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Article ; Online: Nalbuphine

Maxim Logash / Petro Pokotylo / Bożena Zboina / Renata B. Stępień

Studia Medyczne, Vol 33, Iss 2, Pp 146-

some aspects of the research and applications

2017 Volume 154

Abstract: Nalbuphine hydrochloride is a synthetic, non-scheduled opioid agonist/antagonist analgesic, widely ... used across different branches of medicine. Despite the fact that nalbuphine has been used ... the increase of non-medical use of nalbuphine. Moreover, in some countries it was placed in list ...

Abstract	Nalbuphine hydrochloride is a synthetic, non-scheduled opioid agonist/antagonist analgesic, widely used across different branches of medicine. Despite the fact that nalbuphine has been used in the clinical setting for more than 40 years, there is still a lot of controversy regarding its mechanism of action and side-effects, including the development of the addiction to the drug. Recent data demonstrated the increase of non-medical use of nalbuphine. Moreover, in some countries it was placed in list of psychotropic and addictive substances. The increasing popularity of nalbuphine led us to review and analyse the data regarding both clinical and non-clinical applications of the drug. Furthermore, we performed an extensive analysis regarding available experimental models and approaches used in the research of opioid substances. Despite a set of problems in clinical settings due to the opioid nature of nalbuphine, it belongs to an indispensable group of analgesics for pain control.
Keywords	addiction ; experimental model ; nalbuphine ; Medicine ; R
Language	English
Publishing date	2017-06-01T00:00:00Z
Publisher	Termedia Publishing House
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Intrathecal nalbuphine

Kaushal, Sankalp / Kamlakar, Maya / Baburao, Jamale Parbati

Medical gas research

2021 Volume 11, Issue 4, Page(s) 126–130

Abstract: This study aimed to compare the efficacy of intrathecal nalbuphine and buprenorphine as an adjuvant ... nalbuphine group which received 0.5 mL (0.8 mg) of nalbuphine with 3 mL of heavy (0.5%) hyperbaric ... comparable between nalbuphine and buprenorphine groups. The duration of sensory block in the buprenorphine ...

Abstract	This study aimed to compare the efficacy of intrathecal nalbuphine and buprenorphine as an adjuvant to heavy bupivacaine (0.5%) for spinal anesthesia in lower limb orthopedic surgeries to improve the quality of spinal anesthesia (onset, duration, and side effects) and prolongation of postoperative analgesia. Sixty patients were recruited into this single-centered, double-blinded, hospital-based, prospective, comparative study conducted in 2017-2018. They were randomly and equally (n = 30) allocated into two groups: nalbuphine group which received 0.5 mL (0.8 mg) of nalbuphine with 3 mL of heavy (0.5%) hyperbaric bupivacaine and buprenorphine group which received 0.5 mL (60 mg) of buprenorphine with 3 mL of heavy hyperbaric bupivacaine. Intraoperatively, onset and duration of blockade (motor and sensory), and time for first dose of rescue analgesia were recorded in both groups at regular intervals. Heart rate, blood pressure, Visual Analogue Scale score and side effects were also recorded postoperatively for 12 hours. The demographic parameters, time of onset of sensory block and motor block, and duration of motor block were comparable between nalbuphine and buprenorphine groups. The duration of sensory block in the buprenorphine group was longer than in the nalbuphine group. Time to the first dose of rescue analgesia was delayed in buprenorphine group as compared to nalbuphine group. In both groups maximum patients achieved maximum height of sensory block at 90 minutes. There were significant differences in the mean heart rate and blood pressure between buprenorphine and nalbuphine groups. Nalbuphine group patients achieved a Visual Analogue Scale score > 4 earlier as compared to buprenorphine group. Few side effects were observed in both groups. Intrathecal buprenorphine is a better adjuvant to 0.5% bupivacaine in the spinal anesthesia for lower limb orthopedic surgeries, as it provides longer sensory block and delayed administration of first dose of rescue analgesia with negligible side-effects. The study was approved by Institutional Ethics Committee of Krishna Institute of Medical Sciences (approval number: KIMSDU/IEC/03/2017) on November 23, 2017.
MeSH term(s)	Anesthetics, Local/adverse effects ; Buprenorphine/adverse effects ; Double-Blind Method ; Humans ; Lower Extremity/surgery ; Nalbuphine ; Orthopedic Procedures ; Prospective Studies
Chemical Substances	Anesthetics, Local ; Buprenorphine (40D3SCR4GZ) ; Nalbuphine (L2T84IQI2K)
Language	English
Publishing date	2021-07-02
Publishing country	Australia
Document type	Journal Article ; Randomized Controlled Trial
ZDB-ID	2616230-1
ISSN	2045-9912 ; 2045-9912
ISSN (online)	2045-9912
ISSN	2045-9912
DOI	10.4103/2045-9912.318856
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Article: Nalbuphine.

