Antibacterial Drugs Flashcards
sulfisoxazole
Intermediary metabolism: sulfonamide
-inhibit dihydropteroate synthase (1st step in folic acid synthetic pathway; PABA used as substrate)
-PABA (acid) required for folic acid synthesis in (most) bacteria
=an alternative substrate: Thymidine and DNA synthesis
-side effect: crystaluria (drug crystal formation in renal tubules), hemolytic anemia (rbc destroyed and removed from blood stream)
sulfamethoxazole
Intermediary metabolism: sulfonamide
-inhibit dihydropteroate synthase (1st step in folic acid synthetic pathway; PABA used as substrate)
-PABA (acid) required for folic acid synthesis in (most) bacteria
=an alternative substrate: Thymidine and DNA synthesis
-side effect: crystaluria (drug crystal formation in renal tubules), hemolytic anemia (rbc destroyed and removed from blood stream)
sulfacetamide
Intermediary metabolism: sulfonamide
-inhibit dihydropteroate synthase (1st step in folic acid synthetic pathway; PABA used as substrate)
-PABA (acid) required for folic acid synthesis in (most) bacteria
=an alternative substrate: Thymidine and DNA synthesis
-side effect: crystaluria (drug crystal formation in renal tubules), hemolytic anemia (rbc destroyed and removed from blood stream)
mafenide
Intermediary metabolism: sulfonamide
-inhibit dihydropteroate synthase (1st step in folic acid synthetic pathway; PABA used as substrate)
-PABA (acid) required for folic acid synthesis in (most) bacteria
=an alternative substrate: Thymidine and DNA synthesis
-side effect: crystaluria (drug crystal formation in renal tubules), hemolytic anemia (rbc destroyed and removed from blood stream)
trimethoprim
Intermediary metabolism
- bind and inhibit dihydrofolate reductase (2nd step for folic acid formation)
- reduce thymide synthesis (no useful/harmful product)
- additive effect to sulfonamide (used in combination)
- gram+ bacteria more sensitive
penicillin
Cell wall disruptor: penicillin
- have beta-lactam ring nucleus
- inhibit cell wall synthesis/maintenance, bind to specific proteins, bind to specific proteins (PBP=penicillin binding protein), prevents peptidoglycan strand crosslinking, causes osmotic disruption
- degraded by penicillinases or beta-lactamases of bacterial wall
- gram+ bacteria sensitive
- gram- bacteria resistant
- side effect: hypersensitivity (allergic) reactions, anaphylactic shock, GI upset
methacillin
Cell wall disruptor: penicillin
“derivative”
-have beta-lactam ring nucleus (inc GI tract stability, inc penicillinase resistance, inc spectrum of action)
-inhibit cell wall synthesis/maintenance, bind to specific proteins, bind to specific proteins (PBP=penicillin binding protein), prevents peptidoglycan strand crosslinking, causes osmotic disruption
-degraded by penicillinases or beta-lactamases of bacterial wall
oxacillin
Cell wall disruptor: penicillin
“derivative”
-have beta-lactam ring nucleus (inc GI tract stability, inc penicillinase resistance, inc spectrum of action)
-inhibit cell wall synthesis/maintenance, bind to specific proteins, bind to specific proteins (PBP=penicillin binding protein), prevents peptidoglycan strand crosslinking, causes osmotic disruption
-degraded by penicillinases or beta-lactamases of bacterial wall
ampicillin
Cell wall disruptor: penicillin
“derivative”
-have beta-lactam ring nucleus (inc GI tract stability, inc penicillinase resistance, inc spectrum of action)
-inhibit cell wall synthesis/maintenance, bind to specific proteins, bind to specific proteins (PBP=penicillin binding protein), prevents peptidoglycan strand crosslinking, causes osmotic disruption
-degraded by penicillinases or beta-lactamases of bacterial wall
amoxicillin
Cell wall disruptor: penicillin
“derivative”
-have beta-lactam ring nucleus (inc GI tract stability, inc penicillinase resistance, inc spectrum of action)
-inhibit cell wall synthesis/maintenance, bind to specific proteins, bind to specific proteins (PBP=penicillin binding protein), prevents peptidoglycan strand crosslinking, causes osmotic disruption
-degraded by penicillinases or beta-lactamases of bacterial wall
ticaricillin
Cell wall disruptor: penicillin
“derivative”
-have beta-lactam ring nucleus (inc GI tract stability, inc penicillinase resistance, inc spectrum of action)
-inhibit cell wall synthesis/maintenance, bind to specific proteins, bind to specific proteins (PBP=penicillin binding protein), prevents peptidoglycan strand crosslinking, causes osmotic disruption
-degraded by penicillinases or beta-lactamases of bacterial wall
clavulunate
Cell wall disruptor: penicillin
“additive”
-not active antibacterial compounds; additive to penicillins
-inhibit penicillinase (inc spectrum of drug action, inc activity of drug action)
sulbactam
Cell wall disruptor: penicillin
“additive”
-not active antibacterial compounds; additive to penicillins
-inhibit penicillinase (inc spectrum of drug action, inc activity of drug action)
cefazolin
Cell wall disruptor: cephalosporin
- contain beta-lactam ring (as penicillin)
- mechanism of action same as penicillins
- side effect: bone marrow depression, allergic reactions (anaphylactic shock)
cefoxitin
Cell wall disruptor: cephalosporin
- contain beta-lactam ring (as penicillin)
- mechanism of action same as penicillins
- side effect: bone marrow depression, allergic reactions (anaphylactic shock)
cefepime
Cell wall disruptor: cephalosporin
- contain beta-lactam ring (as penicillin)
- mechanism of action same as penicillins
- side effect: bone marrow depression, allergic reactions (anaphylactic shock)
cefazolin
Cell wall disruptor: cephalosporin
- contain beta-lactam ring (as penicillin)
- mechanism of action same as penicillins
- side effect: bone marrow depression, allergic reactions (anaphylactic shock)
cephalexin
Cell wall disruptor: cephalosporin
- contain beta-lactam ring (as penicillin)
- mechanism of action same as penicillins
- side effect: bone marrow depression, allergic reactions (anaphylactic shock)
cefotaxime
Cell wall disruptor: cephalosporin
- contain beta-lactam ring (as penicillin)
- mechanism of action same as penicillins
- side effect: bone marrow depression, allergic reactions (anaphylactic shock)
cefotaxamine
Cell wall disruptor: cephalosporin
- contain beta-lactam ring (as penicillin)
- mechanism of action same as penicillins
- side effect: bone marrow depression, allergic reactions (anaphylactic shock)
vancomycin
Cell wall disruptor: vancomycin
- no beta-lactam ring
- prevents peptidoglycan synthesis (cause osmotic disruption)
- action against gram+ bacteria
- side effect: anaphylactic shock, ototoxicity, nephrotoxicity
erythromycin
50S ribosome inhibitor
- blocks bacterial protein synthesis (inhibits 50S ribosome subunit function)
- use: similar to penicillin
- side effect: GI disturbance, liver injury (result of secretion into bile, *cholestatic hepatitis)
clindamycin
50S ribosome inhibitor
- blocks bacterial protein synthesis (inhibits 50S ribosome subunit function)
- side effect: colitis and diarrhea (due to GI tract superinfection, may be fatal)
tetracycline
30S ribosome inhibitor: tetracycline
- blocks bacterial protein synthesis (inhibits 30S ribosome subunit function)
- side effect: GI upset, liver damage, superinfection (GI tract), renal damage, vestibular damage