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Do cephalosporins pass the BBB ??Why?

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Rajive Goel 19 Jul 2011

Cephalosporins possess high affinity to tissues and organs (except prostate gland). High concentrations of the drugs are found in the lungs, kidneys, liver, muscles, skin, soft tissues, bones and internal fluids. The highest concentrations in bile are produced by ceftriaxone and cefoperazone. The ability to pass the blood-brain barrier is mostly expressed in III and IV generation cephalosporins.

The majority of cephalosporins are not metabolized. Amongst exceptions is cefotaxime, which is transformed into its active metabolite in the body. The drug is excreted via kidneys, therefore very high concentrations of cephalosporins are registered in the urine. The half-life of the drugs varies significantly in each unique case from 1-2 hours for the majority of drugs to 8,5 hours in ceftriazone, which due to that can be administered once a day. In renal insufficiency the dosages of cephalosporins administered should be corrected.

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