Buprenorphine sublingual

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... 

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. 

In a double-blind, randomized study of three groups of 18 patients having abdominal surgery who received single doses of either intramuscular pethidine 75 mg, with sublingual buprenorphine 400 pg, or buprenorphine 300 pg alone, sedation and nausea were the most common adverse effects in all three groups. Patients who received... 

There have been reports of facial and lingual ulcers, the ulceration following repeated injection of buprenorphine into the left superior cervical ganglion for trigeminal neuralgia (6) and the use of sublingual buprenorphine (7). 

Impaired gastric emptying and delayed absorption after sublingual buprenorphine have also been reported (SEDA-17, 87). 

Sublingual buprenorphine is an alternative to methadone in treating opiate dependence, but its opioid agonist effects pose the risk of intravenous abuse and subsequent dependence. This abuse potential may be hmited by using a combination of buprenorphine with naloxone, which will precipitate opiate withdrawal when given... 

Two doses (8 and 16 mg) of sublingual buprenorphine have been compared in a 6-week double-bUnd, placebo-controlled inpatient study of the reinforcing effects of intravenous diamorphine (30). Only eight diamorphine-dependent men were recruited and the authors could only postulate that doses over 16 mg might be more effective in blocking the reinforcing effects of diamorphine. 

Woodham M. Pruritus with sublingual buprenorphine. Anaesthesia 1988 43(9) 806-7. 

Harris DS, Jones RT, Welm S, Upton RA, Lin E, Mendelson J. Buprenorphine and naloxone co-adminis-tration in opiate-dependent patients stabilized on sublingual buprenorphine. Drug Alcohol Depend 2000 61(1) 85-94. 

Chang CH, Wang CJ, Yen YC, Hsu SJ. Effectiveness of sublingual buprenorphine and intramuscular pethidine in acute renal colic. Formosan J Surg 2002 35 9-13. 

Administered sublingually, buprenorphine (0.4-0.8 mg) produces satisfactory analgesia in postoperative patients. Concentrations peak within 5 minutes of intramuscular injection and within 1—2 hours of oral or sublingual administration. The tj of 3 hours bears little relationship to the rate of disappearance of effects (see above). Most of the drug is excreted unchanged in the feces. About 96% of the circulating drug is bound to protein. 

A study in 12 healthy subjects found that both sublingual buprenorphine 400 micrograms and oral amitriptyline 50 mg impaired the performanee of a number of psychomotor tests (digit symbol substitution, flicker fusion, Maddox wing, hand-to-eye coordination, reactive skills), and the subjects felt drowsy, feeble, mentally slow and muzzy. When amitriptyline 30 mg, increased to 75 mg daily was given for 4 days before a single dose of buprenorphine, the psychomotor effects were not significantly increased, but the respiratory depressant effects of the buprenorphine were enhanced. ... 

The onset of action of buprenorphine is 5-15 minutes for intravenous of intramuscular injection and 15-45 minutes for sublingual buprenorphine. Buprenorphine has been seen to have a antinociceptive potency about 20-70 times greater than that of morphine [1]. 

BuUingham R, McQuay H, Dwyer D, Allen M, Moore R. Sublingual buprenorphine used post-operatively clinical observations and preliminary pharmacokinetic analysis. BrJClin Pharmacol 1981 12(2) 117-122. 

Tauzin-Fin P, Saumtally S, Houdek M, Muscagony J. [Analgesia by sublingual buprenorphine in extracorporeal kidney lithotripsy]. Ann FrAnesth Reanim 1993 12(3) 260-264. 

Gaitini L, Moskovitz B, Katz E, Vaisberg A, Vaida S, Nativ O. Sublingual buprenorphine compared to... 

Witjes W, Crul B, Vollaard E, Joosten H, von Egmond J. Application of sublingual buprenorphine in combination with naproxen or paracetamol for post-operative pain relief in cholecystectomy patients in a double-blind study. Acta Anaesthesiol Scand 1992 36(4) 323-327. 

Malinoff H, Barkin R, Wilson G. Sublingual buprenorphine is effective in the treatment of chronic pain syndrome. Am J Titer 2005Sep-Oct 12(5) 379-384. 

Sublingual buprenorphine has been proposed as an effective and well-tolerated treatment for neonatal abstinence syndrome. In a randomized trial, infants with neonatal abstinence syndrome, who had been born to mothers taking maintenance methadone, were randomized to either sublingual buprenorphine 13-39 micrograms/ kg per day ( = 13) or standard-of-care oral neonatal opium solution ( = 13) [29 ]. Buprenorphine administration was associated with a 31% reduction in length of treatment and a 29% reduction in the length of hospital stay. One infant had seizures after buprenorphine, but it was not clear whether buprenorphine was causal. 

Dmg fominlations A novel implant of buprenorphine (Probuphine ) with sustained-release technology has been evaluated in 12 subjects with opioid dependence maintained on sublingual buprenorphine [191. Most of them (92%) had at least one adverse event and 58% had events related to the insertion or removal of the implant. Other adverse events were experienced by 42% and included dizziness, constipation, abdominal pain, implant site reactions, flushing, and pallor. There were no serious events. 

Peyriere H, Tatem L, Bories C, Pageaux G-P, Blayac J-P, Larrey D. Hepatitis after intravenous injection of sublingual buprenorphine in acute hepatitis C carriers report of two cases of disappearance of viral replication after acute hepatitis. Ann Pharmacother 2009 43(5) 973-7. 

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