Absorption, distribution and excretion of trifluoperazine in rats.
In rats receiving a low oral dose (0.35 mg/kg p.o.) of trifluoperazine (TFP), a potent neuroleptic phenothiazine, the parent drug distribution was separate from that of its metabolite trifluoperazine sulfoxide (TFP-SO). This was not seen after intraperitoneal administration (i.p.) of the same or high dose (5mg/kg). TFP-SO was not detected in the brain, wheras TFP was significantly associated with microsomes when its brain level was highest. Absorption, distribution, metabolism, and dose dependent excretion procedded rapidly with 97% of a dose recovered 24 hr after p.o. treatment, only 6% in the urine and the remainder in feces with 87% of this metabolized to compounds other than TFP-SO. TFP and its metabolites arrived in feces via two pathways, largely the bile plus another route. The excretion pattern was unchanges with other drugs or after treatment for 3 wk, although excretion differed on the first day after i.p. and p.o. administration.
D000818:Animals; D001646:Bile / Q000378:metabolism; D001921:Brain / Q000378:metabolism / Q000648:ultrastructure; D005243:Feces / Q000032:analysis; D007408:Intestinal Absorption; D008099:Liver / Q000378:metabolism; D008168:Lung / Q000378:metabolism; D008297:Male; D051381:Rats; D013454:Sulfoxides / Q000378:metabolism; D013997:Time Factors; D014268:Trifluoperazine / Q000378:metabolism*
D013454:Sulfoxides; D014268:Trifluoperazine