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  • 1
    ISSN: 1432-2072
    Keywords: Schizophrenia ; Neuroleptics ; Pharmacokinetics ; Long-acting neuroleptics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The authors review the literature regarding the pharmacokinetics of long-acting injectable neuroleptic drugs (LINS). There are important differences between LINS and oral neurolepties that affect their pharmacokinetics. By avoiding first pass metabolism in gut and liver, LINS result in lower circulating concentrations of metabolites than are found after oral administration. In addition, LINS take more time to reach a stable steady state than their oral counterparts. The clinical significance of these pharmacokinetic properties is discussed. The authors recommend that when patients are being changed from oral neuroleptics to LINS, that this conversion be done gradually over several months.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-2072
    Keywords: Trifluoperazine ; Pharmacokinetics ; Population ; Kurtosis ; Skewness ; Blacks (negro) ; Whites (caucasian)
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The single dose pharmacokinetics of trifluoperazine (5 mg, Stelazine) were investigated in black (n=25) and white (n=32) healthy male subjects. Plasma samples were harvested over 24 h and analysed by a GLC-MS method. There were wide intersubject variations in all pharmacokinetic parameters examined, including C max, AUC, apparent oral volume of distribution at steady state, and elimination half-life. For each of these parameters the distribution was positively skewed in both blacks and whites and the geometric mean gave a better estimate of central tendency than the corresponding arithmetic mean. In all pharmacokinetic parameters examined there was no significant difference detected between black and white subjects or between smokers and non-smokers.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-2072
    Keywords: Fluphenazine ; Pharmacokinetics ; Interpatient variation ; Kurtosis ; Skewness ; Blacks (negro) ; Whites (caucasian) ; Biliary recycling ; Fluphenazine conjugates
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The single dose pharmacokinetics of fluphenazine (2 × 5 mg tablets, Prolixin) were studied in 21 drug free male psychiatric patients (12 black, 9 white). Plasma samples were harvested over a period of 48 h while the patients were on a strictly controlled diet. The results showed wide interpatient variations in all pharmacokinetic parameters including Cmax, AUC, apparent oral clearance, and elimination half-life. It was determined for each of these parameters that the geometric mean gave a better estimate of central tendency than the corresponding arithmetic mean and the distribution was skewed and leptokurtotic. There was no significant difference between blacks and whites in any pharmacokinetic parameter examined. Considerable variations and marked undulations in the elimination portion of the plasma concentration versus time profiles were evident, possibly indicating biliary recycling of the drug. These undulations made it difficult to determine elimination rate constants for several of the patients. Hydrolysis or plasma samples from one patient demonstrated that the conjugate(s) of fluphenazine was present in three to four times the concentration of the unchanged drug.
    Type of Medium: Electronic Resource
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