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药品详细

Sitaxentan(Sitaxentan)

化学结构式图
中文名
Sitaxentan
英文名
Sitaxentan
分子式
C18H15ClN2O6S2
化学名
N-(4-chloro-3-methyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-2H-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide
分子量
Average: 454.905
Monoisotopic: 454.006005309
CAS号
210421-64-0
ATC分类
C02K Other Antihypertensives
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
Not Available
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 Not Available
    Substructures Not Available
    适应症
    药理
    Indication Investigated for use/treatment in pulmonary hypertension, connective tissue diseases, hypertension, and congestive heart failure.
    Pharmacodynamics Sitaxentan belongs to a class of drugs known as endothelin receptor antagonists (ERAs). Patients with PAH have elevated levels of endothelin, a potent blood vessel constrictor, in their plasma and lung tissue. Sitaxentan blocks the binding of endothelin to its receptors, thereby negating endothelin's deleterious effects.
    Mechanism of action Sitaxentan is a competitive antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors. Under normal conditions, endothelin-1 binding of ET-A or ET-B receptors causes pulmonary vasoconstriction. By blocking this interaction, Sitaxentan decreases pulmonary vascular resistance. Sitaxentan has a higher affinity for ET-A than ET-B.
    Absorption 70-100%
    Volume of distribution Not Available
    Protein binding 99% +
    Metabolism
    Hepatic (CYP2C9- and CYP3A4-mediated)
    Route of elimination Renal (50 to 60%) Fecal (40 to 50%)
    Half life 10 hours
    Clearance Not Available
    Toxicity Not Available
    Affected organisms Not Available
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties Not Available
    Predicted Properties
    Property Value Source
    water solubility 1.81e-02 g/l ALOGPS
    logP 3.35 ALOGPS
    logP 3.09 ChemAxon
    logS -4.4 ALOGPS
    pKa (strongest acidic) 6.89 ChemAxon
    pKa (strongest basic) 0.75 ChemAxon
    physiological charge -1 ChemAxon
    hydrogen acceptor count 6 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 107.73 ChemAxon
    rotatable bond count 5 ChemAxon
    refractivity 105.8 ChemAxon
    polarizability 43.12 ChemAxon
    药物相互作用
    Drug Interaction
    Carisoprodol Strong CYP2C19 inhibitors such as sitaxentan may decrease the metabolism of CYP2C19 substrates such as carisoprodol. Consider an alternative for one of the interacting drugs in order to avoid toxicity of the substrate. Some combinations are specifically contraindicated by manufacturers. Suggested dosage adjustments are also offered by some manufacturers. Please review applicable package inserts. Monitor for increased effects of the CYP substrate if a CYP inhibitor is initiated/dose increased, and decreased effects if a CYP inhibitor is discontinued/dose decreased.
    Tamoxifen Sitaxsentan may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Sitaxsentan is initiated, discontinued or dose changed.
    Tamsulosin Sitaxsentan, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Sitaxsentan is initiated, discontinued, or dose changed.
    Tofacitinib Sitaxentan (moderate CYP3A4 inhibitors, strong CYP2C19 inhbitors), when used in combination with tofacitinib, may increase tofaciitinib serum concentration toxicity and adverse effects. It is recommended to adjust therapy by reducing the adult dose of tofacitinib from 5mg twice a day to 5 mg daily.
    Tolbutamide Sitaxsentan, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Tolbutamide, a CYP2C9 substrate. Consider alternate therapy or monitor for changes in Tolbutamide therapeutic and adverse effects if Sitaxsentan is initiated, discontinued or dose changed.
    Tolterodine Sitaxsentan may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity.
    Torasemide Sitaxsentan, a strong CYP2C9 inhibitor, may increase the serum concentration of Torasemide, a CYP2C9 substrate, by decreasing Torasemide metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Torasemide if Sitaxsentan is initiated, discontinued or dose changed.
    Tramadol Sitaxsentan may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance.
    Trazodone The CYP3A4 inhibitor, Sitaxsenten, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Norfloxacin is initiated, discontinued or dose changed.
    Trimethoprim The strong CYP2C9 inhibitor, Sitaxsentan, may decrease the metabolism and clearance of Trimethoprim, a CYP2C9 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimethoprim if Sitaxsentan is initiated, discontinued or dose changed.
    Trimipramine The strong CYP2C19 inhibitor, Sitaxsentan, may decrease the metabolism and clearance of Trimipramine, a CYP2D6 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimipramine if Sitaxsentan is initiated, discontinued or dose changed.
    Voriconazole Sitaxsentan, a strong CYP2C9 inhibitor, may increase the serum concentration of voriconazole by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of voriconazole if sitaxsentan is initiated, discontinued or dose changed.
    Warfarin Sitaxentan, a strong CYP2C9 inhibitor, may decrease the metabolism of warfarin. Warfarin doses should be decreased by 80% upon initiated of concomitant therapy. Monitor for changes in the therapeutic and adverse effects of warfarin if sitaxentan is initiated, discontinued or dose changed.
    Zafirlukast Sitaxentan, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of zafirlukast. Consider alternate therapy or monitor for changes in zafirlukast therapeutic and adverse effects if sitaxentan is initiated, discontinued or dose changed.
    食物相互作用
    • Take without regard to meals

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