Pharmacokinetics and antipyretic effects of an injectable pro‐drug of paracetamol (propacetamol) in children

Granry, J.C.; Rod, B.; Boccard, E.; Hermann, P; Gendron, Amandine; Saint-Maurice, C

doi:10.1111/j.1460-9592.1992.tb00219.x

Cited by 23 publications

(14 citation statements)

References 3 publications

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“…A two-compartment model, rather than a one-compartment model, was realised and bioavailability of propacetamol was compared directly with intravenous PARANEO. Our data confirm a bioavailability of 0.5 for propacetamol to paracetamol with a narrower 90% CI of 0.465 to 0.557 18–20. There was considerable variability associated with this estimate (CV 38.6%) due to the use of adult drug preparations for administration in neonates.…”

Section: Discussionsupporting

confidence: 64%

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The pharmacokinetics of intravenous paracetamol in neonates: size matters most

2011

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Section: Discussionsupporting

confidence: 64%

“…Propacetamol is hydrolysed by plasma esterases so that 1 g of propacetamol is hydrolysed to 0.5 g paracetamol in adults 18–20. Propacetamol bioavailability was compared with paracetamol.…”

Section: Pharmacokinetic Analysismentioning

confidence: 99%

The pharmacokinetics of intravenous paracetamol in neonates: size matters most

2011

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“…[1] and Granry et al. [2] describe the maximum temperature decrease occurring 2 h after peak plasma paracetamol concentrations in children. Nielsen et al.…”

Section: Introductionmentioning

confidence: 99%

Paracetamol plasma and cerebrospinal fluid pharmacokinetics in children

Anderson

Holford

Woollard

et al. 1998

Brit J Clinical Pharma

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Aims Paracetamol has a central action for both antipyresis and analgesia. Maximum temperature decrease and peak analgesia are reported at 1-2 h after peak plasma paracetamol concentration. We wished to determine the relationship between plasma and cerebrospinal fluid (CSF) pharmacokinetics in children. Methods Concentration-time profiles in plasma and CSF after nasogastric paracetamol 40 mg kg −1 were measured in nine children who had indwelling ventricular drains.Estimation of population pharmacokinetic parameters was made using both a standard two-stage population approach (MKMODEL) and a nonlinear mixed effect model (NONMEM). Results were standardized to a 70 kg person using an allometric power model. Results Both approaches gave similar estimates. NONMEM parameter estimates were clearance 10.2 l h −1 (CV 47%), volume of distribution 67.1 l (CV 58%) and absorption rate constant 0.77 h −1 (CV 49%). Cerebrospinal fluid concentrations lagged behind those of plasma. The equilibration half time was 0.72 h (CV 117%). The CSF/plasma partition coefficient was 1.18 (CV 8%). Conclusions Higher concentrations in the CSF probably reflect the lower free water volume of plasma. The CSF equilibration half time suggests that CSF kinetics approximate more closely to the effect compartment than plasma, but further time is required for paracetamol to exert its effects. Effect site concentrations equilibrate slowly with plasma. Paracetamol should be given 1-2 h before anticipated pain or fever in children.

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“…Die Wirkung tritt auch nach intravenöser Gabe verzögert auf. So wurde in einer Untersuchung zu Propacetamol bei Kindern der maximale antipyretische Effekt 2 h nach intravenöser Applikation beobachtet [35]. In einer anderen Untersuchung zeigte sich erst eine Stunde nach Applikation ein signifikanter Unterschied bezüglich der analgetischen Wirkung im Vergleich zu Placebo [36].…”

Section: Intravenöse Gabeunclassified

Paracetamol im Kindesalter Aktueller Wissensstand und Hinweise für einen rationalen Einsatz zur postoperativen Analgesie

Mantzke¹,

Brambrink²

2002

Anaesthesist

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The administration of paracetamol (in the US known as acetaminophen) to children and infants for postoperative pain after minor surgery is a well established and safe treatment option, if appropriately used. However, if paracetamol is dosed according to traditional recommendations (about 20 mg/kg body weight) frequently a sufficient analgetic effect cannot be achieved immediately after painful interventions. Recently, a higher initial dose (40 mg/kg body weight) was suggested for effective postoperative pain control, which seems especially important for children after ambulatory anesthesia, but may also be associated with certain risks to the patient. Current recommendations also involve appropriate timing and route of administration of paracetamol to be most effective under different clinical circumstances. In contrast, the risk for liver toxicity appears to be very low, if the daily paracetamol dose does not exceed 90 mg/kg body weight in otherwise healthy children, and if specific risk factors of the individual patient are always considered. This review discusses the recent publications on pharmacokinetics and -dynamics, the clinical use and dosing, as well as the risks and benefits of paracetamol for the treatment of postoperative pain in children and infants. Based on this information, specific dosing regimes for the postoperative period are suggested for neonates and infants, as well as for children in different age groups.

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Pharmacokinetics and antipyretic effects of an injectable pro‐drug of paracetamol (propacetamol) in children

Cited by 23 publications

References 3 publications

The pharmacokinetics of intravenous paracetamol in neonates: size matters most

The pharmacokinetics of intravenous paracetamol in neonates: size matters most

Paracetamol plasma and cerebrospinal fluid pharmacokinetics in children

Paracetamol im Kindesalter Aktueller Wissensstand und Hinweise für einen rationalen Einsatz zur postoperativen Analgesie

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