Background: Analgesics are the drugs which bring insensibility to pain without loosing
consciousness. Treatment strategy is generally based on the type of pain. Most of the analgesics are associated
with serious side effects, such as NSAIDS can cause severe GI disturbance and opioids can
cause addiction. There are various ways to reduce their side effects The analgesic prodrug approach is
one of the several strategies used to attain the required pharmacological response with a considerable
decrease in side effects. The aim of this paper is to introduce in depth the rational behind the use of the
analgesic prodrug approach from past to present.
Methods: Data is collected from online as well as from extensive literature survey which have appeared
on this subject during the last decades. This review will map the origins and development of the
most important of the analgesic prodrugs to date.
Results: This review indicates that, designing analgesic prodrugs represent successful strategy to gain
the required pharmacological activity with a considerable decrease in side effects. However thorough
knowledge of diverse biological phenomena is needed which enables scientists to invent and design
superior, nontoxic and better-targeted prodrugs.
Conclusion: The newly synthesized chemical entity or prodrugs may or may not have intrinsic pharmacological
activity and also synthesizing novel molecules consume a lot of time and money than developing
prodrugs of existing clinically used analgesic drugs which is surely an attractive and promising
area of research now a days.