Determination of buprenorphine by high-performance liquid chromatography with fluorescence detection: application to human and rabbit pharmacokinetic studies

Ho, Shung Tai; Wang, Jhi Joung; Ho, Wei‐Ting; Hu, Oliver Yoa Pu

doi:10.1016/0378-4347(91)80537-m

Cited by 38 publications

(10 citation statements)

References 14 publications

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“…This study describes IV buprenorphine pharmacokinetics and its primary active metabolite norbuprenorphine across a higher range of acute doses than previously reported in the literature (Bullingham et al, 1981, 1980, 1982; Ho et al, 1991; Kuhlman et al, 1996; Olley and Tiong, 1988). We previously demonstrated the absence of dose-related increases in physiological and subjective effects from 2–16 mg IV buprenorphine, indicating a ceiling effect of buprenorphine administered by the IV route (Umbricht et al, 2004).…”

Section: Discussionmentioning

confidence: 97%

Intravenous buprenorphine and norbuprenorphine pharmacokinetics in humans

Huestis

Cone

Pirnay³

et al. 2013

Drug and Alcohol Dependence

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Background Prescribed sublingual (SL) buprenorphine is sometimes diverted for intravenous (IV) abuse, but no human pharmacokinetic data are available following high-dose IV buprenorphine. Methods Plasma was collected for 72 h after administration of placebo or 2, 4, 8, 12, or 16 mg IV buprenorphine in escalating order (single-blind, double-dummy) in 5 healthy male non-dependent opioid users. Buprenorphine and its primary active metabolite, norbuprenorphine, were quantified by liquid chromatography tandem mass spectrometry with limits of quantitation of 0.1 μg/L. Results Maximum buprenorphine concentrations (mean ± SE) were detected 10 min after 2, 4, 8, 12, 16 mg IV: 19.3±1.0, 44.5±4.8, 85.2±7.7, 124.6±16.6, and 137.7±18.8 μg/L, respectively. Maximum norbuprenorphine concentrations occurred 10–15 min (3.7±0.7 μg/L) after 16 mg IV administration. Conclusions Buprenorphine concentrations increased in a significantly linear dose-dependent manner up to 12 mg IV buprenorphine. Thus, previously demonstrated pharmacodynamic ceiling effects (over 2–16 mg) are not due to pharmacokinetic adaptations within this range, although they may play a role at doses higher than 12 mg.

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Section: Discussionmentioning

confidence: 97%

Intravenous buprenorphine and norbuprenorphine pharmacokinetics in humans

Huestis

Cone

Pirnay³

et al. 2013

Drug and Alcohol Dependence

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“…(1994) estimated t 1/2el of 2.8 h, a V (dss) of 4.2 L/kg and Cl of 23.3 mL/kg/min. Ho et al . (1991) investigated the kinetics in the rabbit, while Garrett and Chandran (1990) studied them in the dog but did not use clinically relevant doses.…”

Section: Discussionmentioning

confidence: 99%

Morphine, pethidine and buprenorphine disposition in the cat

Taylor

Robertson

Dixon

et al. 2001

Vet Pharm & Therapeutics

103

105

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Pharmacokinetics of morphine, buprenorphine and pethidine were determined in 10 cats. Six cats received morphine (0.2 mg/kg) intravenously and four intramuscularly. Five received buprenorphine (0.01 mg/kg) intravenously and six intramuscularly. Six received pethidine (5 mg/kg) intramuscularly. Jugular venous blood samples were collected at time points to 24 h, and plasma morphine concentrations were measured by high performance liquid chromatograpy (HPLC), buprenorphine by radioimmunoassay (RIA) and pethidine by gas chromatography. Our data for morphine show elimination half-life (t1/2el) 76.3 min intravenous (i.v.) and 93.6 min intramuscular (i.m.); mean residence time (MRT) 105.0 and 120.5 min; clearance (Clp) 24.1 and 13.9 mL/kg/min; and volume of distribution (V(dss)) 2.6 and 1.7 L/kg, respectively. Comparable data for buprenorphine are t1/2el 416.8 and 380.2 min; MRT 417.6 and 409.8 min; Clp 16.7 and 23.7 mL/kg/min; and V(dss) 7.1 and 8.9 L/kg. For i.m. pethidine, t1/2el 216.4 min; MRT 307.5 min; Clp 20.8 mL/kg/min and V(dss) 5.2 L/kg. For i.m. dosing, the tmax for morphine, buprenorphine and pethidine were 15, 3 and 10 min, respectively. The pharmacokinetics of the three opioids in cats are broadly comparable with those of the dog, although there is a suggestion that the cat may clear morphine more slowly.

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“…The most important factor in the pharmacokinetics of buprenorphine is its high lipid solubility, which affects distribution, metabolism, and elimination. As characteristic of lipophilic compounds, buprenorphine exhibits multiphasic clearance, an initial rapid clearance followed by slower clearances observed after intravenous injection (38,39,67,79). It has been posited that the slow dissociation of buprenorphine from receptors contributes to its pharmacokinetics, as well as to the mild withdrawal syndrome observed in man (84).…”

Section: Pharmacokineticsmentioning

confidence: 99%

Buprenorphine: An Analgesic with an Expanding Role in the Treatment of Opioid Addiction

Robinson

2002

CNS Drug Reviews

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Buprenorphine, a long-acting opioid with both agonist and antagonist properties, binds to ì-opioid (OP 3 ), ê-opioid (OP 2 ), ä-opioid (OP 1 ), and nociceptin (ORL-1) receptors. Its actions at these receptors have not been completely characterized, although buprenorphine is generally regarded as a ì-opioid receptor partial agonist and a ê-opioid receptor antagonist. Its pharmacology is further complicated by an active metabolite, norbuprenorphine. Although buprenorphine can be used as an analgesic agent, it is of greater importance in the treatment of opioid abuse. Because of its partial agonist activity at ì-opioid receptors and its long half-life, buprenorphine has proven to be an excellent alternative to methadone for either maintenance therapy or detoxification of the opioid addict. Although buprenorphine may ultimately prove to be superior to methadone in the maintenance of the pregnant addict, its effects on the developing fetus must be carefully evaluated.

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Determination of buprenorphine by high-performance liquid chromatography with fluorescence detection: application to human and rabbit pharmacokinetic studies

Cited by 38 publications

References 14 publications

Intravenous buprenorphine and norbuprenorphine pharmacokinetics in humans

Intravenous buprenorphine and norbuprenorphine pharmacokinetics in humans

Morphine, pethidine and buprenorphine disposition in the cat

Buprenorphine: An Analgesic with an Expanding Role in the Treatment of Opioid Addiction

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