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Nicotinic Agonists

Nicotinic Agonists


CHAMPIX®, Chantix, Varenicline


varenicline, varenicline tartrate

Varenicline is a prescription medication used to treat smoking addiction. This medication is the first approved nicotinic receptor partial agonist. Specifically, varenicline is a partial agonist of the alpha4/beta2 subtype of the nicotinic acetylcholine receptor. In addition it acts on alpha3/beta4 and weakly on alpha3beta2 and alpha6-containing receptors. A full agonism was displayed on alpha7-receptors. On March 9, 2015, the U.S. Food and Drug Administration warned that Varenicline, in the form of Pfizer Inc's quit-smoking drug, Chantix, has been associated with seizures and that some patients who drink while taking the drug may become aggressive or black out. Pfizer is conducting an additional safety study of the drug, results of which are expected in late 2015. The FDA said it is keeping the black box in place at least until the results of the trial are announced.

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The T-value in the score for hazard refers to chronic toxicity. Underlying data for  T comes from scientific discussion for Champix (vareniklin), see below. Underlying data for P, B and risk comes from Fass environmental information for Champix, see below.

Below is Hazard and Risk according to data from the scientific discussion for Champix (vareniklin) 11/10/2006

Persistence: No data. "Varenicline did not meet the criteria for PBT/PvBv substances."

Bioaccumulation: No data. "Varenicline did not meet the criteria for PBT/PvBv substances."

Chronic toxicity: There is NOEC for 1 trophic level, crustacean (Ceriodaphnia dubia) 0.003 mg/L.

The risk, PEC/PNEC, from the scientific discussion from a European perspective:

PEC = 0.01 microg/L.

PEC/PNEC = 0.03

Below is Hazard and Risk from Fass environmental information for Champix (downloaded 2011-05-27)

Persistence: The substance breaks down slowly in the environment.

Bioaccumulation: The substance has the potential to be accumulated in aquatic organisms.

Toxicity: There are data for 3 trophic levels, most sensitive crustacean (Ceriodaphnia Dubia) "7-day NOEC of 2.7 ug/L"

PEC/PNEC is based on sales data in Sweden, which year is not stated. PEC/PNEC = 0.007 which gives the risk insignificant.


  1. European Medicines Agency. European public assessment reports (EPAR).
  2. Fass.se för vårdpersonal