Sulfonamides & Misc Abx Flashcards
Sulfonamide Drugs
Sulfamethoxazole+Trimethoprim, Co-trimoxazole, TMP-SMX (Bactrim) - oral and parenteral
Sulfamethoxazole - oral
Sulfasalazine - oral
Silver Sulfadiazine - topical
DOC for UTI
Bactrim - slow excretion and high urine concentration
Sulfasalazine Use
Ulcerative Colitis (GI action)
Silver Sulfadiazine Use
Burns - topical application
Sulfonamide MOA
Antimetabolite, competes with para-aminobenzoic acid (PABA) for incorporation into folic acid:
PREVENTS FOLIC ACID SYNTHESIS
Bacteriostatic, but becomes cidal in the urinary tract
TMP-SMX MOA
SULFAMETHOXAZOLE inhibits folic acid synthesis
TRIMETHOPRIM prevents reduction of dihydrofolate to tetrahydrofolate essential for one carbon transfer
This is a SYNERGISTIC relationship when coadministered as in Bactrim
Sulfonamide Resistance
Increased production of an essential metabolite or drug antagonist (PABA)
Efflux pumps
Decreased permeability
Alternative metabolic pathway for synthesis of essential metabolite (plasmid)
Sulfonamide Spectrum
G+ and G- (generally static unless in the urinary tract)
Sulfonamide Uses
UTI (first attacks) - DOC is Co-trimoxazole (Bactrim)
Chlamydia (second line) - DOC is azythro or tetracycline
Moraxella, E. Coli, Klebsiella, Proteus, Salmonella, Vibrio sp, Burkholderia, Nocardia
Bactrim Administration
Oral - absorption is adequately rapid
Cotrimoxazole is available IV, but is RARELY used!
Sulfa metabolism
Liver primarily as acetylated products and excreted through the kidney.
Urine concentration is 10-20x that of plasma
Sulfa contraindications
Near term pregnancies (crosses placenta and bbb)
Nursing mothers (excreted in breast milk)
Premature or jaundiced infants (immature liver)
Infants <2 months (displaces bilirubin)
Sulfa Toxicities
Aplastic anemia (G6PD deficient - avoid at end of preggo)
Photosensitivity
Hypersensitivity (2nd to PCNs)
SJS and TEN
Kidney and Liver damage, microscopic hematuria
Peripheral nerve damage
KERNICTERUS (bilirubin displacement)
Daptomycin MOA
Binds bacterial membranes and causes rapid depolarization of membrane potential.
Bactericidal against G+ bacteria (MRSA, MSSA) - concentration dependent
Daptomycin Spectrim
Aerobic and Anaerobic G+ bacteria