General properties of macrolides 8. Resistance mechanism: (1)modification of the ribosomal binding site (2) production of esterase that hydrolyze macrolides (3 reduced permeability of cell membrane or active efflux (4)Ribosome mutation(base mutation of 23s rRNA or ribosome protein mutation) Cross-resistance is complete between erythromycin and the other macrolides
8. Resistance mechanism: (1) modification of the ribosomal binding site (2) production of esterase that hydrolyze macrolides (3) reduced permeability of cell membrane or active efflux (4) Ribosome mutation (base mutation of 23s rRNA or ribosome protein mutation) ***Cross-resistance is complete between erythromycin and the other macrolides. General properties of macrolides
General properties of macrolides 9. Drug interaction Erythromycin metabolites can inhibit cytochrome P450 enzyme 正在服用他汀类降血脂药物不能与克拉霉素还 是阿奇霉素合用?
9. Drug interaction • Erythromycin metabolites can inhibit cytochrome P450 enzyme. • 正在服用他汀类降血脂药物不能与克拉霉素还 是阿奇霉素合用？ General properties of macrolides
Macrolides Erythromycin(红霉素): chlamydia(支原体) and chlamydial(农 RA)infections, community-acquired pneumonia, penicillin substitute for staphylococcal, streptococcal or pneumococcal infection. Cause obvious GI reactions and liver toxicity Clarithromycin(克拉霉素): highest activit, stable to acid,is metabolite has activity Has PAe. Azithromycin(阿奇霉素,15): penetrates into most tissues well and released slowly from tissues, permits once daily dosing. High activity against mycoplasma(支原体) and chlamydia(衣原体),G bacteria has pae Telithromycin(泰利霉素 酮内酯类抗生素, good absorption and penetration, high binding to ribosome, low efflux, effective to MLSB resistant bacteria
• Erythromycin (红霉素) : chlamydia (支原体) and chlamydial (衣 原体) infections, community-acquired pneumonia, penicillin substitute for staphylococcal, streptococcal or pneumococcal infection. Cause obvious GI reactions and liver toxicity. • Clarithromycin (克拉霉素) : highest activity, stable to acid, its metabolite has activity. Has PAE. • Azithromycin (阿奇霉素, 15): penetrates into most tissues well and released slowly from tissues, permits once daily dosing. High activity against mycoplasma (支原体) and chlamydia(衣原体), Gbacteria. Has PAE. • Telithromycin (泰利霉素): 酮内酯类抗生素， good absorption and penetration, high binding to ribosome, low efflux, effective to MLSB resistant bacteria. Macrolides
A 5-year-old boy is brought to the physician's office because of a cough. He has episodes of successive and rapid coughs, which seems like he is choking, followed by a deep and loud inspiratory sound. He has vomited a few times after these bursts of cough. His symptoms have been progressively worsening for the past week and were preceded by congestion, serous rhinorrhea and sneezing. His past medical history is insignificant His vital signs are stable. Lung auscultation is unremarkable. Which of the following is the most appropriate pharmacotherapy for this patient? This child most likely has Bordetella pertussis infection O A Erythromycin O B Ampicillin O C Rifampin O D TMP-SMX O E Cephalexin O F. Treatment is ineffective at this stage
Lincomycin clindamycin resemble erythromycin in antimicrobial spectrum, mechanism and resistance bactericidal or bacteriostatic, depending on the concentration, G+ microorganIsm,G- CoccUS, anaerobe, chlamydia(衣原体) but not MRSA, mycobacteria pneumoniae(肺炎支原体, aerobic G bacilli enterococcus, Clostridium difficile(难辨梭状芽孢杆菌) A
• resemble erythromycin in antimicrobial spectrum, mechanism and resistance. bactericidal or bacteriostatic, depending on the concentration, G+ microorganism, G- coccus, anaerobe, chlamydia(衣原体) but not MRSA, mycobacteria pneumoniae (肺炎支原体), aerobic Gbacilli, enterococcus, Clostridium difficile (难辨梭状芽孢杆菌) Lincomycin & Clindamycin