Phencyclidine disposition after intravenous and oral doses

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Abstract
[3H]Phencyclidine (PCP) hydrochloride [a major drug of abuse] was given in i.v. (0.1 or 1 mg) or oral (1 mg) doses to male subjects. After 1 mg i.v., drug and metabolites were recovered in urine (72.8 .+-. 4.0% of dose), feces (4.7 .+-. 0.9%) and perspiration. Fecal excretion was low (3.4 .+-. 0.4%) after oral dosing and oral bioavailability was estimated at 72%. PCP comprised 16% of urinary radioactivity with 31% consisting of enzymatically hydrolyzable conjugates of hydroxylated metabolites. Both cis and trans isomers of 4-phenyl-4-(1-piperidinyl)cyclohexanol were found. Maximum average plasma PCP concentrations of 2.7-2.9 ng/ml were observed after oral and i.v. 1-mg doses. Blood/plasma ratios were .apprx. 1.0 and plasma binding was .apprx. 65%. Parent drug was found in saliva. Apparent terminal phase half-lifes averaged 21 .+-. 3 h (harmonic mean 17 h, range 7-46 h). The volume of distribution averaged 6.2 .+-. 0.3 l/kg. Renal clearances were variable, but the average was 9% of the total clearance. Evidently, PCP is cleared principally by metabolism.

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