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25 Cards in this Set

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When does resistance to penicillin develop?
When the drug is inactivated by the penicillinase or beta-lactamase produced by bacteria.
What was the first beta-lactamase inhibitor developed and marketed?
Clavulanic acid
What is the role of the beta-lactamase inhibitor?
prevent the breakdown of the beta-lactam by organisms that produce the beta-lactamase enzyme.

Thereby enhancing the antibacterial activity of the beta-lactam.
Which resistant organisms can be treated with the beta-lactam / beta-lactamase inhibitor?
Staph aureus

Haemophilus influenzae
What body tissues do the beta-lactamase inhibitors diffuse into?
Most body tissues with the exception of:
brain
CSF
Half-life of beta-lactam and beta-lactam inhibitors?
1 hour for both components in the combination.
How are beta-lactam / beta-lactam inhibitors eliminated?
by glomerular filtration
What would necessitate dosage adjustment with beta-lactam / beta-lactamase inhibitors?
renal dysfunction
Can the beta-lactam / beta-lactamase inhibitors be removed with dialysis?
Yes, both hemodialysis and peritoneal dialysis removes them.
What is the mechanism of action of beta-lactam?
beta-lactam components are cell wall-active agents which interfere with bacterial cell wall synthesis by binding to and inactivating penicillin-binding proteins (PBPs)
What is the mechanism of action of the beta-lactamase inhibitor?
irreversibly bind to most beta-lactamase enzymes, protecting the beta-lactam from degradation and improving their antibacterial activity.
Does the beta-lactam inhibitor exhibit anitbacterial properties?
No, alone they lack significant antibacterial activity.
How does resistance to beta-lactam / beta-lactam inhibitors occur?
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)
Additional mechanism of resistance to beta-lactam?
modification of the penicillin-binding protein can result in decreased activity.
What are the clinical uses of beta-lactam / beta-lactam inhibitors?
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
Adverse events associated with beta-lactam / beta-lactam inhibitors?
Hypersensitivity reactions
GI side effects Nausea / diarrhea
Elevated AST / ALT levels
What antibiotics are beta-lactam / beta-lactam inhibitors physically incompatible with?
Aminoglycosides

Results in inactivation of aminoglycosides in vitro
What are the adult PO dosages of amoxicillin-clavulanic acid (Augmentin)?
250 - 500 mg PO q 8 hours or

500 - 875 mg PO q 12 hours
What are the PO Pediatric dosages of amoxicillin-clavulanic acid (Augmentin)?
20 - 40 mg/kg/d q 8 - 12 hours
What are the adult dosages of IV ampicillin-sulbactam (Unasyn)?
1.5 - 3.0 g IV q6 hours
What are the pediatric dosages of IV ampicillin-sulbactam (Unasyn)?
100 - 400 mg/kg/d q 4 - 6 hours
What are the adult dosages of IV piperacillin-tazobactam (Zosyn)?
4.5 g IV q6 - 8 hours or
3.375 g IV q 4 - 6 hours
What are the pediatric dosages of IV piperacillin-tazobactam (Zosyn)?
240 mg/kg/d q 8 hours
What are the adult dosages of IV ticarcillin-clavulanic acid (Timentin)?
3.1 g IV q4-6 hours
What are the pediatric dosages of IV ticarcillin-clavulanic acid (Timentin)?
200 - 300 mg/kg/d q4 - 6 hours