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Hydralazine
Các tên gọi khác (14 ) :
  • (1Z)-1(2H)-Phthalazinone hydrazone
  • (2H)-Phthalazinone hydrazone
  • 1-Hydrazinophthalazine
  • 1-Phthalazinylhydrazine
  • 6-Hydralazine
  • Hidralazina
  • Hydralazin
  • Hydralazinum
  • Hydrallazine
  • Hydrazinophthalazine
  • Hydrazone 1(2H)-phthalazinone
  • Hypophthalin
  • Idralazina
  • Phthalazin-1-ylhydrazine
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 86-54-4
ATC: C02DB02, C02DB01
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C8H8N4
PTK: 160.1759
A direct-acting vasodilator that is used as an antihypertensive agent. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C8H8N4
Phân tử khối
160.1759
Monoisotopic mass
160.074896276
InChI
InChI=1S/C8H8N4/c9-11-8-7-4-2-1-3-6(7)5-10-12-8/h1-5H,9H2,(H,11,12)
InChI Key
InChIKey=RPTUSVTUFVMDQK-UHFFFAOYSA-N
IUPAC Name
1-hydrazinylphthalazine
Traditional IUPAC Name
hydralazine
SMILES
NNC1=NN=CC2=CC=CC=C12
Độ tan chảy
172-173 °C
Độ hòa tan
2.61e+00 g/l
logP
1.00
logS
-1.8
pKa (strongest acidic)
17.69
pKa (Strongest Basic)
6.4
PSA
63.83 Å2
Refractivity
50.23 m3·mol-1
Polarizability
16.06 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : A vasodilator, hydralazine works by relaxing blood vessels (arterioles more than venules) and increasing the supply of blood and oxygen to the heart while reducing its workload. It also functions as an antioxidant. It inhibits membrane-bound enzymes that form reactive oxygen species, such as superoxides. Excessive superoxide counteracts NO-induced vasodilation. It is commonly used in the condition of pregnancy called preeclampsia.
Cơ Chế Tác Dụng : A direct-acting vasodilator that is used as an antihypertensive agent. [PubChem] Although the precise mechanism of action of hydralazine is not fully understood, the major effects are on the cardiovascular system. Hydralazine apparently lowers blood pressure by exerting a peripheral vasodilating effect through a direct relaxation of vascular smooth muscle. It has also been suggested that cyclic 3',5'-adenosine monophosphate (cyclic AMP) mediates, at least partly, the relaxation of arterial smooth muscle by altering cellular calcium metabolism, which interferes with the calcium movements within the vascular smooth muscle that are responsible for initiating or maintaining the contractile state. In hypertensive patients, the hydralazine-induced decrease in blood pressure is accompanied by increased heart rate, cardiac output, and stroke volume, probably because of a reflex response to decreased peripheral resistance. The drug has no direct effect on the heart. Hydralazine may increase pulmonary arterial pressure, as well as coronary, splanchnic, cerebral, and renal blood flow. The preferential dilatation of arterioles, as compared to veins, minimizes postural hypotension and promotes the increase in cardiac output. Hydralazine usually increases renin activity in plasma, presumably as a result of increased secretion of renin by the renal juxtaglomerular cells in response to reflex sympathetic discharge. This increase in renin activity leads to the production of angiotensin II, which then causes stimulation of aldosterone and consequent sodium reabsorption. Tolerance to the antihypertensive effect of the drug develops during prolonged therapy, especially if a diuretic is not administered concurrently. In patients with CHF, hydralazine decreases systemic vascular resistance and increases cardiac output.
Dược Động Học :
▧ Absorption :
Hydralazine is rapidly and extensively absorbed (up to 90%) from the gastrointestinal tract and undergoes extensive first-pass metabolism by genetic polymorphic acetylation. Oral bioavailability of hydralazine is dependent upon acetylator phenotype. Bioavailability is approximately 31% in slow acetylators and 10% in fast acetylators.
▧ Protein binding :
87%
▧ Metabolism :
Hydralazine, when administered orally, undergoes extensive first-pass metabolism by genetic polymorphic acetylation, which is responsible for a threefold range of oral bioavailability. Intravenously administered hydralazine does not undergo first-pass metabolism and, therefore, is not affected by acetylator phenotype. After the drug reaches the systemic circulation, it is combined with endogenous aldehydes and ketones, including pyruvic acid, to form hydrazone metabolites. The active metabolites, hydralazine acetonide hydrazone and hydralazine pyruvate hydrazone, are equipotent with the parent, hydralazine.
▧ Route of Elimination :
Hydralazine undergoes extensive hepatic metabolism; it is excreted mainly in the form of metabolites in the urine.
▧ Half Life :
3 to 7 hours
Độc Tính : Oral LD50 in rats: 173 and 187 mg/kg
Chỉ Định : For the treatment of essential hypertension, alone or as an adjunct. Also for the management of severe hypertension when the drug cannot be given orally or when blood pressure must be lowered immediately, congestive heart failure (in combination with cardiac glycosides and diuretics and/or with isosorbide dinitrate), and hypertension secondary to pre-eclampsia/eclampsia.
Tương Tác Thuốc :
  • Metoprolol Increased effect of both drugs
  • Propranolol Increased effect of both drugs
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Liều Lượng & Cách Dùng : Powder, for solution - Intravenous
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Alphapharm
    Sản phẩm biệt dược : Alphapress
  • Công ty : Novartis
    Sản phẩm biệt dược : Apresoline
  • Công ty : Johnson
    Sản phẩm biệt dược : Aprezin
  • Công ty : Pharmasant
    Sản phẩm biệt dược : Cesoline W
  • Công ty : Pharmasant
    Sản phẩm biệt dược : Cesoline Y
  • Công ty : The Central
    Sản phẩm biệt dược : Diazide
  • Công ty : Biocontrol
    Sản phẩm biệt dược : Hidral
  • Công ty : Sandoz
    Sản phẩm biệt dược : Hydralazine Hydrochloride
  • Công ty : Nisshin Seiyaku
    Sản phẩm biệt dược : Pressfall
  • Công ty : Washington
    Sản phẩm biệt dược : Serpathiazide
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01275
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3637
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507533
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07040
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01302
ChemSpider
http://www.chemspider.com/Chemical-Structure.3511.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0182-0905-89
PharmGKB
http://www.pharmgkb.org/drug/PA449894
Wikipedia
http://en.wikipedia.org/wiki/Hydralazine
RxList
http://www.rxlist.com/cgi/generic/hydralazine.htm
Drugs.com
http://www.drugs.com/cdi/hydralazine.html
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