About Buprenorphine

What is buprenorphine?

Buprenorphine (BUP) is a unique schedule III opioid used for the treatment of acute and chronic pain, opioid withdrawal, and maintenance treatment of opioid addiction. The most common formulations are sublingual (alone or in combination with naloxone: Suboxone), transdermal (10mcg/hr = about 0.5mg/day), and intravenous (Buprenex).

How long has buprenorphine been around?

Since the 1970’s. Initially, buprenorphine was used as an intravenous, perioperative, analgesic. It was used later because of its long-action ability to block the euphoric effects of heroin. Safety profile sublingual buprenorphine was developed for opioid substitution treatment in the 1990s and was approved for use in the US in 2002. Most recently, buprenorphine is increasingly used for the treatment of chronic pain.

Is buprenorphine safe?

Rates of adverse events following home or emergency department initiation of buprenorphine are very low. Because buprenorphine has a “ceiling” effect at usual doses with opioid receptor agonism, it has a very low rate of respiratory depression or overdose. Case reports have occurred, usually when buprenorphine is coadministered with large amounts of alcohol or benzodiazepines. A more common risk is precipitated withdrawal if buprenorphine is given too soon--this is uncomfortable but not life threatening. In published data, reductions in the use of illicit opioid medications were reported, conferring a presumed safety benefit. Additionally, a Cochrane Analysis reported no difference in adverse event rates with buprenorphine compared to non-opioid treatments for managing opioid withdrawal.

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  4. D'Onofrio G, O'Connor PG, Pantalon MV, Chawarski MC et al. Emergency department-initiated buprenorphine/naloxone treatment for opioid dependence: a randomized clinical trial. JAMA. 2015 Apr 28;313(16):1636-44

  5. D'Onofrio G, Chawarski MC, O'Connor PG, Pantalon MV et al. Emergency Department-Initiated Buprenorphine for Opioid Dependence with Continuation in Primary Care: Outcomes During and After Intervention. J Gen Intern Med. 2017 Jun;32(6) 

How long does buprenorphine take to act and when does it peak?

Sublingual buprenorphine takes 15 minutes to act when held under the tongue and peaks in one  hour. A typical 0.3mg IV buprenorphine begins to work immediately after an IV push with peak effect in 5-10 minutes.

What is the difference between buprenorphine and Suboxone®?

Suboxone is the trademark name for buprenorphine + naloxone. The naloxone component is an abuse deterrent that is inert when the tablet is taken sublingually. The naloxone is only active if the tablet is injected.

Are there contraindications for buprenorphine?

If a patient dependent on opioids takes buprenorphine when they have opioid in their system, the buprenorphine will rapidly block the effects of their opioid causing what is termed “precipitated withdrawal.” The severity of this effect varies from mild discomfort to severe distress. This is why there is a washout period for opioid tolerant patients before starting buprenorphine.

Once significant withdrawal has begun the administration of buprenorphine produces relief of withdrawal, anxiolysis, and analgesia. Some patients with significant liver disease (ALT > 5x normal) may not be able to take buprenorphine long-term. Avoid in patients with hypersensitivity to buprenorphine or naloxone.

Is there a need for an Alpha 2 agonist such as Clonidine?

No, nothing else is needed. However, adjunct medications such as clonidine, zofran, and loperamide can be helpful in some cases. We avoid routine use of benzodiazepines.

How long do people use buprenorphine?

It depends.

An ED patient might receive a few doses buprenorphine to treat withdrawal and then go right back to using street opioids. Most patients with opioid use disorder don’t establish long-term abstinence on the first go around. The hope is that, having a positive experience with buprenorphine treat- ment can be a motivation to pursue long-term treatment.

The evidence is clear: the more weeks of stability on buprenorphine that a person with opioid use disorder can string together, the more their mortality risk goes down. We see patients stop and start frequently and that’s common. Each medical encounter is an opportunity to make another attempt at long-term recovery.

Once patients have stabilized on buprenorphine patients should be contin- ued on it indefinitely. When patients stop their maintenance buprenorphine or methadone, all cause mortality more than doubles. The underlying concept is that the neural architecture of the brain is changed by addiction and it takes years to recover. When patients are in recovery they develop whole new patterns of behavior, stress response, and reward seeking that then get “hardwired” into the brain. This process cannot be rushed and has very little to do with patient motivation or insight.

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