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Jim Mintz - One of the best experts on this subject based on the ideXlab platform.
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Fluphenazine plasma level monitoring for patients receiving Fluphenazine decanoate
Schizophrenia Research, 2002Co-Authors: Stephen R. Marder, Manickam Aravagiri, Donna A Wirshing, Malca B Lebell, William C Wirshing, Jim MintzAbstract:Abstract Background: Finding a dose of an antipsychotic for maintenance therapy that is both safe and effective can be difficult because clinicians are unable to titrate dose against clinical response in patients who are already stable. Therapeutic monitoring of antipsychotic plasma levels has the potential for helping clinicians in dosage selection. With this in mind, we evaluated the usefulness of monitoring Fluphenazine plasma levels for patients with schizophrenia who were receiving maintenance treatment with Fluphenazine decanoate. Method: Thirty-one patients with schizophrenia were randomly assigned to low, medium, or high (0.1–0.3, 0.3–0.6, 0.6–1.0 ng/ml) plasma levels of Fluphenazine. The dose of Fluphenazine decanoate was adjusted in order to maintain patients in their assigned range. Side effects, psychopathology, and psychotic exacerbations were measured during the year following randomization. Results: All of the psychotic exacerbations occurred during the first eight weeks following randomization, before patients had adequate time to reach their plasma level assignments. We did not find a relationship between plasma levels of Fluphenazine and clinical outcomes or side effects. Conclusion: Our results do not provide support for the usefulness of monitoring Fluphenazine plasma levels for patients receiving Fluphenazine decanoate.
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Fluphenazine levels during maintenance treatment of recent onset schizophrenia relation to side effects psychosocial function and depression
Psychopharmacology, 2000Co-Authors: Michael J Gitlin, Jim Mintz, Keith H Nuechterlein, David L Fogelson, George Bartzokis, Joseph Ventura, Kenneth L Subotnik, Manickam AravagiriAbstract:Rationale: The utility of Fluphenazine levels during maintenance treatment of schizophrenia is still unclear. Objectives: This study investigated the relationship between Fluphenazine levels and a variety of clinical measures during maintenance treatment of schizophrenia. Methods: Fluphenazine levels, side effects, depression and psychosocial outcome were measured at five time points over approximately 1 year in 59 recent onset schizophrenic patients treated with a maintenance dose of injectable Fluphenazine decanoate. Negative symptoms were evaluated at the 1-year endpoint. Results: Fluphenazine levels showed marked intraindividual variability even when measurements were restricted to the second 6 months of treatment, by which time steady state levels should have been achieved. No consistent relationship was found between Fluphenazine levels and any of the outcome measures. Conclusions: The results of this study suggest that Fluphenazine plasma levels do not routinely add relevant clinical information beyond that of dose in evaluating potential side effects or negative consequences during maintenance treatment with the decanoate form of the medication.
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Fluphenazine vs placebo supplementation for prodromal signs of relapse in schizophrenia
Archives of General Psychiatry, 1994Co-Authors: Jim Mintz, William C Wirshing, Stephen R. Marder, Theodore Van Putten, Joanne Mckenzie, Kathleen Johnstoncronk, Malca B LebellAbstract:Background: We studied the effectiveness of treating patients with low doses of Fluphenazine decanoate and supplementing them with oral Fluphenazine when there was evidence of prodromal symptoms of psychotic exacerbations. Methods: Eighty schizophrenic patients who were receiving 5 to 10 mg of Fluphenazine decanoate every 2 weeks were monitored for prodromal symptoms using an idiosyncratic prodromal rating scale. When patients met our criteria for a prodromal episode, they were randomly assigned to a double-blind comparison of oral Fluphenazine hydrochloride (5 mg twice daily) or a placebo for the current and future prodromal episodes. We compared rates of psychotic exacerbations in the two treatment groups. Results: Thirty-six patients (45%) met the criteria for a prodrome at some point during the trial and were randomized to drug or placebo. Using survival analysis during the entire 2 years, we did not find a significant difference between Fluphenazine and placebo in the likelihood that a prodrome would continue to an exacerbation. Survival analysis beginning at the start of the second year of treatment did indicate a significant reduction in exacerbation risk for patients receiving drug supplementation ( P =.032). Similarly, there was no difference between the two groups in the proportion of time at risk spent in exacerbation during the first year, but patients receiving active drug supplementation spent less time in an exacerbated state in the second year ( P =.05). Conclusions: Our treatment strategy appeared to be effective for some patients, particularly those who were able to remain in the study beyond the first year. Although the occurrence of a prodrome was a fairly good marker that a patient was at high risk of ultimate exacerbation with our low-dose maintenance protocol, prodromes were not highly sensitive indicators of imminent exacerbation.
