Buprenorphine / Naloxone

What it is and how it works

Mechanism of Action Buprenorphine and naloxone sublingual tablets contain buprenorphine and naloxone. Buprenorphine is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor. Naloxone is an opioid antagonist and produces opioid withdrawal signs and symptoms in individuals physically dependent on full opioid agonists when administered parenterally.

Indications

Buprenorphine and naloxone sublingual tablets are indicated for the maintenance treatment of opioid dependence. Buprenorphine and naloxone sublingual tablets should be used as part of a complete treatment plan that includes counseling and psychosocial support. Buprenorphine and naloxone sublingual tablets contain buprenorphine, a partial opioid agonist, and naloxone, an opioid antagonist, and are indicated for the maintenance treatment of opioid dependence. Buprenorphine and naloxone sublingual tablets should be used as part of a complete treatment plan that includes counseling and psychosocial support.

Dosage and administration (summary)

Administer buprenorphine and naloxone sublingual tablets sublingually as a single daily dose. Strongly consider recommending or prescribing an opioid overdose reversal agent (e.g., naloxone, nalmefene) at the time buprenorphine and naloxone sublingual tablets are initiated or renewed because patients being treated for opioid use disorder have the potential for relapse, putting them at risk for opioid overdose. To avoid precipitating withdrawal, induction with buprenorphine sublingual tablets should be undertaken when objective and clear signs of withdrawal are evident.

Contraindications

Buprenorphine and naloxone sublingual tablets are contraindicated in patients with a history of hypersensitivity to buprenorphine or naloxone as serious adverse reactions, including anaphylactic shock, have been reported . Hypersensitivity to buprenorphine or naloxone.

Warnings and precautions

Addiction, Abuse, and Misuse : Buprenorphine can be abused in a similar manner to other opioids. Clinical monitoring appropriate to the patient’s level of stability is essential. Monitor patients for conditions indicative of diversion or progression of opioid dependence and addictive behaviors. Multiple refills should not be prescribed early in treatment or without appropriate patient follow-up visits. Respiratory Depression : Life-threatening respiratory depression and death have occurred in association with buprenorphine use.

Pregnancy

Pregnancy Risk Summary The data on use of buprenorphine, one of the active ingredients in buprenorphine and naloxone sublingual tablets, in pregnancy, are limited; however, these data do not indicate an increased risk of major malformations specifically due to buprenorphine exposure.

Storage and supply

Buprenorphine and naloxone sublingual tablets, USP are available as follows: 2 mg/0.5 mg – White to off-white, round tablet debossed with on one side and 154 on the other side supplied in bottles of 30 tablets (NDC 0228-3154-03) with a child-resistant closure.

Source: Buprenorphine And Naloxone (Buprenorphine And Naloxone) — US FDA prescribing information, 2026-02-06, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.