Anesthetic Potency of Nalbuphine and Interaction with Morphine in Rats

DiFazio, Cosmo A.; Moscicki, Jeffrey C.; Magruder, Michael R.

doi:10.1213/00000539-198109000-00003

Cited by 45 publications

(12 citation statements)

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“…At low doses (< 0.5 mg kg-'), nalbuphine exhibits an analgesic potency which is approximately two-thirds that of morphine (Bahar et al, 1985;Beaver & Feise, 1978) when used to control postoperative pain in patients. A similar relative potency for nalbuphine has been found when it is used as a supplement to volatile anaesthetic agents (Murphy & Hug, 1982;DiFazio et al, 1981). At higher doses (> 1 mg kg-') the analgesic and anaesthetic effects of nalbuphine appear to 'plateau'.…”

Section: Introductionsupporting

confidence: 54%

The pharmacokinetics of oral and intravenous nalbuphine in healthy volunteers.

Aitkenhead

Lin

Achola

1988

Brit J Clinical Pharma

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The pharmacokinetics of nalbuphine were studied in 10 healthy volunteers on two separate occasions following administration by either the intravenous (20 mg) or oral (60 mg) route. After administration, serum concentrations of nalbuphine were measured for 12 h using a high pressure liquid chromatography assay, and pharmacokinetic parameters were derived using a three compartment model. After i.v. administration, elimination half-life was 222 (111-460) min (mean and range) and total body clearance was 1.5 (0.8-2.3) 1 min-'. Cma, after oral administration was 21.4 (6.0-36.2) ng ml-' and tm. was 46.6 (15.3-89.0) min. Bioavailability of the oral preparation was 11.8 (6.1-20.1)%.

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Section: Introductionsupporting

confidence: 54%

The pharmacokinetics of oral and intravenous nalbuphine in healthy volunteers.

Aitkenhead

Lin

Achola

1988

Brit J Clinical Pharma

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“…Our data on the use of nalbuphine in combination with isoflurane confirmed an earlier study in which nalbuphine plus cyclopropane induced some degree of respiratory depression [13]. At similar infusion rates as used in our study, a plateau effect on respiratory depression was observed.…”

Section: Discussionsupporting

confidence: 91%

Improving animal welfare using continuous nalbuphine infusion in a long-term rat model of sepsis

Jeger

Arrigo

Hildenbrand

et al. 2017

ICMx

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BackgroundSepsis research relies on animal models to investigate the mechanisms of the dysregulated host response to infection. Animal welfare concerns request the use of potent analgesics for the Refinement of existing sepsis models, according to the 3Rs principle. Nevertheless, adequate analgesia is often missing, partly because the effects of analgesics in this particular condition are unknown. We evaluated the use of nalbuphine, an opioid with kappa agonistic and mu antagonistic effects, in rats with and without experimental sepsis.MethodsMale Wistar rats were anesthetized with isoflurane and instrumented with a venous line for drug administration. Arterial cannulation allowed for blood pressure measurements and blood sampling in short-term experiments of non-septic animals. Nalbuphine (or placebo) was administered intravenously at a dose of 1 mg/kg/h. Long-term (48 h) experiments in awake septic animals included repetitive clinical scoring with the Rat Grimace Scale and continuous heart rate monitoring by telemetry. Sepsis was induced by intraperitoneal injection of faecal slurry. Nalbuphine plasma levels were measured by liquid chromatography—high resolution mass spectrometry.ResultsIn anesthetized healthy animals, nalbuphine led to a significant reduction of respiratory rate, heart rate, and mean arterial pressure during short-term experiments. In awake septic animals, a continuous nalbuphine infusion did not affect heart rate but significantly improved the values of the Rat Grimace Scale. Nalbuphine plasma concentrations remained stable between 4 and 24 h of continuous infusion in septic rats.ConclusionsIn anaesthetised rats, nalbuphine depresses respiratory rate, heart rate, and blood pressure. In awake animals, nalbuphine analgesia improves animal welfare during sepsis.

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“…Gal and associates also commented that "marked drowsiness and sedation resulted and may provide an advantageous clinical feature, since they were not associated with profound respiratory depression." Our observations, in the light of the findings of Gal et al, suggest that the preceptor mediated effects of nalbuphine, i.e., analgesia and respiratory depression, are overshadowed by K-receptor effects, i.e., somnolence and sedation (5,6).…”

Section: Discussionsupporting

confidence: 55%

A Comparison of Clinical and Psychological Effects of Fentanyl and Nalbuphine in Ambulatory Gynecologic Patients

Garfield

Philip

et al. 1987

Anesthesia & Analgesia

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comparison of clinical and psychological effects of fentanyl and nalbuphine in ambulatory gynecological patients. Anesth Analg 1987;66:1303-7.Drug dosages, length of stay (LOS), and incidence of psychological side effects of fentanyl and nalbuphine were compared in a randomized, double-blind study using unpremedicated female day-surgery patients undergoing diagnostic laparoscopy. Patients receiued either fentanyl 1.5 pglkg ( F group; n = 142), low-dose nalbuphine 300 pglkg (LN group; N = 103), or high-dose nalbuphine 500 pglkg (HN group; n = 41), intravenously (IV) before anesthesia consisting of thiopental, N 2 0 , 02, and a succinylcholine infusion. Additional IV intraoperatiue and IM postoperatizie opioids were given i f required for signs of inadequate anesthesia or postoperative pain. The patients' clinical and psychological status was evaluated at 20-min intervals postoperatizwly by a team of trained interviewers. The low-and high-dose nalbuphine groups clinically resembled the fentanyl group in terms of dosing frequency and patients' self-ratings of postoperatizie analgesia. Length of stay and postoperative sedation were significantly greater with nalbuphine. The incidence of psychological side effects, including dreaming and postoperative anxiety, was also greater with nalbuphine. Howezler, patient acceptance of nalbuphine was high and was similar to that observed in patients gizien fentanyl.Nalbuphine is a mixed agonist-antagonist opioid with an analgesic duration of action of approximately 3-4 hs. In day-surgery patients having brief (30-45 min) procedures under general anesthesia, this 3-4 hr corresponds to the time between beginning of surgery and discharge from the day-surgery unit (DSU). We hypothesized that a single loading dose of nalbuphine, administered intravenously as the narcotic component of a balanced anesthetic technique in patients having a standard gynecologic procedure might result in effective analgesia throughout the entire time in the DSU, wearing off about the time most patients are ready for discharge. Fentanyl, on the other hand, is a short-acting opioid often given repeatedly postoperatively, thereby increasing the risk of respiratory depression. We attempted to determine whether there were significant differences between the two opioids

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Anesthetic Potency of Nalbuphine and Interaction with Morphine in Rats

Cited by 45 publications

References 0 publications

The pharmacokinetics of oral and intravenous nalbuphine in healthy volunteers.

The pharmacokinetics of oral and intravenous nalbuphine in healthy volunteers.

Improving animal welfare using continuous nalbuphine infusion in a long-term rat model of sepsis

A Comparison of Clinical and Psychological Effects of Fentanyl and Nalbuphine in Ambulatory Gynecologic Patients

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