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青霉素问世已四十年,仍不失为最常用的一种抗生素。 青霉素类药物的基本母核为6—氨基青霉烷酸,它由一个β—内酰胺环接一个噻唑环构成,母核上取代基的改变可导致抗菌谱的改变和药动学性质的改变。 青霉素的抗菌谱特点是对大多数革兰氏阳性球菌、杆菌,阴性球菌和各种螺旋体都有强大的杀菌作用,但对革兰氏阴性杆菌的作用极弱。多数细菌对青霉素不易产生耐药性,但金葡球菌在与青霉素的反复接触影响下,能合成并释放青霉素酶,而破坏青霉素,因而容易出现高度耐药性。邻氯苯唑青霉素、苯唑青霉素,双氯苯唑青霉素等耐酶青霉素对耐药金葡菌仍有高效。
Penicillin has been around for 40 years and remains the most commonly used antibiotic. The basic parent nucleus of penicillins is 6-aminopenicillanic acid, which consists of a β-lactam ring followed by a thiazole ring. Changes in substituents on the parent nucleus can lead to changes in antibiotic spectrum and changes in pharmacokinetic properties . The antibacterial spectrum of penicillin is characterized by a strong bactericidal effect on most gram-positive cocci, bacilli, cocci and various spirochetes, but very little on gram-negative bacilli. Most bacteria is not easy to produce resistance to penicillin, but Staphylococcus aureus in contact with penicillin repeatedly under the influence of the synthesis and release of penicillinase, and the destruction of penicillin, and therefore prone to highly resistant. Penicillin obrompound, oxacillin, dicloxacillin penicillin and other resistant to resistant S. aureus is still highly efficient.