TEST 2 Antimicrobial Pharmacology 1 General principles Flashcards
Define Bactericidal agent?
- Ideal scenario for killing bacteria.
- Lethal to susceptible microorganisms
- Penicillins and Cephalosporins
Define Bacteriostatic Agent
- Inhibitory to growth of susceptible micro-organisms.
- Sulfonamides
Define Post-antibiotic effect (PAE)
- Persistent effect of an antimicrobial on bacterial growth following brief exposure of organisms to a drug.
- Aminoglycosides & fluoroquinolones
What mechanisms of action are used by antimicrobial agents
- CPM - CD
- Inhibitors of
- Cell Wall synthesis
- Protein synthesis or structure
- Metabolism
- Interferes
- Cell membrane function
- DNA/RNA synthesis
What antimicrobial agents inhibit Cell wall synthesis?
- PCCA - VBC
- Penicillins/Cephalosporins/Carbapenems/Aztreonam
- Vancomycin
- Bacitracin
- Cycloserine
How do Penicillins/Cephalosporins/Carbapenems/Aztreonam inhibit cell wall synthesis?
Prevents cross-linking of peptidoglycan strands by inhibiting transpeptidases.
How does Vancomycin inhibit cell wall synthesis?
Inhibits peptidoglycan synthetase and polymerization of linear peptide.
Describe Aminoglycosides?
- Inhibits Protein Synthesis/structure
- Inhibits 30S ribosome
- Causes misreading of mRNA.
Describe Chloramphenicol?
- Inhibits peptidyl transferase and peptide band formation
Describe how Erythromycin, clindamycin, lincomycin inhibit protein synthesis?
Inhibits 50S ribosome
Describe Tetracyclines
- Inhibits binding of aminoacyl tRNA to ribosome
- 30S ribosome
What does Streptogramins/Linezolid effect?
- Inhibit protein synthesis/structure by acting on 23S ribosome.
What is the effect of Rifampin?
Interference with DNA/RNA synthesis by inhibiting DNA-dependent RNA polymerase.
What is the effect of Fluoroquinolones?
Interferes with supercoiling of DNA by action on DNA gyrase (topoisomerase II)
What is the effect of Isoniazid and trimethoprim?
Prevents synthesis of lipids and thus disrupts metabolism
What is the effect of Sulfonamides and trimethoprim?
Prevents synthesis of folic acid and thus disrupts metabolism
What are the basic steps in Antimicrobial treatment?
- Determine infection site
- Determine causative organism
- Select a drug based on:
- Sensitivity of the microorganism
- Physiochemical properties
- Toxicities of the drug
- Patient characteristics
- Follow patient for clinical response
- Alter therapy as necessary
What are the 5 pharmacologic considerations
- Route of administration
- Distribution
- Routes of Elimination
- Drug interactions
- Allergies
How do bacteria resist Penicillins/Cephalosporins?
- B-lactamases
- PBP changes
- Porin channel changes
How do bacteria resist Aminoglycosides?
Enzyme Inactivating
How do bacteria resist Macrolides?
Methyltransferases that alter
drug binding sites on 50S
ribosomal subunit
How do bacteria resist Tetracyclines?
Transport systems that pump drug out of the cell.
How do bacteria resist Sulfonamides?
Increased PABA formation
Target enzyme sensitivity
How do bacteria resist Fluoroquinolones?
Target enzyme changes drug efflux
What is the antimicrobial Ace in the hole?
Aztreonam (Anaphylaxis) AAA
What is the last resort antimicrobial agent?
Colistin