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IOS 10 Exam 2
Clindamycin & Metronidazole
Question | Answer |
---|---|
MOA of Clindamycin | Bacteriostatic that Binds 50S ribosome (like macrolides, chlorphenicol) |
MOA of metronidazole | Ab undergoes reductive bioactivation of its nitrogroup by ferroxin oxidoreductase (obligate anaerobes) to form ROS that interferes with nucleic acd synthesis |
Resistance of Clindamycin | Chromosomal alteration of single AA at 50S (simular to macrolides), plasmid mediated alteration of 23 SRNA of 50 S subunit to methylation of adenine residue at receptor site(MLS phenotype resistance to all macrolides, lincosamides, streptogramins), poor p |
Resistance of metronidazole | Very rare by most anerobes, chromosomal alterations by Actinomycetes, prioprionbacterium, and with H. pylori decreased drug uptake |
Clinamycin activity | Above the belt- Gram + aerobes excellent staph, strep, some MRSA, low strepto, No enterococci, broad anaerobe activity (clostridium & bacteroides fragilis!!), atypical chlamydia |
Clindamycin ADME | Excellent bioav, excellent distribution, extensively metabolised to inactive metabolite, elimination via bile and feces |
Clindamycin SE | ALL rxn, diarrhea (20%), pseudomembraneous, colitis, hepatotoxcity, Superinfection with candidiasis, C.diff |
Clindamycin DI | No significant interactions |
Metronidazole activity | Below the belt- anaerobes-excellent bacterioides, prevtella, fusobacterium, Drug of choice for C. diff, Gram - aerobes- H. pylori, gardenerella vaginitis, Anaerobic protoza- trichomonas vaginalis, entamoeba hystolytica, Giardia, NOT Gram+ aerobic |
Metronidazole ADME | Rapid and complete Abs ((%, distributes to all tissues, CNS, 90% metabolized some to active , elimination via urine, causes red discharge in urine , tears |
Metronidazole SE | GI, fluury gray tongue, Discoloraation of the urine, teratogenic, CNS |
Metronidazole DI | warfarin, alcohol(disulfram), phenobarbital(decrease MTZ), carbamazepine, rifampin (decrease MTZ), cyclosporin, tacrolimus |