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MICABI - Exam 1

Macrolides - erythromycin

QuestionAnswer
erythromycin - general chemistry basic, easily hydrolyzed as free base, destroyed by stomach acids
oral forms of erythromycin (4) Erythromycin free base - enteric coated; Erythromycin estolate, Erythromycin stearate, Erythromycin ethyl succinate
IV forms of erythromycin (2) Erythromycin lactobionate; Erythromycin gluceptate (glucoheptonate)
IM form of erythromycin (1) Erthromycin ethyl succinate
Erythromycin mechanism of action Inhibition of protein synthesis; binds to domain V of 50S subunit of prokaryotic ribosome and inhibits translocation (bacterostatic - not used for severe infections)
four mechanisms of erythromycin resistance in bacteria 1) plasmid mediated methylation of ribosome; 2) altered permeability; 3) mutations in Domain 5 of the 23s rRNA; 4)and mutations of 2 different ribosomal proteins(phenotypes-ML and MSB)
MLSB bacteria are resistant to which classes of antibiotics macrolides, lincosamides, and streptogramin B
MLSB phenotype is conferred to bacteria how by methylation of a single adenine in the bacterial 50s ribosome that binds to erythryomycin (erm)
two forms of MLSB resistance inducible (iMLSB) or constitutive (cMLSB)
primary spectrum of erythromycin gram positive cocci (strep & staph) and atypicals like mycoplasma pneumoniae; Legionella pneumophilia; treponema pallidum; Chlamydia and Some Mycobacteria (TB)
absorption of erythromycin poor oral absorption, must be taken on empty stomach
erythromycin Distribution/Metabolism/Excretion Widely distributed to soft tissues, skin, etc. Crosses poorly into CSF; concentrated in liver/excreted in bile; P450 drug interactions
erythromycin adverse events GI upset from oral administration due to the irritation and stimulation of gastric motility; Cholestatic hepatitis, jaundice (rare - estolate prep); Ototoxicity (rare, v. high dose)
erythromycin - clinical uses Mycoplasma pneumonia; Acne (inflammatory) – topical or oral; Chlamydia (GU or eye); 2ndary to B-lactams for respiratory and soft-tissue infections caused by gram-positive cocci; Syphilis (2nd choice after penicllin); w/neomycin colorectal; ot med (w/sulf
Created by: Krafty
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