Rapid target allopurinol concentrations in the hypoxic fetus after maternal administration during labour

Arch Dis Child Fetal Neonatal Ed. 2014 Mar;99(2):F144-8. doi: 10.1136/archdischild-2013-304876. Epub 2013 Dec 18.

Abstract

Objective: Perinatal hypoxia-induced free radical formation is an important cause of hypoxic-ischaemic encephalopathy and subsequent neurodevelopmental disabilities. Allopurinol reduces the formation of free radicals, which potentially limits hypoxia-induced brain damage. We investigated placental transfer and safety of allopurinol after maternal allopurinol treatment during labour to evaluate its potential role as a neuroprotective agent in suspected fetal hypoxia.

Design: We used data from a randomised, double-blind multicentre trial comparing maternal allopurinol versus placebo in case of imminent fetal hypoxia (NCT00189007).

Patients: We studied 58 women in labour at term, with suspected fetal hypoxia prompting immediate delivery, in the intervention arm of the study.

Setting: Delivery rooms of 11 Dutch hospitals.

Intervention: 500 mg allopurinol, intravenously to the mother, immediately prior to delivery.

Main outcome measures: Drug disposition (maternal plasma concentrations, cord blood concentrations) and drug safety (maternal and fetal adverse events).

Results: Within 5 min after the end of maternal allopurinol infusion, target plasma concentrations of allopurinol of ≥2 mg/L were present in cord blood. Of all analysed cord blood samples, 95% (52/55) had a target allopurinol plasma concentration at the moment of delivery. No adverse events were observed in the neonates. Two mothers had a red and/or painful arm during infusion.

Conclusions: A dose of 500 mg intravenous allopurinol rapidly crosses the placenta and provides target concentrations in 95% of the fetuses at the moment of delivery, which makes it potentially useful as a neuroprotective agent in perinatology with very little side effects.

Trial registration: The study is registered in the Dutch Trial Register (NTR1383) and the Clinical Trials protocol registration system (NCT00189007).

Publication types

  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Allopurinol / pharmacology*
  • Allopurinol / therapeutic use
  • Double-Blind Method
  • Female
  • Fetal Blood / chemistry*
  • Fetal Hypoxia / drug therapy*
  • Fetal Hypoxia / prevention & control
  • Fetus / drug effects
  • Fetus / metabolism
  • Free Radical Scavengers / pharmacology
  • Free Radical Scavengers / therapeutic use
  • Free Radicals / adverse effects
  • Humans
  • Hypoxia-Ischemia, Brain / prevention & control*
  • Infant, Newborn
  • Labor, Obstetric / blood*
  • Labor, Obstetric / drug effects
  • Maternal-Fetal Exchange / drug effects*
  • Neuroprotective Agents / pharmacology*
  • Neuroprotective Agents / therapeutic use
  • Placenta / drug effects
  • Placenta / metabolism
  • Pregnancy

Substances

  • Free Radical Scavengers
  • Free Radicals
  • Neuroprotective Agents
  • Allopurinol

Associated data

  • ClinicalTrials.gov/NCT00189007