Is buprenorphine an opiate / narcotic?

Key Points

• Yes, buprenorphine is an opioid partial agonist and considered a narcotic, but it activates the mu-opioid receptor to a lesser extent than the full opioid agonists (for example: oxycodone, methadone or morphine).
• It is also an antagonist at the kappa-opioid receptor, which means it blocks this receptor which may play a role in opioid dependence.
• Buprenorphine comes in various forms and is used for treatment of opioid dependence as well as moderate to severe pain. Buprenorphine is a Schedule III narcotic under the Controlled Substances Act.

Opiate receptors are found throughout the body and impart functions such as pain relief, sedation, respiratory depression (slowed or halted breathing), and physical dependence.

Buprenorphine is used at higher doses for opioid-use disorder while generally at lower doses to treat moderate to severe pain.

What is a partial agonist?

Buprenorphine still produces the usual opioid effects such as pain relief, euphoria and respiratory depression; however, because it is only a partial agonist, its effects are less than full opioid agonists.

This unique profile may allow for:

• less euphoria ("high") and physical dependence
• a lower potential for misuse
• a ceiling on opioid effects such as respiratory depression
• a more mild withdrawal profile

When used for opioid dependence, buprenorphine helps to relieve symptoms like nausea, insomnia, and irritability normally felt during early opioid withdrawal.

Buprenorphine only partially occupies the opiate receptor. It occupies the receptor but does not produce all the effects. If another opioid, like heroin or oxycodone is also taken, it has trouble attaching to the opiate receptor since it's partially occupied by buprenorphine. Therefore, the patients does not experience an added effect of more opioids.

Buprenorphine tends to block the receptor for a longer time than full opioids do, too. Buprenorphine may remain on the receptor up to 3 days.

Which drugs contain buprenorphine?

Brand names examples of single ingredient buprenorphine products approved to treat opioid dependence include:

• Probuphine (subdermal implant) - brand name discontinued in U.S
• Sublocade (subcutaneous, extended-release injection)

Related: How is Sublocade administered?

Brand names examples of single ingredient buprenorphine products approved to treat pain include:

• Belbuca (buccal film)
• Buprenex (injection) - brand name discontinued in U.S.
• Butrans (transdermal film patch)

Buprenorphine is also found in combination with naloxone for treatment of opioid dependence and addiction. Naloxone is a full opiate antagonist often added to opiates to help prevent misuse of the narcotic. When crushed or dissolved and injected, naloxone can precipitate an unpleasant opioid withdrawal.

• Suboxone (sublingual film)
• Zubsolv (sublingual tablets)

Related questions

• How long does opioid withdrawal last?
• How long does buprenorphine stay in your system?
• What are the different brands of buprenorphine?

How fast does buprenorphine work?

When used as an intravenous injection for pain relief, the effects are quick and start in about 3 minutes with a maximum effect at 60 minutes. Pain relief can last up to 6 hours but varies between patients.

Clinical effects occur at roughly 15 minutes after intramuscular injection and last for 6 hours or longer. Peak effects usually are observed at 1 hour.

When used as a patch for pain relief, each transdermal system (Butrans) provides delivery of buprenorphine for 7 days. Steady state is achieved by the third day.

The Probuphine brand name has been discontinued in the U.S. Probuphine subdermal implants are used for maintenance treatment of opioid dependence in patients who are already clinically stable on low-to-moderate doses of a transmucosal buprenorphine-containing product.

• Maximum plasma concentrations of buprenorphine were reached 12 hours after Probuphine insertion.
• After the peak, plasma buprenorphine concentrations decreased slowly, and steady-state plasma levels were reached by the 4th week after insertion.
• Probuphine provides steady, ongoing blood levels of buprenorphine for six months after a single insertion procedure.

Sublocade is an extended-release injection that only needs to be given once a month. Sublocade starts working quickly with good blood levels reached within a few hours. Studies show it takes about one day (24 hours) for buprenorphine (the active ingredient in Sublocade) to reach maximum levels (peak) after an injection.

Sublingual or buccal preparations used for opioid dependence dissolve at different rates and can take up to 12 minutes. Do not eat, drink, or talk while the film in still dissolving. Relief from withdrawal should start within 30 minutes of the first dose, but several doses may be needed for the full effects. Your doctor may need to adjust your dose based on your response.

Bottom Line

• Buprenorphine is classified as an opioid partial agonist and is considered a narcotic.
• Buprenorphine is used at higher doses for opioid use disorder (opioid dependence) while generally at lower doses to treat moderate to severe pain.
• It is available in a variety of different dosage forms, from sublingual tablets to transdermal patches. Do not switch back and forth between products as this could be deadly.
• Buprenorphine is commonly combined with the opioid antagonist naloxone to help prevent abuse of the opioid (due to crushing, dissolving and injecting) when used in treatment programs for opioid dependence.

This is not all the information you need to know about buprenorphine for safe and effective use and does not replace your healthcare provider's instructions. Review the full product information and discuss this information with your doctor or other health care provider.