Tìm theo
Guanfacine
Các tên gọi khác (3) :
  • Estulic
  • Guanfacina
  • Guanfacinum
antihypertensive agents, adrenergic alpha 2 receptor agonists
Thuốc Gốc
Small Molecule
CAS: 29110-47-2
ATC: C02AC02
ĐG : Actavis Group , http://www.actavis.com
CTHH: C9H9Cl2N3O
PTK: 246.093
A centrally acting antihypertensive agent. The drug lowers both systolic and diastolic blood pressure by activating the central nervous system alpha-2 adrenoreceptors, which results in reduced sympathetic outflow leading to reduced vascular tone. Its adverse reactions include dry mouth, sedation, and constipation. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C9H9Cl2N3O
Phân tử khối
246.093
Monoisotopic mass
245.012267339
InChI
InChI=1S/C9H9Cl2N3O/c10-6-2-1-3-7(11)5(6)4-8(15)14-9(12)13/h1-3H,4H2,(H4,12,13,14,15)
InChI Key
InChIKey=INJOMKTZOLKMBF-UHFFFAOYSA-N
IUPAC Name
N-carbamimidoyl-2-(2,6-dichlorophenyl)acetamide
Traditional IUPAC Name
guanfacine
SMILES
NC(=N)NC(=O)CC1=C(Cl)C=CC=C1Cl
Độ tan chảy
213-216
Độ hòa tan
1892 mg/L
logP
1.7
logS
-3.2
pKa (strongest acidic)
12.94
pKa (Strongest Basic)
6.65
PSA
78.97 Å2
Refractivity
69.63 m3·mol-1
Polarizability
21.75 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
3
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Guanfacine is a phenylacetyl-guanidine derivative hypotensive and a centrally-acting, alpha(2)-adrenergic receptor agonist used alone or in combination with other drugs for the treatment of hypertension.
Cơ Chế Tác Dụng : A centrally acting antihypertensive agent. The drug lowers both systolic and diastolic blood pressure by activating the central nervous system alpha-2 adrenoreceptors, which results in reduced sympathetic outflow leading to reduced vascular tone. Its adverse reactions include dry mouth, sedation, and constipation. [PubChem] Guanfacine selectively stimulates central alpha(2)-adrenergic receptors, resulting in inhibition of sympathetic vasomotor centers, which contributes predominantly to the hypotensive effects of the drug. Central effects of guanfacine lead to reduced peripheral sympathetic nerve impulses from the vasomotor center to the heart and blood vessels. This results in a decrease in peripheral vascular resistance and a reduction in heart rate. The stimulation of peripheral alpha(2)-adrenergic receptors may also contribute to hypotensive effects.
Dược Động Học :
▧ Absorption :
Rapid and complete, with an oral bioavailability of approximately 80%.
▧ Volume of Distribution :
* 6.3 L/kg
▧ Protein binding :
Approximately 70% bound to plasma proteins, independent of drug concentration.
▧ Metabolism :
Hepatic
▧ Route of Elimination :
In individuals with normal renal function, guanfacine and its metabolites are excreted primarily in the urine.
▧ Half Life :
17 hours (range 10-30 hours)
Độc Tính : Symptoms of overdose include drowsiness, lethargy, bradycardia and hypotension. LD50=165mg/kg (orally in mice)
Chỉ Định : For use alone or in combination with other classes of antihypertensive agents in the management of hypertension. Has also been used for the treatment of attention deficit hyperactivity disorder (ADHD) in pediatric patients.
Tương Tác Thuốc :
  • Etravirine Guanfacine, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to increase guanfacine dosage up to 8mg/day, as tolerated, and to monitor gefitinib therapy.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Trimipramine Trimipramine may reduce the antihypertensive effect of the alpha2-agonist, Guanfacine. Trimipramine may also increase the rebound hypertensive effect of Clonidine. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Clonidine if Trimipramine is initiated, discontinued or dose changed. Guanfacine should be withdrawn very gradually to reduce the risk of hypertensive crisis.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Egis
    Sản phẩm biệt dược : Estulic
  • Công ty : Mylan
    Sản phẩm biệt dược : Guanfacine
  • Công ty : Shire
    Sản phẩm biệt dược : Intuniv
  • Công ty : Promius
    Sản phẩm biệt dược : Tenex
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01018
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3519
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506169
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07037
ChemSpider
http://www.chemspider.com/Chemical-Structure.3399.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/55567-051-18
PharmGKB
http://www.pharmgkb.org/drug/PA449825
Wikipedia
http://en.wikipedia.org/wiki/Guanfacine
RxList
http://www.rxlist.com/cgi/generic3/guanfacine.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/gua1657.shtml
Drugs.com
http://www.drugs.com/cdi/guanfacine.html
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