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plasma levels of Fluphenazine in patients receiving Fluphenazine decanoate relationship to clinical response
British Journal of Psychiatry, 1991Co-Authors: Stephen R. Marder, T Van Putten, Manickam Aravagiri, E M Hawes, J W Hubbard, Kamal K. Midha, Gordon Mckay, Jim MintzAbstract:The levels of Fluphenazine and Fluphenazine sulphoxide in schizophrenic patients who were randomly assigned to receive either 5 mg or 25 mg of Fluphenazine decanoate every two weeks were monitored. Patients treated with 25 mg of Fluphenazine decanoate required three months to reach a steady-state plasma level, indicating that those patients who are being converted from oral to depot Fluphenazine should continue to receive oral supplementation during the first three months of treatment with Fluphenazine decanoate. Plasma levels of Fluphenazine sulphoxide were lower than levels of Fluphenazine. At six and nine months following randomisation, there was a statistically significant relationship between lower Fluphenazine plasma levels and an increased risk of psychotic exacerbations. A relatively weak relationship was found between Fluphenazine plasma levels and akinesia, but non-significant relationships between Fluphenazine levels and other neurological side-effects including akathisia, retardation, and tardive dyskinesia. Monitoring the plasma levels may be helpful to clinicians who are attempting to treat stabilised patients with the lowest effective dose of Fluphenazine decanoate.
Stephen R. Marder - One of the best experts on this subject based on the ideXlab platform.
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Fluphenazine plasma level monitoring for patients receiving Fluphenazine decanoate
Schizophrenia Research, 2002Co-Authors: Stephen R. Marder, Manickam Aravagiri, Donna A Wirshing, Malca B Lebell, William C Wirshing, Jim MintzAbstract:Abstract Background: Finding a dose of an antipsychotic for maintenance therapy that is both safe and effective can be difficult because clinicians are unable to titrate dose against clinical response in patients who are already stable. Therapeutic monitoring of antipsychotic plasma levels has the potential for helping clinicians in dosage selection. With this in mind, we evaluated the usefulness of monitoring Fluphenazine plasma levels for patients with schizophrenia who were receiving maintenance treatment with Fluphenazine decanoate. Method: Thirty-one patients with schizophrenia were randomly assigned to low, medium, or high (0.1–0.3, 0.3–0.6, 0.6–1.0 ng/ml) plasma levels of Fluphenazine. The dose of Fluphenazine decanoate was adjusted in order to maintain patients in their assigned range. Side effects, psychopathology, and psychotic exacerbations were measured during the year following randomization. Results: All of the psychotic exacerbations occurred during the first eight weeks following randomization, before patients had adequate time to reach their plasma level assignments. We did not find a relationship between plasma levels of Fluphenazine and clinical outcomes or side effects. Conclusion: Our results do not provide support for the usefulness of monitoring Fluphenazine plasma levels for patients receiving Fluphenazine decanoate.