Schmidt, W K / Tam, S W / Shotzberger, G S / Smith, D H / Clark, R / Vernier, V G

Drug and alcohol dependence

1985 Volume 14, Issue 3-4, Page(s) 339–362

Abstract: Nalbuphine is a potent analgesic with a low side effect and dependence profile in animals and man ... Nalbuphine is distinguished from other agonist/antagonist analgesics in having greater antagonist activity ... At equi-analgesic doses, nalbuphine is quantitatively similar to nalorphine in regard to its large ratio ...

Abstract	Nalbuphine is a potent analgesic with a low side effect and dependence profile in animals and man. Nalbuphine is distinguished from other agonist/antagonist analgesics in having greater antagonist activity and fewer behavioral effects at analgesic doses than pentazocine, butorphanol or buprenorphine. At equi-analgesic doses, nalbuphine is quantitatively similar to nalorphine in regard to its large ratio of antagonist to analgetic activity. Clinical studies have confirmed this balance of strong antagonist to analgesic activity. Nalbuphine has been shown to effectively antagonize the respiratory depressant activity of narcotic analgesics while concomitantly adding to their analgetic responses. Unlike nalorphine or pentazocine, nalbuphine produces few overt behavioral or autonomic effects in animals at doses over 300 times its analgesic range. These findings are confirmed by clinical results which show that nalbuphine produces few psychotomimetic effects, even at elevated dose levels, in contrast to nalorphine or pentazocine. Nalbuphine produces limited respiratory depression in animals and in man. Significant cardiovascular effects have not been found. Nalbuphine was found to produce significantly less inhibition of gastrointestinal activity than any of the clinically useful narcotic or agonist/antagonist analgesics tested in animals. Nalbuphine's analgetic effects are reversed by naloxone doses similar to those which reverse nalorphine's agonist effects. Results in this and other tests suggest that nalbuphine is primarily a kappa-agonist/mu-antagonist analgesic. Unlike pentazocine or buprenorphine, nalbuphine does not suppress the narcotic abstinence syndrome in partly-withdrawn morphine-dependent animals or man. Rather, due to nalbuphine's strong antagonist activity, analgesic-range doses of nalbuphine severely exacerbate the withdrawal syndrome in partly-withdrawn mice, monkeys and humans. Nalbuphine also precipitates a strong abstinence response in non-withdrawn morphine-dependent animals and man. In post-addict humans, analgesic-range doses of nalbuphine are perceived as minimally morphine-like, but higher doses are judged to be progressively more nalorphine-like (i.e. dysphoric), which further limits nalbuphine's abuse potential in drug-seeking individuals. Primary dependence studies have demonstrated that physical dependence is possible at high dose levels that produce marked side effects. Other studies show that dependence is unlikely to be of significance within nalbuphine's usual analgesic range. Six-month studies in patients with chronic pain have confirmed that analgesic tolerance or physical dependence is uncommon.(ABSTRACT TRUNCATED AT 400 WORDS)
MeSH term(s)	Analgesics/pharmacology ; Animals ; Chemical Phenomena ; Chemistry ; Depression, Chemical ; Discrimination (Psychology) ; Dogs ; Guinea Pigs ; Haplorhini ; Humans ; Mice ; Morphinans/pharmacology ; Morphine/adverse effects ; Nalbuphine/adverse effects ; Nalbuphine/pharmacology ; Nalbuphine/therapeutic use ; Naloxone/antagonists & inhibitors ; Rabbits ; Rats ; Receptors, Opioid/drug effects ; Receptors, Opioid, kappa ; Receptors, Opioid, mu ; Respiration/drug effects ; Self Administration ; Sleep Stages/drug effects ; Substance Withdrawal Syndrome/etiology ; Substance-Related Disorders/etiology
Chemical Substances	Analgesics ; Morphinans ; Receptors, Opioid ; Receptors, Opioid, kappa ; Receptors, Opioid, mu ; Naloxone (36B82AMQ7N) ; Morphine (76I7G6D29C) ; Nalbuphine (L2T84IQI2K)
Language	English
Publishing date	1985-02
Publishing country	Ireland
Document type	Journal Article ; Review
ZDB-ID	519918-9
ISSN	1879-0046 ; 0376-8716
ISSN (online)	1879-0046
ISSN	0376-8716
DOI	10.1016/0376-8716(85)90066-3
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Article ; Online: Nalbuphine Tablets for Cough in Patients with Idiopathic Pulmonary Fibrosis.

