Clindamycin hydrochloride, Antibiotic for Culture Media Use Only；(2S,4R)-N-[(1S,2S)-2-chloro-1-[(2R,3R,4S,5R,6R)-3,4,5-trihydroxy-6-methylsulfanyloxan-2-yl]propyl]-1-methyl-4-propylpyrrolidin-1-ium-2-carboxamide;chloride
CAS
21462-39-5
化学式
C18H33ClN2O5S*ClH
mdl
——
分子量
461.45
InChiKey
AUODDLQVRAJAJM-XJQDNNTCSA-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
物化性质
熔点：
141°C
溶解度：
H2O：50 mg/mL，澄清，无色
颜色/状态：
Yellow, amorphous solid
蒸汽压力：
5.28X10-17 mm Hg at 25 °C (est)
稳定性/保质期：
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旋光度：
Specific optical rotation = +214 deg at 25 °C/D (chloroform)
分解：
When heated to decomposition it emits toxic fumes of /chlorine, oxides of sulfur, and oxides of nitrogen/.
碰撞截面：
200.6 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]
Clindamycin is partially metabolized to bioactive and inactive metabolites. The major bioactive metabolites are clindamycin sulfoxide and N-demethyl-clindamycin which are excreted in urine, bile, and feces. Within 24 hours, approximately 10% of an oral dose of clindamycin is excreted in urine and 3.6% is excreted in feces as active drug and metabolites; the remainder is excreted as inactive metabolites.
Only about 10% of the clindamycin admin is excreted unaltered in urine, and small quantities are found in feces ... Clindamycin is inactivated by metabolism to N-demethylclindamycin and clindamycin sulfoxide, which are excreted in the urine and bile.
Clindamycin has been linked to two forms of hepatotoxicity: transient serum aminotransferase elevations usually occurring after several days of high intravenous doses; and, an acute, idiosyncratic liver injury that arises within 1 to 3 weeks of starting therapy and is typically mild and self-limited.
High doses of intravenous clindamycin can be accompanied by elevations in serum ALT levels in the range of 2 to 10 times the upper limit of normal starting after 5 to 15 days of therapy in a manner similar to what occurs with intravenous oxacillin therapy (Case 1). Symptoms, jaundice, and alkaline phosphatase elevations are mild if they occur at all (Case 2), and aminotransferase levels rapidly fall into the normal range (in 1 to 2 weeks) upon stopping clindamycin or switching to lower doses or to oral formulations with which it rarely occurs.
Clindamycin therapy has also been linked to a clinically apparent, idiosyncratic liver injury that arises between 1 to 3 weeks after starting either oral or parenteral therapy (Case 3). The pattern of serum enzyme elevations is typically hepatocellular or mixed, but can be cholestatic. Allergic manifestations such as rash, fever and eosinophilia are typical, but often are not prominent and are not present in all cases. Autoantibodies are generally not present. The acute liver injury may accompany other signs of hypersensitivity such as Stevens Johnson syndrome or other severe skin reactions. The liver injury is usually mild-to-moderate in severity and resolves rapidly with stopping. However, fatal instances have been reported.
Likelihood score: B (highly likely cause of clinically apparent liver injury).
来源:LiverTox
毒理性
相互作用
抗生素诱导的小鼠膈神经-半膈肌准备的可逆性麻痹通过钙和通过新斯的明。
Reversibility of antibiotic-induced paralysis of mouse phrenic nerve-hemidiaphragm preparation by calcium and by neostigmine.
Concurrent use of kaolin- or attapulgite-containing antidiarrheals with oral clindamycin may significantly delay the absorption of oral clindamycin; concurrent use should be avoided or patients should be advised to take adsorbent antidiarrheals not less than 2 hours before or 3 to 4 hours after oral lincomycins.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
相互作用
体外实验有证据表明红霉素和克林霉素之间存在拮抗作用。
There is in vitro evidence of antagonism between erythromycin and clindamycin.
Clindamycin has been reported to antagonize the bactericidal activity of aminoglycosides in vitro, and some clinicians recommend that these drugs not be used concomitantly. However, in vivo antagonism has not been demonstrated, and clindamycin has been administered successfully in conjunction with an aminoglycoside with no apparent decrease in activity.
Clindamycin is nearly completely absorbed following oral admin. Peak plasma concn of 2 to 3 ug/mL are attained within 1 hr after the ingestion of 150 mg. The presence of food in stomach does not reduce absorption. The half-life of the antibiotic is about 2.9 hr, and the modest accumulation of drug is thus expected if it is given at 6-hr intervals.
Clindamycin is widely distributed in many fluids and tissues, including bone. Significant concn are not attained in cerebrospinal fluid, even when the meninges are inflamed. Concn sufficient to treat cerebral toxoplasmosis are achievable .. The drug readily crosses the placental barrier. 90% or more of clindamycin is bound to plasma proteins. Clindamycin accumulates in polymorphonuclear leukocytes, alveolar macrophages, and in abscesses.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
半衰期在肾功能明显受损的患者中只会略微延长...
Half-life ... is lengthened only slightly in patients with markedly impaired renal function ...
