Pharmacologic management of opioid withdrawal symptoms can reduce the intensity of drug craving and improve treatment retention in patients with opioid use disorder who will receive maintenance treatment. Withdrawal management without subsequent maintenance treatment is associated with high rates of relapse, overdose death, and HIV and/or hepatitis C virus infection. Several guidelines on management of opioid withdrawal are available. Maintenance treatment of opioid use disorder was reviewed in a previous issue.

View Expanded Table: Some Drugs for Management of Opioid Withdrawal Symptoms

The FDA has approved lofexidine (Lucemyra – US WorldMeds/Salix), a centrally acting alpha₂ receptor agonist, to manage withdrawal symptoms in adults abruptly stopping opioid use. Available in the UK since 1992, lofexidine is the first nonopioid to be approved in the US for management of opioid withdrawal symptoms. Clonidine (Catapres, and generics), another central alpha₂ receptor agonist, has been used off-label for this indication for many years.

Opioid use disorder is a chronic, relapsing disease with both physical and psychiatric components. It is associated with economic hardship, social isolation, incarceration, increased rates of blood-borne infections such as HIV and viral hepatitis, adverse pregnancy outcomes, and increased mortality. According to the CDC, there were 33,091 deaths related to opioid overdose in the US in 2015, more than in any previous year. Several guidelines on the management of opioid use disorder have recently been published.

The FDA has approved a buccal film formulation of the partial opioid agonist buprenorphine combined with the opioid antagonist naloxone (Bunavail – BioDelivery Sciences) for maintenance treatment of opioid dependence. Sublingual tablet and film formulations of the same combination were approved earlier. The manufacturer of Bunavail claims that the new product is superior to sublingual formulations because of the convenience of buccal administration and better absorption into the blood, permitting use of lower doses.

A new sublingual tablet formulation of the partial opioid agonist buprenorphine combined with the opioid antagonist naloxone (Zubsolv – Orexo) has been approved by the FDA for maintenance treatment of opioid dependence. Zubsolv tablets have relatively greater bioavailability than previously approved sublingual film (Suboxone) and sublingual tablet formulations of buprenorphine/naloxone and, according to an open-label survey, they taste better. The new tablets are smaller and dissolve faster than other tablet formulations, and they are individually sealed in child-resistant packaging.1

Buprenorphine is a Schedule III controlled substance that can be prescribed in an office setting by qualified physicians who register with the Substance Abuse and Mental Health Services Administration.2

Zubsolv is available as triangular tablets containing 1.4 mg of buprenorphine and 0.36 mg of naloxone and round tablets containing 5.7 mg of buprenorphine and 1.4 mg of naloxone, which achieve plasma concentrations of buprenorphine equivalent to those with the 2/0.5-mg and 8/2-mg strengths of other buprenorphine/naloxone tablets. A package of Zubsolv 5.7/1.4-mg tablets costs the same ($211) as a box of Suboxone 8/2-mg films. A bottle of generic buprenorphine/naloxone 8/2-mg tablets costs $250.3

1. A Fischer et al. Pharmaceutical and pharmacokinetic characterization of a novel sublingual buprenorphine/naloxone tablet formulation in healthy volunteers. Drug Dev Ind Pharm 2013 Oct 7 (epub).

2. Buprenorphine: an alternative to methadone. Med Lett Drugs Ther 2003; 45:13.

3. Approximate wholesale acquisition cost (WAC) of 30 tablets or films. Source: $ource® Monthly (Selected from FDB MedKnowledge™) October 5, 2013. Reprinted with permission by FDB, Inc. All rights reserved. ©2013. www.fdbhealth.com/policies/drug-pricing-policy. Actual retail prices may be higher.

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