药品详细
Mezlocillin (美洛西林 )
化学结构式图
中文名
美洛西林
英文名
Mezlocillin
分子式
Not Available
化学名
(2S,5R,6R)-6-[(2R)-2-{[(3-methanesulfonyl-2-oxoimidazolidin-1-yl)carbonyl]amino}-2-phenylacetamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
分子量
Average: 539.582
Monoisotopic: 539.114454181
Monoisotopic: 539.114454181
CAS号
51481-65-3
ATC分类
J01C Beta-lactam Antibacterials, Penicillins
药物类型
small molecule
阶段
商品名
Mezlin;
同义名
基本介绍
Semisynthetic ampicillin-derived acylureido penicillin. It has been proposed for infections with certain anaerobes and may be useful in inner ear, bile, and CNS infections. [PubChem]
生产厂家
- Bayer pharmaceuticals corp
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference |
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剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
antibacterials 抗细菌;
药理
| Indication | Used to treat serious gram–negative infections of the lungs, urinary tract, and skin. |
| Pharmacodynamics | Mezlocillin is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. The name "penicillin" can either refer to several variants of penicillin available, or to the group of antibiotics derived from the penicillins. Mezlocillin has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of mezlocillin results from the inhibition of cell wall synthesis and is mediated through mezlocillin binding to penicillin binding proteins (PBPs). Mezlocillin is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases. Mezlocillin can be used to treat susceptible strains of H. influenzae, Klebsiella species, Pseudomonas species, Proteus mirabilis, E. coli, Enterobacter species, Streptococcus faecelis, Peptococcus species, Peptostreptococcus species, Bacteriodes species (including B. fragilis), Morganella morganii, Serratia species, N. gonorrhoeae, P. vulgaris, and Providencia rettgeri. This drug is discontinued in the U.S. |
| Mechanism of action | By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, mezlocillin inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that mezlocillin interferes with an autolysin inhibitor. |
| Absorption | Not Available |
| Volume of distribution | Not Available |
| Protein binding | 16-59% |
| Metabolism |
Unlike many other penicillins, mezlocillin is either extensively metabolized or is subject to biliary excretion, as only about 50% of the dose was accounted for in normal urine. |
| Route of elimination | Not Available |
| Half life | 1.3 to 4.4 hours |
| Clearance | Not Available |
| Toxicity | Symptoms of overdose include rash, fever, chills, and peeling skin. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
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| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | Not Available | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Demeclocycline | Possible antagonism of action |
| Doxycycline | Possible antagonism of action |
| Ethinyl Estradiol | This anti-infectious agent could decrease the effect of the oral contraceptive |
| Methotrexate | The penicillin increases the effect and toxicity of methotrexate |
| Minocycline | Possible antagonism of action |
| Tetracycline | Possible antagonism of action |
食物相互作用
Not Available
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