Buprenorphine dosing

Dose amounts consist of the buprenorphine dose (the number before the slash) and the naloxone dose (the number after the slash). Do not begin buprenorphine until patient shows evidence of opioid withdrawal. 

Patient should abstain from LAAM for >48 hours before first buprenorphine dose. 

The approval of buprenorphine for the office-based treatment of opioid dependence represents a major departure from the earlier methadone clinic system. Physicians with addiction specialist credentials or those who have completed 8 hours of approved training can become qualified to treat up to 30 patients in their private offices. Stable patients may be given prescriptions for up to a month of medication. The combination buprenorphine/naloxone tablet is expected to have minimal risk for diversion. When taken subhnguaUy, as prescribed, naloxone has minimal biologic activity and does not interfere with the buprenorphine dose. However, if an attempt is made to inject the drug, the addict will experience the full antagonist effect of the naloxone. 

Theoretically buprenorphine metabolism could be inhibited by itraconazole, ketoconazole, grapefruit juice, and erythromycin or any other CYP3A4 inhibitor the effects may be greater than expected for the dose of buprenorphine being given may need to decrease buprenorphine dose. 

Conversely buprenorphine metabolism could by increased by carbamazepine, phenytoin, St. John s wort, efavirenz, and nevirapine, or any other CYP3A4 inducer the effects may be less than expected may need to increase buprenorphine dose. 

Patients taking methadone or other long-acting opioids Withdrawal appears more likely in patients maintained on higher doses of methadone (more than 30 mg) and when the first buprenorphine dose is administered shortly after the last methadone dose. 

Clark NC, Lintzeris N, Muhleisen PJ. Severe opiate withdrawal in a heroin user precipitated by a massive buprenorphine dose. Med J Aust 2002 176(4) 166-7. 

Withdrawal buprenorphine doses should be tapered gradually to prevent signs and symptoms of withdrawal in the physically dependent patient introduction of appropriate immediate-release opioid medication should be considered. 

Lactation An observational study of seven breast-feeding women taking buprenorphine found that the infant is exposed to approximately 0.38% of the maternal buprenorphine dose via breast milk [90 ]. 

The initial dose of buprenorphine should be given at least 12-24 hours after the last heroin dose, 24 hours after the last methadone dose, or 48 hours after the last LAAM dose (see Table 2-3). The methadone dosage of methadone maintenance patients should be reduced to 30 mg/day before the transfer to buprenorphine is attempted. Ideally patients should show clear evidence of opiate withdrawal before receiving the first dose of buprenorphine, to avoid the risk that buprenorphine will precipitate more severe withdrawal. For the first day, sublingual buprenorphine/naloxone doses of 2/0.5-4/1 mg can be given every 2-4 hours, up to a maximum total dose of 8/2 mg/day. On the... 

Symptomatic treatment focuses on minimizing the withdrawal symptoms to help patients be as comfortable as possible (Tables 33-6 through 33-8). This is combined with the use of methadone or buprenorphine (Suboxone or Subutex ) to suppress the withdrawal symptoms by providing a p opioid full or partial agonist in a tapering dose schedule within a controlled environment. 

Naltrexone (ReVia). Naltrexone is a very potent antagonist of the actions of opiates. It has been used to reduce the rewarding effects of not only opiates but alcohol as well. Like buprenorphine, naltrexone appears to reduce craving for opiates by blocking their pleasurable effects. Naltrexone is not useful for detoxification and in fact worsens withdrawal. Naltrexone can be useful for maintenance treatment in those patients motivated to achieve total abstinence. It is taken at a constant dose of 50mg/day. A sustained-release depot formulation currently under development will likely help to overcome adherence issues that often undermine treatment for substance use disorders. 

Incomplete reversal of buprenorphine In animals, nalmefene doses up to 10 mg/kg (437 times the maximum recommended human dose) produced incomplete reversal of buprenorphine-induced analgesia. Hence, nalmefene may not completely reverse buprenorphine-induced respiratory depression. 

Tablets Administer sublingually as a single daily dose in the range of 12 to 16 mg/day. When taken sublingually, buprenorphine and buprenorphine/naloxone have similar clinical effects and are interchangeable. Buprenorphine tablets contain no naloxone and are preferred for use during induction.

Patients taking heroin or other short-acting opioids At treatment initiation, administer the dose of buprenorphine at least 4 hours after the patient last... 

Reducing dosage and stopping treatment - Make the decision to discontinue therapy with buprenorphine or buprenorphine/naloxone after a period of maintenance or brief stabilization as part of a comprehensive treatment plan. Gradual and abrupt discontinuation have been used but there is not a best method of tapering the dose at the end of treatment. 

Children - Buprenorphine has been used in children 2 to 12 years of age at doses between 2 and 6 mcg/kg of body weight given every 4 to 6 hours. There is insufficient experience to recommend a dose in infants below 2 years of age, single doses greater than 6 mcg/kg of body weight, or the use of a repeat or second dose at 30 to 60 minutes (such as is used in adults). 

Pharmacology Buprenorphine is a semisynthetic centrally acting opioid analgesic derived from thebaine a 0.3 mg dose is approximately equivalent to 10 mg morphine in analgesic effects. Buprenorphine exerts its analgesic effect via high affinity binding of CNS opiate receptors. 

Respiratory effects - A therapeutic dose of 0.3 mg buprenorphine can decrease respiratory rate similarly to an equianalgesic dose of morphine (10 mg). 

The abuse potential of buprenorphine is low. While high doses of the drug are perceived by addicts as being... 

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