Background: Sublingual buprenorphine is used as a substitution drug in hero
in addicts. Although buprenorphine inhibits mitochondrial function at high
concentrations in experimental animals, these effects should not occur afte
r therapeutic sublingual doses, which give very low plasma concentrations.
Case reports: We report four cases of former heroin addicts infected with h
epatitis C virus and placed on substitution therapy with buprenorphine. The
se patients exhibited a marked increase in serum alanine amino transferase
(30-, 37-, 13- and 50-times the upper limit of normal, respectively) after
injecting buprenorphine intravenously and three of them also became jaundic
ed. Interruption of buprenorphine injections was associated with prompt rec
overy, even though two of these patients continued buprenorphine by the sub
lingual route. A fifth patient carrying the hepatitis C and human immunodef
iciency viruses, developed jaundice and asterixis with panlobular liver nec
rosis and microvesicular steatosis after using sublingual buprenorphine and
small doses of paracetamol and aspirin,
Conclusions: Although buprenorphine hepatitis is most uncommon even after i
ntravenous misuse, addicts placed on buprenorphine substitution should be r
epeatedly warned not to use it intravenously, Higher drug concentrations co
uld trigger hepatitis in a few intravenous users, possibly those whose mito
chondrial function is already impaired by viral infections and other factor
s. (C) 2001 European Association for the Study of the Liver. Published by E
lsevier Science B.V. All rights reserved.