Serum concentrations of cis(Z)-flupentixol and prolactin in chronic schizophrenic patients treated with flupentixol and cis(Z)-flupentixol decanoate
Abstract
Nine chronic schizophrenic patients selected from three hospital departments were treated with flupentixol (orally and IV) and cis(Z)-flupentixol decanoate in Viscoleo (IM) in a three-phase pharmacokinetic study. Oral administration (single and repeated dosage) showed a relatively slow absorption with maximum serum concentration around 4 h after administration. Intravenous injection indicated multicompartment kinetics for cis(Z)-flupentixol. The biological half-lives calculated after the different doses were the same, indicating that the pharmacokinetics of cis(Z)-flupentixol does not differ between single and repeated administration and does not change when moderately higher doses are given. The bioavailability of orally administered cis(Z)-flupentixol was calculated to be about 40% with IV injection as reference. After IM administration maximum serum concentration was seen between 4 and 10 days in most patients. Calculation of a disappearance half-life gave very variable results, indicating that the release of the drug from the oil depot is not a monoexponential process. The intramuscular depot had a much lower bioavailability than IV injection, which means that steady state has not been obtained after 8 weeks of depot treatment. Serum prolactin concentrations were elevated during neuroleptic treatment, but no correlation was found between prolactin concentrations and the serum concentrations of cis(Z)-flupentixol. A correlation between the changes in clinical ratings and concentrations of cis(Z)-flupentixol or prolactin was not found.
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Wide variability in apparent half-lives of flupentixol decanoate has been reported (5.3-112.6 days), owing to uneven release of the ester from the oil.
“However, wide variability in apparent half-lives has been reported (5.3–112.6 days), owing to uneven release of the ester from the oil.”
From Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview (2021) · cites this paper as [44]
Flupentixol LAI is formulated with the cis(Z)-flupenthixol isomer (the active enantiomer) using a decanoate ester in the coconut-derived oil vehicle Viscoleo.
“The LAI preparation is formulated with cis(Z)-flupenthixol isomer (the active enantiomer) using a decanoate ester in the coconut-derived oil vehicle, Viscoleo [44].”
From Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview (2021) · cites this paper as [44]
The depot properties of flupentixol decanoate depend on the slow release of the ester from the oil vehicle.
“the depot properties depend on the slow release of the ester from the oil vehicle [44]”
From Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview (2021) · cites this paper as [44]
Peak plasma concentrations of flupentixol decanoate are achieved 4-10 days after injection, indicating relatively slow absorption compared with the tmax of oral flupentixol (4 h).
“Peak plasma concentrations of flupentixol decanoate are achieved 4–10 days after injection, indicating a relatively slow absorption compared with the tmax of oral flupentixol (4 h) [44].”
From Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview (2021) · cites this paper as [44]
The mean apparent half-life of flupentixol decanoate was estimated at 17.3 days, based on steady-state concentration data obtained at days 14, 21, and 28.
“The mean apparent half-life was estimated at 17.3 days, based on concentration data at steady state obtained at days 14, 21, and 28 [44].”
From Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview (2021) · cites this paper as [44]
Oral flupentixol 10 mg per day was estimated to be equivalent to intramuscular flupentixol decanoate 40 mg every 2 weeks.
“Oral flupentixol 10 mg per day was estimated to be equivalent to intramuscular flupentixol decanoate 40 mg every 2 weeks [44].”
From Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview (2021) · cites this paper as [44]
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References 40 · Cited by 36
- Authors
- J�rgensen, A., Andersen, J., Bj�rndal, N., Dencker, S. J., Lundin, L., & Malm, U.
- Affiliations
- Lundbeck (Denmark) (DK)
- Sankt Hans Hospital (DK)
- ORCID
- Venue
- Psychopharmacology
- Published
- 1982-05
- Volume
- 77
- Issue
- 1
- Pages
- 58-65
- ISSN
- 0033-3158 (ISSN-L)
- 1432-2072
- OpenAlex
- W2007085449
- Cited by
- 36
- References
- 40
- Citations by year
- 2025: 2 · 2024: 1 · 2021: 1 · 2020: 2 · 2016: 1 · 2014: 2 · 2013: 2 · 2012: 2
- FWCI
- 1.60
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Psychopharmacology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Psychiatry and Mental health › Schizophrenia research and treatment
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Health Sciences › Medicine › Pharmacology › Treatment of Major Depression
- Keywords
- flupentixol, chronic schizophrenia, pharmacokinetics, serum prolactin, antipsychotic adverse effects, bioavailability, intravenous administration, oral administration, half-life
- MeSH terms
- Administration, Oral, Adult, Chronic Disease, Female, Flupenthixol, Half-Life, Humans, Injections, Intravenous, Male, Middle Aged, Prolactin, Schizophrenia, Thioxanthenes
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