A generic version was approved in the U.S. in 2018. In 2017, it was the 288th most commonly prescribed medication in the U.S., with more than one million prescriptions. Medical uses
Buprenorphine/­naloxone is used for the treatment of opioid use disorder. Long-term outcomes are generally better with use of buprenorphine/­naloxone than attempts at stopping opioid use altogether. This includes a lower risk of overdose with medication use. Due to the high binding affinity and low activation at the opioid receptor, cravings and withdrawal for opioids are decreased while preventing a person from getting high and relapsing on another opioid. The combination of the two medications is preferred over buprenorphine alone for maintenance treatment due to the presence of naloxone in the formulation, which helps discourage intravenous use.Buprenorphine/­naloxone has been found to be effective for treating opioid dependence, and serves as a recommended first-line medication according to the U.S. National Institute on Drug Abuse. The medication is an effective maintenance therapy for opioid dependence and has generally similar efficacy to methadone. Both treatments — buprenorphine/­naloxone and methadone — are substantially more effective than abstinence-based treatment. Prescribers need a Drug Addiction Treatment Act (DATA 2000) waiver to prescribe buprenorphine/­nalaxone for opioid dependence.Because it may be prescribed out of an office setting (as opposed to methadone, which requires specialized centers), buprenorphine/naloxone allows people more freedom of administration. It also thus comes with more risks in this vulnerable population.
The glucuronidation of buprenorphine is primarily carried out by the UDP-glucuronosyltransferases (UGTs) UGT1A1 and UGT2B7, while norbuprenorphine is glucuronidated by UGT1A1 and UGT1A3. These glucuronides are then eliminated mainly through excretion into bile. The elimination half-life of buprenorphine is 20 to 73 hours (mean 37 hours). Due to the mainly hepatic elimination, there is no risk of accumulation in people with kidney problems. Naloxone
Naloxone is extensively inactivated by first-pass metabolism in the liver, meaning that use of buprenorphine/­naloxone as prescribed should not lead to active naloxone in the blood (which, as an opioid antagonist, would reverse the effect of buprenorphine or other opioids). Society and culture
Cost
While the cost of the medication buprenorphine/­naloxone is greater than buprenorphine alone, one analysis predicted the overall costs would be less in the United States due to a lower risk of misuse. Access in the United States
Before the Drug Addiction Treatment Act of 2000 (DATA), physicians were not allowed to prescribe narcotics to treat opioid dependence. People with narcotic dependence had to go to registered clinics to receive treatment. With DATA, Suboxone was the first medication approved for office-based treatment for opioid dependence. Suboxone has thus become widely used as a replacement for methadone as it can be prescribed by doctors in their offices, while methadone can only be provided at specialized addiction centers, of which there are a limited number, often making access difficult. Integrating Medication-Assisted Treatment into outpatient primary care practices improves patient access to Suboxone.