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 |
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Term
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Definition
| structure and numbering of tetracycline |
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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 |
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Term
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Definition
| antibacterial activity of tetracyclines |
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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
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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) |
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Definition
| bacterial resistance of tetracyclines |
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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 |
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Definition
| pharmacology of tetracyclines |
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Term
irratative effects
superinfection
effects on teeth and bone
hepatic and renal toxicity
effects on skin |
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Definition
| adverse effects of tetracyclines |
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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 |
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Definition
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