| Title | Pharmacokinetics of antipsychotics | |
| Authors | Dejana T. Ruzic1, Vassiliki Mirtsou-Fidani2 and Slobodan M. Jankovic3
1. Department of Pharmacology, Medical Faculty, Kragujevac, Serbia, FR Yugoslavia 2. Department of Pharmacology, Medical Faculty, Aristotle University of Thessaloniki, Greece 3. Center for Clinical and Experimental Pharmacology, Clinical Hospital Center, Kragujevac, Serbia, FR Yugoslavia |
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| Citation | Ruzic, D.T., Mirtsou-Fidani, V., Jankovic, S.M.: Pharmacokinetics of antipsychotics, Epitheorese Klin. Farmakol. Farmakokinet. 12(3): 9-14 (1998) | |
| Publication Date | Received for publication: 1 October 1997
Accepted for publication: 5 October 1997 |
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| Full Text Language | English | |
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| Keywords | Neuroleptics, pharmacokinetics, dose regimen, individualization. | |
| Other Terms | review article | |
| Summary | The antipsychotics comprise chemically diverse group of heterocyclic compounds, which are effective in relieving positive schizophrenic symptoms and psychotic symptoms in other neuropsychiatric diseases. They are well absorbed from the gastrointestinal tract and undergo substantial pre-systemic elimination (bioavailability: 10-80%). Most of the antipsychotics are highly lipophilic and highly bound to plasma proteins (90-99%). They tend to have large volumes of distribution (usually >7 l/kg). The main route of elimination for most antipsychotics is hepatic metabolism; biotransformation produces mostly biologically inactive metabolites. However, a few oxidized metabolites are active and may contribute to biological activity of the parent drug. There are wide interindividual variabilities in pharmacokinetics, which result in large differences considering steady-state plasma concentrations on the same dose regimen. The influence of age, sex, smoking behavior, renal and liver functional impairment, combined with problems of noncompliance and drug interactions may change clinical response and produce serious adverse effects. Therefore, we suggest individualization of dosage regimen for every particular patient. | |
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