Buprenorphine tablets

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.

Because faster onset of action is associated with higher potential for abuse, abuse-liability assessment should include consideration of whether a formulation can be altered to increase the speed of onset. There are numerous examples of abuse of a medication by a route other than that intended by the manufacturer. The sustained-release oral form of oxycodone, designed to deliver an initial rapid dose followed by slow release, has been widely abused by chewing the tablet, thus releasing the entire content of the tablet at once.65 There is also evidence for intravenous use of sublingual buprenorphine tablets.66 Transdermal systems developed to deliver medication slowly for extended periods of time have been prime targets for misuse,67 as discussed below in the case study of fentanyl. 

Vidal-Trecan, G. et al., Intravenous use of prescribed sublingual buprenorphine tablets by drug users receiving maintenance therapy in France, Drug Alcohol Depend., 69, 175, 2003. 

A 33-year-old man developed severe hepatitis after an oral overdose of buprenorphine tablets 112 mg over 48 hours (8). He presented with an acute confusional state, including disorientation in time and space. The condition led to anuria and hepatorenal insufficiency. He was successfully treated with hemodialysis. 

In a double-blind, randomized comparison of subUngual buprenorphine tablets with oral methadone in a 6-week trial in 58 patients using a flexible dosing procedure the retention rate was significantly better in those using methadone (90 versus 50%) (22). Those who completed the study had a similar number of opioid-positive urine samples, with a mean stabilization dose of 11 mg/day of buprenorphine and 70 mg/day of methadone. This study had several limitations 6 weeks is too short a period to determine any intermediate or long-term treatment outcomes, the sample size was too small, and the comparison of non-equivalent doses makes interpretation difficult. 

In a double-blind, double-dummy, randomized crossover study in 16 opioid-dependent patients stable on buprenorphine 24 mg/day, whole buprenorphine tablets were compared with crushed tablets. Crushing of the tablets in treatment centers was used as an approach to curb the abuse potential and diversion of buprenorphine. There were no differences in the clinical effects of whole and crushed tablets, suggesting that there was no clinical objection to using crushed tablets in order to counter diversion [14 j. 

Drag withdrawal A 2-year-old toddler developed buprenorphine withdrawal after having been given two-thirds of a 2-mg buprenorphine tablet daily from birth by its mother [202 ]. She was irritable and inconsolable and was imable to sleep. She had typical features of opioid withdrawal and was eventually maintained on methadone 1 mg/day. 

Lim CCT, Lee SH, Wong Y-C, Hui F. Embolic stroke associated with injection of buprenorphine tablets. Neurology 2009 73 876-9. 

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. 

Voltarol is a brand-name preparation for diclofenac (NSAID) and modified-release tablets are available in 75 mg and 100 mg strength. Nu-seals is a proprietary preparation of enteric-coated aspirin 75 mg. Fentanyl, co-codamol and Suboxone (buprenorphine and naloxone) consist of opioid drugs. 

Suboxone is a combination of buprenorphine (opioid partial agonist) and naloxone. It is presented as sublingual tablets and is used as an adjunct in the treatment of opioid dependence and in premedication or perioperative analgesia. A side-effect of opioids is drowsiness. 

In October 2002, the FDA approved two new medications for treating opiate addiction, both developed by Reckitt Benckiser Pharmaceuticals. The new drugs, Subutex (buprenorphine hydrochloride) and Suboxone tablets (buprenorphine hydrochloride and naloxone hydrochloride) contain buprenorphine, a partial opioid agonist. Like methadone, buprenorphine binds to the brain s opioid receptors, but produces significantly reduced pleasurable effects than heroin. 

Suboxone tablets (buprenorphine hydrochloride and naloxone hydrochloride)... 

Tablets, sublingual 2 mg buprenorphine base/0.5 mg naloxone, 8 mg buprenorphine base/2 mg naloxone (C-/77) Suboxone (Reckitt Benckiser)...

This probably reflects a common range of methods in practice, although from our own experience I would add that it seems better not to allow too much (or any) prior discussion of forthcoming reductions in dosage, as many reasons tend to be given to avoid these Again as examined in Chapter 2 there is virtually no support for benzodiazepine maintenance as there is for that with methadone and buprenorphine, and almost certainly benzodiazepines are far more often diverted to others than the opioid substitutes whose consumption can be supervised, with in the worst cases the tablets representing little more than currency. 

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... 

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... 

A 22-year-old man snorted an 8 mg crushed tablet of buprenorphine and 2 hours later had crushing chest pain, which resolved within a few minutes (4). The symptom recurred 3 weeks later after another inhalation of buprenorphine. An electrocardiogram suggested an acute anterior myocardial infarction caused by buprenorphine-induced coronary artery spasm. 

Two series of 39 and 78 deaths attributed to buprenorphine have respectively been reported in Strasbourg and 13 other French forensic centers between 1996 and 2000 (14). The risks incurred by the misuse of buprenorphine seem to arise through a combination of (a) the concomitant use of other psychotropic drugs (especially benzodiazepines and neuroleptic drugs) and (b) the improper use of tablets for intravenous administration and/or massive oral doses. The total recorded number of buprenorphine-... 

Although subhngual buprenorphine has been used in the management of heroin addiction (SEDA-16, 88), widespread abuse of buprenorphine by addicts is known (SEDA-16, 88), including the snorting of crushed sublingual tablets (SEDA-16, 88). 

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