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Fluphenazine vs placebo supplementation for prodromal signs of relapse in schizophrenia
Archives of General Psychiatry, 1994Co-Authors: Jim Mintz, William C Wirshing, Stephen R. Marder, Theodore Van Putten, Joanne Mckenzie, Kathleen Johnstoncronk, Malca B LebellAbstract:Background: We studied the effectiveness of treating patients with low doses of Fluphenazine decanoate and supplementing them with oral Fluphenazine when there was evidence of prodromal symptoms of psychotic exacerbations. Methods: Eighty schizophrenic patients who were receiving 5 to 10 mg of Fluphenazine decanoate every 2 weeks were monitored for prodromal symptoms using an idiosyncratic prodromal rating scale. When patients met our criteria for a prodromal episode, they were randomly assigned to a double-blind comparison of oral Fluphenazine hydrochloride (5 mg twice daily) or a placebo for the current and future prodromal episodes. We compared rates of psychotic exacerbations in the two treatment groups. Results: Thirty-six patients (45%) met the criteria for a prodrome at some point during the trial and were randomized to drug or placebo. Using survival analysis during the entire 2 years, we did not find a significant difference between Fluphenazine and placebo in the likelihood that a prodrome would continue to an exacerbation. Survival analysis beginning at the start of the second year of treatment did indicate a significant reduction in exacerbation risk for patients receiving drug supplementation ( P =.032). Similarly, there was no difference between the two groups in the proportion of time at risk spent in exacerbation during the first year, but patients receiving active drug supplementation spent less time in an exacerbated state in the second year ( P =.05). Conclusions: Our treatment strategy appeared to be effective for some patients, particularly those who were able to remain in the study beyond the first year. Although the occurrence of a prodrome was a fairly good marker that a patient was at high risk of ultimate exacerbation with our low-dose maintenance protocol, prodromes were not highly sensitive indicators of imminent exacerbation.
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the determination of the steady state pharmacokinetic profile of Fluphenazine decanoate by gas chromatography mass spectrometry detection
Schizophrenia Research, 1992Co-Authors: William M Glazer, Lawrence T Friedhoff, Stephen R. Marder, Walter A. BrownAbstract:Abstract This study uses the highly sensitive method of gas chromatography/mass spectrometry to compare the basic steady-state pharmacokinetic parameters of two Fluphenazine decanoate formulations. Sixteen stable outpatients participated in a two-way crossover design study of the bioavailability of a new formulation of FPZ Dec, i.e., 10 mg/ml, to the standard 25 mg/ml formulation. When compared to a 1 ml injection of the standard formulation (25 mg/ml) over a two-week, steady-state period, we found bioequivalence as evidenced by similar mean areas under the curve (hrs x ng/ml). We did find that the injection volume of the same dose (2.5 ml of a 10 mg/ml formulation) results in a statistically higher maximum serum level of parent Fluphenazine. A tendency toward faster time to peak level was observed with the 10 mg/ml formulation but the difference was not statistically significant. Both of these differences are considered too small to be clinically significant. In a subgroup of 10 patients, pre-injection serum Fluphenazine levels correlated significantly (Pearson r = 0.78, p
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plasma levels of Fluphenazine in patients receiving Fluphenazine decanoate relationship to clinical response
British Journal of Psychiatry, 1991Co-Authors: Stephen R. Marder, T Van Putten, Manickam Aravagiri, E M Hawes, J W Hubbard, Kamal K. Midha, Gordon Mckay, Jim MintzAbstract:The levels of Fluphenazine and Fluphenazine sulphoxide in schizophrenic patients who were randomly assigned to receive either 5 mg or 25 mg of Fluphenazine decanoate every two weeks were monitored. Patients treated with 25 mg of Fluphenazine decanoate required three months to reach a steady-state plasma level, indicating that those patients who are being converted from oral to depot Fluphenazine should continue to receive oral supplementation during the first three months of treatment with Fluphenazine decanoate. Plasma levels of Fluphenazine sulphoxide were lower than levels of Fluphenazine. At six and nine months following randomisation, there was a statistically significant relationship between lower Fluphenazine plasma levels and an increased risk of psychotic exacerbations. A relatively weak relationship was found between Fluphenazine plasma levels and akinesia, but non-significant relationships between Fluphenazine levels and other neurological side-effects including akathisia, retardation, and tardive dyskinesia. Monitoring the plasma levels may be helpful to clinicians who are attempting to treat stabilised patients with the lowest effective dose of Fluphenazine decanoate.
David Pickar - One of the best experts on this subject based on the ideXlab platform.
