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药品详细

Hydralazine (肼屈嗪 )

化学结构式图
中文名
肼屈嗪
英文名
Hydralazine
分子式
Not Available
化学名
1-hydrazinylphthalazine
分子量
Average: 160.1759
Monoisotopic: 160.074896276
CAS号
86-54-4
ATC分类
C02D 未知;C02D 未知
药物类型
small molecule
阶段
商品名
Apresoline;
同义名
Hydralazine hydrochloride;
基本介绍

A direct-acting vasodilator that is used as an antihypertensive agent. [PubChem]

生产厂家
  • Abraxis pharmaceutical products
  • Actavis totowa llc
  • Akorn inc
  • App pharmaceuticals llc
  • Ascot hosp pharmaceuticals inc div travenol laboratories inc
  • Glenmark pharmaceuticals ltd
  • Halsey drug co inc
  • Heritage pharmaceuticals inc
  • Hetero drugs ltd unit iii
  • Impax laboratories inc
  • Invagen pharmaceuticals inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Luitpold pharmaceuticals inc
  • Mutual pharmaceutical co inc
  • Novartis pharmaceuticals corp
  • Par pharmaceutical inc
  • Pliva inc
  • Purepac pharmaceutical co
  • Quantum pharmics ltd
  • Sandoz inc
  • Smith and nephew solopak div smith and nephew
  • Solopak laboratories inc
  • Superpharm corp
  • Teva parenteral medicines inc
  • Teva pharmaceuticals usa inc
  • Tg united labs llc
  • Usl pharma inc
  • Vangard laboratories inc div midway medical co
  • Vitarine pharmaceuticals inc
  • Watson laboratories inc
  • West ward pharmaceutical corp
  • Zydus pharmaceuticals usa inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Kandler MR, Mah GT, Tejani AM, Stabler SN: Hydralazine for essential hypertension. Cochrane Database Syst Rev. 2010 Aug 4;8:CD004934. Pubmed
剂型
Form Route Strength
Powder, for solution Intravenous
Tablet Oral
规格
Unit description Cost Unit
Hydralazine 20 mg/ml vial 18.0 USD ml
Hydralazine 100 mg tablet 1.65 USD tablet
Hydralazine-HCTZ 50-50 mg capsule 1.2 USD capsule
HydrALAZINE HCl 100 mg tablet 1.05 USD tablet
Hydralazine-HCTZ 25-25 mg capsule 0.81 USD capsule
Hydralazine-HCTZ 100-50 mg capsule 0.75 USD capsule
HydrALAZINE HCl 50 mg tablet 0.67 USD tablet
Apresoline 50 mg tablet 0.65 USD tablet
HydrALAZINE HCl 25 mg tablet 0.53 USD tablet
HydrALAZINE HCl 10 mg tablet 0.47 USD tablet
Hydralazine 50 mg tablet 0.44 USD tablet
Hydralazine 25 mg tablet 0.35 USD tablet
Apo-Hydralazine 50 mg Tablet 0.29 USD tablet
Novo-Hylazin 50 mg Tablet 0.29 USD tablet
Apo-Hydralazine 25 mg Tablet 0.24 USD tablet
Hydralazine 10 mg tablet 0.22 USD tablet
Apo-Hydralazine 10 mg Tablet 0.11 USD tablet
Novo-Hylazin 10 mg Tablet 0.11 USD tablet
化合物类型
Type small molecule
Classes
  • Phthalazines
Substructures
  • Benzene and Derivatives
  • Phthalazines
  • Pyridazines
  • Heterocyclic compounds
  • Aromatic compounds
  • Hydrazine Derivatives
适应症
ANTIHYPERTENSIVES 降血压;
药理
Indication 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.
Pharmacodynamics 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.
Mechanism of action 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.
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.
Volume of distribution Not Available
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
Clearance Not Available
Toxicity Oral LD50 in rats: 173 and 187 mg/kg
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Melting point 172-173 oC
Experimental Properties
Property Value Source
logP 0.7 PhysProp
Predicted Properties
Property Value Source
water solubility 2.61e+00 g/l ALOGPS
logP 0.66 ALOGPS
logP 0.75 ChemAxon Molconvert
logS -1.79 ALOGPS
pKa ChemAxon Molconvert
hydrogen acceptor count 4 ChemAxon Molconvert
hydrogen donor count 2 ChemAxon Molconvert
polar surface area 63.83 ChemAxon Molconvert
rotatable bond count 1 ChemAxon Molconvert
refractivity 50.23 ChemAxon Molconvert
polarizability 16.06 ChemAxon Molconvert
药物相互作用
Drug Interaction
Metoprolol Increased effect of both drugs
Propranolol Increased effect of both drugs
Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
食物相互作用
Not Available

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