Module 2: Basic Pharmacology of Controlled Drugs and Substances

Lesson 2

Buprenorphine and buprenorphine/naloxone (cont’d)

Buprenorphine is metabolised in the liver via the CP450 enzyme system (CYP3A4 and CYP2C8 isozymes). It has a long half-life (20-70 hours) and is relatively safe for patients with kidney disease because it does not accumulate in body tissue. It can be detected in urine and serum; therefore, is useful as a treatment monitoring strategy.

Adverse effects and precautions are similar to other opioids.  Respiratory depression due to the long half-life is the most concerning and a particular risk for substance-naïve individuals who use either form of buprenorphine recreationally.