Drug Class General Action Mode of Action Mechanism Selectivity Spectrum Cidal/Static Resistance Usage/Limitation Side Effect Representative Rx

Fosfomycin Block cell wall Structural analog of - Block reaction: - Cell wall structures Broad Bacteriocidal High frequency - Many
synthesis phosphoenolpyruvate UDP-GluNAc + PEP --> --> UDP-MurNAc unique to bacteria
(PEP) - Inactivate pyruvyl transferase by binding covalently to active site

D-Cycloserine Block cell wall Structural analog of D- - Block synthesis of UDP-MurNAc-Pentapeptide by: - Cell wall structures Broad Bacteriostatic - Tuberculosis - Neurotoxic
synthesis Alanine - Inactivate Alanine Racemase: L-Ala --> D-Ala unique to bacteria - UTI
- D-Alanine Ligase: D-ala+D-ala+ATP-->D-ala-D-ala - Infrequent usage due to its
- Competitive inhibition of both enzymes neurologic effect
Vancomycin Block cell wall Steric hindrance, Inhibits - Inhibit Transglycosylase Rxn: inhibits translocation of - Cell wall structures Narrow Bacteriocidal - Staphlococci Note: this is not
synthesis transpeptidation of D- peptidoglycan from cytoplasmic face to outer face of membrane) unique to bacteria - Enterococci effective for GN
alanine - Binds tightly to D-alal-D-ala residue of pentapeptide bacteria because it is
- Prevents precursor unit from binding to the synthase is too large of a
- Occurs on outer face of cytoplasmic membrane molecule to get
through membranes.
Bacitracin Block cell wall Membrane structure - Inhibit GCL-P regeneration from GCL-PP: - Cell wall structures Bacteriocidal - Topical tx of GP
synthesis precursor regeneration - Binds to the lipid pyrophosphate with Mg2+ or Zn2+, prevent unique to bacteria - Staphlococci
blockade dephosphorylation

B-Lactam Block cell wall Blocks - Prevents pentapeptide from cross-linking - Host does not have Narrow Bacteriocidal Block by B- - GP - Penicillin
synthesis Transpeptidation/Cross- - Inhibit/covalently bind to transpeptidase peptidoglycan (old) and lactamase that - New generation also effective - Cephalosporin
linking; substarte analog - Only effective in Actively Growing bacterias membrane structure Broad cleaves B-lactam against GN enteric and P. - Cephamycin
of D-ala-D-ala-COOH (new) ring. aeruginosa - Carbapenems
region of pentapeptide - Monobactam

