Page 916 - Basic _ Clinical Pharmacology ( PDFDrive )

902 SECTION VIII Chemotherapeutic Drugs

SUMMARY Miscellaneous Antimicrobials

Pharmacokinetics, Toxicities,
Subclass, Drug Mechanism of Action Effects Clinical Applications Interactions
NITROIMIDAZOLE
• Metronidazole Disruption of electron Bactericidal activity Anaerobic infections • vaginitis Oral or IV • hepatic clearance (t ½ 8 h)
transport chain against susceptible • C difficile colitis • disulfiram-like reaction when given with
anaerobic bacteria and alcohol • Toxicity: Gastrointestinal upset
protozoa • metallic taste • neuropathy • seizures

• Tinidazole: Oral; similar to metronidazole but dosed once daily; approved for trichomonas, giardiasis, and amebiasis
MACROLIDE
• Fidaxomicin Inhibits bacterial RNA Bactericidal in C difficile colitis Oral • blood levels negligible • Toxicity:
polymerase Gram-positive bacteria Nonspecific gastrointestinal upset
RIFAMYCIN
• Rifaximin Inhibits bacterial RNA Bactericidal activity in Travelers’ diarrhea, hepatic Oral • blood levels negligible • Toxicity:
polymerase Gram-positive and encephalopathy, C difficile Nausea
Gram-negative bacteria colitis, irritable bowel syndrome
URINARY ANTISEPTICS
• Nitrofurantoin Not fully understood Bacteriostatic or Uncomplicated urinary tract Oral • rapid renal clearance (t ½ 0.5 h) • blood
• disrupts protein synthesis bactericidal activity infections • long-term levels are negligible • contraindicated in renal
and inhibits multiple against susceptible prophylaxis failure • Toxicity: Gastrointestinal upset
bacterial enzyme systems bacteria • neuropathies • hypersensitivity pneumonitis
• Methenamine hippurate and methenamine mandelate: Oral; release formaldehyde at acidic pH in the urine; used only for prophylaxis, not treatment, of urinary tract infections

PREP AR A TIONS
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