Pharmfinal
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- Disrupts cross linkage of peptidoglycan polymers
- Penicillin
- Used to increase the spectrum of activity of various penicillins
- Beta-lactamase inhibitors
-
Used to treat primarily Gram +
-Suseptible to beta-lactamase -
Natural Penicillins
Penicillin G -
Similar to natural penicillins plus are resistant to penicillinase
-Widely used against penicillinase producing Staphylococci -
B-lactamase resistant Penicillin
Methicillin -
Improved activity against Gram + and - relative to natural penicillins.
-Suseptible to B-lactamase -
Extended spectrum Penicillin
Amoxicillin - Adverse effects of Penicillin
-
Allergies
Cross-reactance with most B-lactam antibiotics -
Effective against penicillinase producse S. aureus
Used in patients who exhibit delayed penicillin allergy
Range in spectrum of action (across generations) -
Cephalosporins
Cefazolin (Primarily Gram+) - Adverse effects of Cephalosporins
-
Nephrotoxicity
Hypersensitivity Reactions
Cross-reactions b/t cephalosporins and penicillins --> contraindicated in those with penicillin anaphylaxis -
Effective against Gram - bacteria (including those that produce B-lactamase)
Patients who are allergice to Penicillins and Cephalosporins are generally ok with these - Monobactams
-
Very broad spectrum of activity (Both Gram + and -)
Very resistant to B-lactamase - Carbapenems
-
Non B-lactam Cell Wall Synthesis Inhibitor
Active only against Gram +
Useful for treatment of MRSA
Used to treat staph. infections in those allergic to penicillin and cephalosporins - Vancomycin
-
Prevents translocation of tRNA from the A site to the P site
Extended spectrum
Very active against Gram + and some Gram -
BACTERIOSTATIC
**Used to replace B-lactam antibiotics for allergic individuals
-Resistance: Macrolide efflu -
Macrolides
Clarithromycin -
Broad spectrum active against Gram + and -
BACTERIOSTATIC
-Resistance: reduced permeability of cell membrane, hydrolysis of drug, modification of ribsomal subunit - Clindamycin
-
GI disturbances are fairly frequent
Antibiotic-induced diarrhea in up to 20% of patients - Clindamycin
-
Bind to 30s and directly blocks the binding of tRNA to the acceptor site
Broad spectrum
Very active against Gram + and -
BACTERIOSTATIC
**Resistance: Efflux pumps
ONE OF THE MOST LIKELY ANTIBIOTICS TO CAUSE A SUPERINFECTION - Tetracyclines
-
Inhibits bone growth
Permanently discolors teeth
Superinfection
-Broad Spectrum
-Orally administered
-Incompletely absorbed - Adverse effects Tetracyclines
-
BACTERICIDAL
Inhibits ribosomal function by blocking initiation of subunits and translocation.
Causes miscoding in peptide chain
Most effective against Gram -, limited activity against Gram +
Commonly administered w/ cell wall inhibit - Aminoglycosides
-
Auditory/vestibular toxicity almost always
Nephrotoxicity (8-20%)
Neuromuscular Blockade - Adverse Effects of Aminoglycosides
-
Inhibition of DNA integrity
Prodrug
BACTERICIDAL
Concentration-dependent
Active against obligate anaerobes only
Active against both Gram + and -
Used to treat antibiotic-induced diarrhea - Metroidazole
-
Inhibition of DNA transcription
Inhibits DNA gyrase
BATERICIDAL
Can treat eukaryotic bacteria (no DNA gyrase) with high doses
Most effective orally admin. drugs for a wide variety of infections (UTI & Traveler's diarrhe) - Quinolones
-
Can destroy cartilage in young people
Not used in children under 17 or during pregnancy - Quinolones
- Suseptible to B-lactamase
-
Natural and Extended Spec. Penicillin
Cephalosporins