resp pharm 4
Terms
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- Stage 1 of cell wall synthesis
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- occurs in the cytoplasm and results in the synthesis of MurNAc-pentapeptide
- D-cycloserine - Stage 2 of cell wall synthesis
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occurs on the membrane surface and results in synthesis of MurNAc-GlcNAc its attachement
- Vancomycin and Bacitracin - Stage 3 of cell wall synthesis
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- occurs in the periplasm (-) or on the outside (+)
– it requires no energy
- cross-linking enzymes exchange the DADA peptide bond for a DAG peptide cross-link - B-lactam mechanism
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- structural similarity to the DADA carboxyl terminus
- react w/ PBP's to form a stable complex & inactivate - efficacy of b-lactams in (+) vs (-)
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- in (+), depends on ability to bind PBP
- in (-), depends on ability to bind PBP and ability to cross outer membrane - Resistance to B-lactams (5)
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- Production of a B-lactamase
- ↓ perm of outer membrane
- express efflux pump
- inability to activate autolytic enzymes
- mutations in PBP's - what organisms produce B-lactamase?
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- Staph aureus
- H. influenzae
- N. gonorrhoeae
- (-) enteric rods - what organisms tend to express efflux pumps for B-lactams?
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- N. gonorrhoeae
- P. aeruginosa
- S. typhimirium
- usually in concert w/ ß-lactamase, porin mutations and mutations in PBPs - what organisms tend to have the inability to activate autolytic enzymes (and are resistant to B-lactams)
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- staph
- strep
- listeria
- makes Ab static and not cidal - what organisms tend to have mutations in PBP's
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- staph aureus
- N. gonorrhoeae
- H. influenzae
- Strep pneumoniae - resistance to vancomycin
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- Only in E. faecium and E. faecalis
- plasmid mediated
- genes form a depsipeptide that vancomycin can't recognize - vancomycin mechanism
- binds w/ high affinity to DADA carboxyl terminus to prevent incorporation in stage 2
- Vancomycin Pharmacokinetics
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- oral if GI infections (poorly absorbed)
– IV if other
– 6 hr half life
– eliminated unchanged in kidney - vancomycin toxic effects
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- Severe ototoxicity and nephrotoxicity if high []’s
- Hypersensitivity reactions ovserved - vancomycin antimicrobial activity
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- 1st choice for MRSA and pen-resistant Strep pneum (can be in combo w/ 3rd gen or rifampin)
- alternative for Staph aureus, various Strep, C. difficile - Penicillin pharmokinetics
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- widely distributed except CSF, eyes, prostate
- penV, oxacillin, amoxicillin are oral
- penG, piperacillin, ticarcillin are parenteral
– minial metabolism and renal excretion - Penicillin side effects
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- Anaphylaxis
- hypersensitivity
- neurotoxicity - PenG and PenV for (+) cocci
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- strep groups A, B, C, and G
- E. faecium and E. faecalis (endocarditis and only w/ a aminoglycoside)
- Strep pneum (pneumococcus or diplococcus - resistant strains becoming more common) - PenG and PenV for (+) bacilli
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- anthrax
- C. perfringens
- C. tentani - PenG and PenV for (-) cocci
- – N. meningitidis
- PenG and PenV for enteric (-) bacilli
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- syphilis and other spirochetes
- Actinomycetes israelii
- V is an alternative to G for treating Strep. A, B, C, and G and pneumoniae - PenG and PenV antimicrobial spectrum (only groups)
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- (+) cocci
- (+) bacilli
- (-) cocci
- enteric (-) bacilli - Penicillinase-resistant penicillins
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- for penicillinase-producing Staph
- oxacillin & nafcillin - ampicillin and ampillin + sulbactam
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- oral, penicillinase susceptilbe
– good for penG bacteria, and GDS
– also for (-) bacilli like H. influenzae, E. coli, P. mirabilis, Shigella and S. typhi - amoxicillin & amoxicillin + clavulanate
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– oral, penicillinase susceptilbe
– good for penG ones, and GDS – also for (-) bacilli like H. influenzae, E. coli, P. mirabilis, Shigella and S. typhi - ticarcillin and ticarcillin + clavulanate
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- IV, penicillinase susceptilbe
– good in P. aeruginosa
– alternative for aerobic (-) bacilli like E. coli and Proteus mirabilis - piperacillin and piperacillin + tazobactam
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- used parenterally, good in 50% of Klebsiella and some (-) bacilli (if serious, add aminoglyocside)
- penicillinase susceptilbe
- T is a B-lactimatase inhibitor - cephalexin
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- 1st generation cephalo
– best against (+) cocci
– use for surface infections
– give orally - cefuroxime
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- 2nd generation cephalo
– best for (-) like sinusitis, otitis or LRIs like H. influenzae, B. fragilis and N. gonorrhoeae
– Parenteral admin - ceftriaxone
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- 3rd generation cephalo
- good for (-) bacilli like H. flu and N. gonorrhoeae
- can cross BBB so good foor E. coli or K. pneumoniae
- good for meningitis w/ (-) bacilli (P aeruginosa)
- parenteral admin - cefotaxime
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- 3rd generation cephalo
- good for (-) bacilli like H. flu and N. gonorrhoeae
- can cross BBB so good foor E. coli or K. pneumoniae
- good for meningitis w/ (-) bacilli (P aeruginosa)
- parenteral admin - ceftazidime
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- 3rd generation cephalo
- good for (-) bacilli like H. flu and N. gonorrhoeae
- can cross BBB so good foor E. coli or K. pneumoniae
- parenteral admin - cephalospoin considerations
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- don’t give if hx of Pen anapyhlaxis
– ok if hypersensitiviy or resistance - cephalospoin side effects
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- pain when given IM
- disulfiram-like reaction w/ alcohol
- hypoprothrombinemia and serious bleeding
– risk of superinfections is ↑ w/ 2nd and 3rd generation