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MICABI - Exam 1
Macrolides - erythromycin
Question | Answer |
---|---|
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 |