Class: Opioid Partial Agonist and Antagonist Combination. C-III
Dosage Forms. Sublingual Film: (Buprenorphine/Naloxone) 2 mg/0.5 mg, 8 mg/2 mg; Sublingual Tablet: (Buprenorphine/Naloxone) 2 mg/0.5 mg, 8 mg/2 mg
Common FDA Label Indication, Dosing, and Titration.
1. Opioid dependence: Adults and children >16 y, 12-16 mg (buprenorphine component) once daily sublingually, titrate to response; typical dose range from 4 to 24 mg/d
Off-Label Uses. None
MOA. Buprenorphine is a mu-opioid receptor partial agonist and a kappa-opioid receptor antagonist. Naloxone is a mu-opioid receptor antagonist that causes opioid withdrawal when injected parenterally and is included in the formulation to reduce the risk of abuse.
Drug Characteristics: Buprenorphine/Naloxone
Medication Safety Issues: Buprenorphine/Naloxone
Drug Interactions: Buprenorphine/Naloxone
Adverse Reactions: Buprenorphine/Naloxone
Efficacy Monitoring Parameters. Urine drug screening tests that are negative for illicit drugs. Relief of signs and symptoms associated with narcotic addiction.
Toxicity Monitoring Parameters. Severe skin rash, excessive drowsiness, decreased breathing, severe constipation.
Key Patient Counseling Points. Use a stool softener and/or laxative for preventing constipation. May cause drowsiness; avoid driving or other tasks requiring motor coordination. Avoid alcohol and other CNS depressants. Do not crush or swallow the sublingual tablet. Place the tablet under the tongue until it is dissolved. If you take 2 or more tablets at a time, place all of the tablets under the tongue together. If this is uncomfortable, place 2 tablets at a time under the tongue and repeat the process until all tablets have been taken. If you are using the sublingual film, place the film under the tongue until it is dissolved. If you need to take an additional film, place the new film on the opposite side from the first film. Do not chew, swallow, or move the film after placing it under the tongue.
Clinical Pearls. Taking opioids will result in precipitation of withdrawal symptoms. The opioid agonist properties of buprenorphine are limited by a ceiling effect which occurs at higher doses. The strength of sublingual films and tablets are not interchangeable. Sublingual film exposure is not consistent between doses. For example, one 8 mg film is not equivalent to four 2 mg films. Do not substitute multiple smaller dose films to equal a larger dose.