Metapramine Explained

Metapramine (brand names Prodastene, Timaxel) is a tricyclic antidepressant (TCA) developed by Rhone Poulenc^[1] that was introduced for the treatment of depression in France in 1984.^{[2] [3]} In addition to its efficacy against affective disorders, it also has analgesic properties,^{[4] [5]} and may be useful in the treatment of pain.

Metapramine has desipramine-like effects, acting as a norepinephrine reuptake inhibitor without affecting the reuptake of serotonin or dopamine.^{[6] [7] [8]} It has also been shown to act as a low-affinity NMDA receptor antagonist.^[9] Metapramine's direct effects on serotonin, histamine, and muscarinic acetylcholine receptors have not been assayed, but uniquely among most TCAs, it has anecdotally been reported to lack anticholinergic effects.^{[8] [10]}

Notes and References

1. US . 3622565 . Dibenzazepine derivatives and their preparation . Fouche JC, Alexandre CG . Rhone Poulenc SA . 23 November 1971 .
2. Book: Dictionary of organic compounds . Chapman & Hall . London . 1996 . 13 . 0-412-54090-8 .
3. Book: Vela JM, Buschmann H, Holenz J, Párraga A, Torrens A . Compounds launched in single countries . Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application . Wiley-VCH . Weinheim . 2007 . 248 . 978-3-527-31058-6 . https://books.google.com/books?id=yXD4QA-Y_Z0C&q=metapramine&pg=PA248.
4. Michael-Titus A, Costentin J . Analgesic effects of metapramine and evidence against the involvement of endogenous enkephalins in the analgesia induced by tricyclic antidepressants . Pain . 31 . 3 . 391–400 . December 1987 . 2827090 . 10.1016/0304-3959(87)90167-9 . 39569622 .
5. Fialip J, Marty H, Aumaitre O, Bougerolle AM, Dordain G, Berger JA, Eschalier A . Antinociceptive activity of metapramine in mice. Relationship with its pharmacokinetic properties . Life Sciences . 50 . 3 . 161–168 . 1992 . 1731171 . 10.1016/0024-3205(92)90268-T .
6. Dagonneau H, Fonlupt P, Pacheco H . [Effects, in rats, of metapramine and carpipramine on the uptake of catecholamines and serotonin; relationship with 3H-imipramine binding] . fr . Comptes Rendus des Séances de la Société de Biologie et de Ses Filiales . 180 . 1 . 43–48 . 1986 . 3017518 .
7. Warter JM, Tranchant C, Marescaux C, Depaulis A, Lannes B, Vergnes M . Immediate effects of 14 non MAOI antidepressants in rats with spontaneous petit mal-like seizures . Progress in Neuro-Psychopharmacology & Biological Psychiatry . 14 . 2 . 261–270 . 1990 . 2106711 . 10.1016/0278-5846(90)90106-q . 8332732 .
8. Bonierbale M, Dufour H, Scotto JC, Sutter JM . [Metapramine: antidepressant and psycho-stimulant] . fr . L'Encephale . 2 . 3 . 219–223 . 1976 . 1033059 .
9. Boireau A, Bordier F, Durand G, Doble A . The antidepressant metapramine is a low-affinity antagonist at N-methyl-D-aspartic acid receptors . Neuropharmacology . 35 . 12 . 1703–1707 . 1996 . 9076749 . 10.1016/S0028-3908(96)00122-0 . 7244740 .
10. Dufour P, Billa JP, Fabre J, Roquebert J . [Evaluation of the central anticholinergic activity of antidepressants. Comparison of two experimental methods] . fr . Annales Pharmaceutiques Françaises . 47 . 3 . 135–141 . 1989 . 2634929 .