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药品详细

Pivampicillin(Pivampicillin)

化学结构式图
中文名
Pivampicillin
英文名
Pivampicillin
分子式
C22H29N3O6S
化学名
{[(2S,5R,6R)-6-[(2R)-2-amino-2-phenylacetamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptan-2-yl]carbonyloxy}methyl 2,2-dimethylpropanoate
分子量
Average: 463.547
Monoisotopic: 463.177706365
CAS号
33817-20-8
ATC分类
J01C Beta-lactam Antibacterials, Penicillins
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Pivalate ester analog of ampicillin.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Albertson TE, Louie S, Chan AL: The diagnosis and treatment of elderly patients with acute exacerbation of chronic obstructive pulmonary disease and chronic bronchitis. J Am Geriatr Soc. 2010 Mar;58(3):570-9. Pubmed
    2. Chanteux H, Van Bambeke F, Mingeot-Leclercq MP, Tulkens PM: Accumulation and oriented transport of ampicillin in Caco-2 cells from its pivaloyloxymethylester prodrug, pivampicillin. Antimicrob Agents Chemother. 2005 Apr;49(4):1279-88. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Penicillins
    • Phenethylamines
    Substructures
    • Carbonyl Compounds
    • Carboxylic Acids and Derivatives
    • Acetates
    • Amino Ketones
    • Aliphatic and Aryl Amines
    • Ethers
    • Benzene and Derivatives
    • Beta Lactams
    • Penicillins
    • Thiazoles
    • Phenethylamines
    • Heterocyclic compounds
    • Aromatic compounds
    • Carboxamides and Derivatives
    • Lactams
    • Azetidines
    • Thiazolidines
    适应症
    药理
    Indication or the treatment of respiratory tract infections (including acute bronchitis, acute exacerbations of chronic bronchitis and pneumonia); ear, nose and throat infections; gynecological infections; urinary tract infections (including acute uncomplicated gonococcal urethritis) when caused by non penicillinase-producing susceptible strains of the following organisms: gram-positive organisms, e.g., streptococci, pneumococci and staphylococci; gram-negative organisms, e.g., H. influenzae, N. gonorrhoeae, E. coli, P. mirabilis.
    Pharmacodynamics Pivampicillin is the pivaloyloxymethyl ester of (the semi-synthetic penicillin) ampicillin. It is an inactive pro-drug, which is converted during its absorption from the gastrointestinal tract to the microbiologically active ampicillin, together with formaldehyde and pivalic acid, by non-specific esterases present in most body tissues. Amounts in excess of 99% of the pivampicillin absorbed are converted to ampicillin within 15 minutes of absorption.
    Mechanism of action Ampicillin (the active metabolite of pivampicillin) has a bactericidal action resulting from inhibition of cell wall mucopeptide biosynthesis.
    Absorption Absorbed following oral administration.
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life Approximately 1 hour.
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Enteric bacteria and other eubacteria
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties Not Available
    Predicted Properties
    Property Value Source
    water solubility 3.54e-02 g/l ALOGPS
    logP 1.43 ALOGPS
    logP 2.07 ChemAxon
    logS -4.1 ALOGPS
    pKa (strongest acidic) 11.71 ChemAxon
    pKa (strongest basic) 7.44 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 5 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 128.03 ChemAxon
    rotatable bond count 9 ChemAxon
    refractivity 116.25 ChemAxon
    polarizability 47.54 ChemAxon
    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
    Mestranol This anti-infectious agent could decrease the effect of the oral contraceptive
    Methacycline Possible antagonism of action
    Methotrexate The penicillin increases the effect and toxicity of methotrexate
    Minocycline Possible antagonism of action
    Oxytetracycline Possible antagonism of action
    Rolitetracycline Possible antagonism of action
    Tetracycline Possible antagonism of action
    食物相互作用
    • Take without regard to meals.

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