Pharm Respiratory Moa

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Trim-Sulfa

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bacteriostatic and sometimes bacteriocidal only when given together; always static when given alone

Sulfamethoxazole: inhibits dihydropteroate synthetase
Trimethoprim: blocks dihydrofolate reductase
Overall: synthesis of tetrahydrofolate is blocked (needed for DNA synthesis)

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Inhibitors of protein synthesis

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chloramphenicol
tetracyclines
macrolides
clindamycin
aminoglycosides*
linezolid*

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Inhibitors of protein synthesis are generally....

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bacteriostatic
Exception: aminoglycosides and linezolids

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Inhibitors of cell wall synthesis

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penicillins
carbapenems
monobactams
cephalosporins
vancomycn
telavancin
isoniazid
ethambutol*
bacitracin

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Inhibitors of cell wall synthesis are...

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generally bactericidal
Exceptions: ethambutol

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Inhibitors f DNA/RNA synthesis

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fluoroquinolones
rifampin
nitrofurantoin

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Inhibitors of DNA/RNA synthesis are....

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generally bactericidal

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Increase bacterial membrane permeability

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polymixin B
colistin (polymixin E)

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Drugs that increase bacterial membrane permeability are generally...

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bactericidal

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Beta lactams

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penicillins, carbapenems, monobactams, cephalosporins

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Penicillin

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beta lactam
inhibits cell wall synthesis by binding covalently to PBP (transpeptidase) to prevent peptidoglycan synthesis

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carbapenems

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beta lactam
inhibits cell wall synthesis by binding covalently to PBP (transpeptidase) to prevent peptidoglycan synthesis

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monobactams

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beta lactam
inhibits cell wall synthesis

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cephalosporins

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beta lactam
inhibits cell wall synthesis by binding covalently to PBP (transpeptidase) to prevent peptidoglycan synthesis

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vancomycin

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inhibits cell wall synthesis by binding covalently to D-ala-D-ala of peptide chain

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isoniazid

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inhibits cell wall synthesis
first activated by mycobacterial catalase-peroxidase (TB) to an active metabolite that can covalently bind to acyl carrier protein and beta-ketoacyl carrier protein synthetase..prevents mycolic acid synthesis

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ethambutol

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inhibits cell wall synthesis by inibiting arabinosyl transferase which prevents polymerization of arabinoglycan (mycobacterial cell wall thing)
bacterostatic

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bacitracin

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inhibits cell wall synthesis

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polymixin B

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increases bacterial membrane permeability

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polymixin E/colistin

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increases bacterial membrane permeability

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Fluroquinolones

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inhibits RNA/DNA synthesis by inhibiting topoisomerase 2 and 4 which prevents relaxation of positive supercoiled DNA that is needed for replication and separation of replicated chromosomal DNA

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Rifampin

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inhibits RNA/DNA synthesis by binding to beta subunit of bacterial DNA dependent RNA

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Nitrofurantoin

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inhibits RNA/DNA synthesis
bacterial enzymes reduce nitrofurantoin to reactive intermediate that dmages bacterial DNA...death!

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Chloramphenicol

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inhibits protein synthesis

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Tetracyclines

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inhibits protein synthesis by binding to A site of 30S of bacterial ribosome to prevent binding of aminoacyl tRNA

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Macrolides

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inhibits protein synthesis by binding to 50S subunit of bacterial ribosome which inhibits translocation from A to P

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clindamycin

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inhibits protein synthesis by binding to 50S subunit of bacterial ribosome which inhibits translocation from A to P

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Aminoglycosides

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inhibits protein synthesis by binding to 30S subunit to block initiation complex and allow misreading of mRNA and break up polysomes
BACTERICIDAL

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Linezolid

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inhibits protein synthesis by binding to 23S ribosomal RNA of 50S subunit to block assembly of 70S complex
bactericidal against some drugs

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Oxacillin, nafcillin

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not degraded by s. Aureus penicillinase

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Ceftaroline

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only drug in which MRSA is not resistant

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Oxacillin, nafcillin, cefazolin

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work on MSSA

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Penicillin G

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works on PSSA

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Ceftaroline

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works on MRSA

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Probenecid

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inhibits renal acid transport system so increases half life of penicillin G

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aztreonam

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inhibits cell wall synthesis by binding covalently to PCP and prevent peptidoglycan synthesis

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Telavancin

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inhibits cell wall synthesis by binding covalently to D-ala-D-ala of peptide chain (like vancomycin) AND rapidly depolarizes bacterial PM to increase permeability...death!

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Daptomycin

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binds to bacterial membranes to cause depolarization, loss membrane potential, death

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Fidaxomicin

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inhibits RNA synthesis (and therefore protein synthesis) by inhibiting bacterial RNA pol

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Pyrimethamine-sulfadizaine

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Sulfadiazine: inhibits dihydropteroate synthetase
Pyrimethamine: blocks dihydrofolate reductase
Overall: synthesis of tetrahydrofolate is blocked

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Rifabutin

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prevents RNA synthesis by binding to Beta subunit of bacterial DNA dependent RNA pol

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Pyrazinamide

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interferes w/ synthesis of mycolic acid by affecting gene for FA synthase 1

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Streptomycin

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binds to 30S to block formation of initiation complex and cause misreading of mRNA and break up polysomes

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Amphotericin B

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binds to ergosterol in fungal cell membranes to create pores

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Nystatin

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increases permeability of cell wall to cause loss of IC macromolecules and ions..death!

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beta lactamase inhibitors

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clavalunate, sulbactam, tazobactam

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clavalanate

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beta lactamase inhibitor

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sulbactam

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beta lactamase inhibitor

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tazobactam

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beta lactamase inhibitor

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Aminopenicillins

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extended spectrum PCNS
Ampicillin, amoxicillin
destroyed by beta lactamases so must combine w/ beta lactamase inhibitor

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amoxicillin

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aminopenicillin

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ampicillin

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aminopenicillin