Antibiotics Flashcards
Beta Lactams Site and examples
Beta Lactam Ring is the active site
Examples include: Penicillins Cephalosporins Carbapenems Monobactams
Used for Gram Negative Bacteria resistant to other antimicrobials?
Carbapenems (imipenem and meropenem) and monobactams (aztreonam)
Used for treatment of gram - bacteria determined to be resistant to other antimicrobials
Reserverd for humans/last resort
Beta Lactam MOA
Disrupt cell wall synthesis by binding to Penicillin binding proteins (PBP’s) making them unavailable for cell wall synthesis
Effective only against actively replicating bacteria
Require cell wall to be effective
Inherent resistance to beta lactams
Mycoplasma and L-form bacteria
Why does the spectrum of activity for beta lactam drugs differ?
Bacteria can make numerous PBPs ( some e coli can make 9 distinct pbps)
Penicillin G
Gram + aerobes
Especially streptococcus and suceptible enterococci
Limited Gram - but effective against pasteurella multocida
Aminopenicillins
Ampicillin and amoxicillin
Expand on gram - activity of penicillins
Amoxi first line to treat UTI
Pseud aeruginosa inherently resistant
Ureidopenicillins and Carboxypenicillins
Piperacillin and ticarcillin
Expanded spectrum against organisms like pseud aeruginosa
Potentiated Penicillins
Contains inhibitor for beta-lactamase
Amoxiclav
Clavulonic acid is an antibiotic with limited activity but high affinity for some beta lactamases
Clavulonic acid STRONGER than beta lactamase inhibitor sulbactam in IV Unasyn
Most important small animal pathogen?
Staphylococcus pseudintermedius
Produces beta-lactamase (Gram - can produce many beta lactamases)
Cephalosporins
Beta-Lactams with variable activity
1st-3rd gens: 1st effective against gram +, limited gram - to 3rd effective against gram - , limited gram +
First : Cephalexin and cefazolin
Second: Cefamandole, cefmetazole
Third: Cefpodoxime, cefovecin, and ceftiofur
Fourth: cefquinome
Fluroquinolones
Gram - activity, limited gram +
Aerobic
Use based on culture and sens
Concentration dependent, dosed daily
Fluroquinolones MOA
Bind DNA gyrase and topoisomerase enzymes
Leads to cell death
Fluroquinolone Examples
Enrofloxacin - Baytril Marbofloxacin - Zeniquin Difloxacin - Dicural Orbifloxacin - Orbax Pradofloxacin - veraflox
Fluroquinolone Exception?
Pradofloxacin has expanded gram + and anaerobic activity
Ribosome Binding Antimicrobials
Aminoglycosides, Tetracyclines, Chloramphenicol, and Macrolides/Lincosamides are protein synthesis inhibitors
Target 50s or 30s subunits (targeting same one with two will be antagonistic)
30s: Tetracyclines and Aminoglycosides
50s: Chloramphenicol and Macrolides/Lincosamides
Protein Synthesis inhibitors are Bacteri_____?
Bacteriostatic
EXCEPT for the aminoglycosides: Bactericidal
Aminoglycosides
Aerobic ONLY (oxygen dependent transport into cells)
Gram - primarily
Useful for MDR organisms
Only available in topical and parenteral formulations d/t low gut bioavailability
Tetracyclines
Relatively broad spectrum
Effective against atypicals: Reickkettsials, Leptospira, and Mycoplasma
Wide variety of aerobic bacteria, but resistance widespread among Staph pseuds, E. Coli’s
Chloramphenicol
Very broad spectrum
4 Quadrant:
One of few reliable for MRSP
Macrolides and Lincosamides
Mainly Gram +
Aerobic
Exception: Erythromycin is a macrolide— drug of choice for gram - camplyobacter
Clindmycin most widely used Lincosamide and also has anaerobic activity
Azolides
Derived from macrolides
Azithromycin
Off-label
TMS
Also Ormetroprim-sulfamethoxazole (Primor)
Each drug targets different portion of bacterial folic acid synthesis
Gram + and -
No Anerobic
Bacteristatic individually, together bactericidal
Rifampin
Rifamycin antimicrobial that targets RNA synthesis
Aerobic
Single point mutation can lead to resistance, always use in combo
Mycobacterial infections
Nitrofurantoin
Mechanism poorly understood
UTIs only
Aerobic
E. coli, staph, entero