Tìm theo
Terazosin
Các tên gọi khác (5 ) :
  • 1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-((tetrahydro-2-furanyl)carbonyl)piperazine
  • Terazosin
  • Terazosina
  • Terazosine
  • Terazosinum
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 63590-64-7
ATC: G04CA03
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C19H25N5O4
PTK: 387.4329
Terazosin is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH). It also acts to lower blood pressure, so it is a drug of choice for men with hypertension and prostate enlargement. It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H25N5O4
Phân tử khối
387.4329
Monoisotopic mass
387.190654313
InChI
InChI=1S/C19H25N5O4/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/h10-11,14H,3-9H2,1-2H3,(H2,20,21,22)
InChI Key
InChIKey=VCKUSRYTPJJLNI-UHFFFAOYSA-N
IUPAC Name
6,7-dimethoxy-2-{4-[(oxolan-2-yl)carbonyl]piperazin-1-yl}quinazolin-4-amine
Traditional IUPAC Name
terazosin
SMILES
COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N1CCN(CC1)C(=O)C1CCCO1
Độ tan chảy
273 °C
Độ hòa tan
29.7mg/mL
logP
1
logS
-2.4
pKa (strongest acidic)
19.93
pKa (Strongest Basic)
7.24
PSA
103.04 Å2
Refractivity
105.18 m3·mol-1
Polarizability
41.26 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
8
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Terazosin, classified as a quinazoline, is similar to doxazosin and prazosin. As an α-adrenergic blocking agent, terazosin is used to treat hypertension and BPH. Terazosin produces vasodilation and reduces peripheral resistance but in general has only a slight effect on cardiac output. The antihypertensive effect with chronic dosing is not usually accompanied by reflex tachycardia.
Cơ Chế Tác Dụng : Terazosin is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH). It also acts to lower blood pressure, so it is a drug of choice for men with hypertension and prostate enlargement. It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls. In general, α1-adrenergic receptors mediate contraction and hypertrophic growth of smooth muscle cells. α1-Receptors are 7-transmembrane domain receptors coupled to G proteins, Gq/11. Three α1-receptor subtypes, which share approximately 75% homology in their transmembrane domains, have been identified: α1A (chromosome 8), α1B (chromosome 5), and α1D (chromosome 20). Terazosin is the first α1-receptor antagonist to demonstrate selectivity for the α1A-receptor. All three receptor subtypes appear to be involved in maintaining vascular tone. The α1A-receptor maintains basal vascular tone while the α1B-receptor mediates the vasocontrictory effects of exogenous α1-agonists. Activation of α1-receptors activates Gq-proteins, which results in intracellular stimulation of phospholipases C, A2, and D. This results in mobilization of Ca2+ from intracellular stores, activation of mitogen-activated kinase and PI3 kinase pathways and subsequent vasoconstriction. Terozosin produces its pharmacological effects by inhibiting α1A-receptor activation. Inhibition of these receptors in the vasculature and prostate results in muscle relaxation, decreased blood pressure and improved urinary outflow in symptomatic benign prostatic hyperplasia.
Dược Động Học :
▧ Absorption :
Essentially completely absorbed in man (90% bioavailability).
▧ Protein binding :
90-94%
▧ Metabolism :
Hepatic. One of the four metabolites identified (piperazine derivative of terazosin) has antihypertensive activity.
▧ Route of Elimination :
Approximately 10% of an orally administered dose is excreted as parent drug in the urine and approximately 20% is excreted in the feces.
▧ Half Life :
12 hours
Độc Tính : LD50=259.3mg/kg (IV in mice)
Chỉ Định : For the treatment of symptomatic BPH and mild to moderate hypertension.
Tương Tác Thuốc :
  • Acebutolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Alfuzosin Additive antihypertensive effects may occur. Increase risk of orthostatic hypotension and syncope. Concomitant therapy should be avoided.
  • Amifostine Terazosin may increase the hypotensive effect of Amifostine. At chemotherapeutic doses of Amifostine, Terazosin should be withheld for 24 hours prior to Amifostine administration. Use caution at lower doses of Amifostine.
  • Atenolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Betaxolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Bisoprolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Carteolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Carvedilol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Celiprolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Esmolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Labetalol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Metoprolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Nadolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Nebivolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Oxprenolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Penbutolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Pindolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Propranolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Rituximab Additive antihypertensive effects may occur. Increased risk of hypotension. Consider withholding Terazosin for 12 hours prior to administration of Rituximab.
  • Sildenafil Increased risk of hypotension.
  • Silodosin Additive antihypertensive effects may occur. Increase risk of orthostatic hypotension and syncope. Concomitant therapy should be avoided.
  • Sotalol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Tadalafil Tadalafil may enhance the hypotensive effect of Terazosin. Monitor for hypotension during concomitant therapy.
  • Tamsulosin Concomitant use of alpha1-adrenergic antagonists, Tamsulosin and Terazosin, may result in additive antihypertensive effects. Combination therapy is not recommended.
  • Timolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Vardenafil Additive hypotensive effects of the PDE5 inhibitor, Vardenafil, and alpha1-blocker, Terazosin, may occur. Monitor for hypotension during concomitant therapy.
Liều Lượng & Cách Dùng : Capsule - Oral - 1 mg
Capsule - Oral - 10 mg
Capsule - Oral - 2 mg
Capsule - Oral - 5 mg
Tablet - Oral - 1 mg
Tablet - Oral - 10 mg
Tablet - Oral - 2 mg
Tablet - Oral - 5 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01162
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5401
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509129
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07127
ChemSpider
http://www.chemspider.com/Chemical-Structure.5208.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0904-6126-61
PharmGKB
http://www.pharmgkb.org/drug/PA451612
Wikipedia
http://en.wikipedia.org/wiki/Terazosin
RxList
http://www.rxlist.com/cgi/generic/teraz.htm
Drugs.com
http://www.drugs.com/terazosin.html
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