Pharmacokinetics of chlorpromazine after single and chronic dosage

  title={Pharmacokinetics of chlorpromazine after single and chronic dosage},
  author={Svein G. Dahl and Roald E. Strandjord},
  journal={Clinical Pharmacology \& Therapeutics},
  • Svein G. Dahl, Roald E. Strandjord
  • Published 1 April 1977
  • Medicine, Psychology
  • Clinical Pharmacology & Therapeutics
Plasma concentrations of chlorpromazine and its sulfoxide were measured after single intramuscular, single oral, and multiple oral doses of chlorpromazine. In four out of nine patients, intramuscular doses gave stable chlorpromazine plasma levels which were maintained for 12 hr or longer. Chlorpromazine sulfoxide was found in plasma from all patients after oral doses but not after intramuscular doses, which indicates that sulfoxidation took place presystemically. The biologic availability of… 
Oral contraceptives increase the plasma concentrations of chlorpromazine.
A 21-year-old female inpatient who was enrolled in a population pharmacokinetic study of chlor Promazine was given an oral chlorpromazine dose of 100 mg three times daily, and plasma concentrations of chlorPromazine were measured weekly, suggesting that the oral contraceptive increased the plasma concentration of chlor promazine.
Pharmacokinetics and relative bioavailability of levomepromazine after repeated administration of tablets and syrup
Plasma levels of levomepromazine and its sulphoxide were measured in 8 psychiatric patients after repeated doses of levitepromazine tablets or syrup, and it was postulated that individual variation in the dose required for therapy was due in part to individual variations in the pharmacokinetics of the drug.
Pharmacokinetics of Chlorimipramine, Chlorpromazine and their N‐Dealkylated Metabolites in Plasma of Healthy Volunteers After a Single Oral Dose of the Parent Compounds
The response to single doses of these two drugs in healthy subjects highlights the two distinct dispositional processes involved, thus offering pharmacokinetic explanation of the hitherto empirical discrepancy in dosage levels in chronic treatment.
Chlorpromazine metabolism. IX. Pharmacokinetics of chlorpromazine following oral administration in man
Results suggest that Chlorpromazine absorption is zero order, and a closer random scatter of the observed concentration data around the calculated curve with no apparent systematic deviations from the curve.
Pharmacokinetics of chlorpromazine and key metabolites
The data suggest that the high degree of variability in the pharmacokinetics of CPZ is a result of extensive first pass metabolism rather than variation in half life, whereas half life did not appear to be dose dependant.
Pharmacokinetics and first-pass metabolism of levomepromazine in the rat.
It is concluded that the rat provides a suitable model for the kinetics of levomepromazine in man, and that the sulfoxide and N-monodesmethyl metabolites of the drug are mainly formed by first-pass metabolism after oral doses in the rat, either in the liver or in the gut.
Single-dose kinetics of the neuroleptic drug perazine in psychotic patients
There was a significant positive correlation between AUC and age and large interindividual variations in plasma levels of perazine and its demethylated metabolite, with maximal concentrations as well as AUC values ofperazine differing more than 10-fold.
Pharmacokinetics of promethazine and its sulphoxide metabolite after intravenous and oral administration to man.
Evidence is presented to support the hypothesis that S-oxidation of promethazine is predominantly an hepatic event and the role of the gut mucosa in S-Oxidation of phenothiazines is critically assessed.
Single oral dose kinetics of zotepine and its relationship to prolactin response and side effects.
The current results clearly indicate that the tmax and t1/2 of zotepine are much longer than those previously reported, which is reflected in the changes in prolactin concentrations and side effect scores.
Preliminary studies of the pharmacokinetics and pharmacodynamics of prochlorperazine in healthy volunteers.
The pharmacokinetics and pharmacodynamics of prochlorperazine were studied in healthy volunteers using a recently developed h.l.p.c. assay and the main adverse effect was akathisia which was reported by five out of eight subjects after the higher i.v. dose.


Pharmacokinetics of methotrimeprazine after single and multiple doses
  • S. Dahl
  • Medicine, Biology
    Clinical pharmacology and therapeutics
  • 1976
The sulfoxide could not be traced in plasma after a 25‐mg intramuscular dose, but was found in higher plasma concentrations than the unmetabolized drug after single and multiple oral doses.
Studies of delayed‐action medication V. Plasma levels and urinary excretion of four different dosage forms of chlorpromazine
The use of the long‐acting oral dosage form does not seem warranted for a drug such as chlorpromazine; liquid or tablet dosage forms were more reliable and satisfied the claims made for long‐ acting dosage forms in chronic treatment.
The relationship of plasma chlorpromazine to its 7-hydroxy and sulphoxide metabolites in a large population of chronic schizophrenics.
It is suggested that a prediction of therapeutic response to chlorpromazine may be provided in the form of the ratio of the plasma concentration of biologically active metabolite to the concentration of either the unchanged drug or its inactive metabolite.
Effects of mode of management on plasma chlorpromazine in psychiatric patients
The study suggests that schizophrenic patients with negligible plasma levels of chlorpromazine are not likely to improve clinically, and interpatient and intrapatient data suggest that trihexyphenidyl tends to lower plasma Levels of chlor Promazine.
Physiologic and clinical effects of chlorpromazine and their relationship to plasma level
Plasma levels and clinical improvement were weakly related during the first 2 weeks of treatment only; clinical improvement correlated with palmar skin conductance (sweating) and with some latencies of the electroencephalographic‐evoked response.
GLC determination of methotrimeprazine and its sulfoxide in plasma.
A GLC method, based on flame-ionization detection, was developed for the assay of methotrimeprazine and its sulfoxide in plasma and was applied to the analysis of promazine and chlorpromazine in patient plasma.
Route of administration and drug metabolism.
Influence of first-pass effect on availability of drugs on oral administration.
Plasma level data for propranolol in man have been used to indicate the utility of these equations, and the significance of these calculations to the design of clinical studies with new drugs intended for oral use is discussed.
The present studies indicate that in the dog chlorpromazine, prochlorperazine, and trifluoperazine are rapidly absorbed from the intestine and that there is a rapid hepatic clearance of the
Blood Levels of Drug at the Equilibrium State after Multiple Dosing
THERE is ample evidence1–20 that when a fixed dose of drug is administered in a fixed multiple-dose regimen, the blood levels of drug eventually reach a steady state in which the blood level time