Phosphodiesterase inhibitors

Phosphodiesterase inhibitors (PDE inhibitors) are medicines that inhibit enzymes from the group of phosphodiesterases .

Either all enzymes of this group can be inhibited non-selectively or a specific enzyme can be inhibited selectively .

• Non-selective phosphodiesterase inhibitors (PDE inhibitors): methylxanthines such as caffeine , theophylline , theobromine , which non-specifically inhibit various phosphodiesterases. Theophylline is used to treat chronic lung diseases, particularly chronic obstructive pulmonary disease . Another non-specific PDE inhibitors is for the treatment of coronary heart disease used Trapidil .
• Selective phosphodiesterase inhibitors
  • PDE-3 inhibitors in acute heart failure
  • PDE-4 inhibitors for chronic lung diseases and plaque psoriasis / psoriatic arthritis
  • PDE-5 inhibitors for erectile dysfunction and pulmonary hypertension

According to a recent review, PDE inhibitors - especially PDE-2 inhibitors and PDE-9 inhibitors - are promising agents for improving cognition . The aim here is to develop PDE inhibitors that have few side effects.

Individual evidence

1. ↑ J. Semmler, H. Wachtell, S. Endres: The specific type IV phosphodiesterase inhibitor rolipram suppresses tumor necrosis factor-α production by human mononuclear cells. In: International Journal of Immunopharmacology , Vol. 15, No. 3, 1993, pp. 409-413.
2. ↑ J. Tesarik, C. Mendoza, A. Carreras: Effects of phosphodiesterase inhibitors caffeine and pentoxifylline on spontaneous and stimulus-induced acrosome reactions in human sperm. In: Fertility and Sterility , Vol. 58, No. 6, 1992, pp. 1185-1190, PMID 1333994 .
3. ↑ FW Smellie et al .: Alkylxanthines: inhibition of adenosine-elicited accumulation of cyclic AMP in brain slices and of brain phosphodiesterase activity . In: Life Sciences , Vol. 24, No. 26, 1979, pp. 2475-2481.
4. ↑ AG Dulloo, J. Seydoux, L. Girardier: potentiation of the thermogenic antiobesity effects of ephedrine by dietary methylxanthines: adenosine antagonism or phosphodiesterase inhibition? In: Metabolism , Vol. 41, No. 11, 1992, pp. 1233-1241.
5. ↑ Olga AH Reneerkens, Kris Rutten, Harry WM Steinbusch, Arjan Blokland, Jos Prickaerts: Selective phosphodiesterase inhibitors: a promising target for cognition enhancement . In: Psychopharmacology . tape 202 , no. 1-3 , November 20, 2016, pp. 419-443 , doi : 10.1007 / s00213-008-1273-x , PMID 18709359 , PMC 2704616 (free full text).

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