Interaction of drugs of abuse and maintenance treatments with human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2).
The international journal of neuropsychopharmacology August 1, 2010 Nicolas Tournier, Lucie Chevillard, Bruno Megarbane et al. 122 citations
Several drugs used in addiction treatment and substances of abuse inhibit the efflux transporters P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) in vitro, which could alter their distribution in the body, including across the blood-brain barrier. Norbuprenorphine, buprenorphine, methadone, ibogaine, and THC inhibited P-gp in a concentration-dependent manner, with norbuprenorphine being the strongest. Buprenorphine, norbuprenorphine, ibogaine, and THC inhibited BCRP. Cocaine, amphetamine, nicotine, morphine, and others did not inhibit either transporter. Norbuprenorphine and methadone were transported by P-gp, but no tested compounds were transported by BCRP. The clinical relevance of norbuprenorphine's interaction with P-gp remains unclear.