Cell Wall Synthesis Inhibitors Flashcards
Cephalosporins: antibiotic type
cell-wall synthesis inhibitor; B-lactam antibiotic
Cephalosporins: mechanism of action
inhibit cell-wall synthesis in stage 3: peptidoglycan cross-linking
Cephalosporins: susceptibilities
- cephalosporinase 2. less susceptible to penicillinase/B-lactamases than penicillins
Cephalosporins: pharmacokinetics
oral & parenteral admin; penetrates well into most tissues except brain/CSF; primarily renal extcretion
Cephalosporins: major classifications
first generataion (e.g. Cefazolin), second generation (e.g. Cefuroxime), third generation (Cefdinir), fourth generation (Cefepime), and “fifth”/next generation (ceftaroline)
Cephalosporins-1st Generation: spectrum
gram+ cocci (e.g. staph/strep but not enterococci/MRSA), gram- cocci, gram- bacilli (e.g. E. Coli UTIs)
Cephalosporins-2nd Generation: spectrum
maintain 1st gen. coverage + extended activity against gram- bacteria + anaerobes (bacteriodes); no pseudomonas
Cephalosporins-3rd Generation: spectrum
expanded gram- coverage (enteric gram- bacilli; e.g. N. gonorrheae); some have moderate antipseudomonal
Cephalosporins-4th Generation: spectrum
good against pseudomonas and S. pneumonaie
Cephalosporins-5th Generation: spectrum
MRSA
Cephalosporins: adverse reactions/tocivity
allergy/hypersensitivity (not as severe as penicillins, but don�t use if documented immeadeate penicillin rxn), nausea/vomit, superinfection w/broader spectrum agents, can intensify effect of oral anticoagulants
Carbapenems: antibiotic type
cell-wall synthesis inhibitor
Carbapenems: mechanism of action
inhibit cell-wall synthesis in stage 3: peptidoglycan cross-linking; bactericidal
Carbapenems: susceptibilities
B-lactamase resistant
Carbapenems: pharmacokinetics
parenterally only (IV/IM); penetrates all tissues including CSF; renal excretion
Carbapenems: major clinical uses
resrved for treatment of infections resistant to multiple drugs
Carbapenems: spectrum
- gram+ aerobic+anaerobic 2. gram- aerobic+anaerobic (e.g. bacteriodes) 3. enterocci 4. gram - bacilli (Pseudomonas aeruginos, E. Coli)
Monobactam: mechanism of action
inibit cell wall synthesis
Carbapenems: susceptibilities
B-lactamase resistant
Carbapenems: pharmacokinetics
no oral, use IM; widely distributed, including CSF; kidney excretion
Carbapenems: major clinical uses
gram - bacilli; syngerm w/aminoglycosides against P. aeruginosa
Penicillins: antibiotic type
cell-wall synthesis inhibitor; B-lactam antibiotic
Penicillins: mechanism of action
inhibit cell-wall synthesis @ stage 3: peptidoglycan cross-linking; bind to penicillin binding proteins (PBPs); trigger autolytic activity
Penicillins: susceptibilities
- penicillinase/B-lactamases 2. altered PBPs prevent effective activity
Penicillins: pharmacokinetics
moderately strong acids/acid stability dictates absorption; penetrates tissues poorly except inflamed tissues/membranes; kidney excretion
Penicillins: major classifications
- prototype penicillins 2. penicillinase-resistant penicillins 3. extended spectrum penicillins 4. B-lactamase inhibitor combinations
Prototype Penicillins: Examples and use
- Penicillin G: severe hospital infections 2. Penicillin V: acid-fast, mild-moderate infections
Penicillinase-restitant Penicillins: Examples and use
e.g. Oxacillin – use when penicillinase-producing organisms are encountered or renale insuffieciency (b/c renal+hepatic elimination)
Extended-Spectrum Penicillins: Examples and use
- Ampicillin & Amoxicillin: gram - bacilli (but are not resistant to penicillinase 2. Anti-pseudomonal penicillins
B-lactamase inhibitors: Examples and use
- Clavulanic Acid 2. Sulbactam 3. Tazobactam; potent-irreversible inhibitors of B-lactamase & extends spectrum of accompanying penicillin
Penicillins: Gram+ cocci spectrum
- Streptocci 2. Enterocci 3. Staphylococcus aureus
Penicillins: Gram- cocci spectrum
- Neisseria meningitis 2. Neisseria gonorrhea
Penicillins: Gram- bacilli spectrum
- H. influenzae 2. E. Coli 3. Pseudomonas aeruginosa
Penicillins: Anaerobes spectrum
Bacteriodes fragilis (gram - rod)
Penicillins: Adverse reactions
hypersensitivity/allergy possible; most common=reversible skin rash
Vancomycin: mechanism of action
cell-wall synthesis inhibitor @ stage 2 (polymerization of cell wall)
Vancomycin: pharmacokinetics
poor oral, usually IV; renal excretion
Vancomycin: clinical use/spectrum
reserved for when less toxic agents ineffective or not tolerated; gram+ cocci (MRSA, strep, staph) & anaerobes (Clostridium difficile)
Daptomycin: clinical use/spectrum
alternative to vancomycin; action at bacterial membrane –> cell death