PHARMACOKINETICS

Absorption
Most penicillins in aqueous solution are
rapidly absorbed from parenteral sites.
Absorption from the upper GI tract differs
markedly in amount and rate among the
various penicillins.
Serum concentrations of penicillins generally
peak within 2 hr of PO administration.

Distribution
After absorption, penicillins are widely
distributed in body fluids and tissues.
Potentially therapeutic concentrations of the
various penicillins are generally found in the liver,
bile, kidneys, intestines, muscle, and lungs.
Penicillins are reversibly and loosely bound to
plasma proteins. The extent of this binding varies
with particular penicillins and their
concentration, eg, ampicillin is usually 20%
bound, and cloxacillin may be 80% bound

Biotransformation
Penicillins are generally excreted unchanged,
but fractions of a given dose may undergo
metabolic transformations by unknown
mechanisms (usually <20% metabolized).

Excretion
Most (6090%) of a parenterally penicillin is
eliminated in the urine within a short time
(eg, up to 90% of penicillin G within 6 hr),
which results in high concentrations in urine.
About 20% of renal excretion occurs by
glomerular filtration and 80% by tubular
secretion