LUT infect & STI Flashcards
Penicillins (admin)
Penicillin G (IV,IM)
Aminopenicillins (admin)
Ampicillin (PO,IV,IM)
Cephalosporins (admin)
Ceftriaxone 3rd Gen. [Rocephin] (IV, IM)
B-Lactamase Inhibitors (admin)
Ampicillin-sulbactam [Unasyn] (IV)
Fluoroquinolones (admin)
Ciprofloxacin [Cipro] (PO, IV, topical)
Macrolides/Ketolides (admin)
Azithromycin [Zithromax, Z-pak] (PO, IV, topical)
Metronidazole (admin)
Metronidazole [Flagyl] (PO, IV, topical)
Sulfonamides/Trimethoprim (admin)
Sulfamethoxazole/trimethoprim [Bactrim] (PO, IV)
Urinary Tract Antiseptics (admin)
1) Methenamine (PO)
2) Nitrofurantoin (PO)
Azole Antifungals
Fluconazole
Trimethoprim/sulfamethoxazole (TMP/SMX) MOA
Sulfonamide=bacteriostatic, competitive inhibition of dihydropteroate synthase
Trimethoprim= synergistic, inhibits dihydrofolate reductase
Together inhibits sequential steps in Folic acid pathway & inhibits bacterial use of PABA for folic acid synthesis, Inhibits final reduction step.
Trimethoprim/sulfamethoxazole (TMP/SMX) PK
SMX t1/2= 10 H
TMP t1/2= 11 H
Dose adjust for prolonged renal impairment
Hepatic Metabolism: SMX 25-50% excreted in urine24H
TMP 60%
Trimethoprim/sulfamethoxazole (TMP/SMX) ADR
allergic skin rashes nausea vomiting CNS (headache, depression) photosensitivity renal dysfunction Stevens-Johnson syndrome
Trimethoprim/sulfamethoxazole (TMP/SMX) DDi
Inhibits CYP metabolism:
potentiates Warfarin!
inc. serum conc. Digoxin, Phenytoin
Enhance HyperK effects of ACEIs, ARBs, Spironolactone
Nitrofurantoin MOA
Highly reactive intermediates damage DNA:
Bacteria reduce drug more rapidly= more selective activity
Nitrofurantoin PK
Macro-crystalline formula absorbed/excreted slowly.
Antibacterial Conc. not found in plasma due to rapid elimination (t1/2 0.3-1 H)
Excretion rate related to CrCl
Nitrofurantoin ADRs
Nausea, vomiting, diarrhea
Macro-crystalline formula better tolerated
Not exceed 14 day therapy –> repeated course needs rest period
Nitrofurantoin Ci
Pregnant women
impaired REnal Fxn (40 mL/min)
children <1 month
Methenamine
Not primary UTI durg. Used for chronic suppressive therapy
Methenamine MOA
Decomposes to formaldehyde in h2o
Acidification of urine promotes formaldehyde formation
3 hours to complete = slow process
Methenamine PK
10-30% decomposition in gastric juice unless enteric coating
Methenamine ADRs
GI distress painful/frequent micturition hematuria rash low systemic toxicity at usual doses
Methenamine Ci
Hepatic insufficiency due to Ammonia production
Fosfomycin MOA
bactericidal; Inhibits early stage cell wall synthesis.
Inactivates pyruvyl transferase leading to dec. formation of N-acetylmuramic acid–> only found in bacterial cell walls
Fosfomycin PK
rapidly absorbed: Oral only ins U.S. (IV elsewhere)
renal elimination; t1/2 4H, if CrCl<54 mL/min t1/2 50H
Fosfomycin ADRs
diarrhea
nausea
abdominal pain
HA
Fluoroquinolones MOA
Conc. dependent killing: Targets DNA Gyrase and Topoisomerase IV
Fluoroquinolones PK
Well absorbed: divalent/trivalent cations impair absorption
Renal Clearance, Dose adjust in renal impairment
Fluoroquinolones ADRs
GI 3-17% most common (mild nausea, vomiting, abdominal discomfort)
CNS 0.9-11% (mild HA, dizziness, delirium, rare hallucinations)
rash
photosensitivity
Achilles tendon rupture
B- Lactams MOA
inhibits Transpeptidation rxn: last step in peptidoglycan synthesis. D-Ala-D-Ala: B-lactams covalently bind PBPd preventing cross linking= cell lysis
Penicillin G benzathine PK
IM injection; Abs slowly Avg. duration of antimicrobial activity ~26 days