Cefoperazone biliary excretion

The great biliary excretion of cefoperazone causes changes in bowel flora and diarrhea may often occur. Containing a 7V-methylthiotetrazole side chain, cefoperazone may also cause hypoprothrombinemia and a disulfiram-like reaction with alcohol (alcohol intolerance). This antibiotic should be avoided by patients receiving anticoagulants. 

Although immediate reactions of anaphylaxis, bronchospasm, and urticaria have been reported, most commonly patients exhibiting an adverse reaction develop a maculopapular rash, usually after several days of therapy. They may also develop fever and eosinophilia (80,219). Cefoperazone (34) and ceftriaxone (39), having greater biliary excretion than other cephalosporins, are associated with an increased risk of diarrhea, which may be caused by selection of cytotoxin producing stains of Clostridium difficile (219). 

Antimicrobial drugs that are eliminated via hepatic metabolism or biliary excretion include erythromycin, cefoperazone, clindamycin, doxycycline, isoniazid, ketoconazole, and nafcillin. The answer is (C). 

Renal function impairment Cephalosporins may be nephrotoxic use with caution in the presence of markedly impaired renal function (Ccr less than 50 mL/min/1.73 m ). Hepatic function impairment Cefoperazone is extensively excreted in bile. Serum half-life increases 2-fold to 4-fold in patients with hepatic disease or biliary obstruction. 

Urinary excretion is the major elimination path for most cephalosporins. When prescribing cephalosporins to patients with renal failure, practitioners must consider dose reduction or dose interval extension (Table 45.2). Renal tubular secretion contributes to the elimination of some cephalosporins, and an increase in cephalosporin plasma concentrations may occur when probenecid blocks renal tubular secretion of cephalosporins. Biliary elimination is important for some cephalosporins. Cefmetazole, cefoperazone (Cefobid), cefoxitin, and ceftriaxone achieve biliary concentrations greater than those in plasma. After parenteral administration of cefoperazone, 70% of the dose appears in the bile within 24 hours. Practitioners should decrease the dose of cefoperazone when prescribing for patients with hepatic failure or biliary obstruction. Metabolism is not a major elimination path for most cephalosporins. Cefotaxime is one of the few cephalosporins having an active metabolite, desacetyl cefotaxime. 

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