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SGU Pharmacology
Antimicrobials - Other Cell Wall Syn. Inhibitors
14
Medical
Professional
08/31/2010

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Term
Cephalosporins
Definition
Beta-lactams, bactericidal, same MOA as penicillins, same resisance, not active against enterococci or L. monocytogenes. As we move down from 1st to 3rd generation they cover more gm -ves and less +ves. Poor oral absorp, well dist, only (3) reach TC in CNS, all cross placenta, mainly eliminated by kidney except 2 (3). If given IM is painful at site, thrombophlebitis (IV),
Term
Cefazolin & Cephalexin (1)
Definition
Penicillin G sub, resistant to staph penicillinase, active against gm+ve cocci plus PEcK (P. mirabilis, E.coli, K. pneumoniae). NB that B. fragilis is not sensitive
Term
Cefaclor & Cefoxitin (2)
Definition
Gr8er activity against H. influenza, Enterobacter aerogenes (?) & Neisseria species
Term
Cefixime; Ceftriaxone & Cefotaxime (meningitis); Ceftazidine & Cefoperazone (P. aeruginosa) (3)
Definition
Ceftriaxone & Cefoperazone are excreted via bile, Cefoperazone also has a methyl-thiotetrazole grp thus causes: a) hypoprothrombinemia (vit. K1 admin can prevent this), b) disulfiram-like rxn (thus avoid alcohol)
Term
Cefepime (4)
Definition
Given parenterally only, wide spec, active against staph, strep, gm-ves (enterobacter, E.coli, pneumoniae, P. mirabilis, P. aeruginosa)
Term
Carbapenems
Definition
Synthetic beta-lactam antibiotic, good for mixed aerobic and anaerobic infections, is the beta-lactam of choice for enterobacter infections + extended-spectrum beta-lactamases producing gm-ves
Term
Imipenem & Meropenem
Definition
Resistant to most beta-lactamases thus active against (gm+ves and -ves, anaerobes & P. aeruginosa), IV, well dist, excreted by kidney (NB that imipenem is broken down at the PCT via an enzyme but cilastatin blocks this enzyme preventing the nephrotoxicity)
Term
Monobactams
Definition
Beta-lactam ring is not fused to another ring thus resistant to the axn of beta-lactamases
Term
Aztreonam
Definition
Targets aerobic gm-ve rods (including pseudomonas), no activity against gm+ves or anaerobes, given IV or IM and excreted in urine, nontoxic, lil immunological potential and lil cross-reactivity w/ other beta-lactam antibiotics
Term
Beta-lactamase inhibitors (Clavulanic acid, sulbactam, tazobactam)
Definition
contain the beta lactam ring but have lil activity so think of them as the sacrifice for beta-lactamases so that other beta-lactam antibiotics can have a go at the target organism
Term
Vancomycin
Definition
Bacterial glycoprotein, effective against multi-Rx resistant strains (MRSA, MRSE, PRSP (penicillin-resistant S. pneumoniae), enterococci), active mainly against staph, MOA is inhibiting bacterial cell wall syn + peptidoglycan polymerization -> weakened cell wall & damage to cell membrane. Can be used on allergic pts too, resistance is via: a) decreased permeability via plasmid, b) decreased binding to cell wall precursor via modification to D-Ala-D-Ala -> D-Lactate. Slow IV systemic infection or prophylaxis, given orally only to Tx C. difficile (& staph???), 95% excreted by glomerular filtration. A/Es: fever, chills, phlebitis at site, dose-related hearing loss, red neck syndrome (cause of rapid infusion -> flushing & shock), nephrotoxicity if comobined with another Rx w/ same effect. Synergistic w/ aminoglycosides to Tx enterococcal endocarditis (serious penicillin allergy?), vanco + gentamicin used as an alternative Tx plan for meningitis caused by PRSP
Term
Daptomycin
Definition
Bactericidal (), effective against resistant gm+ves (MRSA, enterococci, vancomycin-resistant strains of enterococci + S. aureus), ???, ???, 90% protein bound, renally excreted, A/Es: sonstipation, nausea, headache, insomnia, elevated creatine phosphokinases, recommended to discontinue coadmin of statins (why?)
Term
Bacitracin
Definition
Peptide antibiotic, interferes in late stage of cell wall syn., target gm+ves, there is marked nephrotoxicity thus use tropically only
Term
Fosfomycin
Definition
Inhibits very early stage in cell wall syn., inhibits cytoplasmic enzyme enolpyruvate transferase, active against gm+ve and -ve, given orally & IV, Txs uncomplicated UTIs
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