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25 Cards in this Set
- Front
- Back
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When does resistance to penicillin develop?
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When the drug is inactivated by the penicillinase or beta-lactamase produced by bacteria.
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What was the first beta-lactamase inhibitor developed and marketed?
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Clavulanic acid
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What is the role of the beta-lactamase inhibitor?
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prevent the breakdown of the beta-lactam by organisms that produce the beta-lactamase enzyme.
Thereby enhancing the antibacterial activity of the beta-lactam. |
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Which resistant organisms can be treated with the beta-lactam / beta-lactamase inhibitor?
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Staph aureus
Haemophilus influenzae |
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What body tissues do the beta-lactamase inhibitors diffuse into?
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Most body tissues with the exception of:
brain CSF |
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Half-life of beta-lactam and beta-lactam inhibitors?
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1 hour for both components in the combination.
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How are beta-lactam / beta-lactam inhibitors eliminated?
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by glomerular filtration
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What would necessitate dosage adjustment with beta-lactam / beta-lactamase inhibitors?
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renal dysfunction
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Can the beta-lactam / beta-lactamase inhibitors be removed with dialysis?
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Yes, both hemodialysis and peritoneal dialysis removes them.
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What is the mechanism of action of beta-lactam?
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beta-lactam components are cell wall-active agents which interfere with bacterial cell wall synthesis by binding to and inactivating penicillin-binding proteins (PBPs)
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What is the mechanism of action of the beta-lactamase inhibitor?
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irreversibly bind to most beta-lactamase enzymes, protecting the beta-lactam from degradation and improving their antibacterial activity.
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Does the beta-lactam inhibitor exhibit anitbacterial properties?
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No, alone they lack significant antibacterial activity.
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How does resistance to beta-lactam / beta-lactam inhibitors occur?
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1. An overproduction of penicillinases not susceptible to the beta-lactamase inhibitors.
2. Beta-lactamases produced are less sensitive to inhibitors. (Can result in cross-resistance among all combinations) |
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Additional mechanism of resistance to beta-lactam?
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modification of the penicillin-binding protein can result in decreased activity.
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What are the clinical uses of beta-lactam / beta-lactam inhibitors?
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Treating polymicrobial infections
Extensively used to treat: intra-abdominal infections gynecological infections skin and soft tissue infections including human and animal bites Foot infections in diabetics Respiratory tract infections including aspiration pneum. sinusitis lung abscesses |
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Adverse events associated with beta-lactam / beta-lactam inhibitors?
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Hypersensitivity reactions
GI side effects Nausea / diarrhea Elevated AST / ALT levels |
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What antibiotics are beta-lactam / beta-lactam inhibitors physically incompatible with?
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Aminoglycosides
Results in inactivation of aminoglycosides in vitro |
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What are the adult PO dosages of amoxicillin-clavulanic acid (Augmentin)?
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250 - 500 mg PO q 8 hours or
500 - 875 mg PO q 12 hours |
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What are the PO Pediatric dosages of amoxicillin-clavulanic acid (Augmentin)?
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20 - 40 mg/kg/d q 8 - 12 hours
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What are the adult dosages of IV ampicillin-sulbactam (Unasyn)?
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1.5 - 3.0 g IV q6 hours
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What are the pediatric dosages of IV ampicillin-sulbactam (Unasyn)?
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100 - 400 mg/kg/d q 4 - 6 hours
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What are the adult dosages of IV piperacillin-tazobactam (Zosyn)?
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4.5 g IV q6 - 8 hours or
3.375 g IV q 4 - 6 hours |
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What are the pediatric dosages of IV piperacillin-tazobactam (Zosyn)?
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240 mg/kg/d q 8 hours
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What are the adult dosages of IV ticarcillin-clavulanic acid (Timentin)?
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3.1 g IV q4-6 hours
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What are the pediatric dosages of IV ticarcillin-clavulanic acid (Timentin)?
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200 - 300 mg/kg/d q4 - 6 hours
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