New effective analgesics are needed for the treatment of pain. Buprenorphine,
a partial mu-opioid agonist which has been in clinical use for over 25 years,
has been found to be amenable to new formulation technology based on its physiochemical
and pharmacological profile. Buprenorphine is marketed as parenteral, sublingual,
and transdermal formulations. Unlike full mu-opioid agonists, at higher doses,
buprenorphine's physiological and subjective effects, including euphoria, reach
a plateau. This ceiling may limit the abuse potential and may result in a wider
safety margin. Buprenorphine has been used for the treatment of acute and chronic
pain, as a supplement to anesthesia, and for behavioral and psychiatric disorders
including treatment for opioid addiction. Prolonged use of buprenorphine can
result in physical dependence. However, withdrawal symptoms appear to be mild
to moderate in intensity compared with those of full mu agonists. Overdoses
have primarily involved buprenorphine taken in combination with other central
nervous system depressants. Johnson RE, Fudala PJ, Payne R. J Pain Symptom Manage. 2005 Mar;29(3):297-326.
PMID: 15781180 [PubMed - in process]
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=15781180
Credit: All abstracts retrieved from PubMed, developed by the National Center for
Biotechnology Information (NCBI) at the
National Library of Medicine (NLM).
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