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11 Cards in this Set

  • Front
  • Back

Beta Lactam - Penicillins

MOA


- β-lactam ring is structural analogue of the D-alanine that is involved in cross-linking


- this facilitates binding of β-lactamring to active site of PBPs.


- Inhibits action of PBP --> no enzyme to catalyse reaction --> no cross-linking of peptidoglycan (cell wall) --> accumulation of cell wall precursors --> production of autolytic enzymes --> cell lysis.




Examples


- Penicillin G and V.


- Ampicillin and Amoxycillin (additional G- use)


- Flucloxacillin, Dicloxacillin (beta-lactamase resistant)


- Clavulanic acid (beta lactamase inhibitor; given with amoxycillin)


- Ticarcillin, Piperacillin (anti-Pseudomonal)

Beta Lactam - Cephalosporins

MOA


- similar structure to Penicillins; less susceptible to beta-lactamases.


- cover broader range of pathogens




Examples


1st Gen: Cephalexin, Cephazolin


2nd Gen: Cefaclor, Cefurozime


3rd Gen: Cefotaxime, Ceftriaxone


4th Gen: Cefipime, Ceftazidine

Glycopeptides

MOA


- bind to AA preventing enzymes forming cross-links.


- interferes with cell wall peptidoglycan synthesis




Examples


- Vancomycin, Teicoplanin

5-Nitroimadazoles

MOA


- Inhibitors of Nucleic Acid Synthesis (ie. DNA)


- exact mechanism unknown


- enters microbial cell, reduced, activated


- conc gradient facilitates infusion


- reduced intermediate products interact with intracellular targets




Examples


- Metronidazole, Tinidazole

Fluoroquinolones

MOA


- Inhibitors of Nucleic Acid Synthesis


- inhibits DNA gyrase, which removes helical twists for replication


- inhibits topoisomerase IV, which allows chromosomes to separate


- interferes with DNA synthesis




Examples


- Nofloxacin, Ciprofloxacin, Moxifloxacin

Aminoglycosides

MOA


- blocks protein synthesis


- enters by active transport


- irreversibly binds to 30S ribsome sub-unit.


- freezes initiation complex (50S can't attach)


- slows down protein synthesis that's already commenced.






Examples


- Gentamicin

Macrolides

MOA


- blocks protein synthesis


- Binds to 23S ribosomal RNA in 50S subunit.


- prevents transfer of peptidyl tRNA from A-site to P-site


- Prevents formation of peptide bonds and transfer of AA




Examples


- Erythromycin, Clarithromycin, Roxithromycin, Azithromycin


- newer have more reliable absorption and longer t 1/2 - A>R>C>E

Amphenicols

MOA


- blocks protein synthesis


- binds to 50S ribosome subunit


- blocks action of peptidyl transferase and prevents peptide bond formation.




Example


- Chloramphenicol

Tetracyclines

MOA


- blocks protein synthesis


- binds reversibly to 30S subunit


- distorts subunit


- anticodons of charged tRNA can't align properly with codons of mRNA.


- blocks bacterial translation




Example


- Tetracycline, Doxycycline, Minocycline, Tigecycline

Metabolic Analogues - Sulphonamides

MOA


- metabolic analogue of para-aminobenzoic acid (PABA)


- inhibits dihydropteroate synthase


- stops folate synthesis




Example


- Sulphonamide

Metabolic Analogues - Trimethoprim

MOA


- metabolic analogue of dihydrofolic acid


- inhibits dihydrofolate reductase


- inhibits folate synthesis




Example


- Trimethoprim