Pharmacokinetics and pharmacodynamics of multiple sublingual buprenorphine tablets in dose-escalation trials
by
Ciraulo DA, Hitzemann RJ, Somoza E, Knapp CM, Rotrosen J,
Sarid-Segal O, Ciraulo AM, Greenblatt DJ, Chiang CN.
Boston University School of Medicine,
Doctors Office Building, Suite 914,
720 Harrison Avenue, Boston, MA 02118.
AJ Clin Pharmacol. 2006 Feb;46(2):179-92.

ABSTRACT

In this investigation, the pharmacokinetic and pharmacodynamic properties were determined of multiple doses of sublingual tablets containing either buprenorphine alone or buprenorphine and naloxone. Subjects were experienced opiate users who received escalating doses (4-24 mg) of buprenorphine either alone or in combination with naloxone. Peak concentration (Cmax) and area under the concentration-time curves (AUCs) increased for both buprenorphine and naloxone with escalating doses. Significant differences were found across the range of doses administered for dose-adjusted Cmax for both tablet formulations and for the dose-adjusted AUCs for the buprenorphine-naloxone tablets. For both formulations, the maximal buprenorphine-induced decreases in respiratory rate and pupil diameter did not vary significantly across doses. Several of the subjective effects of buprenorphine did not increase as the dose of buprenorphine administered was increased. These findings are consistent with the ceiling effect associated with the partial agonist actions of buprenorphine. They also indicate a lack of dose proportionality for buprenorphine sublingual tablets, at least during the times at which levels of this agent are highest.

HS-599
Methadone
Quality of life
Sugar junkies
Norbuprenorphine
LAAM v methadone
Subutex and Suboxone
Opioids and depression
Buprenorphine : structure
Buprenorphine and reward
Buprenorphine and naltrexone
Buprenorphine and the receptors
Buprenorphine for speedball users
Buprenorphine as an antidepressant
Buprenorphine: the standard wisdom
Buprenorphine : behavioral pharmacology
Buprenorphine versus buprenorphine/nalaxone
Buprenorphine (Buprenex, Temgesic) versus placebo or methadone

Refs
and further reading

HOME
HedWeb
Nootropics
cocaine.wiki
Future Opioids
BLTC Research
MDMA/Ecstasy
Superhapiness?
Utopian Surgery?
The Abolitionist Project
The Hedonistic Imperative
The Reproductive Revolution
Critique of Huxley's Brave New World

The Good Drug Guide
The Responsible Parent's Guide
To Healthy Mood Boosters For All The Family