从药理学看厄他培南1.ppt

* * * 碳青霉烯结合了青霉素5元环和头孢烯的共轭双键，碳青霉烯强力的抗菌活性，取决于环的张力和邻位双键的双重活化影响。 ?A 反式-1-羟乙基基团使得厄他培南对产β-内酰胺酶（包括ESBL和AmpC酶）菌株具有抗菌活性 ?B.1β-甲基基团使得厄他培南对肾脏脱氢肽酶-1稳定，因此不需要同时使用肾脏脱氢肽酶-1抑制剂 ?C. 苯甲酸基团增加了分子量及亲脂性，羧酸基团在生理pH条件下可离子化，使得厄他培南带有负电荷，从而导致厄他培南具有较高的蛋白结合率及较长的半衰期 * * * * * * IVZ 2008-W-1259216-SS MS* A recent publication uses the term “collateral damage” to describe the ecological adverse effects of antibiotic therapy, namely, selection of drug-resistant organisms and the unwanted development of colonization or infection with multidrug-resistant organisms.1 Cephalosporins and fluoroquinolones have been associated with collateral damage: ? Cephalosporin use has been linked to subsequent infection with vancomycin-resistant enterococci, ESBL-producing K?pneumoniae, β-lactam–resistant Acinetobacter spp, and  Clostridium difficile.1 ? Fluoroquinolone use has been linked to infection with methicillin- resistant Staphylococcus aureus and increasing quinolone resistance in gram-negative bacilli, such as P aeruginosa.1 The author concludes that “neither third-generation cephalosporins nor fluoroquinolones appear suitable for sustained use in hospitals as ‘workhorse’ antibiotic therapy.”1 The following slides explore the impact of ertapenem, a group 1 carbapenem,2 on hospital ecology. References Paterson DL. “Collateral damage” from cephalosporin or quinolone antibiotic therapy. Clin Infect Dis. 2004;38(suppl 4):S341–S345. Shah PM, Isaacs RD. Ertapenem, the first of a new group of carbapenems. J Antimicrob Chemother. 2003;52:538–542. 1/Paterson, p S341, C1, ?1, L5-10, 11-17 1/Paterson, p S341, C1, ?1, L5-10 1/Paterson, p S341, C1, ?1, L11-17; p S343, Table 1 1/Paterson, p S341, ?1, L8-9 1/Paterson, p S341, C1, ?1, L5-10, 11-17 1/Paterson, p S341, C1, ?1, L5-10 1/Paterson, p S341, C1, ?1, L11-17; p S343, Table 1 1/Paterson, p S341, ?1, L8-9 2/Shah, p 541, C2, ?1, L8-11, ?2, L1 NEW 这些耐药的产生往往是由于喹诺酮类和头孢菌素治疗筛选了耐药菌株的结果。 我们都知道敏感的菌株存在着自发的突变，而喹诺酮类和头孢菌素类药物对于这些突变的菌株没有杀菌作用