Buprenorphine is a partial agonist at mu-opioid receptors. When administered to a patient physically dependent on full agonist opioids such as heroin, it can precipitate acute withdrawal. This occurs because buprenorphine:

• A Has high receptor affinity but low intrinsic activity, displacing the full agonist ✓
• B Has low receptor affinity but high intrinsic activity
• C Acts as an inverse agonist at mu-opioid receptors
• D Inhibits CYP3A4, increasing full agonist plasma levels

Explanation

Buprenorphine has high affinity for mu receptors but low intrinsic activity. It displaces full agonists like heroin from receptors but activates them less, netting a reduced opioid effect and precipitating withdrawal in dependent patients. Low affinity would not displace full agonists effectively. Inverse agonists produce opposite effects, and CYP3B4 inhibition would increase, not decrease, opioid effects.

Reference: Goodman and Gilman's The Pharmacological Basis of Therapeutics, 14th ed.

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Written and medically reviewed by the StethoPrep medical team.