Plasma haloperidol levels and clinical response in acute schizophrenia

Wistedt, B.; Johanidesz, Gesa; Omerhodzic, Majda; Arthur, Holger; Petters, Inga

doi:10.3109/08039488409093330

Cited by 9 publications

(6 citation statements)

References 7 publications

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“…Compared with the variation between patients, the steady-state plasma concentrations of antipsychotic drugs usually remain relatively stable in each individual, as shown in figure 2, provided the daily dose, route of administration and any concomitant administration of other drugs remain unchanged (Axelsson & Martensson 1977;Bigelow et al 1985;Dahl 1976;Gjerris et al 1981;Jeste et al 1982;Morselli et al 1982;Wistedt et al 1984;Young & Nysewander 1984). 38 …”

Section: Pharmacokinetic Factorsmentioning

confidence: 96%

“…Some recent reviews have expressed the more optimistic view that plasma level monitoring of some antipsychotic drugs may have clinical value, but have emphasised the need for more reliable data (BalantGorgia et al 1985;Morselli 1981;Morselli et al 1982;Rivera-Calimlim & Hershey 1984;Wistedt et al 1984). Morselli et al (1983) suggested that plasma level monitoring of haloperidol and chlorpromazine may be useful in paediatric neuropsychiatry.…”

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Plasma Level Monitoring of Antipsychotic Drugs Clinical Utility

Dahl

1986

Clinical Pharmacokinetics

145

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The steady-state plasma concentrations of antipsychotic drugs show large interpatient variations but remain relatively stable from day to day in each individual patient. Monitoring of antipsychotic drug concentrations in plasma might be of value provided the patients are treated with only 1 antipsychotic drug. Some studies have reported a relationship between therapeutic response and serum antipsychotic drug 'concentrations' as measured using the radioreceptor assay (RRA) method, which measures dopamine receptor-blocking activity in plasma. Most studies, however, have failed to demonstrate such a relationship, and the RRA does not seem to provide the generally useful tool for plasma concentration monitoring of antipsychotic drugs that was hoped for initially. A lack of correlation between dopamine receptor-blocking activity in plasma and therapeutic response may be due to differences in the blood-brain distribution of both antipsychotic drugs and their active metabolites. Chemical assay methods (e.g. GLC and HPLC) have been used in studies which examined the relationships between therapeutic response and antipsychotic drug concentrations in red blood cells and in plasma. It seems that for these drugs, measuring red blood cell concentrations does not offer any significant advantage over measuring plasma concentrations. Reasonably controlled studies of plasma concentration-response relationships using randomly allocated, fixed dosages of chlorpromazine, fluphenazine, haloperidol, perphenazine, sulpiride, thioridazine and thiothixene have been published but often involve relatively few patients. A correlation between therapeutic response and plasma concentrations of thioridazine and its metabolites has not been demonstrated, and plasma level monitoring of thioridazine and its metabolites therefore appears to have no clinical value. Clinical behavioural deterioration concomitant with high plasma concentrations of chlorpromazine and haloperidol have been reported. A dosage reduction might be considered after 2 to 4 weeks' treatment in non-responders who have plasma chlorpromazine concentrations above 100 to 150 micrograms/L or plasma haloperidol concentrations above 20 to 30 micrograms/L. Non-responders and good responders to chlorpromazine treatment, however, have plasma drug concentrations in the same range, and a therapeutic range of plasma chlorpromazine levels has not been defined. Therapeutic plasma haloperidol concentrations (i.e. 'window') in the range of 5 to 20 micrograms/L have been reported by some investigators, but others have found no such relationship.(ABSTRACT TRUNCATED AT 400 WORDS)

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Section: Pharmacokinetic Factorsmentioning

confidence: 96%

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confidence: 96%

Plasma Level Monitoring of Antipsychotic Drugs Clinical Utility

Dahl

1986

Clinical Pharmacokinetics

145

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“… References: a: [ 71 ]; b: [ 33 ]; c: [ 77 ]; d: [ 128 ]; e: [ 45 ]; f: [ 4 ]; g: [ 110 ]; h: [ 70 ]; i: [ 6 ]; j: [ 97 ]; k: [ 109 ]; l: [ 93 ]; m: [ 59 ]; n: [ 103 ]; o: [ 57 ]; p: [ 114 ]; q: [ 95 ]; r: [ 125 ]; s: [ 121 ]; t: [ 120 ]. …”