Maher, Toby M / Avram, Cristina / Bortey, Enoch / Hart, Simon P / Hirani, Nikhil / Molyneux, Philip L / Porter, Joanna C / Smith, Jaclyn A / Sciascia, Thomas

NEJM evidence

2023 Volume 2, Issue 8, Page(s) EVIDoa2300083

Abstract: Nalbuphine for Cough with Idiopathic Pulmonary FibrosisIn patients ... controlled, crossover trial, extended-release nalbuphine (NAL ER), an opioid agonist-antagonist, was compared ...

Abstract	Nalbuphine for Cough with Idiopathic Pulmonary FibrosisIn patients with idiopathic pulmonary fibrosis, cough may have a negative impact on daily life. In a randomized, 22-day treatment period, placebo-controlled, crossover trial, extended-release nalbuphine (NAL ER), an opioid agonist-antagonist, was compared to placebo for cough control and adverse effects. During active treatment there was a 75.1% reduction in daytime objective cough frequency compared with 22.6% in the placebo treatment period. Nausea, fatigue, constipation, and dizziness were more common with NAL ER than with placebo.
MeSH term(s)	Humans ; Nalbuphine ; Analgesics, Opioid ; Cough/chemically induced ; Idiopathic Pulmonary Fibrosis/chemically induced ; Tablets/therapeutic use
Chemical Substances	Nalbuphine (L2T84IQI2K) ; Analgesics, Opioid ; Tablets
Language	English
Publishing date	2023-05-22
Publishing country	United States
Document type	Randomized Controlled Trial ; Journal Article
ISSN	2766-5526
ISSN (online)	2766-5526
DOI	10.1056/EVIDoa2300083
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Article ; Online: Effects of nalbuphine on the cardiotoxicity of ropivacaine in rats.

Wang, Chenran / Sun, Shen / Jiao, Jing / Yu, Xinhua / Huang, Shaoqiang

Fundamental & clinical pharmacology

2022 Volume 36, Issue 5, Page(s) 811–817

Abstract: When combined with nalbuphine, local anesthetics show a longer duration of nerve block ... without increasing complications. However, no evidence is available concerning the effect of nalbuphine ... on the cardiotoxicity of local anesthetics. The objective of this work is to investigate whether nalbuphine pretreatment ...

Abstract	When combined with nalbuphine, local anesthetics show a longer duration of nerve block without increasing complications. However, no evidence is available concerning the effect of nalbuphine on the cardiotoxicity of local anesthetics. The objective of this work is to investigate whether nalbuphine pretreatment can increase the lethal dose threshold of ropivacaine in rats. Anesthetized Sprague Dawley rats were pretreated with different doses of nalbuphine (0.4, 0.8, 1.5, 3.0, 5.0 mg/kg) or NS (normal saline, negative control) or 30% LE (lipid emulsion, positive control) 2 ml/kg/min for 5 min (n = 6). Then 0.5% ropivacaine was infused at a rate of 2.5 mg/kg/min until asystole occurs. Time of arrhythmia, 50% mean arterial pressure- and 50% heart rate-reduction, and asystole were recorded, and ropivacaine doses were calculated. Nalbuphine (0.4-5.0 mg/kg) did not affect ropivacaine-induced arrhythmia, 50% mean arterial pressure-reduction and 50% heart rate-reduction, and asystole in rats compared with NS pre-treatment. The asystole dose threshold (in milligrams per kilogram) of group LE was higher than that of group NS (NS 28.25(6.32) vs. LE, 41.58(10.65); P = 0.04; 95% confidence interval 0.23 to 26.45), while thresholds of arrhythmia, 50% mean arterial pressure-reduction, and 50% heart rate-reduction were not affected by LE. Nalbuphine doses of 0.4-5.0 mg/kg pretreatment did not increase the threshold of ropivacaine cardiotoxicity compared with NS control; 30% LE increases the lethal dose threshold of ropivacaine in rats.
MeSH term(s)	Amides/toxicity ; Anesthetics, Local/toxicity ; Animals ; Arrhythmias, Cardiac/chemically induced ; Bupivacaine ; Cardiotoxicity/etiology ; Heart Arrest/chemically induced ; Nalbuphine/toxicity ; Rats ; Rats, Sprague-Dawley ; Ropivacaine/toxicity
Chemical Substances	Amides ; Anesthetics, Local ; Ropivacaine (7IO5LYA57N) ; Nalbuphine (L2T84IQI2K) ; Bupivacaine (Y8335394RO)
Language	English
Publishing date	2022-04-09
Publishing country	England
Document type	Journal Article
ZDB-ID	639134-5
ISSN	1472-8206 ; 0767-3981
ISSN (online)	1472-8206
ISSN	0767-3981
DOI	10.1111/fcp.12778
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Article ; Online: Nalbuphine #381.

