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					                    ABX - Non-lactam Cell Wall inhibitors + Replication Inhibitors + Antifolates
Non-Lactam Cell Wall Inhibitors                                                      Replication Inhibitors                                                   ANTI-FOLATES

           Vancomycin                                                       Flouroquinolones                                                      Sulfonamides (PABA analogues)
                                           MOA: Inhibit replication (GN: Topoisomerase II; GP: Topoisomerase IV); bacteriocidal,        Sulfamethoxazole (SMX) Sulfadoxine (t½ 7-9d) --
Use: GP only – MRSA/MRSE, Strep            concentration dependant killing (target 4-5 x MIC) w/ postantibiotic effect.                 Sulfisoxazole (t½ 6-8h) – Dapsone
spp., Enterococci spp (some R in           PK: F, wide dist, long t½ so BID dosing for 1st/2nd gens; QD for 3rd/4th; limited BBB       AE:
faecium), GP anaerobes, Clostridium        penetration                                                                                     sulfa allergies
difficile (PO only)                        AE:                                                                                             GI upset
PK: Vd=0.7 L/kg (TBW!); CSF level 10-         GI: N/V/D (esp w/ grepa);                                                                   photosensitivity (rash)
20% of serum level; plasma goal trough        CNS: anxiety, nervousness, insomnia (esp. trova); HA, dizziness, rare seizures in pre-      rare- hemolytic anemia in G6PD def., Kernicterus in
10-15 mcg/mL                                   disposed pts, esp w/ co-NSAIDs                                                               neonates, crystaluria (so  water intake)
                                              Dermatologic: rash, severe photosensitivity (esp spar, lome)
Elimination: Renal – protein bound so                                                                                                   DDI: protein binding so displaces other protein-bound drugs);i
                                              Cartilage:pre-clinicals show risk – avoid in children, pg/lactating, CF if possible;
t½  in dialysis pts.                         Tendonitis rare, but can happen w/ short-term tx ( risk = old, RF, transplants, co-    DAP Uses: Mycobacterium leprae (w/ rifampin), PCP Tx
                                               corticosteroids, DM, athletes)                                                             (w/TMP), PCP proph (w/ PYR and leucovorin)
AE: “Red neck”, BP from too fast
infusion; ototox, nephrotox concerns not      Cardiac: QTc prolongation
supported                                     Rare: hepatic abnormalities, Hematologic (anemia, neutropenia, thrombocytopenia),
                                               Acute RF                                                                                         Aminopyrimidines (DHFR Inhibitors)
Resistance: VRE (D-Ala-D-Ser), one         DDI: Many are P450 inhibitors (so  wararin metab – monitor INR)
report of VRSA                                                                                                                          Trimethoprim (TMP), Pyrimethamine (+S-doxine = Fansidar)
                                           DFI: Quinolones chelate w/ multivalent cations and ppt – avoid antacids, iron, zinc,
                                                                                                                                        AE:
                                           sucralfate (2h pre/4h post)
                                                                                                                                           Rash
                                                                                                                                           anemia/thrombocytopenia (esp if immune fxn)
                                           1st Generation
          Nitrofurantion                   Norfloxacin (Noroxin)                                                                           K
                                           GN: PEK + CAPES                                                                                 HA, confusion (> w/ PYR; so give leucovorin, a form of THF)
Macrobid (BID) or Macrdurantin (QID)
                                           Intestinal pathogens: Shigella spp., Campylobacter jejuni, Salmonella spp.                      C/I in pg
Spectrum: aerobic GN bacilli and cocci,                                                                                                 PYR PK: used qwk for phrphylaxis
incl. enterococcus; SEE (Staph.            2nd Generation                                                                               PYR Uses: toxoplasmosis (w/ S-diazine), malaria (w/ S-doxine)
saprophytius, E. coli, Enterobacter)       Ciprofloxacin (Cipro) [R+H], Ofloxacin (Floxin) [R], Lomefloxacin (Maxaquin)
                                           GP: variable vs. MRSE, MRSE
MOA: Inhibit “enzyme systems” so                                                                                                       TMP/SMX (1:5 in tablet  1:20 in serum) antibacterial
                                           GN: HNPEK + CAPES + M. Catarrhalis + Chlamydia trachomatis + Legionella
metabolism and cell wall synth                                                                                                          spectrum (t½ for both 10-12h):
                                           Note: Cipro is the only PO tx for Pseudomonas!
Uses: absorbed, but Cl, so only used                                                                                                  Uses: UTIs [E. coli, Klebsiella, Enterobacter spp]; H. influenza,
for cystitis (not even pyelonephritis)     3rd Generation                                                                                 Listeria (use if allergic to Ampicillin), Nocardia spp (DOC),
                                           Levofloxacin (Levaquin) [Renal], Moxifloxacin (Avelox) [non-Renal], Gatifloxacin (Tequin)      GNR (bordatella pertussis, Stenotrophomonas, Maltophilla,
C/I: ClCr < 40mL/min (dose adj before
                                           [Renal], Sparfloxacin (Zagam), Grepafloxacin (Raxar), Gemifloxacin (Factive)                   Vibrio cholerae), P. carinii
that)
                                           GP: excellent against Pneumococcus, MSSA                                                     Holes: MRSA/E, Enterococcus spp., P. aeruginosa, H. Pylori, all
AE: N/V; very rare pulmonary fibrosis      GN: Same as 2nd generation; Moxi esp. good vs. B. fragilis                                     anaerobes, atypicals
(usually in first weeks of use); G6PD      Atypicals: excellent vs. Chalmydia pneumoniae, Legionella, Mycoplasma pneumoniae,            PK: widely dist (even CNS, prostate), RENAL elim w/ active
def. predisposes to hemolytic anemia       Mycobacterium spp.                                                                             secretion – so [ ] in urine – good for UTI
                                           Holes in spectrum: Stenotrophomonas maltophilia, Nocardia spp., MRSA
                                                                                                                                        AE: of component drugs;  incidence and severity in HIV pts;
                                           4th Generation                                                                                 sulfa cross-reactivity w/ thiazide and loop diuretics, oral
                                           Trovafloxacin (Trovan): PO, but limited to <14d, in hospital due to hepatotoxity. Same         sulfonylureas, acetazolamide
                                           coverage as 3rd gen (incl. B. fragilis)




Pseudomonas coverage: ceftazadime, cefepime, imipenem, meropenem, aztreonam, ciprofloxacin, 3 rd generation quinolones (levo, moxi, gati…), ticarcillin, pipercillin, AG’s

				
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posted:11/15/2011
language:English
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