Attenuation of ethanol withdrawal by ceftriaxone-induced upregulation of glutamate transporter EAAT2

Neuropsychopharmacology. 2014 Jun;39(7):1674-84. doi: 10.1038/npp.2014.14. Epub 2014 Jan 23.

Abstract

Alcohol withdrawal syndrome (AWS) is a potentially fatal outcome of severe alcohol dependence that presents a significant challenge to treatment. Although AWS is thought to be driven by a hyperglutamatergic brain state, benzodiazepines, which target the GABAergic system, comprise the first line of treatment for AWS. Using a rat model of ethanol withdrawal, we tested whether ceftriaxone, a β-lactam antibiotic known to increase the expression and activity of glutamate uptake transporter EAAT2, reduces the occurrence or severity of ethanol withdrawal manifestations. After a 2-week period of habituation to ethanol in two-bottle choice, alcohol-preferring (P) and Wistar rats received ethanol (4.0 g/kg) every 6 h for 3-5 consecutive days via gavage. Rats were then deprived of ethanol for 48 h during which time they received ceftriaxone (50 or 100 mg/kg, IP) or saline twice a day starting 12 h after the last ethanol administration. Withdrawal manifestations were captured by continuous video recording and coded. The evolution of ethanol withdrawal was markedly different for P rats vs Wistar rats, with withdrawal manifestations occurring >12 h later in P rats than in Wistar rats. Ceftriaxone 100 mg/kg per injection twice per day (200 mg/kg/day) reduced or abolished all manifestations of ethanol withdrawal in both rat variants and prevented withdrawal-induced escalation of alcohol intake. Finally, ceftriaxone treatment was associated with lasting upregulation of ethanol withdrawal-induced downregulation of EAAT2 in the striatum. Our data support the role of ceftriaxone in alleviating alcohol withdrawal and open a novel pharmacologic avenue that requires clinical evaluation in patients with AWS.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alcohol Drinking / drug therapy
  • Analysis of Variance
  • Animals
  • Brain / drug effects
  • Brain / metabolism
  • Ceftriaxone / therapeutic use*
  • Central Nervous System Depressants / adverse effects*
  • Choice Behavior / drug effects
  • Choice Behavior / physiology
  • Dose-Response Relationship, Drug
  • Epilepsies, Myoclonic / etiology
  • Ethanol / adverse effects*
  • Excitatory Amino Acid Transporter 2 / metabolism*
  • Male
  • Rats
  • Rats, Wistar
  • Substance Withdrawal Syndrome / drug therapy*
  • Substance Withdrawal Syndrome / pathology
  • Substance Withdrawal Syndrome / physiopathology
  • Time Factors
  • Up-Regulation / drug effects*

Substances

  • Central Nervous System Depressants
  • Excitatory Amino Acid Transporter 2
  • Slc1a2 protein, rat
  • Ethanol
  • Ceftriaxone