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  • 1
    Electronic Resource
    Electronic Resource
    .beta.-Aminopropionohydroxamic acids and .beta.-aminopropionic esters with hypotensive properties (1969)
    s.l. : American Chemical Society
    Journal of medicinal chemistry 12 (1969), S. 940-941 
    Details
    ISSN: 1520-4804
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/jm00305a064
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  • 2
    Electronic Resource
    Electronic Resource
    Mass spectrometric analysis of the isotopomeric species for the solvolysis of 1,2-diphenyl-2-[2H5]phenyl[2-13C]vinyl bromide in 70% HOAc-30% H2O (1983)
    s.l. : American Chemical Society
    The @journal of organic chemistry 48 (1983), S. 1025-1029 
    Details
    ISSN: 1520-6904
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/jo00155a019
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of long-acting injectable neuroleptic drugs: clinical implications (1989)
    Springer
    Psychopharmacology 98 (1989), S. 433-439 
    Details
    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
    URL: http://dx.doi.org/10.1007/BF00441937
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  • 4
    Electronic Resource
    Electronic Resource
    Fluphenazine plasma levels in patients receiving low and conventional doses of fluphenazine decanoate (1986)
    Springer
    Psychopharmacology 88 (1986), S. 480-483 
    Details
    ISSN: 1432-2072
    Keywords: Schizophrenia ; Neuroleptic ; Fluphenazine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Plasma fluphenazine concentrations (FLU) were measured in 45 patients with schizophrenic disorders who participated in a double-blind comparison of 5 and 25 mg fluphenazine decanoate (FD). The rise in plasma level of FLU 24 h after a “test dose” was significantly correlated with steady state FLU concentration at 12 weeks (for 5 mg patients, r=0.45, P=0.04; for 25 mg, r=0.78, P=0.005). Patients who had low FLU at baseline required nearly 6 months to reach a steady state when they received 25 mg. Patients who received 5 mg and had low FLU at baseline continued to demonstrate relatively low plasma levels for the entire 1st year. Although the mean FLU at 6 months was lower for patients who relapsed during the subsequent 18 months (0.57 ng/ml for relapsers vs 1.01 ng/ml for nonrelapsers), this difference was not statistically significant. When plasma levels from both dosage groups were combined, FLU at 12 weeks correlated significantly with factor scores for akinesia (r=0.52, P=0.002) and BPRS cluster scores for retardation (r=0.52, P=0.002). These results indicate that the measurement of fluphenazine plasma levels may be useful in determining when patients treated with FD are receiving drug doses which are likely to cause discomforting side effects.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00178510
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  • 5
    Electronic Resource
    Electronic Resource
    A pharmacokinetic study of trifluoperazine in two ethnic populations (1988)
    Springer
    Psychopharmacology 95 (1988), S. 333-338 
    Details
    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
    URL: http://dx.doi.org/10.1007/BF00181943
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  • 6
    Electronic Resource
    Electronic Resource
    The sulfoxidation of fluphenazine in schizophrenic patients maintained on fluphenazine decanoate (1987)
    Springer
    Psychopharmacology 93 (1987), S. 369-373 
    Details
    ISSN: 1432-2072
    Keywords: Schizophrenia ; Fluphenazine decanoate ; Metabolic sulfoxidation ; Fluphenazine sulfoxide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Highly sensitive radioimmunoassays were applied to study the sulfoxidation of fluphenazine in 30 schizophrenic patients maintained on either 5 mg or 25 mg fluphenazine decanoate by intramuscular injection every 14 days over a period of 6 months. The presence of the sulfoxide metabolite was detected in all but one of the patients, such that 97% of the 340 plasma samples analysed contained the metabolite. Interpatient variations in plasma levels of fluphenazine, fluphenazine sulfoxide, and in drug to metabolite plasma level ratios were several fold higher than the corresponding intrapatient variations at both dosages. There were statistically significant tendencies for mean plasma fluphenazine levels to rise and mean plasma sulfoxide levels to fall over the 6-month period of study among patients on the high dose, consistent with our previously reported observation that it takes 3–6 months to establish a steady state of fluphenazine with this dosage regimen. By contrast, there were no statistically significant changes in mean plasma levels of either fluphenazine or its sulfoxide in patients on the low dose. Nevertheless, there was a significant rise in fluphenazine to fluphenazine sulfoxide mean plasma level ratios in both dosage groups. It is difficult to assess the significance of the changes in the drug to metabolite ratios with time, since there are no kinetic data on the phase II metabolism (conjugation) of fluphenazine or fluphenazine sulfoxide. This study shows that sulfoxidation is an important major pathway in the metabolism of intramuscularly-administered fluphenazine, and implies that metabolic sites other than gut wall are also involved in the process.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00187259