Linezolid Inhibit protein Inhibits formation of 70S Prevents formation of the 70S ternary complex binding to the 23S 70S ribosomal subunit Bacteriocidal Not approved for the treatment
(oxazolidinones) synthesis initiation complex peptidyltransferase center of the 50S ribosomal subunit unique to bacteria (streptococci) of catheter-related bloodstream,
AND catheter-site, or GN infections
Bacteriostatic
(staphylococci
and
enterococci)
Aminoglycosides Inhibit protein - Bind 30S ribosomal - Cause misreading of mRNA (insertion of incorrect amino acid) - 30S ribosome subunit Broad, Bacteriocidal Altered 30S - GP/GN Ototoxic, Ineffective against
-Streptomycin synthesis, inhibitors subunit - Cyclic Polysomal Blockade (70S complex forms and falls apart) unique to bacteria; effective ribosome/target, - Aerobe only nephrotoxic intracellular bacteria.
Kanamycin Tobramycin of recognition - Faulty protein synthesis (translational misreading results in mutant actively transported into against decreased uptake - Antagonized by low pH, Induce biofilm
Gentamycin Neomycin outer membrane that cause membrane to be leaky. More drug can bacteria, not eukaryotic Pseudomo into cell, enzymatic Mg2+, PO42-, and anaerobiasis formation
Amikacin be taken up by cell) cells nas modifications of the
Paramomycin - Premature mRNA release aminoglycoside
Spectinomycin (an Inhibit protein - Bind 30S ribosomal - Formation of unstable 70S, does not inhibit: - 30S ribosome subunit Broad Bacteriostatic - Gonorrhea (B-lactamase-
aminocyclitol) synthesis subunit - Polyribosome unique to bacteria producing gonococci or patients
(recognition) - Misreading allergic to penicillin)
Tetracyclines Inhibit protein - Bind 30S ribosomal - Bind to 30S ribosomal subunit and inhibit binding of aa-tRNA to - Selectively uptaken Broad Bacteriostatic - Decreased uptake - Selected GP/GN
synthesis subunit the A site by bacteria but not host (OmpF porin) - Chlamydia
(recognition) - Active efflux - Mycoplasma
- Elongation factor- - Richettsiae
like proteins protect
30S
Chloramphenicol Inhibit protein - Bind reversibly to 50S - Bind reversibly with 50S subunit and alters tRNA structure - Does not bind 60S Broad Bacteriostatic - Plasmid-
synthesis (inhibit ribosomal subunit - Inhibit peptidyl transfer and block peptide elongation ribosome transferred
peptidyl transfer) - Cannot enter resistance
mitochondrial (acetyltransferase
membrane that catalyzes the
acetylaton os -OH
groups. Prevents
50S binding
Lincomycin Inhibit protein - Bind 50S ribosomal - Inhibit peptidyl transfer and block peptide elongation - Does not bind 60S Narrow Bacteriostatic - Methylation of - GP- very effective!
Clindamycin synthesis (inhibit subunit ribosome 23S ribosome - Staphylococcal
peptidyl transfer) prevents binding to - Anaerobic GN
50S - Bacterioides

Erythromycin Inhibit protein Bind 50S ribosome ~prevention of elongation, prevention of release of empty tRNA, - Does not bind 60S Medium Bacteriostatic Methylation of 23S Mycoplasma, Legionella,
Azithromycin synthesis, inhibit blockage of transpeptidation ribosome ribosome which Chlamydia, Campylobactor, and
Clarithromycin translocation prevents binding of GP in patients allergic to
(Macrolides) drug, hydrolysis of Penicillin
lactone ring by an
esterase, efflux of
Telithromycin Inhibit protein Bind within exit tunnel Bind within exit tunnel of the large ribosomal subunit, blocking the unique ribosome Bacteriostatic
drug
(ketolides) synthesis and block translocation exit of nascent polypeptides or
Bacteriocidal

Streptogramins Inhibit protein Dalfopristin: binds to 50S to prevent elongation and facilitates Staphylococci, streptococci, and
(natural antibiotic) synthesis, inhibit binding of quinupristin to the 50S. Quinupristin: premature release vancomycin-resistant
translocation of peptide chains from the ribosome. Synercid: QUINUPRISTIN + Enterococcus faecium
DALFOPRISTIN, alone each is bacteriostatic, together they are infections.
bacteriocidal

Sulfonamides Antimetabolite - Inhibit folate synthesis, - Competitive inhibition of Dihydropteric acid synthetase: - Bacteria synthesize Broad Bacteriostatic - GP/GN Only inhibit NEW
folic acid is essential in Guanosine -->--> Dihydropteric acid --> FH4 folate, while animal - Chlamydia synthesis of
the production of obtain folate through - Protozoa tetrohydrofolic acid.
thymidine and uridine. diet (bacteria lack - Acute UTI
uptake system) - Pneumocystis carinii with
trimethoprim

Trimethoprim Antimetabolite - Inhibit folate pool - Competitive inhibition of Dihydrofolate reductase: - Structural difference Bacteriostatic - Acute/chronic UTI Precludes the
cycling D2F--> FH4 between host and - GP/GN utilization of pre-
- Block cell from cycling existing folate pool microbe dihydrofolate - Pneumocystis carinii with existing pools of
reductase sulfonamides dihydrofolate.

