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药品详细

Nitrendipine(尼群地平)

化学结构式图
中文名
尼群地平
英文名
Nitrendipine
分子式
C18H20N2O6
化学名
3-ethyl 5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
分子量
Average: 360.3612
Monoisotopic: 360.132136382
CAS号
39562-70-4
ATC分类
C08C 未知
药物类型
small molecule
阶段
approved
商品名
Bayotensin;Baypress;Bylotensin;Deiten;Nidrel;Nitrepin;
同义名
Nitrendipin;Nitrendipino [INN-Spanish];Nitrendipinum [INN-Latin];
基本介绍

A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive. [PubChem]

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference Not Available
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Nitrobenzenes
    Substructures
    • Dihydropyridines
    • Carboxylic Acids and Derivatives
    • Nitrobenzenes
    • Acetates
    • Oxoazaniums
    • Ethers
    • Benzene and Derivatives
    • Nitro compounds
    • Enamines
    • Heterocyclic compounds
    • Aromatic compounds
    • Anilines
    适应症
    ANTIHYPERTENSIVES 降血压;
    药理
    Indication For the treatment of mild to moderate hypertension
    Pharmacodynamics Nitrendipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Nitrendipine is similar to other peripheral vasodilators. Nitrendipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
    Mechanism of action By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, Nitrendipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding > 99%
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Humans and other mammals
    Pathways
    Pathway Name SMPDB ID
    Smp00382 Nitrendipine Pathway SMP00382
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 156-160 °C Not Available
    water solubility Insoluble Not Available
    logP 2.88 MASUMATO,K ET AL. (1995)
    Caco2 permeability -4.77 ADME Research, USCD
    Predicted Properties
    Property Value Source
    water solubility 1.42e-02 g/l ALOGPS
    logP 3.21 ALOGPS
    logP 2.17 ChemAxon
    logS -4.4 ALOGPS
    pKa (strongest basic) 5.43 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 5 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 110.45 ChemAxon
    rotatable bond count 7 ChemAxon
    refractivity 96.91 ChemAxon
    polarizability 36.25 ChemAxon
    药物相互作用
    Drug Interaction
    Cimetidine Cimetidine increases the effect of the calcium channel blocker, nitrendipine.
    Telithromycin Telithromycin may reduce clearance of Nitrendipine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Nitrendipine if Telithromycin is initiated, discontinued or dose changed.
    Thiopental The CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Nitrendipine, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Nitrendipine if Thiopental is initiated, discontinued or dose changed.
    Tipranavir Tipranavir may decrease the metabolism and clearance of the calcium channel blocker, Nitrendipine. Monitor for changes in Nitrendipine therapeutic and adverse effects if Tipranavir is initiated, discontinued or dose changed.
    Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
    Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of nitrendipine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of nitrendipine if voriconazole is initiated, discontinued or dose changed.
    食物相互作用
    Not Available

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