Macrolides & ketolides
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| MOA of macrolides is | Reversible binding of the 50S subunit of domain V thus inhibiton of translation (same as clindamycin and chloramphemicol)
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| MOA of ketolides | Reversible binding to Domain V and Domain II of 50 S subunit of ribosome thus blocking translation
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| Macrolides are considered what type of killing | Bacterostatic for many but for S. pyrogenes (group A) and S. pneumoniae they are bacteriocidal.
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| Resistance of macrolides | Permibility (gram-), enzymatic inactivation, efflux, single alterations in 23S subunit of 50S decreased binding, methylation of 23S subunit of 50S caused alteration o binding
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| Resistance of ketolide | Scarce, alteration in telithromycin binding site via chromosomal or plasmid mutations
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| Erythromycin ADME | inactivated byy gastric acids requires capsulation, distribution into all tissues (not CNS), metabolism via p450, elimination fecal
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| Clarithromycin ADME | Good stability, extensive distribution,active metabolite
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| Azrithromycin ADME | Acid stable, reduced with food. Hepatic metaoblism, Elimination may require weeks!!!
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| Gram + aerobe activity of macrolides | Good,: staph, strep (poor-MRSA, enterococci)
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| Gram- aerobic activity of macrolides | Moderate: neisseria gonorrhowae, M. catarrhalis, H. inf, Some activity against enterobacteriaw (shigellam campylobacter, vibrio)
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| Anaerobic acitivty of macrolides | Little
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| Atypical activity of macrolides | DRUGS OF CHOICE
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| Other microbes macrolides cover | Borrelia burgdorferi, mycobacterium, H. pylori
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| Macrolide side effects | GI (N/V, DIa), thrombophlebitis, ALL, hepatotoxic, ototoxic, superinfection, torsades de points, pseudomembraneous colitis
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| Erythromycin DI | buspirone, carbamazepines, clomiramine respiradone, clozapine, cyclosporin, digoxin, felodpine, lovastatin, methylprednisolone, midazolam, phenytion, tacrolimus, theophylline,valproate, warfarin
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| Claithromycin DI | carbamazepine, cyclosporin, digoxin, rifampin, rifabutin, ritnoravie, zidovudine
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| Azithromycin DI | Cyclosporin
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| Ketolides ADME | moderate abs, VD moderare 2.9L, T1/2 10 hours, metabolism is Cp450 inhibition (huge), with 80%various elimination methods
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| Ketolide spectrum of activity: | Respiratory tract, S. pneumonia, pyrogenes, agalactiaw, H. infl, M. catarrhalis, C. pneumoniaw, L. pneumoniaw, M. pneumoniae, B. pertussis, MSSA
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| Ketolide SE | GI most common, hepatotoxcity, ocular rate
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| Ketolide DI | Simvastatin and lovastatin can cause increase in statin and decrease AB. Rifampin causes autoinduction of self and ketolides
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