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Penticort

中文名称
——
中文别名
——
英文名称
Penticort
英文别名
[2-(12-fluoro-11-hydroxy-9,13-dimethyl-16-oxospiro[5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-diene-6,1'-cyclopentane]-8-yl)-2-oxoethyl] acetate
Penticort化学式
CAS
——
化学式
C28H35FO7
mdl
——
分子量
502.6
InChiKey
ILKJAFIWWBXGDU-UHFFFAOYSA-N
BEILSTEIN
——
EINECS
——
  • 物化性质
  • 计算性质
  • ADMET
  • 安全信息
  • SDS
  • 制备方法与用途
  • 上下游信息
  • 反应信息
  • 文献信息
  • 表征谱图
  • 同类化合物
  • 相关功能分类
  • 相关结构分类

计算性质

  • 辛醇/水分配系数(LogP):
    3.6
  • 重原子数:
    36
  • 可旋转键数:
    4
  • 环数:
    6.0
  • sp3杂化的碳原子比例:
    0.75
  • 拓扑面积:
    99.1
  • 氢给体数:
    1
  • 氢受体数:
    8

ADMET

毒理性
  • 在妊娠和哺乳期间的影响
◉ 母乳喂养期间使用总结:阿米诺尼德在母乳喂养期间尚未进行研究。由于只有大量使用最强效的皮质类固醇才可能在母亲体内产生系统性影响,因此短期使用外用皮质类固醇不太可能通过进入母乳而对哺乳婴儿构成风险。然而,最好还是使用最弱效的药物,并且尽可能在最小的皮肤区域上使用。特别是要确保婴儿的皮肤不直接接触到已经治疗过的皮肤区域。只有低效皮质类固醇可以用于乳头或乳晕区域,因为婴儿可能会直接从皮肤上摄取药物。应仅用水溶性乳膏或凝胶产品涂抹乳房,因为软膏可能会使婴儿通过舔舐接触到高水平的矿物石蜡。如果外用皮质类固醇应用于乳房或乳头区域,应在哺乳前彻底擦干净。 ◉ 对哺乳婴儿的影响:将相对高矿皮质激素活性的皮质类固醇(异氟泼尼松醋酸酯)涂在母亲的乳头上,导致她的2个月大的哺乳婴儿出现QT间期延长、库欣综合征外貌、严重高血压、生长减缓和电解质异常。这位母亲从婴儿出生起就因为乳头疼痛而使用这种乳膏。 ◉ 对泌乳和母乳的影响:截至修订日期,没有找到相关的已发布信息。
◉ Summary of Use during Lactation:Amcinonide has not been studied during breastfeeding. Since only extensive application of the most potent corticosteroids may cause systemic effects in the mother, it is unlikely that short-term application of topical corticosteroids would pose a risk to the breastfed infant by passage into breastmilk. However, it would be prudent to use the least potent drug on the smallest area of skin possible. It is particularly important to ensure that the infant's skin does not come into direct contact with the areas of skin that have been treated. Only the lower potency corticosteroids should be used on the nipple or areola where the infant could directly ingest the drugs from the skin. Only water-miscible cream or gel products should be applied to the breast because ointments may expose the infant to high levels of mineral paraffins via licking. Any topical corticosteroid should be wiped off thoroughly prior to nursing if it is being applied to the breast or nipple area. ◉ Effects in Breastfed Infants:Topical application of a corticosteroid with relatively high mineralocorticoid activity (isofluprednone acetate) to the mother's nipples resulted in prolonged QT interval, cushingoid appearance, severe hypertension, decreased growth and electrolyte abnormalities in her 2-month-old breastfed infant. The mother had used the cream since birth for painful nipples. ◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.
来源:Drugs and Lactation Database (LactMed)

文献信息

  • Oligomer-Corticosteroid Conjugates
    申请人:Zhang Wen
    公开号:US20100286107A1
    公开(公告)日:2010-11-11
    The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.
  • OLIGOMER-CORTICOSTEROID CONJUGATES
    申请人:NAKTAR THERAPEUTICS
    公开号:US20140309398A1
    公开(公告)日:2014-10-16
    The invention provides corticosteroids that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits different properties compared to the properties of the corticosteroid not attached to the water-soluble oligomer.
  • US8796248B2
    申请人:——
    公开号:US8796248B2
    公开(公告)日:2014-08-05
  • [EN] OLIGOMER-CORTICOSTEROID CONJUGATES<br/>[FR] CONJUGUÉS D'OLIGOMÈRES ET CORTICOSTÉROÏDES
    申请人:NEKTAR THERAPEUTICS AL CORP
    公开号:WO2009045539A2
    公开(公告)日:2009-04-09
    The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.
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