Reboxetine; hemodynamic effects in healthy males

Hemodynamic effects of reboxetine
in healthy male volunteers.

Denolle T, Pellizzoni C, Jannuzzo MG, Poggesi I

Biotrial Research Centre,
Rennes, France.
Clin Pharmacol Ther 1999 Sep; 66(3):282-7

ABSTRACT

BACKGROUND: Reboxetine [(R,S)-2[(R,S)-alpha-(2-ethoxyphenoxy)benzyl]morpholine methanesulfonate] is a racemic compound that consists of equal proportions of R,R- and S,S-enantiomers. This study investigated the hemodynamic effects of reboxetine and the R,R-enantiomer compared with placebo in volunteers. The pharmacokinetics of reboxetine and its enantiomers were also investigated in the study.

METHODS: Nine healthy, male volunteers received single doses of 4 mg reboxetine, 2 mg R,R-enantiomer, and placebo at weekly intervals. Reboxetine and the R,R-enantiomer were well tolerated in all volunteers.

RESULTS: The heart rates of patients in the supine and standing positions were increased after reboxetine administration compared with the R,R-enantiomer (P < .05, except supine heart rate at 6 hours) and placebo (P < .05). Supine systolic and diastolic blood pressure was also increased by 3 4 and 1 4 mm Hg, respectively, after reboxetine compared with R,R-enantiomer (-2 4 and -4 3 mm Hg) and placebo (-4 4 and -4 4 mm Hg) administration. The systolic and diastolic blood pressure measurements for subjects while standing did not differ significantly among treatments. There was no significant difference between the maximum plasma concentration, mean time to maximum plasma concentration, plasma half-life, or area under the plasma concentration-time curve (AUC) of the R,R-enantiomer after reboxetine or R,R-enantiomer administration. The ratio of the mean AUC values for the R,R- and S,S-enantiomers was 2.1.

CONCLUSION: These findings suggest that the S,S-enantiomer is responsible for the hemodynamic effects of reboxetine in humans. Increases in supine blood pressure after reboxetine administration may be interpreted as regression to the mean value and not caused by any treatment effect.

Tianeptine | Moclobemide | Deprenyl | Picamilon
Home | Order

Reboxetine  research / abstracts

  1. Reboxetine role in antidepressant therapy
2. Reboxetine efficacy and tolerability
  3. Reboxetine clinical pharmacologic profile
4. Reboxetine Inhibiting noradrenaline and serotonin reuptake
5. Reboxetine and depression in the elderly
6. Reboxetine with severe major depressive disorder
7. Reboxetine clinical efficacy in major depression
8. Reboxetine tolerability and safety for major depression
9. Reboxetine comparison with fluoxetine
10. Reboxetine versus fluoxetine, impact on social functioning
11. Reboxetine  versus fluoxetine, differential effects
12. Reboxetine prevents relapse in major depression
13. Reboxetine efficacy compared with imipramine
14. Noradrenaline reuptake inhibition
15. Antidepressants noradrenergic versus serotonergic
16. Reboxetine in the treatment of bulimia
17. Reboxetine hemodynamic effects in healthy males
18. Reboxetine effects of antidepressant therapy
19. Reboxetine place in antidepressant therapy
20. Reboxetine stimulant effects in patients with narcolepsy
21. Reboxetine selective noradrenaline reuptake inhibitor (NARI)
    Reboxetine manufacturer's product insert

HOME to order

Hit Counter