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Opioid Analgesics Opium is the natural extract obtained from the juice of the poppy flower Papaver somniferum and is composed of over 20 different alkaloids Opiate is a term used to describe all drugs derived from opium Because this excludes all synthetic compounds or endogenous analogues the term opioid has evolved to be all encompassing Hence Opioid Analgesics refers to all compounds both natural or synthetic that have similar pharmacological properties to opiates They are the most powerful analgesics known to Man and over the past 100 years no one has succeeded in finding other pain relievers that are as potent At the same time these drugs are classic examples of addictive substances that have and still are exacting a massive toll on society Due to the powerful analgesic effects of these drugs it became important to understand how these drugs brought about their pain relieving effects The main aim behind this work was to try to devise synthetic substances that had the pain alleviating effect of the opioids but none of the deleterious side effects such as addition The first observation that helped throw some light on the mechanism of action was the observation that the opioids are potent at very low doses a small fraction of a milligram This indicated that the opioids probably act very specific cell-surface receptors This evidence was further substantiated by the discovery of specific drugs that reverse the effects of the opioids ie opioid antagonists The first evidence for opioid receptors in the brain came in 1973 from the results of a series of binding study experiments which used 3H-naloxone opioid antagonist to bind to the receptors The potencies of the binding of specific opiates was seen to mimic their opiate-like pharmacological effects The specific locations of the opiate receptors in the CNS were determined using the same radiolabelled naloxone and a sensitive autoradioagraphic techniques that allowed the locations of the bound naloxone
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