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药品详细

Carbetocin(卡贝缩宫素)

化学结构式图
中文名
卡贝缩宫素
英文名
Carbetocin
分子式
C45H69N11O12S
化学名
(2S)-2-{[(2S)-1-{[(3R,6S,9S,12S,15S)-12-[(2S)-butan-2-yl]-9-(2-carbamoylethyl)-6-(carbamoylmethyl)-15-[(4-methoxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentaazacycloicosan-3-yl]carbonyl}pyrrolidin-2-yl]formamido}-N-(carbamoylmethyl)-4-methylpentanamide
分子量
Average: 988.161
Monoisotopic: 987.484787417
CAS号
37025-55-1
ATC分类
H01B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Carbetocin is a drug used to control postpartum hemorrhage, bleeding after giving birth. It is an analogue of oxytocin, and its action is similar to that of oxytocin — it causes contraction of the uterus.

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    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 Used to control postpartum hemorrhage and bleeding after giving birth.
    Pharmacodynamics Carbetocin is a drug used to control postpartum hemorrhage, bleeding after giving birth. It is sold under the trade name Duratocin. It is an analogue of oxytocin, and its action is similar to that of oxytocin; it causes contraction of the uterus.
    Mechanism of action Carbetocin binds to oxytocin receptors present on the smooth musculature of the uterus, resulting in rhythmic contractions of the uterus, increased frequency of existing contractions, and increased uterine tone. The oxytocin receptor content of the uterus is very low in the non-pregnant state, and increases during pregnancy, reaching a peak at the time of delivery.
    Absorption Bioavailability is 80% following intramuscular injection.
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life 40 minutes
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    logP -2 Not Available
    Predicted Properties
    Property Value Source
    water solubility 2.65e-02 g/l ALOGPS
    logP 0.14 ALOGPS
    logP -3.6 ChemAxon
    logS -4.6 ALOGPS
    pKa (strongest acidic) 11.42 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 12 ChemAxon
    hydrogen donor count 10 ChemAxon
    polar surface area 362.51 ChemAxon
    rotatable bond count 18 ChemAxon
    refractivity 250.18 ChemAxon
    polarizability 101 ChemAxon
    药物相互作用
    Drug Interaction
    Dinoprostone Dinoprostone may enhance the therapeutic effect of carbetocin. Avoid concomitant use of carbetocin with dinoprostone. The oxytocic activity of carbetocin (oxytocin analogue) may be augmented by agents used to promote cervical ripening (eg, dinoprostone, misoprostol). Dinoprostone (vaginal insert) prescribing information recommends waiting at least 30 minute following its removal before initiating treatment with oxytocic agents. A similar approach might be anticipated with misoprostol use.
    Misoprostol Misoprostol may enhance the therapeutic effect of Carbetocin. Avoid the concomitant use of carbetocin and misoprostol. The oxytocic activity of carbetocin (oxytocin analogue) may be augmented by agents used to promote cervical ripening (eg, dinoprostone, misoprostol). Dinoprostone (vaginal insert) prescribing information recommends waiting at least 30 minute following its removal before initiating treatment with oxytocic agents. A similar approach might be anticipated with misoprostol use.
    食物相互作用
    Not Available

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