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The Brain Metabolic Patterns of Clozapine- and Fluphenazine-Treated Female Patients with Schizophrenia: Evidence of a Sex Effect
Neuropsychopharmacology, 1999Co-Authors: Robert M Cohen, Thomas E Nordahl, William E Semple, David PickarAbstract:The regional cerebral glucose metabolic rates of clozapine-treated and Fluphenazine-treated women with schizophrenia and normal controls were obtained by positron emission tomography (PET) using [^18F]-2-fluoro-2-deoxy-D-glucose (FDG) as the tracer. The regional metabolic patterns were compared to each other and to the changes previously observed in men. In women, as in men, both clozapine- and Fluphenazine-treatment were associated with lower metabolism in the superior prefrontal cortex and higher metabolism in the medial temporal lobe. In both men and women, clozapine treatment led to a greater lowering of inferior prefrontal cortex activity than Fluphenazine, which was statistically significant in the larger male cohort. Fluphenazine led to higher metabolic rates in the lateral temporal lobe than clozapine did, but the differences between the two neuroleptics were not statistically significant in either group. The greatest differences in the female as compared to the male responses to Fluphenazine and clozapine were in the cingulate and striatum. As compared to controls, the cingulate metabolic rates of women were reduced by 9.1% and 11.4% on clozapine and Fluphenazine, respectively; whereas, men have a statistically nonsignificant reduction of 0.1% with clozapine and a 3.2% increase with Fluphenazine. In men, Fluphenazine was associated with a much greater elevation in basal ganglia metabolic rates than was clozapine, 23.5 % as compared to 3.75%; whereas, in women, basal ganglia metabolic rates are nearly equally increased by Fluphenazine (21.6%) and clozapine (15.1%).
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the brain metabolic patterns of clozapine and Fluphenazine treated patients with schizophrenia during a continuous performance task
Archives of General Psychiatry, 1997Co-Authors: Robert M Cohen, Robert E Litman, Thomas E Nordahl, William E Semple, Paul J Andreason, David PickarAbstract:Background: The comparison of the effects of 2 classes of neuroleptic drugs on regional brain functional activities may reveal common mechanisms of antipsychotic drug efficacy. Methods: The regional cerebral glucose metabolic rates of patients with schizophrenia who were and were not receiving neuroleptic drugs and normal control subjects were obtained by positron emission tomography using fludeoxyglucose F 18 as the tracer. Results: Compared with normal controls and patients not receiving medication, Fluphenazine hydrochloride—and clozapine-treated patients had lower global gray matter absolute metabolic rates throughout the cortex. When normalized regional glucose metabolic rates were examined, both medications lowered rates in the superior prefrontal cortex and increased rates in the limbic cortex. Fluphenazine, but not clozapine, increased metabolic rates in the subcortical and lateral temporal lobes, whereas clozapine, but not Fluphenazine, decreased inferior prefrontal cortex activity. Conclusions: These changes are consistent with the idea that neuroleptic drugs lead to "compensation" and "adaptation" rather than "normalization" of the functional activities of brain structures in schizophrenia. The overall similarity of their global and regional metabolic effects suggests that both classes of antipsychotic drugs share some common mechanisms of action. One possibility is that of inducing a shift in the balance of cortical to limbic cortex activity. Differential effects in the inferior prefrontal cortex and the basal ganglia might underlie differences in the therapeutic efficacy and side effect profile of clozapine and Fluphenazine.
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Idazoxan, an α2 Antagonist, Augments Fluphenazine in: Schizophrenic Patients A Pilot Study
Journal of clinical psychopharmacology, 1993Co-Authors: Robert E Litman, William Z. Potter, Walter W. Hong, Ellen M. Weissman, David PickarAbstract:Idazoxan, a selective alpha 2-adrenergic antagonist, was added to stable doses of Fluphenazine treatment in six patients with schizophrenia who participated in a double-blind, placebo-controlled pharmacologic study. Compared with Fluphenazine alone, combining idazoxan (mean dose, 120 mg/day) with Fluphenazine (mean dose, 28 mg/day) resulted in a significant decrease in Brief Psychiatric Rating Scale total symptoms (p < 0.05). Symptom ratings returned to baseline upon idazoxan discontinuation. No significant effects of idazoxan were observed on Fluphenazine levels in plasma or on extrapyramidal symptoms. These pilot data are compatible with the notion that increased noradrenergic neurotransmission may enhance the therapeutic effects of typical neuroleptics in schizophrenia.
