Olanzapine transfer by human placenta.
1. The present study assessed the human transplacental transport of olanzapine, a new antipsychotic drug effective in the treatment of schizophrenia. 2. Using the normal-term placenta perfused single cotyledon system, we show that: (i) 5-14% of labelled olanzapine crosses from the maternal to foetal compartments in 4 h; (ii) transport depends significantly on binding characteristics, especially of albumin; (iii) no oxidative metabolites of olanzapine appear in the placental perfusate over 4 h; and (iv) approximately 17% of olanzapine, on average, is converted to the glucuronide, which is transferred by the placenta at a rate slightly slower than the parent drug.
Schenker
S
S
Department of Medicine, University of Texas Health Science Center at San Antonio 78284-7878, USA.
Yang
Y
Y
Mattiuz
E
E
Tatum
D
D
Lee
M
M
D014150:Antipsychotic Agents / Q000493:pharmacokinetics*; D001569:Benzodiazepines; D005260:Female; D020719:Glucuronides / Q000493:pharmacokinetics*; D006801:Humans; D008431:Maternal-Fetal Exchange / Q000187:drug effects / Q000502:physiology*; D000077152:Olanzapine; D010890:Pirenzepine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D010920:Placenta / Q000502:physiology*; D011247:Pregnancy
D014150:Antipsychotic Agents; D020719:Glucuronides; D001569:Benzodiazepines; D010890:Pirenzepine; D000077152:Olanzapine