Analgesic effect of L-threo-3,4-dihydroxyphenylserine (L-DOPS) in patients with chronic pain

Previous pharmacological studies using animals indicated that a systemic administration of L-threo-3,4-dihydroxy-phenylserine (L-DOPS), a precursor of noradrenaline, induces an antinociceptive effect and an increase in the CNS level of noradrenaline which serves an inhibitory role at the spinal dorsal horn and the supraspinal pain afferent system. The aim of the present study was to investigate the analgesic effect of L-DOPS in patients with chronic pain. We selected 18 patients with various kinds of pain. In nine patients, L-DOPS (tablets) was orally administered and pain was assessed by the visual analogue scale (VAS) before and after the L-DOPS administration. Administration of L-DOPS resulted in dose-dependent analgesia. The maximum analgesia (VAS change: from 10 to 4.1 +/- 0.9) was observed 60 min after an administration of 100 mg and it lasted for 2-5 h depending on the patient. In the other nine patients, oral administration of placebo tablets produced only a slight analgesia (VAS change: from 10 to (9.2 +/- 0.3). The difference between the L-DOPS-induced effect and the placebo-induced one was statistically significant. After repeated administration of L-DOPS for 4-5 weeks, neither tolerance nor side effects were observed.