171500-79-1
基本信息
達(dá)巴霉素
達(dá)巴萬星
道古霉素
鹽酸達(dá)巴萬星
道古霉素鹽酸鹽
道古霉素(達(dá)巴萬星)
道古霉素,達(dá)巴萬星,達(dá)巴霉素
Dalbavancin
Dalbavancin(BI 397, MDL 63397)
A-A-1, Dalbavancin Ao, BI 397, MDL 63397
物理化學(xué)性質(zhì)
常見問題列表
達(dá)巴萬星作用機制與萬古霉素和替考拉寧相同,抑制G+菌細(xì)胞壁的生物合成,被廣泛用作治療皮膚和軟組織感染的藥物。體內(nèi)、外試驗表明,達(dá)巴萬星對于G+菌包括耐甲氧西林金葡球菌(MRSA)、甲氧西林敏感金葡球菌(MSSA)、凝固酶陰性葡萄球菌(CoNS)、鏈球菌等具有抗菌活性。對耐G+病原菌包括耐青霉素和頭孢曲松肺炎鏈球菌、替考拉寧不敏感CoNS、非vanA型腸球菌具有活性;對G+厭氧菌也具有活性。達(dá)巴萬星具有獨特的藥動學(xué)性質(zhì),可每周間隔用藥。目前,達(dá)巴萬星在治療導(dǎo)管相關(guān)的血源性感染以及皮膚和軟組織感染已取得了良好的效果,其具有優(yōu)良的體內(nèi)抗菌活性和安全性,是理想的第二代糖肽抗生素。
MIC90: 0.06 μg/mL ( Staphylococcus aureus ) and 0.25 μg/mL ( Bacillus anthracis )
Dalbavancin is a parenterally administered semisynthetic lipoglycopeptide developed to combat infections caused by resistant gram-positive pathogens. Dalbavancin exhibits potent in vitro bactericidal activity against gram-positive pathogens including S. aureus (MRSA), VISA, and non-VanA strains of VRE. Dalbavancin is developed for the treatment of complicated skin and skin structure infections (cSSSIs), predominantly those caused by MRSA and β-hemolytic streptococci , organisms against which it has shown greater potency than existing glycopeptide therapeutic agents.
Dalbavancin (15-240 mg/kg; intraperitoneal injection; every 36 h or 72 h; for 14 days; female BALB/c mice) treatment has a survival rate of 80% to 100% of mice with all dose regimens.
Animal Model: | Female BALB/c mice (6-8 weeks) challenged with Ames strain of B. anthracis |
Dosage: | 15 mg/kg, 30 mg/kg, 60 mg/kg, 120 mg/kg, 240 mg/kg |
Administration: | Intraperitoneal injection; every 36 h or 72 h; for 14 days |
Result: | The efficacy was 80 to 100%, as determined by the rate of survival at 42 days, when treatment was initiated 24 h postchallenge with regimens of 15 to 120 mg/kg every 36 h or 30 to 240 mg/kg every 72 h. |