21 February 2020

Varenicline is no more dangerous than nicotine

A new study has confirmed the safety of varenicline

Polina Gershberg, Naked Science

A study published in the journal Addiction shows that varenicline does not generate more side effects than nicotine replacement therapy (in which the patient, in order to give up the habit of smoking, receives nicotine without other accompanying harmful components). Partially excessive, the authors recognized the restrictions towards another drug, bupropion, but on the contrary, they confirmed another portion of claims against it.

Varenicline is a partial agonist of α4β2 nicotinic acetylcholine receptors (h-ACHR), today one of the most effective means of quitting smoking. By activating these receptors with less internal force, it simultaneously blocks nicotine access to them. Bupropion is an atypical antidepressant, a selective inhibitor of norepinephrine and dopamine reuptake, also effective in quitting smoking.

Earlier studies expressed concern about a possible increase in the frequency of side effects when quitting smoking with varenicline. Due to data on a possible increase in the risk of psychiatric problems, in particular, suicidal intentions, the FDA (US Food and Drug Administration) has introduced a strict warning level for this drug.

In the new study, 618,497 adult participants who had no history of depression before trying to quit smoking were examined. Data analysis showed that taking varenicline is not associated with an increased risk of cardiovascular diseases or a higher frequency of neuropsychiatric hospitalizations compared to NRT. On the contrary, the risks were lower: for cardiovascular hospitalizations - by 20% during the year, for psychiatric profile – by 35%. According to earlier studies, it is more effective for quitting smoking than bupropion and NRT.

At the same time, the new work shows that the use of bupropion (which also received earlier warnings) is associated with a lower risk of cardiovascular hospitalization compared with NRT (by 25%, which is even lower than that of varenicline), but also with a higher risk of neuropsychiatric hospitalization (by 21% compared with NRT).

Lead author of the paper, Dr. Greg Carney, says: "While we support the FDA's efforts to monitor the safety of approved products, warnings about varenicline and bupropion are becoming increasingly inconsistent with data from subsequent clinical trials and observational studies. We hope that the results of our work will contribute to a better understanding of these smoking cessation medications."

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