Mathai, Fay / Portugal, Frank / Mehta, Zankhana / Davis, Mellar

Journal of palliative medicine

2019 Volume 22, Issue 11, Page(s) 1471–1472

MeSH term(s)	Analgesics, Opioid/administration & dosage ; Analgesics, Opioid/metabolism ; Analgesics, Opioid/pharmacology ; Analgesics, Opioid/therapeutic use ; Humans ; Nalbuphine/administration & dosage ; Nalbuphine/metabolism ; Nalbuphine/pharmacology ; Nalbuphine/therapeutic use
Chemical Substances	Analgesics, Opioid ; Nalbuphine (L2T84IQI2K)
Language	English
Publishing date	2019-10-28
Publishing country	United States
Document type	Journal Article
ZDB-ID	1427361-5
ISSN	1557-7740 ; 1096-6218
ISSN (online)	1557-7740
ISSN	1096-6218
DOI	10.1089/jpm.2019.0482
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Article ; Online: Effect of nalbuphine on rocuronium injection pain.

Huang, Wenfang / Huang, Jinjin / Wang, Dongpi / Hu, Yaoqin / Wang, Jiangmei / Lin, Hongfei

World journal of pediatric surgery

2021 Volume 4, Issue 3, Page(s) e000249

Abstract: ... induction of anesthesia. The aim of this study was to systematically evaluate the benefits of nalbuphine ... nalbuphine group (group N). Routine 0.1 mg/kg midazolam and 2 mg/kg propofol were injected intravenously ... of saline, lidocaine (10 mg/mL), or nalbuphine hydrochloride (2 mg/mL), respectively, at a dosage of 0.1 mL ...

Abstract	Objective: Rocuronium-associated intravenous injection pain occurs frequently in children during induction of anesthesia. The aim of this study was to systematically evaluate the benefits of nalbuphine in patients with rocuronium-associated injection pain. Methods: Ninety children undergoing tonsillectomy and adenoidectomy in our hospital between October 2019 and September 2020 were randomly divided into the following groups, with 30 patients per group: control group (group C), lidocaine group (group L), and nalbuphine group (group N). Routine 0.1 mg/kg midazolam and 2 mg/kg propofol were injected intravenously. After sedation, children in group C, group L, and group N were administered an intravenous injection of saline, lidocaine (10 mg/mL), or nalbuphine hydrochloride (2 mg/mL), respectively, at a dosage of 0.1 mL/kg. Intravenous injection of rocuronium stock solution (0.6 mg/kg) was administered 2 minutes later. Pain was evaluated using Ambeshs 4-pointscale. The incidence of rocuronium injection pain was compared among the three groups, and postoperative adverse reactions, such as drowsiness, bradycardia, hypotension, and respiratory depression, were evaluated. Results: The incidence of injection pain among children in group N was significantly lower than that in group C and group L (p<0.05). The incidence of drowsiness in group N was significantly higher than that in the other groups (p<0.05). The incidences of hypotension, bradycardia, and respiratory depression were not significantly different among the three groups (p>0.05). Conclusions: Intravenous nalbuphine during induction of anesthesia effectively prevented rocuronium-associated injection pain in children. Drowsiness is a complication.
Language	English
Publishing date	2021-05-27
Publishing country	England
Document type	Journal Article
ISSN	2516-5410
ISSN (online)	2516-5410
DOI	10.1136/wjps-2020-000249
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Article: Effective Doses of Nalbuphine Combined with Propofol in Painless Hysteroscopy.

Zhong, Weiwei / Chen, Chen / Tang, Weixiang

International journal of general medicine

2022 Volume 15, Page(s) 5609–5614

Abstract: Purpose: Nalbuphine is becoming a common analgesic used in hysteroscopic operations. The aim ... of this study was to identify the median effective dose (ED50) and 95% effective dose (ED95) of nalbuphine ... for painless hysteroscopy were recruited. The initial dose of nalbuphine was set at 0.15 mg/kg and varied by 0 ...

