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Infectious Disease EXAM 1 Nieto - Tetracyclines
Infectious Disease EXAM 1 Nieto - Tetracyclines
9
Pharmacology
Graduate
01/12/2011

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Term
have an acid, base, and zwitterionic form
strong chelating agents
labile to acid and base degradation
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Definition
chemical properties of tetracyclines
Term
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Definition
structure and numbering of tetracycline
Term
acid and base degradation:
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epimerization may occur in acidic solution:
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Definition
degradation of tetracyclines through acids, bases, and epimerization
Term
broad spectrum
Definition
antibacterial activity of tetracyclines
Term
BACTERIOSTATIC
bind to the 30s ribosomal subunit
charge interactions with one edge
hydrophobic interactions with the other edge
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lipophilic tetracyclines: disrupt cytoplasmic membrane function (bactericidal)
lipophilic tetracyclines: passive diffusion
water soluble tetracyclines: water-lined protein porin routes (same as aminoglycosides)
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Definition
MOA of tetracyclines
Term
mainly through acquired resistance
energy dependent efflux
ribosomal protection: proteins associated with ribosome that bind tetracyclines to allow protein synthesis to continue
chemical modifications, modified membranes (decreased membrane permeability of the drug)
Definition
bacterial resistance of tetracyclines
Term
absorption: is absorbed from the stomach and upper GI tract (chelates decrease absorption)
distribution: high plasma protein binding, penetrate most tissues, bacteriostatic levels achieved in pleural and synovial fluids, poor penetration into CSF, pass the placenta
excretion: eliminated by renal and extra renal mechanisms, doxycycline eliminated through digestive tract
Definition
pharmacology of tetracyclines
Term
irratative effects
superinfection
effects on teeth and bone
hepatic and renal toxicity
effects on skin
Definition
adverse effects of tetracyclines
Term
30s subunit inhibition
blocking the entry of the acylamino tRNA
not affected by any tetracycline mechanism of resistance
broader spectrum than the classical tetracyclines
Definition
MOA of tigecycline
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