Bioavailability of Sublingual Buprenorphine

@article{Mendelson1997BioavailabilityOS,
  title={Bioavailability of Sublingual Buprenorphine},
  author={John E. Mendelson and Robert A. Upton and E. Thomas Everhart and Peyton Jacob Iii and Reese T. Jones},
  journal={The Journal of Clinical Pharmacology},
  year={1997},
  volume={37}
}
Buprenorphine administered sublingually is a promising treatment for opiate dependence. Utilizing a new, sensitive, and specific gas chromatographic electron‐capture detector assay, the absolute bioavailability of sublingual buprenorphine was determined in six healthy volunteers by comparing plasma concentrations after 3‐ and 5‐minute exposures to 2 mg sublingual and 1 mg intravenous buprenorphine. The amount of unabsorbed buprenorphine in saliva was measured after 2‐, 4‐, and 10‐minute… 
Rifampicin decreases exposure to sublingual buprenorphine in healthy subjects
TLDR
Concomitant use of rifampicin and low‐dose sublingual buprenorphine may compromise the analgesic effect of bupenorphine and this can be mainly explained by an enhancement of CYP3A‐mediated first‐pass metabolism, which sublingUAL bupreliminary bypasses.
Voriconazole greatly increases the exposure to oral buprenorphine
TLDR
Voriconazole greatly increases exposure to oral buprenorphine, mainly by inhibiting intestinal and liver CYP3A4, and effect on some transporters may explain elevated norbuprenorphines concentrations.
The Pharmacokinetics and Local Tolerability of a Novel Sublingual Formulation of Buprenorphine
TLDR
The results suggest that this novel sublingual buprenorphine wafer may provide enhanced clinical utility in the management of both acute and chronic pain.
Formulation of buprenorphine for sublingual use in neonates.
TLDR
An ethanolic buprenorphine solution is stable at room temperature for 30 days and the potency was maintained for samples stored either in the original amber glass source bottles or in oral syringes.
Buprenorphine: clinical pharmacokinetics in the treatment of opioid dependence.
TLDR
The pharmacokinetic and pharmacodynamic properties of buprenorphine allow it to be a feasible option for substitution therapy in the treatment of opioid dependence.
Pharmacokinetics of Buprenorphine: A Comparison of Sublingual Tablet Versus Liquid after Chronic Dosing
TLDR
A randomized, double-blind, crossover study with dose increases was conducted to determine steady state buprenorphine plasma levels for the 2 formulations and to assess the relative bioavailability of each.
PK-PD modeling of buprenorphine in cats: intravenous and oral transmucosal administration.
TLDR
Overall, OTM administration of buprenorphine is as effective as i.v. treatment and offers a simple, noninvasive method of administration which produces thermal antinociception for up to 6 h in cats.
Systemic uptake of buprenorphine by cats after oral mucosal administration
TLDR
The pharmacokinetic data obtained after the intramuscular and intravenous administration of buprenorphine to cats from the same colony, suggesting that the mucosal route of administration should be as effective as intravenous and intramUScular injections.
...
...

References

SHOWING 1-10 OF 17 REFERENCES
Sublingual buprenorphine used postoperatively: clinical observations and preliminary pharmacokinetic analysis.
TLDR
It is suggested that this route may be particularly appropriate for highly lipophilic drugs like buprenorphine, as it caused a significant fall in the postoperatively elevated plasma glucose, and prevented any further rise in plasma cortisol.
Sublingual buprenorphine used postoperatively: ten hour plasma drug concentration analysis.
TLDR
Plasma drug concentrations after sublingual buprenorphine were significantly higher than those in the placebo group by 1 h and remained significantly higher over the succeeding nine hours.
Buprenorphine: a new maintenance opiate?
TLDR
Sublingual buprenorphine was acceptable to opiate‐addicted outpatients as a maintenance treatment, however, daily doses of greater than 4 mg will probably be required to suppress concurrent opiate abuse, and detoxification will need to be undertaken gradually.
Biopharmaceutical evaluation of transnasal, sublingual, and buccal disk dosage forms of butorphanol
TLDR
Transnasal dosage form of butorphanol was selected for further clinical trials of treatment of moderate to severe pain on the basis of the results of three‐way crossover randomized studies.
Sublingual absorption of selected opioid analgesics
TLDR
The results indicate that although the sublingual absorption and apparent sublingUAL bioavailability of morphine are poor, the sublingsual absorption of methadone, fentanyl, and buprenorphine under controlled conditions is relatively high.
Use of buprenorphine in the treatment of opiate addiction. I. Physiologic and behavioral effects during a rapid dose induction
TLDR
It is indicated that a rapid dose induction with buprenorphine is acceptable to heroin‐dependent persons and that it causes minimal withdrawal symptoms.
Substitution pharmacotherapies for opioid addiction: from methadone to LAAM and buprenorphine.
TLDR
The recent approval of l-alpha-acetylmethadol (LAAM) as a maintenance treatment agent represents the first opioid substitution alternative to methadone and full realization of its advantages could move opioid substitution therapy into mainstream medical care and draw into treatment a substantial number of new patients able to benefit from such treatment.
Drug delivery via the mucous membranes of the oral cavity.
The delivery of drugs via the mucous membranes lining the oral cavity (i.e., sublingual and buccal), with consideration of both systemic delivery and local therapy, is reviewed in this paper. The
Goodman & Gilman's The Pharmacological Basis of Therapeutics
TLDR
Goodman and Gilman's the pharmacological basis of therapeutics , Goodman and Gilmann's the pharmaceutica basis for drug discovery, and more.
...
...