TITLE:
Differences in the Receptor Binding Profile of Lofexidine Compared to Clonidine
AUTHORS:
Robert B. Raffa, Joseph V. Pergolizzi, Robert Taylor, Robert P. James, Mark Pirner
KEYWORDS:
Lofexidine, Clonidine, Opioid Withdrawal, Receptor Affinity, Alpha-2 Agonist
JOURNAL NAME:
Pharmacology & Pharmacy,
Vol.10 No.1,
January
3,
2019
ABSTRACT: Lucemyra? (lofexidine hydrochloride) has recently
been approved by the US FDA for the mitigation of withdrawal symptoms to
facilitate abrupt discontinuation of opioids in adults. Lofexidine is an
alpha-2 adrenoceptor agonist. However, the clinical attributes of lofexidine
differ in advantageous ways from the classical alpha-2 adrenoceptor agonist
clonidine. In the present study, we measured the receptor binding profile of
lofexidine and clonidine in an effort to gain an insight into the clinical
difference(s).