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clinical and biologic response to clozapine in patients with schizophrenia crossover comparison with Fluphenazine
Archives of General Psychiatry, 1992Co-Authors: David Pickar, Richard R Owen, Robert E Litman, Eric P Konicki, Rolando Gutierrez, Mark Hyman RapaportAbstract:• Twenty-one patients with schizophrenia who met criteria for neuroleptic treatment resistance or intolerance participated in a crossover, placebo-controlled, double-blind comparison of long-term typical neuroleptic and clozapine treatment. Clozapine significantly reduced total as well as positive and negative symptoms in comparison with both Fluphenazine and placebo. Of the 21 patients, eight (38%) showed clozapine superiority on the basis of prospective response criteria. High levels of extrapyramidal side effects during Fluphenazine treatment and later onset of illness were clinical predictors of clozapine superiority. Clozapine and Fluphenazine equally reduced plasma homovanillic acid levels in comparison with placebo, although Fluphenazine but not clozapine increased plasma prolactin level. A striking biologic difference between clozapine and Fluphenazine was clozapine's enhancement of indexes of noradrenergic activity. Superior clozapine response was predicted by low ratios of cerebrospinal fluid homovanillic acid to 5-hydroxyindoleacetic acid, consistent with the notion that balance between dopaminergic and serotoninergic systems is important for clozapine's mechanism of action.
Manickam Aravagiri - One of the best experts on this subject based on the ideXlab platform.
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adverse extrapyramidal effects in four horse given Fluphenazine decanoate
Javma-journal of The American Veterinary Medical Association, 2006Co-Authors: John D Baird, Manickam Aravagiri, Kimberly M J Mcgurrin, Alexander Rodriguezpalacios, Daniel G Kenney, Modest Vengust, Luis G Arroyo, George A MaylinAbstract:Case Description—4 racehorses were examined because of markedly abnormal behavior following administration of Fluphenazine decanoate. Clinical Findings—Clinical signs included restlessness, agitation, profuse sweating, hypermetria, aimless circling, intense pawing and striking with the thoracic limbs, and rhythmic swinging of the head and neck alternating with episodes of severe stupor. Fluphenazine was detected in serum or plasma from all 4 horses. The dose of Fluphenazine decanoate administered to 3 of the 4 horses was within the range (25 to 50 mg) routinely administered to adult humans. Treatment and Outcome—In 2 horses, there was no response to IV administration of diphenhydramine hydrochloride, but the abnormal behavior in these 2 horses appeared to resolve following administration of benztropine mesylate, and both horses returned to racing. The other 2 horses responded to diphenhydramine administration. One returned to racing. The other was euthanized because of severe neurologic signs, respiratory...
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Fluphenazine plasma level monitoring for patients receiving Fluphenazine decanoate
Schizophrenia Research, 2002Co-Authors: Stephen R. Marder, Manickam Aravagiri, Donna A Wirshing, Malca B Lebell, William C Wirshing, Jim MintzAbstract:Abstract Background: Finding a dose of an antipsychotic for maintenance therapy that is both safe and effective can be difficult because clinicians are unable to titrate dose against clinical response in patients who are already stable. Therapeutic monitoring of antipsychotic plasma levels has the potential for helping clinicians in dosage selection. With this in mind, we evaluated the usefulness of monitoring Fluphenazine plasma levels for patients with schizophrenia who were receiving maintenance treatment with Fluphenazine decanoate. Method: Thirty-one patients with schizophrenia were randomly assigned to low, medium, or high (0.1–0.3, 0.3–0.6, 0.6–1.0 ng/ml) plasma levels of Fluphenazine. The dose of Fluphenazine decanoate was adjusted in order to maintain patients in their assigned range. Side effects, psychopathology, and psychotic exacerbations were measured during the year following randomization. Results: All of the psychotic exacerbations occurred during the first eight weeks following randomization, before patients had adequate time to reach their plasma level assignments. We did not find a relationship between plasma levels of Fluphenazine and clinical outcomes or side effects. Conclusion: Our results do not provide support for the usefulness of monitoring Fluphenazine plasma levels for patients receiving Fluphenazine decanoate.
