Influence of food intake on the bioavailability of zuclopenthixol. 1987

T Aaes-Jørgensen, and H Liedholm, and A Melander
Department of Biochemistry, H. Lundbeck A/S, Copenhagen, Denmark.

The single-dose kinetics of the neuroleptic thioxanthene zuclopenthixol was assessed in 12 healthy volunteers who ingested 10 mg of the drug orally, both on an empty stomach and together with a standardized breakfast of 1840 kj (440 kcal). The serum concentrations of zuclopenthixol were measured by HPLC. Concomitant food intake did not influence the peak concentration nor the time to reach the peak concentration or the elimination half-life of zuclopenthixol, but the AUC values were significantly increased. Hence it seems likely that concomitant food intake enhances the bioavailability of zuclopenthixol, without influencing its absorption rate. The most likely mechanism is that food reduces the presystemic clearance of the drug. As the increase in AUC was only 26%, it is doubtful whether zuclopenthixol has to be administered in a standardized relation to meals.

UI MeSH Term Description Entries
D008297 Male Males
D003006 Clopenthixol A thioxanthene with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors. Cisordinol,Zuclopenthixol,alpha-Clopenthixol,alpha Clopenthixol
D005260 Female Females
D005502 Food Substances taken in by the body to provide nourishment. Foods
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities
D013892 Thioxanthenes Compounds with three aromatic rings in linear arrangement with a SULFUR in the center ring.

Related Publications

T Aaes-Jørgensen, and H Liedholm, and A Melander
January 1976, Acta medica Scandinavica,
T Aaes-Jørgensen, and H Liedholm, and A Melander
January 1996, European journal of clinical pharmacology,
T Aaes-Jørgensen, and H Liedholm, and A Melander
June 1989, International journal of clinical pharmacology, therapy, and toxicology,
T Aaes-Jørgensen, and H Liedholm, and A Melander
April 2009, British journal of clinical pharmacology,
T Aaes-Jørgensen, and H Liedholm, and A Melander
January 1982, European journal of clinical pharmacology,
T Aaes-Jørgensen, and H Liedholm, and A Melander
January 1989, Pediatric hematology and oncology,
T Aaes-Jørgensen, and H Liedholm, and A Melander
May 1977, Acta pharmacologica et toxicologica,
T Aaes-Jørgensen, and H Liedholm, and A Melander
January 1982, Therapie,
T Aaes-Jørgensen, and H Liedholm, and A Melander
September 1986, Journal of pharmaceutical sciences,
T Aaes-Jørgensen, and H Liedholm, and A Melander
January 1977, Acta medica Scandinavica,
Copied contents to your clipboard!