Tìm theo
Alfuzosin
Các tên gọi khác (6 ) :
  • (±)-N-[3-[(4-amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro-2-furamide
  • Alfuzosin
  • Alfuzosina
  • Alfuzosine
  • Alfuzosinum
  • N-[3-[(4-amino-6,7-dimethoxy-quinazolin-2-yl)- methyl-amino]propyl] tetrahydrofuran- 2-carboxamide
Thuốc hỗ trợ trong điều trị bệnh đường tiết niệu
Thuốc Gốc
Small Molecule
CAS: 81403-80-7
ATC: G04CA01
ĐG : A-S Medication Solutions LLC , http://orders.a-smeds.com
CTHH: C19H27N5O4
PTK: 389.4488
Alfuzosin (INN, provided as the hydrochloride salt) is an alpha-adrenergic blocker used to treat benign prostatic hyperplasia (BPH). It works by relaxing the muscles in the prostate and bladder neck, making it easier to urinate. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H27N5O4
Phân tử khối
389.4488
Monoisotopic mass
389.206304377
InChI
InChI=1S/C19H27N5O4/c1-24(8-5-7-21-18(25)14-6-4-9-28-14)19-22-13-11-16(27-3)15(26-2)10-12(13)17(20)23-19/h10-11,14H,4-9H2,1-3H3,(H,21,25)(H2,20,22,23)
InChI Key
InChIKey=WNMJYKCGWZFFKR-UHFFFAOYSA-N
IUPAC Name
N-{3-[(4-amino-6,7-dimethoxyquinazolin-2-yl)(methyl)amino]propyl}oxolane-2-carboxamide
Traditional IUPAC Name
alfuzosin
SMILES
COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N(C)CCCNC(=O)C1CCCO1
Độ hòa tan
2.82e-01 g/l
logP
1.4
logS
-3.1
pKa (strongest acidic)
14.64
pKa (Strongest Basic)
7.3
PSA
111.83 Å2
Refractivity
107.11 m3·mol-1
Polarizability
42.71 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
8
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Alfuzosin is a quinazoline-derivative alpha-adrenergic blocking agent used to treat hypertension and benign prostatic hyperplasia. Accordingly, alfuzosin is a selective inhibitor of the alpha(1) subtype of alpha adrenergic receptors. In the human prostate, alfuzosin antagonizes phenylephrine (alpha(1) agonist)-induced contractions, in vitro, and binds with high affinity to the alpha1a adrenoceptor, which is thought to be the predominant functional type in the prostate. Studies in normal human subjects have shown that alfuzosin competitively antagonized the pressor effects of phenylephrine (an alpha(1) agonist) and the systolic pressor effect of norepinephrine. The antihypertensive effect of alfuzosin results from a decrease in systemic vascular resistance and the parent compound alfuzosin is primarily responsible for the antihypertensive activity.
Cơ Chế Tác Dụng : Alfuzosin (INN, provided as the hydrochloride salt) is an alpha-adrenergic blocker used to treat benign prostatic hyperplasia (BPH). It works by relaxing the muscles in the prostate and bladder neck, making it easier to urinate. [Wikipedia] Alfuzosin is a non-subtype specific alpha(1)-adrenergic blocking agent that exhibits selectivity for alpha(1)-adrenergic receptors in the lower urinary tract. Inhibition of these adrenoreceptors leads to the relaxation of smooth muscle in the bladder neck and prostate, resulting in the improvement in urine flow and a reduction in symptoms in benign prostate hyperplasia. Alfuzosin also inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation.
Dược Động Học :
▧ Absorption :
Absorption is 50% lower under fasting conditions
▧ Volume of Distribution :
* 3.2 L/kg [healthy male middle-aged volunteers]
▧ Protein binding :
82%-90%
▧ Metabolism :
Hepatic. Alfuzosin undergoes extensive metabolism by the liver, with only 11% of the administered dose excreted unchanged in the urine. Alfuzosin is metabolized by three metabolic pathways: oxidation, O-demethylations, and N-dealkylation. The metabolites are not pharmacologically active. CYP3A4 is the principal hepatic enzyme isoform involved in its metabolism.
▧ Route of Elimination :
Following oral administration of 14C-labeled alfuzosin solution, the recovery of radioactivity after 7 days (expressed as a percentage of the administered dose) was 69% in feces and 24% in urine.
▧ Half Life :
10 hours
Độc Tính : Side effects are dizziness (due to postural hypotension), upper respiratory tract infection, headache, and fatigue.
Chỉ Định : For the reduction of urinary obstruction and relief of associated manifestations (eg. sensation of incomplete bladder emptying or straining, urgency, interrupted or weak stream) in patients with symptomatic beningn prostatic hyperplasia.
Tương Tác Thuốc :
  • Aliskiren Monitor therapy due to enhanced hypotensive effect of aliskiren.
  • Boceprevir Boceprevir increases levels by affecting CYP3A4 metabolism. Concomitant therapy is contraindicated.
  • Conivaptan CYP3A4 Inhibitors (Strong) may increase the serum concentration of Alfuzosin. Concomitant use of alfuzosin with a strong CYP3A4 inhibitor is a listed contraindication according to alfuzosin prescribing information.
  • Itraconazole The antifungal increases the effect of alfuzosin
  • Ketoconazole The antifungal increases the effect of alfuzosin
  • Ritonavir Ritonavir increases the effect/toxicity of alfuzosin
  • Tadalafil Tadalafil may enhance the hypotensive effect of Alfusozin. Monitor for hypotension during concomitant therapy.
  • Tamsulosin Concomitant use of alpha1-adrenergic antagonists, Tamsulosin and Alfuzosin, may result in additive antihypertensive effects. Combination therapy is not recommended.
  • Telaprevir Telaprevir increases levels by affecting CYP3A4 metabolism. Concomitant therapy is contraindicated.
  • Telithromycin Telithromycin may reduce clearance of Alfuzosin. Consider alternate therapy.
  • Terazosin Additive antihypertensive effects may occur. Increase risk of orthostatic hypotension and syncope. Concomitant therapy should be avoided.
  • Vardenafil Additive hypotensive effects of the PDE5 inhibitor, Vardenafil, and alpha1-blocker, Alfuzosin, may occur. Monitor for hypotension during concomitant therapy.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of alfuzosin by decreasing its metabolism. Use of alfuzosin with strong CYP3A4 inhibitors is contraindicated by the manufacturer.
Liều Lượng & Cách Dùng : Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
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  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Uroxatral
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Xantral
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Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00346
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2092
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508512
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01692
ChemSpider
http://www.chemspider.com/Chemical-Structure.2008.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0024-4200-30
PharmGKB
http://www.pharmgkb.org/drug/PA164774795
Wikipedia
http://en.wikipedia.org/wiki/Alfuzosin
RxList
http://www.rxlist.com/cgi/generic/uroxatral.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/uro1685.shtml
Drugs.com
http://www.drugs.com/cdi/alfuzosin.html
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