Test 2: antibiotics Flashcards
Penicillin and Cephalosporins
Cell wall synthesis inhibitor: Blocks transpeptidation; extracellular
Bacitracin
Cell wall synthesis inhibitor: Complexes with inactive lipid, causes dolichol-P recycling; extracellular
Vancomycin
Cell wall synthesis inhibitor: Blocks elongation of peptidoglycan backbone; extracellular
Cycloserine
Cell wall synthesis inhibitor: D-ala analog interferes with transpeptidation; cytoplasm
Phsophonomycin
Cell wall synthesis inhibitor: PEP analog inhibits conversion of NAM to NAG; cytoplasm
Isoniazid (INH) and ethionamide
inhibits mycolic acid (TB drug that disrupts mycobacterial cell wall synthesis)
-similar structure to nicotinamide
Ethambutol
TB drug disrupting cell wall: inhibits arabinogalactan synthesis (major component of mycobacterial cell wall)
Aminoglycosides (streptomycin, gentomycin, neomycin)
Protein syntehsis inhibitor: blocks initiation of protein syntehsis; targets S12 of 30s subunit; targets polysomes, bactericidal
Macrolides (erythromycin, azithromycin)
-linezolid (new drug)
Protein syntehsis inhibitor: inhibits initiation complex formation, targets 50s; both cidal and static
Tetracycline
Protein syntehsis inhibitor: inhibits attachment of charged aminoacyl-tRNA, bacteristatic
Chloramphenicol
Protein syntehsis inhibitor: Inhibits peptidyl transferase on 50s; bacteristatic
Rifamycins (rifampin)
nucleic acid inhibitor: Inhibits DNA-dependent RNA polymerase, bactericidal that disrupts transcription, also anti TB therapy
Quinolones (Cipro) and Levoquin
nucleic acid inhibitor: Inhibits DNA gyrase and regulation, disrupts replication; bactericidal
Metronidazole/Flagyl
nucleic acid inhibitor: metabolites cause DNA strand breaks; induces fragmentation; bactericidal
Polyenes (Nystatin, amphoteracin B)
Cell membrane inhibitor: antifungals that complex with ergosterol
Imidazoles (miconazole and ketoconazole)
Cell membrane inhibitor: antifungal; blocks ergosterol synthesis
Polymyxins
Cell membrane inhibitor: targets gram negative organisms; acts like a detergent and makes membranes leaky
Sulfonamides (SMX)
antimetabolic: competes with PABA in folate biosynthetic pathway
Trimethoprim (TMP)
Antimetabolic: Inhibits dihydrofolate reductase; bacteriostatic
Penicillin+Streptomycin
penicillin enhances uptake of streptomycin
Trimethoprom+sulfamethoxazole
blocks consecutive steps in folate metabolism
Augmentin (amoxicillin+clavulonic acid)
clavulinic acid is beta lactamase inhibitor, used to help with MRSA
Ideal antibiotic characteristics
- Bactericidal
- non-resistant
- non-allergenic
- stable under physiologic conditions
- SELECTIVE
Therapeutic margin
Effective dose/toxic dose