum
antihypertensive agents, adrenergic alpha 1 receptor antagonists, adrenergic alpha antagonists
Thuốc Gốc
Small Molecule
CAS: 19216-56-9
ATC: C02CA01
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C19H21N5O4
PTK: 383.4011
Prazosin is a selective α-1-adrenergic receptor antagonist used to treat hypertension. It has also been used to decrease urinary obstruction and relieve symptoms associated with symptomatic benign prostatic hyperplasia. 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. Prazosin has also been used in conjunction with cardiac glycosides and diuretics in the management of severe congestive heart failure. It has also been used alone or in combination with β-blockers in the preoperative management of signs and symptoms of pheochromocytoma.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H21N5O4
Phân tử khối
383.4011
Monoisotopic mass
383.159354185
InChI
InChI=1S/C19H21N5O4/c1-26-15-10-12-13(11-16(15)27-2)21-19(22-17(12)20)24-7-5-23(6-8-24)18(25)14-4-3-9-28-14/h3-4,9-11H,5-8H2,1-2H3,(H2,20,21,22)
InChI Key
InChIKey=IENZQIKPVFGBNW-UHFFFAOYSA-N
IUPAC Name
2-{4-[(furan-2-yl)carbonyl]piperazin-1-yl}-6,7-dimethoxyquinazolin-4-amine
Traditional IUPAC Name
prazosin
SMILES
COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N1CCN(CC1)C(=O)C1=CC=CO1
Độ tan chảy
279 °C
Độ hòa tan
0.5 mg/mL (HCl salt)
logP
1.3
logS
-2.7
pKa (Strongest Basic)
7.24
PSA
106.95 Å2
Refractivity
104.5 m3·mol-1
Polarizability
40.49 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
7
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-4.36
Dược Lực Học : Prazosin is an alpha-adrenergic blocking agent used to treat hypertension and benign prostatic hyperplasia. Accordingly, Prazosin is a selective inhibitor of the alpha1 subtype of alpha adrenergic receptors. In the human prostate, Prazosin 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 Prazosin competitively antagonized the pressor effects of phenylephrine (an alpha1 agonist) and the systolic pressor effect of norepinephrine. The antihypertensive effect of Prazosin results from a decrease in systemic vascular resistance and the parent compound Prazosin is primarily responsible for the antihypertensive activity.
Cơ Chế Tác Dụng : Prazosin is a selective α-1-adrenergic receptor antagonist used to treat hypertension. It has also been used to decrease urinary obstruction and relieve symptoms associated with symptomatic benign prostatic hyperplasia. 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. Prazosin has also been used in conjunction with cardiac glycosides and diuretics in the management of severe congestive heart failure. It has also been used alone or in combination with β-blockers in the preoperative management of signs and symptoms of pheochromocytoma. Prazosin 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 :
Well-absorbed from gastrointestinal tract; bioavailability is variable (50 to 85%).
▧ Protein binding :
97%
▧ Metabolism :
Primarily hepatic. Several metabolites have been identified in humans and animals (6- O -demethyl, 7- O -demethyl, 2-[1-piperazinyl]-4-amino-6, 7-dimethoxyquinazoline, 2,4-diamino-6,7-dimethoxyquinazoline).
▧ Route of Elimination :
Animal studies indicate that prazosin hydrochloride is extensively metabolized, primarily by demethylation and conjugation, and excreted mainly via bile and feces. Less extensive human studies suggest similar metabolism and excretion in man.
▧ Half Life :
2-3 hours
Chỉ Định : For treatment of hypertension, symptomatic benign prostatic hyperplasia, and severe congestive heart failure. May also be used alone or in combination with β-blockers in the preoperative management of signs and symptoms of pheochromocytoma.
Tương Tác Thuốc :
  • Acebutolol Risk of hypotension at the beginning of therapy
  • Atenolol Risk of hypotension at the beginning of therapy
  • Betaxolol Beta-Blockers such as betaxolol may enhance the orthostatic hypotensive effect of Alpha1-Blockers such as prazosin. The risk associated with ophthalmic products is probably less than systemic products. Exercise caution if an alpha1-blocker is added to existing beta-blocker therapy. Monitor for hypotension during first few days of concomitant therapy. A priori reduction in alpha1-blocker (especially systemic) dose may be warranted. Administering the first dose of systemic agents at bedtime may help minimize risk of severe hypotension. The risk associated with the use of ophthalmic products in either interacting group is probably less than that associated with systemic agents. If the alpha1-blocker is being used to treat BPH, consider using tamsulosin since its alpha1-A selectivity is least likely to cause hypotension.
  • Bevantolol Risk of hypotension at the beginning of therapy
  • Bisoprolol Risk of hypotension at the beginning of therapy
  • Carteolol Risk of hypotension at the beginning of therapy
  • Carvedilol Risk of hypotension at the beginning of therapy
  • Dabigatran etexilate P-Glycoprotein inducers such as prazosin may decrease the serum concentration of dabigatran etexilate. This combination should be avoided.