Para-aminosalicylic Antimetabolite Similar to that of sulfonamides - TB (sulfonamides are not

Acid (PAS) effective against M.
tubercolosis)
Rifampin Inhibit RNA - Inhibit DNA-dependent - Binds beta-subunit of RNA-pol - Host RNA-pol not Narrow Bacteriocidal - GP (staph and streptococci)
Rifabutin synthesis RNA pol - Prevent transcription initiation sensitive - Neisseria
- Does not stop transcription in progress - Mitochondrial - Mycobacteria
membrane not - M. avium (rifabutin) (rifabutin)
permeable to rifampin

Quinolones Nalidixic Inhibit DNA - Inhibit DNA gyrase - Prevent DNA unwinding, blocking DNA replication, transcription, specifically inhibits Nalidixic Bacteriocidal - Mutation of DNA - Nalidixic Acid: UTI of GN
acid Norfloxacin synthesis repair bacterial DNA gyrases Acid: gyrase (E.coli, Proteus, Flebsiella,
Ciprofloxacin Ofloxacin (replication) Narrow - Decreased uptake Enterobactor, bur not
Levofloxacin All others: Pseudomonas). The rest ARE
Lomefloxacin Sparfloxacin Broad effective against Pseudomonas.

Metronidazole Inhibit DNA Disrupts DNA stucture, This is administered as a prodrug, It is inactive until the prodrug is Enzymes required to Narrow Bacteriocidal Mutations in the Treatment of anaerobic
(Flagyl) synthesis inhibits DNA replication, metabolized in vivo into an active form. The nitro group of convert drug to active oxidoreductases infections, H. pylori infections
causes DNA breaks and metronidazole is reduced by bacterial oxidoreductases to become form are present in that affect and Protozoal infections due to
secondary mutations active. some bacteria and not conversion to the Entamoeba histolytica and
host cells. pro-drug Giardia lamblia

Polymyxin Cell membrane - Membrane perforation - Hydrophobic tail inserts into cell membrane, hydrophilic head - LPS and PE specific Narrow Bacteriocidal - in GN bacteria, - Pseudomonas infections Nephrotoxic
Colistin damage binds to the polar region of phosphatidylethanolamine (PE) and LPS to bacterial cell wall structural
and disrupts cytoplasmic membrane modification of lipid
- High affinity for bacterial membrane PE, LPS A moiety of LPS,
- Association --> leaky membrane, active against GROWING and render OM
NON-GROWING cells impermeable to
drugs
Amphotericine B Cell wall disruption - Membrane perforation, - Amphoteric structure, the drug inserts into membranes - Ergosterol specific to Fungocidal - Mammalian cell - Antifungal (treatment of Nausea,
(polyene antibiotics) targets ergosterol! hydrophobic portion associates with sterols, forming hydrophilic fungal cell wall lack ergosterol systemic mycoses and topically vomiting,
"channel". in ointments) diarrhea,
- High affinity for fungal cell wall ergosterol nephrotoxic,
- Association --> leaky membrane and anemia
Azoles: fluconazole, Inhibit synthesis of Block the 14-alpha- Block the 14-alpha-demethylase - Ergosterol specific to Fungocidal changes in drug - Antifungal (Voriconazole is Side effects
itraconazole, ergosterol demethylase fungal cell wall target and effective against Aspergillus) not as bad as
ketoconazole, increased efflux Amphotericin
ravuconazole, from cell. B
posaconazole,
voriconazole
Terbinafine Inhibit synthesis of Inhibit Squalene epoxidase - Ergosterol specific to Fungocidal drug degradation, - Antifungal
(allylamines) ergosterol fungal cell wall increased target,
possible efflux
Glucan Synthesis Block fungal cell Inhibit 1,3-beta-glucan synthase - Ergosterol specific to Fungocidal increase beta- - Antifungal, effective against
Inhibitors/Echinocand wall synthesis fungal cell wall glucan synthase Azole resistant strains
ins Caspofungin expression
Micofungin Anidukafungin
Fluccytosine Fungal Inhibits fungal protein Repaces uracil with 5-flurouracil in fungal RNA. Inhibits thymidylate Fungocidal changes in genes - Antifungal
Antimetabolite synthesis synthetase via 5-fluorodeoxy-uridine monophosphate, interfering involved in
with fungal DNA synthesis DNA/RNA synthesis