Pharmacokinetics of Intravenous and Rectal Ketoprofen in Young Children
Rent the article at a discountRent now
* Final gross prices may vary according to local VAT.Get Access
Objective: To evaluate the relative bioavailabilities of ketoprofen after intravenous and rectal administration to young children.
Design: Open-label prospective parallel-group study.
Patients: Participants were 28 children aged 7 to 93 months.
Methods: Eighteen children received a single intravenous injection of ketoprofen 1 mg/kg, and ten children, weight 16–24 kg, received a 25mg ketoprofen suppository. Venous blood samples were collected at selected times after administration, ranging from 2 minutes to 8 hours for the intravenous group and from 30 minutes to 8 hours for the suppository group. A validated high performance liquid chromatography method was used to measure plasma ketoprofen concentrations.
Results: In the intravenous group, the maximum plasma concentration of ketoprofen ranged between 10.5 and 22.2 mg/L, and in the suppository group, following dose normalisation to 1 mg/kg of ketoprofen, between 3.8 and 7.4 mg/L. In the intravenous group, area under the concentration-time curve from zero to infinity ranged between 9.2 and 23.5 mg · h/L, and in the suppository group after dose normalisation between 8.8 and 12.9 mg · h/L. The bioavailability of ketoprofen from the suppository was about 73%. Volume of distribution was 0.04–0.10 L/kg in the intravenous group and 0.08–0.16 L/kg in the suppository group. The terminal half-life was comparable in both study groups, ranging between 0.7 and 3.0 hours in the intravenous group and between 1.2 and 2.9 hours in the suppository group.
Conclusion: Absorption of ketoprofen after rectal administration is reasonably rapid and predictable. Because the bioavailability of rectal ketoprofen is also relatively high, a suppository may be used in children in whom the drug cannot be given intravenously or by mouth.
- Schirm E, van den Berg P, Gebben H, et al. Drug use of children in the community assessed through pharmacy dispensing data. Br J Clin Pharmacol 2000; 50: 473–8 CrossRef
- Fossgreen J. Ketoprofen: a survey of current publications. Scand J Rheumatol 1976; 14: 7–32
- Keinänen-Kiukaanniemi S, Similä S, Kouvalainen K. Oral antipyretic therapy evaluation of the propionic acid derivates, ibuprofen, ketoprofen, fenoprofen and naproxen. Padiatr Padol 1980; 15: 239–44
- Kantor TG. Ketoprofen: a review of its pharmacologic and clinical properties. Pharmacotherapy 1986; 6: 93–103
- Kokki H, Nikanne E, Ahonen R. The feasibility of pain treatment at home after adenoidectomy with ketoprofen tablets in small children. Paediatr Anaesth 2000; 10: 531–5 CrossRef
- Kokki H, Le Liboux A, Jekunen A, et al. Pharmacokinetics of ketoprofen syrup in small children. J Clin Pharmacol 2000; 40: 354–9 CrossRef
- Kokki H, Tuomilehto H, Tuovinen K. Pain management after adenoidectomy with ketoprofen: comparison of rectal and intravenous routes. Br J Anaesth 2000; 85: 836–40 CrossRef
- Ishizaki T, Sasaki T, Suganuma T, et al. Pharmacokinetics of ketoprofen following single oral, intramuscular and rectal doses and after repeated oral administration. Eur J Clin Pharmacol 1980; 18: 407–14 CrossRef
- Debruyne D, Hurault de Ligny B, Ryckelynck JP, et al. Clinical pharmacokinetics of ketoprofen after single intravenous administration as a bolus or infusion. Clin Pharmacokinet 1987; 12: 214–21 CrossRef
- World Medical Association Declaration of Helsinki. Ethical principles for medical research involving human subjects. 52nd World Medical Association, General Assembly; 2000 Oct; Edinburgh, Scotland
- Upton RA, Buskin JN, Guentert TW, et al. Convenient and sensitive high-performance liquid chromatography assay for ketoprofen, naproxen and other allied drugs in plasma or urine. J Chromatogr 1980; 190: 119–28 CrossRef
- Akaike H. An information criterion (AIC). Math Sci 1976; 14: 5–9
- Kokki H, Tuomilehto H, Karvinen M. Pharmacokinetics of ketoprofen following oral and intramuscular administration in young children. Eur J Clin Pharmacol 2001; 57: 643–7 CrossRef
- Nahata MC, Durrell DE, Powell DA, et al. Pharmacokinetics of ibuprofen in febrile children. Eur J Clin Pharmacol 1991; 40: 427–8 CrossRef
- Kelley MT, Walson PD, Edge JH, et al. Pharmacokinetics and pharmacodynamics of ibuprofen isomers and acetaminophen in febrile children. Clin Pharmacol Ther 1992; 52: 181–9 CrossRef
- Montgomery CJ, McCormack JP, Reichert CC, et al. Plasma concentrations after high-dose (45mg kg-1) rectal acetaminophen in children. Can J Anaesth 1995; 42: 982–6 CrossRef
- van der Marel CD, van Lingen RA, Pluim MA, et al. Analgesic efficacy of rectal versus oral acetaminophen in children after major craniofacial surgery. Clin Pharmacol Ther 2001; 70: 82–90 CrossRef
- Barbanoj MJ, Antonijoan RM, Gich I. Clinical pharmacokinetics of dexketoprofen. Clin Pharmacokinet 2001; 40: 245–62 CrossRef
- Pharmacokinetics of Intravenous and Rectal Ketoprofen in Young Children
Volume 42, Issue 4 , pp 373-379
- Cover Date
- Print ISSN
- Online ISSN
- Springer International Publishing
- Additional Links
- Industry Sectors