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Fluphenazine levels during maintenance treatment of recent onset schizophrenia relation to side effects psychosocial function and depression
Psychopharmacology, 2000Co-Authors: Michael J Gitlin, Jim Mintz, Keith H Nuechterlein, David L Fogelson, George Bartzokis, Joseph Ventura, Kenneth L Subotnik, Manickam AravagiriAbstract:Rationale: The utility of Fluphenazine levels during maintenance treatment of schizophrenia is still unclear. Objectives: This study investigated the relationship between Fluphenazine levels and a variety of clinical measures during maintenance treatment of schizophrenia. Methods: Fluphenazine levels, side effects, depression and psychosocial outcome were measured at five time points over approximately 1 year in 59 recent onset schizophrenic patients treated with a maintenance dose of injectable Fluphenazine decanoate. Negative symptoms were evaluated at the 1-year endpoint. Results: Fluphenazine levels showed marked intraindividual variability even when measurements were restricted to the second 6 months of treatment, by which time steady state levels should have been achieved. No consistent relationship was found between Fluphenazine levels and any of the outcome measures. Conclusions: The results of this study suggest that Fluphenazine plasma levels do not routinely add relevant clinical information beyond that of dose in evaluating potential side effects or negative consequences during maintenance treatment with the decanoate form of the medication.
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plasma levels of Fluphenazine in patients receiving Fluphenazine decanoate relationship to clinical response
British Journal of Psychiatry, 1991Co-Authors: Stephen R. Marder, T Van Putten, Manickam Aravagiri, E M Hawes, J W Hubbard, Kamal K. Midha, Gordon Mckay, Jim MintzAbstract:The levels of Fluphenazine and Fluphenazine sulphoxide in schizophrenic patients who were randomly assigned to receive either 5 mg or 25 mg of Fluphenazine decanoate every two weeks were monitored. Patients treated with 25 mg of Fluphenazine decanoate required three months to reach a steady-state plasma level, indicating that those patients who are being converted from oral to depot Fluphenazine should continue to receive oral supplementation during the first three months of treatment with Fluphenazine decanoate. Plasma levels of Fluphenazine sulphoxide were lower than levels of Fluphenazine. At six and nine months following randomisation, there was a statistically significant relationship between lower Fluphenazine plasma levels and an increased risk of psychotic exacerbations. A relatively weak relationship was found between Fluphenazine plasma levels and akinesia, but non-significant relationships between Fluphenazine levels and other neurological side-effects including akathisia, retardation, and tardive dyskinesia. Monitoring the plasma levels may be helpful to clinicians who are attempting to treat stabilised patients with the lowest effective dose of Fluphenazine decanoate.
J W Hubbard - One of the best experts on this subject based on the ideXlab platform.
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the roles of depot injection sites and proximal lymph nodes in the presystemic absorption of Fluphenazine decanoate and Fluphenazine ex vivo experiments in rats
Pharmaceutical Research, 1998Co-Authors: J W Hubbard, K K MidhaAbstract:Purpose. The release and presystemic absorption of Fluphenazine and its decanoate ester from intramuscular depots were investigated.
