The formulation of buprenorphine with naloxone carries some clinical controversy. 16 Headache, withdrawal syndrome, pain, and diaphoresis were among the most reported adverse events following the use of Suboxone. 15 Canadian labeling of the same products has limitations for both renal and hepatic impairment. US labeling has no limitations in patients with renal impairment, but it suggests using caution in hepatically impaired patients. The film should be taken whole and placed under the tongue until it completely dissolves. Table 1: Available Doses of Buprenorphine/Naloxone Combination Products* Table 1 illustrates the comparable doses available for these 3 products. Bunavail and Zubsolv are also only indicated for maintenance therapy following induction by Suboxone. 15Īlthough the pharmacokinetics among these 3 products are similar to the sublingual formulations, bioequivalence is variable. This medication is indicated for the treatment of opioid dependence and is used for heroin or other opioid dependency, both for induction and maintenance therapy. The buprenorphine transmucosal film is formulated in conjunction with naloxone. No dosage adjustments are recommended for renal or hepatic impairment. The most common adverse events seen after the use of this product were nausea, dizziness, sweating, hypotension, headache, vomiting, nausea, vomiting, hypoventilation, and miosis, while sedation was the most prevalent. This formulation is also used off-label for the treatment of opioid withdrawal in heroin-dependent hospitalized patients. 13īuprenex is approved for the relief of moderate to severe pain. The elimination half-life ranged from 1.2 to 7.2 hours in pharmacokinetic studies, with an average of 2.2 hours after IV administration. Peak effects of analgesia are observed 1 hour after injection, with initial effects occurring 15 minutes after injection and persisting 6 hours or longer. The IV formulation should be delivered slowly over at least 2 minutes. 12 It is intended for intravenous (IV) or intramuscular (IM) administration and contains 0.3 mg of buprenorphine per mL. Prior to the recent release of Belbuca, several formulations of buprenorphine were already available: a parenteral formulation (Buprenex), transmucosal film formulated in conjunction with naloxone (Bunavail, Suboxone, Zubsolv), sublingual tablet (Subutex), and transdermal patch (Butrans).īuprenex was released in 1985 in the United States as an injectable formulation of buprenorphine. 10 A clinical study later discovered in 1988 that naloxone reversal of buprenorphine failed to precipitate abstinence and abrupt withdrawal in animals and humans, producing only mild withdrawal effects. The higher the dose, the more effect an opioid has on the feedback loop.īecause of its “ceiling effect” at the opioid receptor, buprenorphine has a much lower likelihood of respiratory depression. Opioids block the carbon dioxide feedback loop that is used to stimulate the brainstem to increase respiratory rate. As the dosage increases, activity that buprenorphine exhibits as a partial agonist plateaus regardless of subsequent increases. 6,7īecause of this unique pharmacology, buprenorphine provides analgesia at therapeutic doses but also has a suggested “ceiling effect” on respiratory depression. 5,6 Mu-opioid receptor activity produces the analgesic effects of buprenorphine, while a strong affinity for the kappa receptors render them inactive. However, buprenorphine’s mechanism of action of is quite different from the others’.īuprenorphine is a partial agonist at the mu-opioid receptors and an antagonist at the kappa receptors. 4 It is a dehydroxylated phenanthrene similar in chemical structure to oxycodone, hydromorphone, oxymorphone, and several other opioids. 3īuprenorphine is approved in the Unites States to treat opioid abuse disorder and moderate to severe chronic pain. 2 Then, a separate study published in 1982 demonstrated that buprenorphine offered excellent analgesia with a blunted abuse liability. That same year, a clinical study determined that buprenorphine could be helpful in reducing cravings of pure opioids in patients with an opioid abuse disorder. 1 This article will review the development of various buprenorphine dosage forms, as well as their unique pharmaceutical properties and use in the treatment of pain.īuprenorphine was developed by UK-based Reckitt & Colman Products and released in the United Kingdom in 1978. Endo Pharmaceuticals recently announced the availability of Belbuca, the first buccal formulation of buprenorphine approved by the FDA for the treatment of pain.Ĭurrently, Belbuca is the only formulation of buprenorphine that can be delivered by dissolving a film that is placed on the inner lining of the cheek for the treatment of chronic pain.
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