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Therapeutics Pregnancy cat.: Side effects: Monitoring: Notes: 111 B antibiotic-associated colitis (rarely) none poor gram (−) activity neuromuscular blocking properties may enhance other neuromuscular agents good anaerobic coverage Sadick NS. Systemic Antibacterial Agents. In: Wolverton SE. ed., ed. Compre-hensive Dermatologic Drug Therapy. Philadelphia: W. B. Saunders Co. 2001: p. 28. Ray WA, Murray KT, Meredith S et al. Oral erythromycin and the risk of sudden death from cardiac causes. N Engl J Med 2004; 351: 1089–1096. Yee CL, Duffy C, Gerbino PG et al. Tendon or joint disorders in children after treatment with fluoroquinolones or azithromycin. Pediatr Infect Dis J 2002; 21: 525–529. 112 Pocket Guide for Cutaneous Medicine and Surgery Topical Antimicrobials Bacitracin r inhibits bacterial cell wall synthesis – inhibits peptidoglycan synthesis r gram (+): S. aureus, S. pneumoniae, Neisseria, H. influenzae, T. pallidum r gram (−): minimal coverage r SE: contact sensitization, rare anaphylaxis Mupirocin (Bactroban) r inhibits bacterial RNA and protein synthesis (isoleucyl tDNA synthetase) r gram (+): Staphylococci (MRSA), Streptococci r gram (−): some gram (−) cocci r SE: local irritant r does not cross-react with other topical antimicrobials r renal toxicity when used on large denuded areas r uncommon contact sensitization Neomycin r inhibits protein synthesis (binds 30S subunit) r gram (+): good coverage vs. S. aureus (weak for Strep) r gram (−): yes r SE: ototoxic and nephrotoxic; contact sensitization; virtually always used in combination Polymyxin B r antibacterial via surface detergent-like mechanisms r gram (+): no activity r gram (−): Proteus, Pseudomonas, Serratia r SE: rare contact sensitization Spann CT et al. Topical antibacterial agents for wound care: A primer. Der-matol Surg 2003; 29: 620–626. Therapeutics 113 Systemic Antifungals Terbinafine (allylamine) Mechanism: Metabolism: Excretion: Dosing: Pregnancy cat.: Side effects: Monitoring: Notes: inhibits squalene epoxidase (↑squalene and impairs ergosterol synthesis) hepatic (80%); fecal (20%) −15 metabolites renal 250 mg po qd (12 wks – toenails; 6 wks – fingernails) 125 mg po qd (20–40 kg) 62.5 mg po qd (<20 kg) B (excreted in breast milk; not rec. in pregnancy) headache, GI symptoms, morbilliform rash, dysguesia LFTs (transaminases) and CBC after 6 wks less effective for Candida than azole antifungals caution with concomitant doxepin due to terbinafine CYP 2D6 interaction caution with renal insufficiency/hepatic dysfunction safe and effective in children for same duration use / dose with elevated creatine Itraconazole (triazole) Mechanism: Metabolism: Excretion: inhibits lanosterol 14-a demethylase (inhibits lanosterol → ergosterol) hepatic (side-chain hydroxylation to hydroxyitraconazole) renal (urine 35%; feces 54%) 114 Dosing: Pocket Guide for Cutaneous Medicine and Surgery 200 mg po bid × 1 week/month (pulse regimen) (2 pulses for fingernails; 3–4 pulses for toenails) Pregnancy cat.: Side effects: Monitoring: Notes: Ketoconazole Mechanism: Metabolism: Excretion: Dosing: Pregnancy cat.: Side effects: Monitoring: Notes: Fluconazole Mechanism: Metabolism: Excretion: C (excreted in breast milk) headache, GI symptoms, morbilliform rash LFTs after 4 wks (some do not check) highest po bioavailability with full meal/carbonated safe and effective in children CYP 3A4 inhibitor (less than terbinafine) inhibits lanosterol 14-a demethylase hepatic (side-chain hydroxylation) renal 200–400 mg po qd C (excreted in breast milk) headache, GI symptoms, morbilliform rash LFT after 2 weeks highest po bioavailability with full meal caution with hepatic dysfunction T. versicolor dosing: 400 mg/day qweek × 2 weeks inhibits fungal lanosterol 14-a demethylase hepatic (no significant 1st-pass hepatic metabolism) renal Therapeutics Dosing: Pregnancy cat.: Side effects: Monitoring: Notes: Griseofulvin Mechanism: Metabolism: Excretion: Dosing: Adult: Pediatric: Pregnancy cat.: Side effects: Monitoring: 115 150 mg po qweek (vulvovaginal candidiasis) 300–450 mg po qweek (off-label, onychomycosis) C few adverse effects usually not needed penetrates into CSF well excellent po bioavailability (>90%) no need to renal dose for single dose multiple drug interactions (cytochrome P-450) minimal CYP 3A4 inhibition at doses <300 mg qd CYP 2C9 inhibition (extreme caution with warfarin) inhibits microtubule formation hepatic renal 250 mg po bid 20 mg/kg po qd (microsize and ultramicrosize) C granulocytopenia, hepatotoxicity, urticaria none ... - tailieumienphi.vn
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