Mechanism Adverse effects
Sulfonamides Inhibits dihydropteroate (a step in folate
metabolism)
DHFR Inhibit dihydrofolate reductase (DHFR)
inhibitors  production of tetrafolate
Quinolones Block activity of gyrase and
topoisomerase IV at the step where
DNA has a double stranded break —
Presence of a break in DNA leads to
bacterial death
Rifamycins Block RNA synthesis by binding B-
subunit of RNA pol (binding within
DNA/RNA channel of pol stops nucleic
acid form progressing through channel)
Fidaxomicin Blocks RNA synthesis by binding RNA
pol-DNA complex before DNA strands
are separated to initiate RNA synthesis
Uses
Involve skin Hypersensitivity reactions; rash/itch
—(true anaphylaxis is rare)
Stevens-Johnson syndrome occurs rarely
(widespread death of skin and mucosa with
desquamation) — due to hemolysis with G6PD
Trimethoprim: rare suppressive effect on bone
marrow cells, reducing production of RBC, WBC
and platelets (occurs in patients with low folate) =
anemia, granulocytopenia, thrombocytopenia
Connective tissue: in animal models = weakened
cartilage in juveniles
Adults = rare tendintis and tendon rupture
May predispose to cardiac arrythmias
Discoloration of secretions (orange tears, urine,
saliva)
Can injury liver in presence of other sources of
hepatic injury
Can induce expression of hepatic metabolic
enzymes leading to increased metabolism of
other drugs
Well tolerated
Can be used as monotherapy for UTI (reaches
high conc. in urine bc excreted by urine)
Often used in combo with trimethoprim (synergistic
bc inhibit separate step in single pathway of
tetrahydrofolate)
Combo = broad spectrum (many Gram + and -)
Combo use: GI infections,
enterobacteriaceae
S. aureus (including most MRSA)
Trimethoprim is a selective inhibitor of bacterial
DHRF, it is rarely used as monotherapy
Often used in combo with sulfonamides (see
above) combo = broad spectrum
Several DHFR inhibitors, have different targets
Naladixic acid (used to treat UTIs)
Fluroquinolones (F atom  blood levels, tissue
penetration and half-life) — many kinds with
different spectrum (Gram +, Gram -, anaerobic,
mycobacterium)
Fluroquin has good activity against urinary and
resp pathogens = can be used as empiric therapy
for these
- Enterobacteria, P. arginosa, N. gonorrhea,
Streptococcus, Staphylococcus,
Mycobacteria, Anaerobic
Broad spectrum of activity but resistance quickly
develops if used alone (so when rifamycins used
for serious infections they are used in combo with
other antibiotics)
Lipid soluble (excellent penetration into tissues
and secretion)
Used in combo for treatment of mycobacterium TB
and staphylococcal endocarditis/arthritis
Used as monotherapy to eradicate colonizing N.
meningitides from people exposed during outbreak
C. difficile infection
Narrow spectrum of activity (poor lipid solubility)
Poorly absorbed from GI tract so it is concentrated
at site of C. diff infection
As effective as vancomycin for treatment of C. diff
infection (fewer relapses with fidaxomicin)