Buprenorphine: A New Potent Long-Acting Synthetic Analgesic. Comparison With Morphine

Downing, J. W.; Leary, W. P.; White, Eric S.

doi:10.1093/bja/49.3.251

Cited by 94 publications

(30 citation statements)

References 2 publications

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“…In humans, the analgesic effect of BNP is prolonged for several hours (Downing et al 1977;Cook et al 1982), while the drug level in plasma declines very rapidly, with a half-life of 2-3 h (Bullingham et al 1980). Ohtani et al (1995) have characterized the analgesic effect induced by BNP, based on pharmacokinetic-pharmacodynamic modeling using rats.…”

Section: Discussionmentioning

confidence: 99%

P-glycoprotein mediates brain-to-blood efflux transport of buprenorphine across the blood–brain barrier

Suzuki

Zaima

Moriki

et al. 2007

Journal of Drug Targeting

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The involvement of P-glycoprotein (P-gp) in buprenorphine (BNP) transport at the blood-brain barrier (BBB) in rats was investigated in vivo by means of both the brain uptake index technique and the brain efflux index technique. P-gp inhibitors, such as cyclosporin A, quinidine and verapamil, enhanced the apparent brain uptake of [3H]BNP by 1.5-fold. The increment of the BNP uptake by the brain suggests the involvement of a P-gp efflux mechanism of BNP transport at the BBB. [3H]BNP was eliminated with an apparent elimination half-life of 27.5 min after microinjection into the parietal cortex area 2 regions of the rat brain. The apparent efflux clearance of [3H]BNP across the BBB was 0.154 ml/min/g brain, which was calculated from the elimination rate constant (2.52 x 10- 2 min- 1) and the distribution volume in the brain (6.11 ml/g brain). The efflux transport of [3H]BNP was inhibited by range from 32 to 64% in the presence of P-gp inhibitors. The present results suggest that BNP is transported from the brain across the BBB via a P-gp-mediated efflux transport system, at least in part.

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Section: Discussionmentioning

confidence: 99%

P-glycoprotein mediates brain-to-blood efflux transport of buprenorphine across the blood–brain barrier

Suzuki

Zaima

Moriki

et al. 2007

Journal of Drug Targeting

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“…Buprenorphine is used in laboratory animal and human medicine because it has a long duration of action (Downing et al 1977) and fewer cardiovascular and respiratory effects than do most other opioid analgesics for pain management (Taylor & Houlton 1984). Potential acute adverse effects of buprenorphine in humans are diffuse mild mental status changes, mild to minimal respiratory depression, small pupils and relatively normal vital signs (Sporer 2004).…”

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confidence: 99%

Effects of buprenorphine on body temperature, locomotor activity and cardiovascular function when assessed by telemetric monitoring in rats

2008

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SummaryBuprenorphine is a potent analgesic commonly used clinically in humans and rodents experiencing severe pain. However, effects of therapeutic doses on locomotor activity and the cardiovascular system have not been studied in conscious animals. The effects of buprenorphine were therefore evaluated in this study using telemetric monitoring in conscious animals. Telemetry transmitters were implanted in the peritoneal cavity of Wistar rats with a pressure catheter in the aorta and electrodes for electrocardiogram (ECG) recording subcutaneously. After a single subcutaneous administration of saline, each rat was administered single subcutaneous doses of 0.006, 0.03 or 0.15 mg/kg body weight (bw) of buprenorphine. During a 10 h period after administration, buprenorphine induced a varying dose-dependent increase in body temperature, heart rate, dP/dt and systolic-diastolic blood pressure, as well as a corresponding decrease in QT time. At high dose, however, QT time was still decreased 24 h post-administration, but no arrhythmias or visual changes were observed in the ECG complex. Body temperature and heart rate increased at the high dose of buprenorphine, even at 20 -24 h after administration. Moreover, the high dose of buprenorphine induced a biphasic response in diastolic blood pressure, with an early and pronounced increase that, at 14 h after administration, reversed to a decrease, failing to normalize within 24 h post-dosage. The results indicate that buprenorphine induces long-lasting effects (such as body temperature and cardiovascular effects) in the rat after a single subcutaneous dose at 0.15 mg/kg bw.

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“…Compare, for example, equianalgesic doses of buprenorphine and morphine by the two routes of administration. A standard parenteral dose of buprenorphine is 0.3 mg. Lanz et al 2 directly compared epidural doses of 0.3 mg and 0.15 mg buprenorphine, and showed that the former gave better analgesia; these data suggest that the parenteral/epidural (P/E) analgesic dose ratio for buprenorphine equals I. This P/E ratio is confirmed by other, less rigorous, single epidural dose studies.…”

Section: Epidural Buprenorphinementioning

confidence: 89%

Epidural buprenorphine

Fox

1990

Can J Anaesth

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REPLY Epidural buprenorphineTo the Editor: Ackerman et al., 1 from the University of Cincinnati, Ohio, report a well-conducted study of pruritus associated with epidural opiates. The drugs studied were 5 mg morphine, 50 ttg fentanyl, 0.3 mg buprenorphine, or 1 mg butorphanol in 10 ml. Two concerns emerge about the use of buprenorphine by this route of administration: (i) the absence of approval by the appropriate regulatory authorities, and (ii) whether this route of administration leads to any pharmacokinetic or pharrnacodynamic advantage.As a pharmaceutical physician at Norwich Eaton, the company responsible for Buprenex | in the USA, I am obliged to point out that this is not an approved route of administration for buprenorphine in this country. While the parenteral formulation may be attractive for epidural studies because it contains no organic preservatives, the anaesthetist should be informed that he or she uses this route of administration with the risks which attend unapproved usage.Buprenorphine is a highly lipophilic, potent and parenterally long-acting analgesic, 2'3 and is an exception to the general rule that epidural doses of opioids are smaller than parenteral doses. Compare, for example, equianalgesic doses of buprenorphine and morphine by the two routes of administration. A standard parenteral dose of buprenorphine is 0.3 mg. Lanz et al. 2 directly compared epidural doses of 0.3 mg and 0.15 mg buprenorphine, and showed that the former gave better analgesia; these data suggest that the parenteral/epidural (P/E) analgesic dose ratio for buprenorphine equals I. This P/E ratio is confirmed by other, less rigorous, single epidural dose studies. ,.4-sThe low P/E dose ratio, and the similarity of duration of action by the epidural and parenteral routes, suggest that there is no advantage to be gained by the administration of buprenorphine using the epidural route. Furthermore, these data are consistent with an analgesic effect which may be entirely due to systemic absorption. The profile of adverse effects dependent upon this route of administration is relatively unknown.6 In the absence of any pharmacokinetic or pharmacodynamic advantage, the epidural route of administration must be considered to be redundant for buprenorphine.

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Buprenorphine: A New Potent Long-Acting Synthetic Analgesic. Comparison With Morphine

Cited by 94 publications

References 2 publications

P-glycoprotein mediates brain-to-blood efflux transport of buprenorphine across the blood–brain barrier

P-glycoprotein mediates brain-to-blood efflux transport of buprenorphine across the blood–brain barrier

Effects of buprenorphine on body temperature, locomotor activity and cardiovascular function when assessed by telemetric monitoring in rats

Epidural buprenorphine

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