Desmetramadol a safer, more effective analgesic than tramadol

Desmetramadol is able to provide the analgesic benefits of tramadol without the associated metabolic liabilities, according to a recent series of trials.

The study involved two consecutive randomized, double-blind, three-period cross-over, placebo- and active comparator-controlled trials. Researchers randomly assigned 103 healthy participants to receive 50 mg tramadol and 20 mg desmetramadol either with (trial A; n=43; mean age, 28.4±8.0 years; 100 percent male) or without (trial B; n=60; mean age, 28.0±6.8 years; 70 percent male) cotreatment with paroxetine.

In trial A, participants treated with tramadol (mean change, –0.46±0.19; p=0.022) and desmetramadol (mean change, –0.60±0.15; p=0.0005) exhibited significant decreases in average cold-induced pain perception at 30 seconds relative to placebo controls. No significant differences were reported when the two active treatments were compared against each other (p=0.47).

In the male subgroup of trial B, tramadol failed to produce significantly better analgesia relative to placebo (p=0.90), while desmetramadol significantly outperformed both tramadol (p=0.003) and placebo (p=0.036).

Moreover, in the presence of paroxetine, desmetramadol provided 44-percent longer pain tolerance duration relative to placebo than did tramadol.

In trial A, tramadol and desmetramadol showed comparable safety profiles. Cotreatment with paroxetine seemed to result in fewer adverse events.

“Desmetramadol thus obviates the metabolic liabilities of tramadol while preserving its safety profile, because it does not rely on the activity of CYP enzymes for its activity,” said researchers.