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Mechanisms of Action of Antipsychotic Drugs of Different Classes, Refractoriness to Therapeutic Effects of Classical Neuroleptics, and Individual Variation in Sensitivity to their Actions: PART II

Miller

2009

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Rapid-onset psychotic rebound is uncommon on discontinuation of most antipsychotic drugs, as might be expected for antipsychotic drugs with (hypothetically) indirect actions at their final target receptors. Rapid-onset psychosis is more common on withdrawal of clozapine, which might be expected if its action is direct. Drugs other than clozapine (notably thioridazine) may have hitherto unrecognised similarities to clozapine (but without danger of agranulocytosis), and may be useful in treatment of refractory psychosis. Quetiapine fulfils only some criteria for a clozapine-like drug. Clinical response to neuroleptics varies widely at any given plasma level. Haase’s “neuroleptic threshold” concept suggests that the dose producing the slightest motor side effects produces most or all of the therapeutic benefit, but analyses presented here suggest that antipsychotic actions are not subject to a sharp “all-or-none” threshold but increase over a small dose range. This concept could provide a method for quantitative determination of individualized optimal doses.

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“…A number of investigators have examined the association between haloperidol concentrations and clinical response in the treatment of schizophrenia. These reports fall into three general groups: (1) those that found no clear association between concentration and response (Ericksen et al 1978;Bjorndal et al 1980;Morselli et al 1980;Rimon et al 1981;Moulin et al 1982;Balant-Gorgia et al 1984;Bleeker et al 1984;Itoh et al 1984;Linkowski et al 1984;Neborsky et al 1984;Wistedt et al 1984;Bigelow et al 1985;Gerlach et al 1985); (2) those in which higher concentrations were associated with a better response (Smith et al 1979;Tune 1980;Cohen and Baldessarini 1981;DeBuck et al 1981;Evans 1981); and (3) those in which both low and high concentrations were associated with a poor clinical response in comparison with a middle range of apparently optimal concentrations, resulting in a curvilinear relationship or therapeutic window (Rao et al 1980;Magliozzi et al 1981;Extein et al 1982Extein et al , 1983Hollister and Kim 1982;Smith et al 1982Smith et al , 1984Smith et al , 1985Mavroidis et al 1983;Garver et al 1984;Miller et al 1984;Davis et al 1985;Potkin et al 1985;Van Putten et al 1985). As would be expected, these studies taken as a whole are fairly consistent in indicating a lower limit of serum or plasma concentrations below which patients do not optimally respond.…”

mentioning

confidence: 99%

“…These reports fall into three general groups: (1) those that found no clear association between concentration and response (Ericksen et al 1978; Bjorndal et al 1980; Morselli et al. 1980; Rimón et al 1981; Moulin et al 1982; Balant-Gorgia et al 1984; Bleeker et al 1984; Itoh et al 1984; Linkowski et al 1984; Neborsky et al 1984; Wistedt et al 1984; Bigelow et al 1985; Gerlach et al. 1985); (2) those in which higher concentrations were associated with a better response (Smith et al.…”

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confidence: 99%

Serum Haloperidol Concentration and Clinical Response in Schizophrenia

Kirch¹,

Bigelow²,

Korpi³

et al. 1988

Schizophrenia Bulletin

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Previous studies have reported a therapeutic window (i.e., a curvilinear relationship between clinical response and drug level) for haloperidol concentrations in serum or plasma. The authors treated 30 acutely decompensated schizophrenic inpatients with a fixed dose of haloperidol (.4 mg/kg/day). After 6 weeks there was no statistically significant correlation between clinical improvement and serum haloperidol concentration. Fifteen subjects with serum concentrations of 5-15 ng/ml did not differ in clinical improvement compared with 15 subjects who had concentrations above 15 ng/ml. These data are consistent with a therapeutic plateau, rather than a window, and suggest that in most cases there is no clinical advantage to the use of haloperidol doses greater than approximately 30 mg/day in schizophrenic patients.

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Plasma haloperidol levels and clinical response in acute schizophrenia

Cited by 9 publications

References 7 publications

Plasma Level Monitoring of Antipsychotic Drugs Clinical Utility

Plasma Level Monitoring of Antipsychotic Drugs Clinical Utility

Mechanisms of Action of Antipsychotic Drugs of Different Classes, Refractoriness to Therapeutic Effects of Classical Neuroleptics, and Individual Variation in Sensitivity to their Actions: PART II

Serum Haloperidol Concentration and Clinical Response in Schizophrenia

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