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药品详细

Meropenem (美罗培南 )

化学结构式图
中文名
美罗培南
英文名
Meropenem
分子式
Not Available
化学名
(4R,5S,6S)-3-{[(2S,5S)-5-(dimethylcarbamoyl)pyrrolidin-2-yl]sulfanyl}-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
分子量
Average: 383.463
Monoisotopic: 383.151491615
CAS号
119478-56-7
ATC分类
J01D Other Beta- lactam Antibacterials
药物类型
small molecule
阶段
商品名
Meronem;Merrem;Merrem I.V.;
同义名
Antibiotic SM 7338;meropenem;Meropenem anhydrous;Meropenemum [INN-Latin];
基本介绍

Meropenem is a broad-spectrum carbapenem antibiotic. It is active against Gram-positive and Gram-negative bacteria. Meropenem exerts its action by penetrating bacterial cells readily and interfering with the synthesis of vital cell wall components, which leads to cell death.

生产厂家
  • Astrazeneca uk ltd
  • Hospira inc
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
Form Route Strength
Powder, for solution Intravenous
规格
Unit description Cost Unit
Merrem 1 gm Solution Vial 81.32 USD vial
Merrem iv 1 gm vial 78.19 USD vial
Merrem 500 mg Solution Vial 48.79 USD vial
化合物类型
Type small molecule
Classes
  • Carbapenems and Derivatives
Substructures
  • Carbapenems and Derivatives
  • Hydroxy Compounds
  • Acetates
  • Amino Ketones
  • Carboxylic Acids and Derivatives
  • Pyrrolidines
  • Aliphatic and Aryl Amines
  • Beta Lactams
  • Heterocyclic compounds
  • Carboxamides and Derivatives
  • Lactams
  • Azetidines
  • Alcohols and Polyols
  • Pyrrolines
适应症
antibacterials 抗细菌;
药理
Indication For use as single agent therapy for the treatment of the following infections when caused by susceptible isolates of the designated microorganisms: complicated skin and skin structure infections due to Staphylococcus aureus (b-lactamase and non-b-lactamase producing, methicillin-susceptible isolates only), Streptococcus pyogenes, Streptococcus agalactiae, viridans group streptococci, Enterococcus faecalis (excluding vancomycin-resistant isolates), Pseudomonas aeruginosa, Escherichia coli, Proteus mirabilis, Bacteroides fragilis and Peptostreptococcus species; complicated appendicitis and peritonitis caused by viridans group streptococci, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Bacteroides fragilis, B. thetaiotaomicron, and Peptostreptococcus species. Also for use in the treatment of bacterial meningitis caused by Streptococcus pneumoniae, Haemophilus influenzae (b-lactamase and non-b-lactamase-producing isolates), and Neisseria meningitidis.
Pharmacodynamics Meropenem is a broad-spectrum carbapenem antibiotic. It is active against Gram-positive and Gram-negative bacteria. Meropenem exerts its action by penetrating bacterial cells readily and interfering with the synthesis of vital cell wall components, which leads to cell death.
Mechanism of action The bactericidal activity of meropenem results from the inhibition of cell wall synthesis. Meropenem readily penetrates the cell wall of most Gram-positive and Gram-negative bacteria to reach penicillin-binding- protein (PBP) targets. Its strongest affinities are toward PBPs 2, 3 and 4 of Escherichia coli and Pseudomonas aeruginosa; and PBPs 1, 2 and 4 of Staphylococcus aureus.
Absorption Not Available
Volume of distribution Not Available
Protein binding Approximately 2%.
Metabolism

Primarily excreted unchanged. There is one metabolite which is microbiologically inactive.

Route of elimination Approximately 70% of the intravenously administered dose is recovered as unchanged meropenem in the urine over 12 hours, after which little further urinary excretion is detectable.
Half life Approximately 1 hour in adults and children 2 years of age and older with normal renal function. Approximately 1.5 hours in children 3 months to 2 years of age.
Clearance Not Available
Toxicity In mice and rats, large intravenous doses of meropenem (2200-4000 mg/kg) have been associated with ataxia, dyspnea, convulsions, and mortalities.
Affected organisms
  • Enteric bacteria and other eubacteria
Pathways Not Available
理化性质
Properties
State solid
Melting point Not Available
Experimental Properties
Property Value Source
water solubility Sparingly PhysProp
logP -0.6 PhysProp
Predicted Properties
Property Value Source
water solubility 5.64e+00 g/l ALOGPS
logP -0.80 ALOGPS
logP -4.32 ChemAxon Molconvert
logS -1.83 ALOGPS
pKa 15.00 ChemAxon Molconvert
hydrogen acceptor count 6 ChemAxon Molconvert
hydrogen donor count 3 ChemAxon Molconvert
polar surface area 110.18 ChemAxon Molconvert
rotatable bond count 5 ChemAxon Molconvert
refractivity 97.77 ChemAxon Molconvert
polarizability 40.11 ChemAxon Molconvert
药物相互作用
Drug Interaction
Divalproex sodium Decreased plasma antiepileptic levels
食物相互作用
Not Available

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