Anifolate Drugs:

A)Sulfonamides:
MOA: PABA analogue, comp inhibit dihydropteroate synthase
-bacteriostatic
-not active against pseudo
Oral: sulfisoxazole and sulfamethoxazole- UTI
Sulfadiazine- toxoplasmosis
Sulfadoxine- malaria
Oral, nonabsorbable (for bowel stuff)
-Sulfasalazine
Topical: Silver sulfadiazine- burn
-sodium sulfacetamide opthalmic- eyes bacterial conjunctivitis
IV: sulfamethoxazole/trimethoprim (SMX/TMP)

Adv effects: Hematologic (anemia, thrombocytopenia) esp in patients G6P dehydrogenase deficient
-allergic rxn: skin rashes
-idiosyncratic: Stevens-johnson Syndrome
B) Trimethoprim (TMP)
MOA: inhibits BACTERIAL DHF-reductase
indic: UTI
C) Pyrimethamine:
MOA: inhibits PROTOZOAN DHF-reductase
indic: malaria, toxoplasmosis...
Resistance: over production of DHF -reductase
Adv effects: Hematologic (as above) and Hyperkalemia
D) SMX/TMP combo (IV)
5:1 ratio. Ratio is always same, and dose according to TMP
indic : UTI
active against CA-MRSA
Dont use for: strep pneumo, nosocomial (pseudo)

DNA Gyrase inhibitors:
A)Fluoroquinolones: NOT FIRST LINE THERAPY
Resistance:- mutation in quinolone binding region
-Efflux pump (moxifloxacin is less effect because its bulky)
Activity: ALL QUINOLONES are active against atypicals (mycoplasma, mycobac TB)
Second Gen: bind only one topoisomerase
Ciprofloxacin: G(-) -> DOC for GI infections
Levofloxacin G (-) and strep pneumo
*Can use for Pseudo. G(-)*
Third gen: bind both topoisomerase II and IV
Moxifloxacin: anaerobic + Strep pneumo
*remember, moxifloxacin has bulky side chain, is less affected by efflux pump
*also, dont use moxi for UTI.
Gemifloxacin: strep pneumo
*better G(+) and covers Strep Pneumo. BUT lost Pseudo activity. dont use for nosocomial*
PK: Concentration-dependent (want high peaks!)
ADME: good oral bioavailability -- high! Almost same as IV and oral
good distribution, including BONE!
metab/elim= renal adjustment needed. Use for UTI
*EXCEPT Moxifloxacin. dont use for UTI*
Adv effcts: Tendonitis (black box warning), cartilage damage
-prolonged QT interval (torsades de poites)
-Seizures!
(rash not very common)

adv: ONLY oral agent for pseudo
disadv: resistance is high
c.diff is higher than others