Bupropion

Detailed information

Assessment report

Assessment report for Mysimba (naltrexon/bupropion) 18 december 2014, EMA/805547/2015.

Hazard

Persistence: "OECD 301: 1.21 % in 14 days. Not ready biodegradable. OECD 301B: 0.2–1.0 % CO2. Not ready biodegradable. OECD 302: 90 % in 14 days. Inherent biodegradable. [---] CHMP recommends the following points for further investigation: The Applicant is requested to perform all the planned studies for the environmental risk assessment for bupropion (e.g. OECD 106, 210 and 211) and naltrexone (OECD 106, 201, 209, 210, 211 and 301) as well as OECD 308 for both compounds, should the results from the respective OECD 301 studies deem this necessary." According to contact person at the Swedish Medical Products Agency, no new data has been received (email 2018-09-04).

Bioaccumulation: log K_ow pH 5: -0.207, pH 7: 1.83, pH 9: 3.18. Conclusion: not B.

Toxicity: There are data for 2 trophic levels, most sensitive algae (Pseudokirchneriella sucapitata) NOEC = 11.1 microg/L.

Risk

The risk, PEC/PNEC, calculated from data in the assessment report from a European perspective:

PEC = 0.068 microg/L

PNEC = Lowest NOEC, 11.1 microg/L/50 (assessment factor (AF) for two chronic studies) = 0.222 mikrog/L.

PEC/PNEC = 0.306 gives the risk low.

Fass environmental information

Fass environmental information for Voxra (bupropion) from GlaxoSmithKline (downloaded 2023-03-15).

Hazard

Persistence: "Bupropion is not readily degradable but it does undergo inherent primary biodegradation. This substance is predicted to degrade via hydrolysis and the half-life is less than 40 days. However, the relevant degradation products have not been identified or characterised. The phrase “Bupropion is potentially persistent” is thus chosen."

Bioaccumulation: Log D_ow = 1.54 vid pH 7.4.

Toxicity: There are data for 3 trophic levels, most sensitive NOEC for fish 100 microg/L.

Risk

PEC/PNEC is based on sales data in Sweden in year 2021. PEC/PNEC = 0.38/10 = 0.038 which gives the risk insignificant. If one instead use the PNEC value according to the assessment report above and uses the PEC value from Fass, the risk becomes moderate (PEC/PNEC = 0.38/0.222 = 1.712).

Report from Goodpoint from a Swedish perspective

Concentrations of bupropion in the environment have been well below the lowest effect concentrations. Bupropion has been found in wild fish, though quite far below therapeutic concentrations. Mechanism based efficacy data is lackning.

Pharmaceuticals residues in the aquatic environment in Region Stockholm

Bupropion has been found in treated wastewater and surface water within Region Stockholm during measurements in 2021.