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IOS 10 Exam 2

Clindamycin & Metronidazole

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
Created by: liza001



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