Clindamycin is distributed into many body tissues and fluids including saliva, ascites fluid, pleural fluid, synovial fluid, bone, and bile. However, even in the presence of inflamed meninges, only small amounts of the drug diffuse into CSF. The concentration of clindamycin in synovial fluid and bone is reported to be 60-80% of concurrent serum concentrations of the drug; the degree of penetration does not appear to be affected by joint inflammation. Clindamycin readily crosses the placenta, and cord blood concentrations of the drug have been reported to be 46% of concurrent maternal blood concentrations. Clindamycin is distributed into milk.
[EN] PEPTIDE-BASED MULTIPLE-DRUG DELIVERY VEHICLE<br/>[FR] VÉHICULE D'ADMINISTRATION DE MÉDICAMENTS MULTIPLES À BASE DE PEPTIDES
申请人：ARIEL-UNIVERSITY RES AND DEV COMPANY LTD
公开号：WO2017068577A1
公开（公告）日：2017-04-27
A molecular structure comprising a targeting moiety, a multi-functional peptide platform and a plurality of controllably released bioactive agents attached thereto is provided herein.
Provided herein is a drug delivery (DD) system for ratiometric luminescence determination of drug release degree in drug delivery monitoring, which includes a drug, a switchable reporter and non-switchable reporter providing two distinguishable signals for detection; or a single switchable reporter providing two distinguishable signals for detection, and a cleavable linker connecting a drug to a switchable reporter, as well as a method for ratiometric luminescence determination of drug release in a target in vivo or in vitro), which is effected by administering the DD system provided herein that is capable of releasing a drug from the DD system, measuring two luminescent signals provided by the switchable reporter and the non-switchable reporter, or the single switchable reporter, determining the ratio between these two luminescence signals, and determining the drug release degree through the ratio between the two luminescence signals.
CONJUGATE-BASED ANTIFUNGAL AND ANTIBACTERIAL PRODRUGS
申请人：Bapat Abhijit S.
公开号：US20140364595A1
公开（公告）日：2014-12-11
The invention provides conjugate-based antifungal or antibacterial prodrugs formed by coupling at least one anti-fungal agent or antibacterial agent with at least one linker and/or carrier. The prodrugs are of formula: (i) (AFA)
m
-X-(L)
n
; (ii) [(AFA)
m′
-X]
p
-L; (iii) AFA-[X-(L)
n′
]
q
; or (iv) (AFA)
m″
-X, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m ranges from 1 to 10; n ranges from 2 to 10; m′ is 1 to 10; p is 1 to 10; n′ is 1 to 10; and q is 1 to 10, provided that q′ and n are not both 1; and m″ is 1 to 10. The invention also provides nanoparticles comprising the conjugate-based prodrugs. Additionally, the invention also provides non-conjugated antifungal and antibacterial agents in the form of nanoparticles.
该发明提供了由至少一种抗真菌剂或抗菌剂与至少一种连接剂和/或载体偶联形成的基于共轭的抗真菌或抗菌前药。这些前药的公式为：(i) (AFA)
m
-X-(L)
n
; (ii) [(AFA)
m′
-X]
p
-L; (iii) AFA-[X-(L)
n′
]
q
; 或 (iv) (AFA)
m″
-X，其中：AFA是抗真菌剂或抗菌剂；L是载体；X是连接剂；m范围从1到10；n范围从2到10；m′为1到10；p为1到10；n′为1到10；q为1到10，前提是q'和n不同时为1；m″为1到10。该发明还提供了包含基于共轭的前药的纳米粒子。此外，该发明还提供了以纳米粒子形式的非共轭抗真菌和抗菌剂。
[EN] GOLD COMPOUNDS AND THEIR USE IN THERAPY<br/>[FR] COMPOSÉS D'OR ET LEUR UTILISATION DANS LE CADRE D'UNE THÉRAPIE
申请人：AUSPHERIX LTD
公开号：WO2018220171A1
公开（公告）日：2018-12-06
Compound of formula (I) and pharmaceutically acceptable salts and solvates thereof are described, wherein: Px selected from (P1), (P2) or (P3); The compounds are useful in the prevention or treatment of a bacterial infection.
[EN] TYPE II TOPOISOMERASE INHIBITORS AND METHODS OF MAKING AND USING THEREOF<br/>[FR] INHIBITEURS DE TOPOISOMÉRASE DE TYPE II ET PROCÉDÉS DE PRODUCTION ET D'UTILISATION DE CES DERNIERS
申请人：OHIO STATE INNOVATION FOUNDATION
公开号：WO2018195098A1
公开（公告）日：2018-10-25
Disclosed are Type II Topoisomerase Inhibitors, analogs thereof, pharmaceutical compositions thereof, and methods of making and using these compounds and compositions. Methods of using the disclosed compounds to treat infections, such as MRSA, MDR P. aeruginosa, and other pathogens are also described.
披露了II型拓扑异构酶抑制剂及其类似物、药物组合物以及制备和使用这些化合物和组合物的方法。还描述了利用所披露的化合物治疗感染，如MRSA、MDR P. aeruginosa和其他病原体的方法。
