author={Jennifer S. Orman and Gillian M. Keating},
SummaryAbstractBuprenorphine/naloxone (Suboxone®) comprises the partial μ-opioid receptor agonist buprenorphine in combination with the opioid antagonist naloxone in a 4: 1 ratio. When buprenorphine/naloxone is taken sublingually as prescribed, the naloxone exerts no clinically significant effect, leaving the opioid agonist effects of buprenorphine to predominate. However, when buprenorphine/naloxone is parenterally administered in patients physically dependent on full agonist opioids, the… 

Naltrexone-facilitated buprenorphine discontinuation: a feasibility trial.

Buprenorphine/naloxone addiction in a pharmacist as a result of migraine self-treatment

A 35-year-old female hospital pharmacist was admitted to treatment for opioid use disorder for using buprenorphine/naloxone film to self-medicate her migraine headaches and maintains sobriety at the treatment center.

Urine naloxone concentration at different phases of buprenorphine maintenance treatment.

It is suggested that naloxone in urine can act as an indicator of compliance with BNX, and the use/abuse of buprenorphine alone.

Patients that benefit from buprenorphine-naloxone on medically assisted treatment for opioid dependence in Malaysia.

Buprenorphine-naloxone is a safe and effective drug substitution therapy for opioid dependence that has fewer interactions with other medications, and has similar efficacy to methadone.

Buprenorphine/naloxone versus methadone and lofexidine in community stabilisation and detoxification: A randomised controlled trial of low dose short-term opiate-dependent individuals

Methadone/lofexidine and buprenorphine/naloxone had comparable outcomes during rapid outpatient stabilisation and detoxification in low dose opiate users.

Buprenorphine/naloxone versus methadone opioid rotation in patients with prescription opioid use disorder and chronic pain: study protocol for a randomized controlled trial

This is one of the first studies comparing buprenorphine/naloxone and methadone for treating prescription OUD in a broad patient group with chronic non-malignant pain.

Oxycodone/Naloxone Prolonged-Release: A Review of Its Use in the Management of Chronic Pain While Counteracting Opioid-Induced Constipation

Although more comparative data are needed, oxycodone/naloxone PR is an effective option for use in patients with severe chronic pain, particularly among those with opioid-induced constipation.

Buprenorphine analogue BU08028 is one step closer to the Holy Grail of opioid research

  • Jun-Xu Li
  • Medicine, Biology
    Proceedings of the National Academy of Sciences
  • 2016
A systematic evaluation of a novel opioid, BU08028, which may lead research one step closer to the “Holy Grail” of opioid analgesic research: the development of opioids that retain the analgesic efficacy with reduced side effects.



Effects of buprenorphine/naloxone in opioid-dependent humans

Intramuscular injection of buprenorphine/naloxone precipitates withdrawal in opioid dependent persons; therefore, the combination has a low abuse potential by the injection route in this population.

Blockade of hydromorphone effects by buprenorphine/naloxone and buprenorphine

The addition of naloxone to buprenorphine may deter the parenteral abuse of bupRenorphine/nalox one, but it does not enhance the therapeutic efficacy of bu prenorphines.

Buprenorphine and naloxone interactions in methadone maintenance patients

Buprenorphine/naloxone reduces the reinforcing and subjective effects of heroin in heroin-dependent volunteers

These data demonstrate that both 8/2 and 32/8 mg buprenorphine/naloxone were well tolerated and effective in reducing the reinforcing and subjective effects of heroin, relative to the 2/0.5-mg dose, and show for the first time in humans that it is possible to quantify the efficacy and affinity of heroin for mu opioid receptors.

Buprenorphine-Containing Treatments

Because of its relative safety and lower risk of illegal diversion, buprenorphine has been made available in several countries for treating opioid addiction in the private office setting, greatly enhancing treatment options for this condition.

Effects of buprenorphine and naloxone in morphine-stabilized opioid addicts.

Buprenorphine: how to use it right.

Buprenorphine's physical dependence potential: antagonist-precipitated withdrawal in humans.

It is indicated that buprenorphine maintenance produces physical dependence and that i.m. naloxone and p.o. naltrexone produce equivalent effects in withdrawal precipitation under these conditions.

Buprenorphine and naloxone alone and in combination in opioid-dependent humans

Overall, the naloxone-buprenorphine combinations produced effects which were qualitatively similar to the effects of n aloxone alone, suggesting a low potential for abuse of the combination product by opioid-dependent individuals.

Pharmacokinetics and Subjective Effects of Sublingual Buprenorphine, Alone or in Combination with Naloxone

Less than dose-proportional increases in plasma buprenorphine concentrations may contribute to the observed plateau for most pharmacodynamic effects as the dose is increased, according to the evaluated pharmacokinetics and pharmacodynamics of expected therapeutic doses.