Spiramycin is widely distributed and persists
for long periods in many tissues.
The large volume of distribution and tissue
volume are indicative of the particularly high
tissue affinity of spiramycin.
Concentrations many times higher than those
found in serum have been reported in lung, liver,
kidney, spleen, prostate, placenta ,muscle,
bone and tonsillar tissue.
High levels may persist for as long as 72 hours
following a single oral dose.
Spiramycin levels have also been measured in
variety of human secretions and high concentration
have been found in bile, saliva and lacrimal
fluid.
Intracellular concentrations in
phagocytic cells are markedly elevated over
prolonged periods and this is likely to account
for the efficacy of spiramycin against number
of intracellular organisms (Chlamyia, Toxoplasma,
Legionella)
Placental transfer is poor and
only 9-16 % of the maternal blood concentration
appear in the amniotic fluid.
Spiramycin binds poorly to serum
proteins, only15% being bound to serum albumin.
Spiramycin is extensively biotransformed in
the tissues, with only 14% of the dose excreted
unchanged in urine.
 |