Journal of Pharmacological Sciences (Jan 2014)

Intravenous Paracetamol as an Antipyretic and Analgesic Medication: the Significance of Drug Metabolism

  • Evangelos J. Giamarellos-Bourboulis,
  • Aikaterini Spyridaki,
  • Athina Savva,
  • Marianna Georgitsi,
  • Thomas Tsaganos,
  • Maria Mouktaroudi,
  • Maria Raftogiannis,
  • Anastasia Antonopoulou,
  • Vassilios Papaziogas,
  • Fotini Baziaka,
  • Kalliopi Sereti,
  • Petros Christopoulos,
  • Androniki Marioli,
  • Theodora Kanni,
  • Panagiota Maravitsa,
  • Ilianna Pantelidou,
  • Konstantinos Leventogiannis,
  • Panagiotis Tsiaoussis,
  • Korina Lymberopoulou,
  • Ioannis M. Koutelidakis

Journal volume & issue
Vol. 124, no. 2
pp. 144 – 152

Abstract

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One prospective, open-label, non-randomized study was conducted in 100 patients to define the antipyretic and analgesic effect of a new intravenous formulation of 1 g of paracetamol; 71 received paracetamol for the management of fever and 29 received paracetamol for pain relief after abdominal surgery or for neoplastic pain. Serial follow-up measurements of core temperature and of pain intensity were done for 6 h. Additional rescue medications were recorded for 5 days. Blood was sampled for the measurement of free paracetamol (APAP) and of glucuronide-APAP and N-sulfate-APAP by an HPLC assay. Defervescence, defined as core temperature below or equal to 37.1°C, was achieved in 52 patients (73.2%) within a median time of 3 h. Patients failing to become afebrile with the first dose of paracetamol became afebrile when administered other agents as rescue medications. Analgesia was achieved in 25 patients (86.4%) within a median time of 2 h. Serum levels of glucuronide-APAP were greater among non-responders to paracetamol. The presented results suggest that the intravenous formulation of paracetamol is clinically effective depending on drug metabolism. Keywords:: intravenous paracetamol, fever, pain, analgesia