Term
| Fungus that produces penicillin |
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Definition
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Term
| B-Lactam Drugs: Bactericidal or static |
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Definition
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Term
| Resistance due to B lactamases can be overcome by |
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Definition
| combining a B-lactamase inhibitor with the B-lactam drug |
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Term
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Definition
1. 4 membered B-lactam ring
2. R substituents affect penetration at porins, suceptibility to B-lactamases, binding to target enzymes |
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Term
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Definition
| gram negative anaerobes, not susceptible to their B-lactamases |
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Term
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Definition
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Term
| B-Lactam Drugs: Mechanisms of Resistance |
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Definition
Target alteration (PBP): MRSA, PRSP
B-lactamases: cleave C-N bond of the B-lactam ring-->Penicilloic acid. Many different B-lactamases that vary in specificity |
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Term
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Definition
1) Skin rashes
2) Rare: serum-sickness and anaphylaxis
ASSUME CROSS-ALLERGENICITY among all penicillins
Nausea, diarrhea, pseudomembranous colitis (overgrowth of S aureus) or mucositis (C albicans)
Renal failure: Na+ or K+ can produce seizures |
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Term
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Definition
| removes acyl substituent from B-lactam ring-->6-aminopenicillanic acid (LEAD COMPOUND). Allows for the generation of semi-synthetic penicillins |
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Term
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Definition
improve penetration thru porins-enhance gram - activity
decrease B lactamase susceptibility-broadens spectrum
alter PBP binding pattern-changes spectrum |
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Term
| B-lactam: pharmacokinetics |
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Definition
| Penicillin G (IM) has the highest bioavailability; then Penicillin V(oral), then penicillin G (oral); repository forms are the most slowly absorbed. Only enters the meninges when inflamed |
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Term
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Definition
| PBP binding. Inhibits crosslinking by acting as a D-ala-D-ala mimic suicide substrate. Transpeptidase activity |
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Term
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Definition
| Eliminated by the kidney. Reduce dose in patients with severe renal disease. PROBENECID inhibits tubular secretion to prolong 1/2 life |
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