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  • 7
    Electronic Resource
    Electronic Resource
    Variation in the single dose pharmacokinetics of fluphenazine in psychiatric patients (1988)
    Springer
    Psychopharmacology 96 (1988), S. 206-211 
    Details
    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
    URL: http://dx.doi.org/10.1007/BF00177561
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  • 8
    Electronic Resource
    Electronic Resource
    Individual Bioequivalence: Attractive in Principle, Difficult in Practice (1998)
    Springer
    Pharmaceutical research 15 (1998), S. 1321-1325 
    Details
    ISSN: 1573-904X
    Keywords: individual bioequivalence ; average bioequivalence ; drug regulation ; generic drugs
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1011972732530
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  • 9
    Electronic Resource
    Electronic Resource
    The Roles of Depot Injection Sites and Proximal Lymph Nodes in the Presystemic Absorption of Fluphenazine Decanoate and Fluphenazine: Ex Vivo Experiments in Rats (1998)
    Springer
    Pharmaceutical research 15 (1998), S. 1485-1489 
    Details
    ISSN: 1573-904X
    Keywords: fluphenazine decanoate ; prodrug ; fluphenazine ; lymph nodes ; intramuscular administration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The release and presystemic absorption of fluphenazine and its decanoate ester from intramuscular depots were investigated. Methods. Rats were sacrificed in groups of three at various times after injection of drug or prodrug in sesame oil. Muscle tissues at the injection sites and various lymph nodes were excised. Blood (plasma) was harvested by cardiac puncture. Results. Following administration of fluphenazine decanoate, the amount of prodrug at the sites of injection declined exponentially (half-life 3.4 days). Highest concentrations of drug and prodrug were found in iliac and hypogastric lymph nodes nearest to injection sites in which both analytes were detectable 28 days post dose. The half-life for the decline of fluphenazine from lymph nodes (4.6 days) was similar to that from plasma (4.3 days). Following administration of fluphenazine base, only 2.8% of the dose remained at the sites of injection after 2 days. Concentrations of drug in iliac and hypogastric lymph nodes were comparable to those in distal lymph nodes. Fuphenazine concentrations in the lymphatic tissues decreased at about the same rate as plasma concentrations. Conclusions. The rate limiting step appeared to be slow partitioning of the decanoate from oily deposits at the injection site and proximal lymph nodes with subsequent hydrolysis of the ester group.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1011978327504
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  • 10
    Electronic Resource
    Electronic Resource
    Synthesis and Properties of Haptens for the Development of Radioimmunoassays for Thioridazine, Mesoridazine, and Sulforidazine (1987)
    Springer
    Pharmaceutical research 4 (1987), S. 207-213 
    Details
    ISSN: 1573-904X
    Keywords: synthesis ; properties ; haptens ; thioridazine ; mesoridazine ; sulforidazine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract For the separate development of radioimmunoassay procedures for thioridazine and its two major active metabolites, mesoridazine and sulforidazine, three haptens, respectively, 2-methylthio-, 2-methylsulfinyl-, and 2-methylsulfonyl-substituted 10-[2-[l-(2-carboxyethyl)-2-piperidinyl]ethyl]-10H-phenothiazine, were synthesized and characterized. Thioridazine hapten was coupled to bovine serum albumin, whereas the haptens for mesoridazine and sulforidazine were coupled to porcine thyroglobulin. The number of hapten residues per mole of carrier protein was determined in each case by an ultraviolet spectrophotometric method. Polyclonal antibodies to each hapten–protein conjugate were obtained in rabbits, and titers of the antisera were checked by evaluating their binding characteristics to the appropriate tritiated analyte. A hapten for the ring sulfoxide metabolite of thioridazine was also synthesized.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1016451926984
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