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sensitive method for the simultaneous measurement of Fluphenazine decanoate and Fluphenazine in plasma by high performance liquid chromatography with cuolometric detection
Journal of Chromatography B: Biomedical Sciences and Applications, 1997Co-Authors: J W Hubbard, Kamal K. MidhaAbstract:Abstract A highly sensitive and specific high-performance liquid chromatographic method with coulometric detection was developed for the simultaneous assay of Fluphenazine decanoate and Fluphenazine in plasma. The extraction and sample clean-up procedures are simple, rapid to execute, yet yield chromatograms relatively free of any interference from endogenous plasma constituents, such that the extraordinary sensitivity of the coulometric detector can be exploited fully. This is the first analytical procedure for the simultaneous determination of Fluphenazine decanoate and Fluphenazine. The detection limits for both Fluphenazine decanoate and Fluphenazine were 0.1 ng/ml plasma and the limits of quantitation were 0.25 ng/ml plasma. Standard curves from 0.25 to 10 ng/ml were linear with coefficients of variation
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sensitive method for the simultaneous measurement of Fluphenazine decanoate and Fluphenazine in plasma by high performance liquid chromatography with coulometric detection
Journal of Chromatography B: Biomedical Sciences and Applications, 1997Co-Authors: Jiangping Luo, J W Hubbard, K K MidhaAbstract:A highly sensitive and specific high-performance liquid chromatographic method with coulometric detection was developed for the simultaneous assay of Fluphenazine decanoate and Fluphenazine in plasma. The extraction and sample clean-up procedures are simple, rapid to execute, yet yield chromatograms relatively free of any interference from endogenous plasma constituents, such that the extraordinary sensitivity of the coulometric detector can be exploited fully. This is the first analytical procedure for the simultaneous determination of Fluphenazine decanoate and Fluphenazine. The detection limits for both Fluphenazine decanoate and Fluphenazine were 0.1 ng/ml plasma and the limits of quantitation were 0.25 ng/ml plasma. Standard curves from 0.25 to 10 ng/ml were linear with coefficients of variation < 10%. The method was applied to measure plasma levels of Fluphenazine decanoate and Fluphenazine in patients under medication with 25-50 mg biweekly intramuscular (i.m.) injections of Fluphenazine decanoate. It was possible to monitor the plasma levels of Fluphenazine in all cases. Fluphenazine decanoate was present in measurable concentration in the plasma of 4 out of 5 patients who received biweekly i.m. injections of 50 mg Fluphenazine decanoate. In a pilot experiment with a dog, the method was used to follow Fluphenazine decanoate and Fluphenazine plasma levels up to 13 days, at least, after i.m. single dose (10 mg/kg).
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the role of the lymphatic system in the presystemic absorption of Fluphenazine after intramuscular administration of Fluphenazine decanoate in rats
European Journal of Pharmaceutical Sciences, 1995Co-Authors: Y. Huang, J W Hubbard, Kamal K. MidhaAbstract:Abstract Sprague Dawley rats (n = 16) were injected intramuscularly with Fluphenazine decanoate (78 mg/kg) in sesame oil. Groups of four rats were surgically prepared on days 1, 7, 15 and 32 post-injection and samples of lymph obtained from the thoracic duct. Fluphenazine was found in similar concentrations in lymph and plasma, although the decanoate was not detected in either body fluid. These data suggest that the lymphatic system plays a role in the presystemic absorption of Fluphenazine after i.m. administration of Fluphenazine decanoate in the rat. In vitro experiments showed that Fluphenazine decanoate was very rapidly hydrolyzed when incubated with rat plasma ( t 1 2 0.6 h ) or muscle homogenates ( t 1 2 1.0 h ). Rates of hydrolysis of Fluphenazine decanoate were lower in dog muscle homogenates ( t 1 2 4.3 h ), and very much lower when incubated with plasma from dog 42.9 h) or humans ( t 1 2 50.9 h).
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plasma levels of Fluphenazine in patients receiving Fluphenazine decanoate relationship to clinical response
British Journal of Psychiatry, 1991Co-Authors: Stephen R. Marder, T Van Putten, Manickam Aravagiri, E M Hawes, J W Hubbard, Kamal K. Midha, Gordon Mckay, Jim MintzAbstract:The levels of Fluphenazine and Fluphenazine sulphoxide in schizophrenic patients who were randomly assigned to receive either 5 mg or 25 mg of Fluphenazine decanoate every two weeks were monitored. Patients treated with 25 mg of Fluphenazine decanoate required three months to reach a steady-state plasma level, indicating that those patients who are being converted from oral to depot Fluphenazine should continue to receive oral supplementation during the first three months of treatment with Fluphenazine decanoate. Plasma levels of Fluphenazine sulphoxide were lower than levels of Fluphenazine. At six and nine months following randomisation, there was a statistically significant relationship between lower Fluphenazine plasma levels and an increased risk of psychotic exacerbations. A relatively weak relationship was found between Fluphenazine plasma levels and akinesia, but non-significant relationships between Fluphenazine levels and other neurological side-effects including akathisia, retardation, and tardive dyskinesia. Monitoring the plasma levels may be helpful to clinicians who are attempting to treat stabilised patients with the lowest effective dose of Fluphenazine decanoate.