Which medications in the drug class Analgesics, Opioid Partial Agonist are used in the treatment of Opioid Abuse?

Updated: Jun 21, 2018
  • Author: David W Dixon, DO; Chief Editor: Glen L Xiong, MD  more...
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Answer

Analgesics, Opioid Partial Agonist

The sublingual product is used predominantly for induction dosing followed by maintenance with buprenorphine/naloxone SL. The buprenorphine subdermal implant may be considered for maintenance therapy of opioid addiction in patients who have achieved prolonged clinical stability on low-to-moderate buprenorphine/naloxone doses. Additionally, a once-monthly SC injection is also an option.

Buprenorphine

Partial opioid agonist and potent antagonist, is a potent analgesic that can be administered once a day to block withdrawal symptoms. The agonist effect is limited by a ceiling effect (ie, higher doses [>12-16 mg] do not produce more analgesia). The sublingual tablet is used for initial detoxification treatment of opioid addiction. It is administered in a stepwise regimen over 4-5 days before switching to maintenance treatment with buprenorphine/naloxone. Stabilization with buprenorphine transmucosal also precedes maintenance with a long-acting buprenorphine product (eg, once monthly SC injection, every 6 month subdermal implant).

Buprenorphine subdermal implant (Probuphine)

Semisynthetic narcotic mixed agonist-antagonist analgesic; exerts partial agonistic effects at the mu opioid receptor in the CNS and antagonistic effects at the kappa opioid receptor. The implant is indicated for the maintenance treatment of opioid dependence in patients who have achieved and sustained prolonged clinical stability on low-to-moderate doses of a transmucosal buprenorphine-containing product. The implants are inserted in the upper arm and provide 6 months of continuous buprenorphine.

Buprenorphine, long-acting injection (Sublocade)

Once monthly SC injection that forms a solid mass upon contact with body fluids from the Atrigel delivery mechanism. Must be administered in a healthcare setting to avoid inadvertent IV administration that could result in death. The half-life is 43-60 days. It is indicated for treatment of moderate-to-severe opioid use disorder (OUD) in adults who have initiated treatment with a transmucosal buprenorphine-containing product and have been on a stable dose of transmucosal buprenorphine treatment for ≥7 days.


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