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16 Cards in this Set
- Front
- Back
What is the mechanism of action for Tetracyclines?
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Inhibition of the 30S ribosomal subunit by preventing binding of aatRNA
Bacteriostatic |
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Mechanism of resistance to tetracyclines
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Efflux: main mechanism
Decreased penetration (active transport is required for entry) Competitive binding to ribosome by cellular proteins |
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What are unique properties of Tigecycline
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Binds more strongly to 30S subunit
Not able to be pumped out as easily The super tetracycline! |
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What is the absorption of Tetracyclines? What can complicate this?
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Orally absorbed
Di and tri valent cations chelate - don't have it with milk! |
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Tetracycline Distribution
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Vd > body water; sequestered in boty
Doesn't penetrate CSF |
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Tetracycline Metabolism
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Concentrated in liver
T1/2 = 6 - 16 hr. |
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Tetracycline excretion
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mostly excreted renally
some excreted hepatically |
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Tigecycline absorption
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IV only
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Tigecycline distribution
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Well distributed
Greater Vd than water Most concentrated in respiratory tissues |
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Tigecycline metabolism
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Some in liver (<10%)
T1/2 > 27 hr |
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Tigecycline excretion
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Bile - 60%
Renal - 30% Hepatic - 10% |
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Who shouldn't you prescribe tetracyclines to? Why?
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Pregnant women, young children
Tetracyclines chelate to calcium. Effect bone growth, stain teeth |
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Adverse effects of tetracyclines
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Large dose hepatotoxicity
If expired, nephrotoxicity Photosensitivity Failure of oral contraceptives (use barrier contraceptives for 2 weeks after) Staining of teeth |
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Tetracycline clinical uses
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Intracellular bugs!
Rickettsia Chlamydia Mycroplasma pneumoniae Acne (topically) |
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Tigecycline clinical uses
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Complicated skin, intra-abdominal infections
Drug resistant organisms |
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Tigecycline adverse effects
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GI nausea, vomiting, diarrhea
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