Cytisine, a member of the tropane alkaloids family, is a potent agonist of nicotinic acetylcholine receptors (nAChRs). It has been extensively studied for its therapeutic potential in tobacco cessation therapies. Cytisine acts by binding to α4β2 nAChR subtypes, which are highly expressed in the central nervous system and involved in nicotine addiction. Derivatives of cytisine have also been developed to enhance its pharmacological properties, such as improved efficacy and reduced side effects. In addition to its well-documented use in smoking cessation, research is ongoing into other potential therapeutic applications of cytisine derivatives. These include the treatment of neurological disorders like Parkinson’s disease and Alzheimer's disease due to their ability to modulate nAChRs. The chemical modifications of cytisine aim to optimize its pharmacokinetic profile and expand its clinical utility. Cytisine and its derivatives are characterized by their structural complexity, which allows for a wide range of potential applications in pharmaceutical research. Ongoing studies continue to explore the therapeutic potential of these compounds in various medical conditions.