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Infections: Antibiotics
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==Characteristics of Antibiotics by Class== ===Aminopenicillins=== *Ampicillin and amoxicillin have been used often in the past for the treatment of UTIs, but the '''emergence of resistance''' in 40-60% of common urinary '''isolates has lessened the usefulness of these drugs (See Toronto antibiograms''') *'''The effects of ampicillin and amoxocillin on the normal bowel and vaginal flora can''' predispose patients to reinfection with resistant strains and '''often lead to candida vaginitis''' *'''The addition of the β-lactamase inhibitor clavulanate to amoxicillin greatly improves activity against β-lactamase–producing bacteria resistant to amoxicillin alone. However, its high cost and frequent gastrointestinal side effects limit its usefulness.''' *'''The extended-spectrum penicillin derivatives (e.g., pivmecillinam, piperacillin, mezlocillin, azlocillin) retain ampicillin’s activity against enterococci and offer activity against many ampicillin-resistant gram-negative bacilli''' *'''Safe for use in pregnancy''' ===Cephalosporins=== *'''In general, as a group, activity is high against Enterobacteriaceae and poor against enterococci''' *First-generation cephalosporins have greater activity against gram-positive organisms, as well as common uropathogens such as E. coli and Klebsiella pneumoniae, whereas second-generation cephalosporins have activity against anaerobes. Third-generation cephalosporins are more reliably active against community-acquired and nosocomial gram-negative organisms than other β-lactam antimicrobials. *Use of these broad-spectrum agents should be limited complicated infections and situations in which parenteral therapy is required and resistance to standard antimicrobial agents is likely. *'''Safe for use during pregnancy''' *'''Ceftriaxone is contraindicated in neonates''' ===Nitrofurantoin=== *'''Effective against common uropathogens'''; '''not effective against Pseudomonas and Proteus''' *Rapidly excreted in the urine but '''does not obtain therapeutic levels in most body tissues. Therefore, not useful for upper tract and complicated infections.''' *'''Minimal effects on the resident bowel and vaginal flora''' and has been used effectively in prophylactic regimens *Acquired bacterial resistance is exceedingly low *'''Pregnancy''' **'''2017 American College of Obstetricians and Gynecologists recommendations'''§''':''' ***'''First trimester''' ****Consider and discuss with patients the benefits as well as the potential unknown risks of teratogenesis and fetal and maternal adverse reactions. ****'''Prescribing sulfonamides or nitrofurantoin in the first trimester is still considered appropriate when no other suitable alternative antibiotics are available.''' ***'''Second and third trimesters''' ****'''Can be used as first-line agents''' for the treatment and prevention of urinary tract infections and other infections caused by susceptible organisms. ***Contraindicated in patients with glucose-6-phosphate dehydrogenase deficiency, or in pregnant women identified to be at risk of this condition. **'''CW12 page 1186-1187''' ***'''First and second trimester''' ****'''May be used safely in patients without glucose-6-phosphate dehydrogenase deficiency''' ***'''Third trimester''' ****'''Should be discontinued at 35 weeks''' because of an increased risk of hemolytic anemia in the neonate. ===Trimethoprim (TMP)-sulfamethoxazole (SMX)=== *'''TMP alone or in combination with SMX is effective against most common uropathogens; not effective against Enterococcus and Pseudomonas.''' **TMP alone is as effective as the combination for most uncomplicated infections and may be associated with fewer side effects; however, the addition of SMX contributes to efficacy in the treatment of upper tract infection via a synergistic bactericidal effect and may diminish the emergence of resistance and attains therapeutic levels in most tissues. *Advantages are inexpensive and have '''minimal adverse effects on the bowel flora''' *Disadvantages are relatively common adverse effects, consisting primarily of rashes and gastrointestinal complaints. *'''Trimethoprim blocks the tubular secretion of creatinine.''' **Since creatinine is produced at a steady state, the serum creatinine will rise, but the GFR does not change *'''<span style="color:#ff0000">TMP-SMX should be avoided during pregnancy because of early potential for teratogenicity and late potential for kernicterus''' *'''<span style="color:#ff0000">Trimethoprim alone should be avoided in pregnancy due to risk of megaloblastic anemia; trimethoprim alone can be used in neonates''' ===Fosfomycin=== *Effective against most uropathogens; '''not effective against Pseudomonas''' *Effective against the majority of gram-negative organisms and vancomycin-resistant Enterococcus (VRE) *Limited cross-resistance between most other common antibacterial agents *Shown to be effective as a single-dose agent when used as an empirical treatment for uncomplicated cystitis *Generally well tolerated with low incidences of GI upset and headache and very rare adverse events ===Fluoroquinolones=== *'''Broad spectrum of activity''' **'''Highly effective against Enterobacteriaceae and P. aeruginosa''' **'''Activity is also high against S. aureus and S. saprophyticus, but, in general, anti-streptococcal coverage is marginal''' **'''Modest activity against enterococcus''' *'''Most anaerobic bacteria are resistant to these drugs; therefore, the normal vaginal and bowel flora are not altered''' *'''Increasing rates of resistance due to indiscriminate use of these agents''' *Not nephrotoxic, but renal insufficiency prolongs the serum half-life, '''requires dose adjustment in patients with creatinine clearances of <30 mL/min.''' *'''<span style="color:#ff0000">Contraindicated in children, adolescents, and pregnant or nursing women due to concerns of damage to developing cartilage''' *'''Drug interactions''': **'''Rare increases in the anticoagulant effects of warfarin when taken with fluoroquinolones'''. **'''Concomitant antacid''' (containing magnesium or aluminum)''', iron, zinc, or sucralfate use dramatically decreases oral absorption''' **Antacids containing magnesium or aluminum interfere with absorption of fluoroquinolones. **Certain fluoroquinolones (enoxacin and ciprofloxacin) elevate plasma levels of theophylline and prolong its half-life **'''Avoid with other drugs that prolong QT interval, such as amiodarone'''
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