Buprenorphine

Buprenorphine is derived from thebaine. It is a partial mu agonist with kappa antagonist activity. Buprenorphine has 25 to 50 times the potency of morphine. It is used to produce a longer-lasting analgesia than morphine. Effects of buprenorphine last longer because it is released more slowly from mu receptors than morphine. It is available as an injectable for intramuscular (IM) or intravenous administration in a 1-ml solution containing 0.3 mg buprenorphine (as buprenorphine HC1) for the relief of moderate to severe pain. It is also available to treat opioid dependence in the formulation of a tablet,51 alone or in combination with naloxone, in 2- or 8-mg 

Pharmacological effects occur within 15 min of IM administration, peaking at approximately 

1 h and persisting for up to 6 h. After SL administration, peak pharmacological effects typically occur after 100 min. After an intravenous dose of 0.3 mg, plasma concentrations are typically less than 1 ng/ml. Sublingual maintenance therapy of 8 mg/day resulted in plasma buprenorphine concentrations of 1 to 8 ng/ml.52 

The bioavailability of the buprenorphine/naloxone tablet appears to be greater than the buprenor-phine-alone formulation, with the former similar to the drug in liquid form. Buprenorphine is approximately 96% plasma protein bound, primarily to a- and [3-globulin. The plasma half-life is 

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The quest for compounds that combined the analgesic properties of morphine, were nonaddictive, and lacked the side effects of nalorphine, led to the development of the dmgs shown in Table 3. These compounds have both agonist and antagonist activities. Nalbuphine (14) (23) and buprenorphine... 

A common strategy for treating chronic opiate addiction iavolves the substitution of methadone which can either be provided as maintenance therapy or tapered until abstinence is achieved. Naltrexone and buprenorphine [52485-79-7] have also been used ia this manner. The a2 adrenergic agonist clonidine [4205-90-7] provides some rehef from the symptoms of opiate withdrawal, probably the result of its mimicking the inhibitory effect of opiates on the activity of locus coerukus neurons. 

Buprenorphine 2, 321 Bupropion l 4 Buquinolate U 346 Burimamide 251 Buspirone 300 Butabarbital 1, 268 Butacaine J, T2 Butacetin 2 95 Butaclamol 2, 226 Butalbital 1, 268 Butami rate 7, 76 Butamisole 226 Butaperazine 381... 

Substitution therapy with methadone or buprenorphine has been veiy successfiil in terms of harm reduction. Some opiate addicts might also benefit from naltrexone treatment. One idea is that patients should undergo rapid opiate detoxification with naltrexone under anaesthesia, which then allows fiuther naltrexone treatment to reduce the likelihood of relapse. However, the mode of action of rapid opiate detoxification is obscure. Moreover, it can be a dangerous procedure and some studies now indicate that this procedure can induce even more severe and long-lasting withdrawal symptoms as well as no improvement in relapse rates than a regular detoxification and psychosocial relapse prevention program. 

Alfentanil, codein, dihydromorphine, etor-phine, fentanyl, heroin, hydromorphone, levo-methadone, morphine, oxycodone, pethidine, piritramide, remifentanil, sufentanil, tilidine, tramadol Buprenorphine, pentazocine Naloxone, naltrexone... 

C4H5CIO 4023-34-1) see Buprenorphine Fexofenadine hydrochloride Naltrexone Prazepam cyclopropanecarboxylic acid ethyl ester (C(,H o02 4606-07-9) see Pimozide... 

C4H7Br 7051-34-5) see Betaxolol Ciraetropium bromide Flutoprazepam Naltrexone Prazepam A -cyclopropylmethyI-6,14-e do-ethano-7a-I(lS)-l-hy-droxy-1,2,2-trim ethylpropyijtetrahydronorthebaine (C30H43NO4 16524-65-5) sec Buprenorphine (2-cyc)opropyl-2-oxoethyl)triphenyIphusphomum bromide... 

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... 

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. 

It is anticipated that buprenorphine will be an acceptable treatment for younger addicts and for individuals with smaller habits and shorter histories of dependence, thus permitting earlier intervention in the course of the addiction. Clinical experience suggests that buprenorphine is less effective for individuals with larger opioid habits. Methadone or LAAM remains the preferred medication for those patients. 

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