Buprenorphine

Medically Reviewed by Dr. Harshi Dhingra, M.D.

Last Reviewed: Oct 30, 2023

Uses


Buprenorphine Uses

Buprenorphine is used in opioid treatment programs as part of medication-assisted treatment. It is used to treat opioid dependency, i.e., dependency on narcotic pain relievers such as oxycodone, hydrocodone, and other prescription medications used to treat severe pain. In addition to the treatment of prescription opioid analgesic addiction, buprenorphine is also used to treat addiction to the illegal drug heroin, which is also an opioid drug.

There may be other uses of buprenorphine’s opioid effects. Your doctor or pharmacist can give you a more detailed buprenorphine pharmacology review.

Buprenorphine Mechanism of Action

Buprenorphine is a potent opioid agonist. It is used as opioid substitution therapy for the treatment of opioid addiction. This drug is an opioid partial agonist that binds to mu-opioid receptors in the central nervous system. It thereby prevents opioid drugs, which are full opioid agonists, from binding to these receptors. In other words, buprenorphine lowers mu-opioid receptor availability. Buprenorphine, therefore, reduces the high or euphoria opioid-dependent patients experience after taking opioid drugs. The effects of buprenorphine also include easing cravings and lowering the risk of opioid withdrawal symptoms. 

Buprenorphine Doses

Buprenorphine comes in the form of 2 mg and 8 mg sublingual tablets. 

Combination buprenorphine-naloxone sublingual tablets (brand name Zubsolv) are available in the following dosages:

  • 0.7 mg/0.18 mg 
  • 1.4 mg/0.36 mg
  • 2.9 mg/0.71 mg 
  • 5.7 mg/1.4 mg 
  • 8.6 mg/2.1 mg 
  • 11.4 mg/2.9 mg

Combination buprenorphine-naloxone buccal films (brand name Bunavail) are available in the following dosages:

  • 2.1mg/0.3mg 
  • 4.2mg/0.7mg
  • 6.3mg/1mg

Doctors usually prescribe buprenorphine sublingual tablets as a single daily dose when starting opioid treatment programs. The sublingual tablets that do not contain naloxone are typically used at the start of substance abuse treatment with buprenorphine. Later, a combination of buprenorphine and naloxone (which belongs to a group of drugs called opioid antagonists) is preferred. The presence of naloxone allows buprenorphine patients to take the medicine unsupervised at home (rather than in an outpatient setting such as a buprenorphine or methadone clinic). The unsupervised administration of buprenorphine sublingual tablets (without naloxone) is restricted to patients who cannot tolerate the combination of buprenorphine and naloxone sublingual tablets, for example, people who have had allergic reactions to naloxone.

Your doctor will prescribe enough buprenorphine to last until your next follow-up visit. Multiple refills are generally not given without appropriate follow-up visits.

Buprenorphine extended-release injection (BUP-ER, Sublocade) can be used to manage moderate to severe opioid use disorder in people who are clinically stable on 8 mg to 24 mg per day of the transmucosal buprenorphine products (sublingual tablets or buccal films) along with behavioral therapy. The intravenous injection removes the need to take medicine on a daily basis.