How is Cytisine Related to Smoking?

November 12, 2012

How is Cytisine Related to Smoking?

If you want to quit smoking, you might want to look into a little something called cytisine.

Smoking and Quitting

Everybody knows that smoking is one of the most common causes of disabilities and deaths the world over. It also happens to be a preventable one, though. Unfortunately, despite this fact, most smokers who want to quit never succeed in doing so.

Nicotine replacement therapy would be one way to quit smoking, but it only ever works in 15% of the cases. Cytisine, on the other hand, is a partial agonist that chooses to use nicotinic acetylcholine receptors, which plays a huge part in nicotine addiction by modulating the release of dopamine in the reward pathway.

What is Cytisine?

Overall, cytisine is comparable to varenicline, as well, in that they both modulate the discriminative stimulus effects of nicotine. They have both also been used for decades as a method to quit smoking in Europe.

Still, since it hasn’t been properly evaluated in terms of efficacy and safety yet, it cannot be approved for today’s standards. However, one of the more recent uncontrolled and open trials of it have suggested success rates comparable to nicotine replacement therapy, but at a much more affordable cost. Another study has also shown that it is more effective in the long run due to the fact that its pharmacology and chemistry have already been reviewed in an extensive manner.

How Should It be Taken?

In general, when taken by its recommended dosage, people might experience appetite changes, taste changes, mouth dryness, headaches, nausea, irritability, constipation, light arterial pressure changes, and tachycardia. Plus, people might have a hard time following its regimen to begin with. So, if you would like to alleviate some of its side effects, you might have to look into modern pharmaceutical technology for help. However, this approach hasn’t been addressed for it so far.

Most of the time, this form of therapy seems to be especially attractive for structural changes. Substituting the basic atom of nitrogen seems to lower its functional potency and affinity, in general, due to the unacceptably low values associated therewith. Conversely, introducing carbon atom 3 substituents is fairly straightforward, so they end up being incredibly effective. Numerous derivatives have also been synthesized, but they haven’t shown higher affinities compared to the former and the majority of them have better selectivities, while others surpass varenicline altogether.

Still, an absence of agonist activity seems evident and they seem to have low potency in terms of being nicotinic antagonists. Another disadvantage would be the mere fact that it takes ages for them to synthesize, which mainly suggests that any drug that appears from here would be more pricey compared to regular cytosine in the end.


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