Pharmacokinetics of Raclopride FormulationsInfluence of Prolactin and Tolerability in Healthy Male Volunteers
作者:
Gunilla Movin-Osswald,
Anna-Lena Nordström,
Margareta Hammarlund-Udenaes,
Anita Wahlén,
Lars Farde,
期刊:
Clinical Pharmacokinetics
(ADIS Available online 1992)
卷期:
Volume 22,
issue 2
页码: 152-161
ISSN:0312-5963
年代: 1992
出版商: ADIS
数据来源: ADIS
摘要:
The pharmacokinetic and pharmacodynamic properties of raclopride, a new antipsychotic, were investigated in 16 healthy men. Single 4mg doses were administered as intravenous infusion, oral solution and 2 extended release (ER) formulations.Total plasma clearance was about 100 ml/min (6.0 L/h), of which renal clearance accounted for 0.2 ml/min, indicating extensive metabolism. The volume of distribution was 1.5 L/kg; mean absolute bioavailability was 65 to 67% following the oral solution and the ER formulations.A transient increase in plasma prolactin levels followed both the intravenous infusion and the oral solution. The ER formulations resulted in a lower increase, which appeared later. However, the area under the prolactin level curve was similar after administration of all dosage forms.The frequency and severity of the most commonly reported side effects (tiredness and restlessness) were higher after the intravenous infusion than after the ER capsules. These findings indicate that such capsules may be advantageous for clinical antipsychotic treatment with raclopride.
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