Buprenorphine sublingual administration

Comer SD, Collins ED, Fischman MW. Buprenorphine sublingual tablets effects on IV heroin self-administration by humans. Psychopharmacology (Berl) 2001 154(1) 28-37. 

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. 

Buprenorphine is a semi-synthetic derivative of thebaine, one of the opium alkaloids. It is approximately 30 times as potent as morphine. A dose of 0.3 mg intramuscularly has a duration of analgesic action of 6-18 h. Buprenorphine is also effective sublingually. The average bio-availability by this route is about 55%, but absorption is slow and the time to achieve peak plasma concentrations is variable, with a range of 90-360 min. The onset of action is rather slow (5-15 min) after both intramuscular and intravenous administration, possibly due to slow receptor association. Buprenorphine binds to and dissociates from the p receptor very slowly, which may account for its low potential for physical abuse. It also means that buprenorphine-induced respiratory depression is difficult to reverse with naloxone, even with very high doses. Doxapram may in these circumstances be useful. Drowsiness and dizziness are the most common side effects, although they rarely... 

Administration (FDA) for the treatment of opioid addiction. Treatment is initiated with buprenorphine alone administered sublingually, followed by maintenance therapy with a combination of buprenorphine and naloxone (Suboxone) to minimize abuse potential. The partial agonist properties of buprenorphine limit its usefulness for the treatment of addicts who require high maintenance doses of opioids. However, conversion to maintenance treatment with higher doses of methadone, a full agonist, is possible. 

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. 

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