Zubsolv (buprenorphine and naloxone)

The following drug information is obtained from various newswires, published medical journal articles, and medical conference presentations.

Company:

Approval Status:

Approved July 2013

Specific Treatments:

maintenance treatment of opioid dependence

Therapeutic Areas

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General Information

Zubsolv is a sublingual tablet formulation of buprenorphine, an opioid analgesic, and naloxone, an opioid antagonist. It was designed to counteract the high effect that may arise following the intravenous injection of a disolved tablet. Combining buprenorphine and naloxone in a single tablet reduces the risk of intravenous abuse.

Zubsolv is specifically indicated for the maintenance treatment of opioid dependence and should be used as part of a complete treatment plan to include counseling and psychosocial support.

Zubsolv is supplied as a tablet for sublingual administration. The recommended target dosage of Zubsolv sublingual tablet is 11.4 mg/2.8 mg buprenorphine/naloxone/day (two 5.7/1.4 mg tablets) as a single daily dose. The dosage of Zubsolv should be progressively adjusted in increments/decrements of 1.4 mg/0.36 mg or 2.8 mg/0.72 mg buprenorphine/naloxone to a level that holds the patient in treatment and suppresses opioid withdrawal signs and symptoms.

Clinical Results

FDA Approval
The FDA approval of Zubsolv was based on efficacy data from a drug that has already been approved, Suboxone. Approval was also based on bioavailability and pharmacokinetic studies. Compared with other buprenorphine/naloxone treatments, Zubsolv has higher bioavailability, faster dissolve time, and smaller tablet size with a new menthol taste.

Side Effects

Adverse effects associated with the use of Zubsolv may include, but are not limited to, the following:

  • headache
  • nausea
  • vomiting
  • hyperhidrosis
  • constipation
  • signs and symptoms of withdrawal
  • insomnia
  • pain
  • peripheral edema

Mechanism of Action

Zubsolv ontains buprenorphine and naloxone. Buprenorphine is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor. Naloxone is a potent antagonist at mu-opioid receptors and produces opioid withdrawal signs and symptoms, if administered parenterally, in individuals physically dependent on full opioid agonists.

Additional Information

For additional information regarding Zubsolv or opiod addiction, please visit the Orexo web page.