Cytisine - From the Past to the Future.

Abstract

INTRODUCTION:

Neuronal nicotinic acetylcholine receptors are ligand-gated ion channel receptors, distributed throughout central nervous system, as well as in peripheral ganglia and some non-neuronal cells. Cytisine, a qulinolizidine alkaloid, could be considered a high affinity ligand of those receptors. It is a partial agonist of β2*-containing receptors and a full agonist of α7 and β4*-containing receptors.

Current indication:

At present, pharmacodynamic properties of cytisine are leveraged only in a few European countries where it is available as medicinal product (Desmoxan and Tabex) indicated in the pharmacotherapy of nicotine addiction. Cytisine mimics the influence of nicotine on α4β2* receptors, but with higher affinity and lower activity. It lowers rewarding and reinforcing effects of nicotine in smoking persons and reduces withdrawal symptoms and craving in quitting ones.

Potential indications:

The results of non-clinical studies suggest that cytisine could affect ethanol consumption, has an antidepressant and neuroprotective effect and could be useful in reducing body mass and preventing weight gain. Although there is a lack of research on cytisine in the treatment of areca nuts usage, the preliminary data suggest its usefulness. The combination of cytisine and Trolox C was selected as a possible effective treatment for type 2 diabetes. Though these drugs alone are not effective, their theoretical usefulness was confirmed in animal models.

SUMMARY:

Treatment with cytisine is an effective, cost-efficient, affordable and well tolerated nicotine addiction therapy. Potential new indications for cytisine include the treatment of alcoholism, areca nuts usage, Parkinson's disease, an autonomic-system failure. Further studies are necessary.

• Authors: Aleksandra Paduszyńska, Maciej Banach, Jacek Rysz, Marek Dąbrowa, Paulina Gąsiorek, Agata Bielecka-Dąbrowa
• Journal: Current pharmaceutical design (Curr Pharm Des) Vol. 24 Issue 37 Pg. 4413-4423 ( 2018) ISSN: 1873-4286 [Electronic] United Arab Emirates
• PMID: 30885113 (Publication Type: Journal Article)
• Copyright: Copyright© Bentham Science Publishers; For any queries, please email at [email protected].

Chemical References

• Alkaloids
• Antidepressive Agents
• Azocines
• Neuroprotective Agents
• Nicotinic Agonists
• Quinolizines
• Receptors, Nicotinic
• cytisine

Topics

• Alkaloids (pharmacology)
• Animals
• Antidepressive Agents (pharmacology)
• Azocines (pharmacology)
• Diabetes Mellitus, Type 2 (drug therapy)
• Humans
• Neuroprotective Agents (pharmacology)
• Nicotinic Agonists (pharmacology)
• Quinolizines (pharmacology)
• Receptors, Nicotinic (metabolism)