TheraQuest believes its unique formulation, TQ-1017, slated for phase III clinical trials in 2005, may have significant safety advantages over other formulations currently in development.
Tramadol’s pain relieving effects are due to serotonin and norepinephrine reuptake inhibition, and through a narcotic (opioid) effect similar to oxycodone, the active ingredient in Purdue Pharma’s OxyContin.
Tramadol is an unscheduled narcotic and is therefore readily available like any ordinary prescription drug. Commercially available short-acting tramadol (Johnson & Johnson’s Ultram) releases 50mg of tramadol per tablet into the bloodstream over several hours. New, long-acting formulations in development are designed to gradually release their much larger tramadol content over a 24-hour period.
Dr Najib Babul, president and CEO of TheraQuest, stated: “A formulation with a secure timed-release mechanism is especially needed because if the release mechanism is defeated, the entire 24-hour drug supply can be released into the bloodstream, with resulting potential for toxic effects.”
In a recent JAMA report, tramadol was the third most frequently mentioned abused opioid, coming in ahead of fentanyl, oxycodone or hydromorphone, and thus suggesting a real potential for abuse.
In 2002, there were 1,714 drug-related hospital emergency room episodes for tramadol and a total of 7,890 episodes from 1998 through 2002. Drug Abuse Warning Network (DAWN) medical examiners reported that tramadol was involved in 95 drug-related deaths in 2002 and a total of 382 deaths from 1998 through 2002.