  • Digoxin Prazosin increases the effect of digoxin
  • Esmolol Risk of hypotension at the beginning of therapy
  • Labetalol Risk of hypotension at the beginning of therapy
  • Metoprolol Risk of hypotension at the beginning of therapy
  • Nadolol Risk of hypotension at the beginning of therapy
  • Oxprenolol Risk of hypotension at the beginning of therapy
  • Penbutolol Risk of hypotension at the beginning of therapy
  • Pindolol Risk of hypotension at the beginning of therapy
  • Practolol Risk of hypotension at the beginning of therapy
  • Propranolol Risk of hypotension at the beginning of therapy
  • Sotalol Risk of hypotension at the beginning of therapy
  • Tadalafil Tadalafil may enhance the hypotensive effect of Prazosin. Monitor for hypotension during concomitant therapy.
  • Tamsulosin Concomitant use of alpha1-adrenergic antagonists, Tamsulosin and Prazosin, may result in additive antihypertensive effects. Combination therapy is not recommended.
  • Timolol Risk of hypotension at the beginning of therapy
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Vardenafil Additive hypotensive effects of the PDE5 inhibitor, Vardenafil, and alpha1-blocker, Prazosin, may occur. Monitor for hypotension during concomitant therapy.
  • Verapamil Risk of hypotension at the beginning of therapy
Liều Lượng & Cách Dùng : Capsule - Oral - 1 mg
Capsule - Oral - 2 mg
Capsule - Oral - 5 mg
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Minipress 2 mg capsule
    Giá bán buôn : USD >1.14
    Đơn vị tính : capsule
  • Biệt dược thương mại : Minipress 5 mg capsule
    Giá bán buôn : USD >1.97
    Đơn vị tính : capsule
  • Biệt dược thương mại : Vasoflex tablet
    Giá bán buôn : USD >0.15
    Đơn vị tính : tablet
  • Biệt dược thương mại : Apo-Prazo 1 mg Tablet
    Giá bán buôn : USD >0.22
    Đơn vị tính : tablet
  • Biệt dược thương mại : Novo-Prazin 1 mg Tablet
    Giá bán buôn : USD >0.22
    Đơn vị tính : tablet
  • Biệt dược thương mại : Nu-Prazo 1 mg Tablet
    Giá bán buôn : USD >0.22
    Đơn vị tính : tablet
  • Biệt dược thương mại : Vasoflex forte capsule
    Giá bán buôn : USD >0.29
    Đơn vị tính : capsule
  • Biệt dược thương mại : Apo-Prazo 2 mg Tablet
    Giá bán buôn : USD >0.29
    Đơn vị tính : tablet
  • Biệt dược thương mại : Novo-Prazin 2 mg Tablet
    Giá bán buôn : USD >0.29
    Đơn vị tính : tablet
  • Biệt dược thương mại : Nu-Prazo 2 mg Tablet
    Giá bán buôn : USD >0.29
    Đơn vị tính : tablet
  • Biệt dược thương mại : Vasoflex hd caplet
    Giá bán buôn : USD >0.38
    Đơn vị tính : caplet
  • Biệt dược thương mại : Prazosin 1 mg capsule
    Giá bán buôn : USD >0.4
    Đơn vị tính : capsule
  • Biệt dược thương mại : Apo-Prazo 5 mg Tablet
    Giá bán buôn : USD >0.4
    Đơn vị tính : tablet
  • Biệt dược thương mại : Novo-Prazin 5 mg Tablet
    Giá bán buôn : USD >0.4
    Đơn vị tính : tablet
  • Biệt dược thương mại : Nu-Prazo 5 mg Tablet
    Giá bán buôn : USD >0.4
    Đơn vị tính : tablet
  • Biệt dược thương mại : Prazosin HCl 1 mg capsule
    Giá bán buôn : USD >0.41
    Đơn vị tính : capsule
  • Biệt dược thương mại : Prazosin 2 mg capsule
    Giá bán buôn : USD >0.55
    Đơn vị tính : capsule
  • Biệt dược thương mại : Prazosin HCl 2 mg capsule
    Giá bán buôn : USD >0.57
    Đơn vị tính : capsule
  • Biệt dược thương mại : Minipress 1 mg capsule
    Giá bán buôn : USD >0.83
    Đơn vị tính : capsule
  • Biệt dược thương mại : Prazosin 5 mg capsule
    Giá bán buôn : USD >0.94
    Đơn vị tính : capsule
  • Biệt dược thương mại : Prazosin HCl 5 mg capsule
    Giá bán buôn : USD >0.98
    Đơn vị tính : capsule
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Hypovase
  • Công ty : Pfizer
    Sản phẩm biệt dược : Minipress
  • Công ty : Pfizer
    Sản phẩm biệt dược : Minipress Xl
  • Công ty :
    Sản phẩm biệt dược : Pressin
  • Công ty :
    Sản phẩm biệt dược : Vasoflex
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00457
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4893
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508594
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07368
ChemSpider
http://www.chemspider.com/Chemical-Structure.4724.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=29568
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0069-4310-71
PharmGKB
http://www.pharmgkb.org/drug/PA451093
Wikipedia
http://en.wikipedia.org/wiki/Prazosin
RxList
http://www.rxlist.com/cgi/generic3/prazosin.htm
Drugs.com
http://www.drugs.com/cdi/prazosin.html
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