Pharmacokinetics of Intravenous Dantrolene in Children
Open Access
- 1 April 1989
- journal article
- research article
- Published by Wolters Kluwer Health in Anesthesiology
- Vol. 70 (4) , 625-629
- https://doi.org/10.1097/00000542-198904000-00013
Abstract
To determine the pharmacokinetics of iv dantrolene and its metabolites in children, ten children 2-7 yr of age scheduled for minor elective surgery, were studied. After induction of anesthesia and tracheal intubation, dantrolene (2.4 mg/kg) was administered iv over 10.2 .+-. 0.83 min. Venous blood samples (3 ml) were obtained 1, 5, 10, 20, and 30 min and 1, 2, 4, 8, 12 and 20 h after the dantrolene infusion. Whole blood concentrations of dantrolene, 5-hydroxydantrolene, and nitroreduced acetylated dantrolene were measured by high-performance liquid chromatography. The whole blood concentration of dantrolene decreased rapidly from a mean (.+-.SD) of 6.03 .+-. 0.93 .mu.g/ml 1 min after the end of the dantrolene infusion to 3.56 .+-. 0.49 .mu.g/ml at 1 h. Between 1 and 4 h, the concentration of dantrolene either remained constant or increased slightly. Thereafter, the concentration of dantrolene decreased slowly with an elimination half-life (mean .+-. SD) of 10.0 .+-. 2.6 h. The mean (.+-.SD) time for the concentration of dantrolene to decrease to 3.0 .mu.g/ml was 6.55 .+-. 2.88 h. The whole blood concentrations of 5-hydroxydantrolene reached a maximum of 0.60 .+-. 0.18 .mu.g/ml approximately 7 h after the dantrolene and decreased thereafter with an elimination half-life of 9.0 .+-. 2.5 h. The concentration of nitroreduced acetylated dantrolene was below the limit for detection at all times. All children recovered without complications. Intravenous dantrolene, 2.4 mg/kg, produces safe and predictable blood concentrations in children similar to those reported in adults.Keywords
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