Plasma Haloperidol and Clinical Response

Shostak, Michael; Perel, James M.; Stiller, Richard L.; Wyman, W.C.; Curran, Suzanne

doi:10.1097/00004714-198712000-00004

Cited by 40 publications

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“…Ereshefsky et a1.21 reported that RHL is -10-25% as active as HL in animals and humans and may act as a dopaminergic partial agonist, whereas Shostak et a1. 22 reported that the ratio of RHL and HL concentrations in plasma of nonresponding patients is higher than that of responding patients. In the present study, the ratio of AUCRHL to AUCHL in plasma also varied widely among patients.…”

Section: Discussionmentioning

confidence: 99%

Steady-State Pharmacokinetics of Haloperidol and Reduced Haloperidol in Schizophrenic Patients: Analysis of Factors Determining their Concentrations in Hair

Matsuno

Sato

Hirayama

et al. 1992

Journal of Pharmaceutical Sciences

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Section: Discussionmentioning

confidence: 99%

Steady-State Pharmacokinetics of Haloperidol and Reduced Haloperidol in Schizophrenic Patients: Analysis of Factors Determining their Concentrations in Hair

Matsuno

Sato

Hirayama

et al. 1992

Journal of Pharmaceutical Sciences

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Pharmacokinetics of reversible metabolic systems

Cheng

Jusko

1993

Biopharm & Drug Disp

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Clinical Pharmacokinetics of Antipsychotics

Javaid

1994

The Journal of Clinical Pharma

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The antipsychotics are a chemically diverse group of heterocyclic compounds, which ameliorate many symptoms of schizophrenia. Most of the antipsychotics are very lipophilic and cross lipoidal membranes freely. When administered orally, they are well absorbed and undergo substantial pre-systemic elimination (bioavailability: 10-70%), are highly bound to plasma proteins (75-99%) and tissues, and are extensively distributed (VD: 100-1000 L). Primary route of elimination for most of antipsychotics is hepatic metabolism and biotransformation produces active metabolites. There is no linear relationship between the concentration of parent compound and different metabolites, and clinical relevance of pharmacologically active metabolites is not well understood. There are wide interindividual variabilities in pharmacokinetics, which result in large differences in steady-state plasma concentrations on the same dose regimen. The existence of optimal therapeutic ranges for most antipsychotics remains controversial. One of the major problems is the lack of well-designed studies that involve sufficient numbers of patients to clearly establish a therapeutic range for these drugs and is further complicated by the presence of a large number of pharmacologically active metabolites. However, the pronounced interindividual kinetic variabilities, combined with problems of noncompliance and drug interactions, and the delayed onset of clinical response in relation to initiation of treatment with antipsychotics are reasons why drug monitoring in conjunction with clinical status of the patient can be useful. Indications for antipsychotic drug monitoring include lack of response, non-compliance, toxicity, and drug interactions when other drugs are coadministered.

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Plasma Haloperidol and Clinical Response

Cited by 40 publications

References 0 publications

Steady-State Pharmacokinetics of Haloperidol and Reduced Haloperidol in Schizophrenic Patients: Analysis of Factors Determining their Concentrations in Hair

Steady-State Pharmacokinetics of Haloperidol and Reduced Haloperidol in Schizophrenic Patients: Analysis of Factors Determining their Concentrations in Hair

Pharmacokinetics of reversible metabolic systems

Clinical Pharmacokinetics of Antipsychotics

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