Ralfinamide, an original Na(+) channel blocker developed for the treatment of
chronic pain, inhibits monoamineoxidase-B with no apparent effect on monoamineoxidase-A. To evaluate the pressor response to oral
tyramine under fasting conditions during treatment with
ralfinamide in healthy normotensive subjects. Ten women and 10 men aged 52.9 ± 5.5, sensitive to the oral
tyramine pressor effect in the dose range 200-400 mg, received
ralfinamide 320 mg daily during 7 days of confinement. Starting on day 5, ascending doses of
tyramine 50, 100 and 200 mg were daily administered to subjects, who had responded to 200 mg at screening, and 100, 200 and 400 mg to the 400 mg responders. Vital parameters were monitored. The systolic blood pressure peak (ΔSBP), the time to achieve the peak (Δt) and the area under the pressure curve (over baseline) were calculated. ΔSBP ≥ 30 mmHg were measured for one subject with
tyramine 200 mg and for 11 subjects with 400 mg, whilst ΔSBP was <30 mmHg for eight subjects at all the tested doses. ΔSBP, Δt and AUC after co-treatment with
ralfinamide and
tyramine were not significantly different from those measured after
tyramine alone.
Ralfinamide did not potentiate the pressor response to single oral doses of
tyramine from 50 to 400 mg. These preliminary results give an evidence for the specificity of
ralfinamide for
MAO-B in comparison with
MAO-A, analogously to the observations previously done for
safinamide. Dietary
tyramine restrictions may not be necessary in
neuropathic pain patients receiving
ralfinamide as a
therapy.