Cell Wall Inhibitors Flashcards
penicillin G
penicillins:
Acid-labile
parenteral admin (IM usually) IV for serious
Procaine and benzathine added in IM injection
Water-insoluble, slow release
Adverse Effect:
- Allergy
- Dose dep. neurotoxicity and seizures
- STEVEN JOHNSON syndrome
- rashes, swelling
penicillin V
penicillins:
Acid stable
Oral Admin
Absorption 65%
oxacillin
beta–lactamase resistant
Hepatitis at high levels
Use to treat penicillinase containing staph and strep
amoxicillin
extended spectrum
Aminopenicilin
Better absorption
- not affected by food
Prophylaxis against bac endocarditis
ampicillin
extended spectrum
Aminopenicillin
piperacillin
extended spectrum
Ureidopenicillin
Parenteral
Anti-pseudomonal
Reserved for severe infections caused by Klebs. and Pseudomonas
- Combo with aminoglycoside to resist resistance
carbenicillin
extended spectrum
carboxypenicillin
Parenteral administration
Anti-pseudomonas
clavulanic acid
beta lactamase inhibitors
sulbactam
beta lactamase inhibitors
tazobactam
beta lactamase inhibitors
cefazolin
cephalosporins:
1st generation:
Broadest spectrum against gram + cocci
Effective against gram - bacilli
cefuroxime
cephalosporins:
2nd generation:
Only group to kill ANAEROBES
cefotaxime
cephalosporins:
3rd generation:
Anti-pseudomonal/pneumococcal
Serious gram - infections
Meningitis, pneumonia, gonorrhea
MOST widely used in treatment of children/infants with moderate to severe infections
cefepime
cephalosporins:
4th generation:
Anti-pseudomonal
High resistance to B lactamase for treating ENTEROBACTER and PENICILLIN-RESISTANT streptococci
imipenem
carbapenems:
Broadest activity
B lactam ring that binds more efficiently than pens/cephs
Resistant to B lactamases
- However, induce expression of those that affect cephalosporins and B lactams
Parenteral
Renal metabolism and inactivation
ADMINISTER WITH CILASTATIN to prevent metabolism
meropenem
carbapenems
cilastatin
carbapenems
peptidase inh
aztreonam
monobactams:
Anti pseudomonas
Resistant to B lactamase
Gram - UTI
Lower RTIs
Systemic infection
bacitracin
other:
Cell wall synth inhibitor
Depletes lipid carrier for PDG synth
TOPICAL only, poorly absorbed
NARROW (g+, Neisseria. T pallidum)
Toxicity:
- Severe nephrotoxicity
USE:
- Skin
- Opthalmologic infections
Good in combination with polymyxin B
cycloserine
other
Cell wall synth inhibitor
Blocks step 2 in PDG synth
- Analog of D-ala
Oral
Good CNS penetration
Active form in URINE
Toxicity:
SERIOUS CNS
Reversible
Broad spectrum
Restricted second-line therapy for M. tuberculosis
daptomycin
other
Cell membrane agent
Membrane depolarization
Bactericidal
IV administration
RENAL elimination
Vanc spectrum
Adverse effects:
- MYOPATHY
fosfomycin
other
Cell wall synth inh.
Block Step 1 PDG synth
- analog PEP
Broad Spectrum (G- also)
Toxicity:
- diarrhea, vaginitis
Use:
- Oral treatment of uncomplicated UTIs (E. faecalis and E. coli)
Excreted unchanged in URINE
vancomycin
other
Non-beta lactam
Mechanism:
- Binds D-ala-D-ala terminus
Blocks X linking of PDG by binding substrate
Rapidly bactericidal for dividing bacteria
Exception (static in enterococcus)
IV administration
Rarely, oral: poor absorption
Distribution excellent (bone, CNS if meninges inflamed)
Renal excretion
Narrow spectrum
Gram + mainly MRSA
Resistance:
- 2 mech:
- VRE: enterococcus vanA, vanB, van C genes make different wall subunits
- VRSA: Overexpression of D-ala-D-ala
Toxicity:
- Red man
- Ototoxicity and nephrotoxicity
Synergistic with aminoglycosides but ototoxic also
nafcillin
beta-lactamase inhibitor