|Trade names||Suboxone, Bunavail, Zubsolv|
|ATC code||N07BC51 (WHO)|
Buprenorphine/naloxone (trade name Suboxone) is a combination drug formulation of buprenorphine, a μ-opioid receptor (MOR) weak partial agonist and κ-opioid receptor antagonist, and naloxone, a MOR silent antagonist, in a 4:1 ratio. It is used in the treatment of opioid dependence. The purpose of naloxone is to deter intravenous abuse; parenteral administration rapidly induces opioid withdrawal symptoms, while regular, intended use does not (as naloxone is minimally bioavailable with sublingual ingestion). The drug is intended to treat opioid dependence
This combination is available as sublingual tablets or film.
Buprenorphine/naloxone is used for the treatment of opioid dependence in combination with psychosocial support and counseling for the patient.
Side effects are basically the same as those of buprenorphine and other opioids. In addition, naloxone can induce withdrawal symptoms in people who are addicted to opioids.
Dependence and withdrawal
Even though controlled trials in human subjects suggest that buprenorphine and naloxone at a 4:1 ratio will produce unpleasant withdrawal symptoms if taken intravenously by people who are addicted to opioids, these studies administered buprenorphine/naloxone to people already addicted to less powerful opiates such as morphine. These studies show the strength of buprenorphine/naloxone in displacing opiates, but do not show the effectiveness of naloxone displacing buprenorphine and causing withdrawal. The Suboxone formulation still has potential to produce an opioid agonist "high" if injected by non-dependent persons, which may provide some explanation to street reports indicating that the naloxone is an insufficient deterrent to injection of Suboxone. The addition of naloxone and the reasons for it are conflicting. Published data show that the μ-opioid receptor binding affinity of buprenorphine is higher than naloxone's (K(i) = 0.2157 nM for buprenorphine, K(i) = 1.1518 nM for naloxone; smaller K(i) mean higher affinity). Furthermore, the IC50 or the half maximal inhibitory concentration for buprenorphine to displace naloxone is 0.52 nM, while the IC50s of other opiates in displacing buprenorphine, is 100 to 1,000 times greater. These studies help explain the ineffectiveness of naloxone in preventing Suboxone abuse, as well as the potential dangers of overdosing on buprenorphine, since a continuous infusion of naloxone can be necessary in order to reverse its respiratory effects.
The sedating/narcotic effect of buprenorphine is increased by other sedating drugs such as other opioids, benzodiazepines, older antihistamines, alcohol, and antipsychotics. In addition, opioids and especially benzodiazepines increase the risk for potentially lethal respiratory depression.
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