Abstract	Purpose: Nalbuphine is becoming a common analgesic used in hysteroscopic operations. The aim of this study was to identify the median effective dose (ED50) and 95% effective dose (ED95) of nalbuphine combined with propofol in painless hysteroscopy. Patients and methods: Twenty-five patients aged 18-60 years with an American Society of Anesthesiologists classification of I-II who were scheduled for painless hysteroscopy were recruited. The initial dose of nalbuphine was set at 0.15 mg/kg and varied by 0.01 mg/kg according to the Dixon sequential method. The ED50/ED95 of nalbuphine combined with propofol for hysteroscopy was calculated by the probit method. Results: The ED50 of nalbuphine was 0.122 (95% confidence interval (CI) 0.092-0.137) mg/kg, and the ED95 of nalbuphine was 0.153 (95% CI 0.138-0.361) mg/kg. Conclusion: The ED50/ED95 values of nalbuphine combined with propofol in painless hysteroscopy are 0.122 mg/kg and 0.153 mg/kg, respectively. Nalbuphine at 0.153 mg/kg combined with propofol is effective and safe for painless hysteroscopy.
Language	English
Publishing date	2022-06-11
Publishing country	New Zealand
Document type	Journal Article
ZDB-ID	2452220-X
ISSN	1178-7074
ISSN	1178-7074
DOI	10.2147/IJGM.S367449
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Article ; Online: Pharmacodynamics and pharmacokinetics of nalbuphine in xylazine‑sedated horses.

Hammad, Amal / Gadallah, Shaaban / Misk, Tarek / Sharshar, Ahmed / Thabet, Nahed / Mourad, Ahmed

Veterinaria italiana

2022 Volume 58, Issue 3

Abstract: This study describes the selected pharmacodynamics and pharmacokinetics of nalbuphine (NAL ...

Abstract	This study describes the selected pharmacodynamics and pharmacokinetics of nalbuphine (NAL) in xylazine (XYL)‑sedated horses. Five adult healthy horses were randomly received 2 treatments at a 1‑week interval; XYL treatment (0.55 mg/kg IV) and XYL/NAL treatment (XYL, 0.55 mg/kg IV; NAL, 0.3 mg/kg IV). The measured pharmacodynamic variables were sedative and analgesic effects and the effect on ataxia and some physiological parameters. for the pharmacokinetics of NAL, its plasma concentrations were measured using HPLC and a 2‑compartment analysis was performed. Greater and prolonged sedation was evident after XYL/NAL treatment compared with XYL treatment. Slightly improved and prolonged analgesia was demonstrated after XYL/NAL treatment. Significant changes in blood pressure and respiratory rate lasted for a shorter duration with XYL/NAL treatment than with XYL treatment. After XYL treatment, rectal temperature was significantly different from baseline and XYL/NAL treatment. Elimination half‑life of NAL was 3.47 ± 1.39 hours and total body clearance was 2.88 ± 0.73 L/kg/hour. In conclusion, addition of NAL to XYL resulted in remarkable advantages on the measured parameters. The obtained pharmacokinetics of NAL could be useful in determining the effective NAL infusion rate, which could be further evaluated as an adjunctive agent to XYL for prolonged sedation in horses.
MeSH term(s)	Animals ; Horses ; Xylazine ; Nalbuphine
Chemical Substances	Xylazine (2KFG9TP5V8) ; Nalbuphine (L2T84IQI2K)
Language	English
Publishing date	2022-12-31
Publishing country	Italy
Document type	Journal Article
ZDB-ID	2536397-9
ISSN	1828-1427 ; 0505-401X
ISSN (online)	1828-1427
ISSN	0505-401X
DOI	10.12834/VetIt.2408.16506.1
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Article ; Online: Immobilization of Raccoons (Procyon lotor) with Nalbuphine, Medetomidine, and Azaperone.

Doub, Emily E / Thompson, Alec T / Korns, Avery L / Cleveland, Christopher A / Yabsley, Michael J / Ruder, Mark G

Journal of wildlife diseases

2023 Volume 59, Issue 3, Page(s) 520–523

Abstract: ... handling of animals. A combination of nalbuphine (40 mg/mL), azaperone (10 mg/mL), and medetomidine (10 mg ... nalbuphine, 3 mg medetomidine, and 3 mg azaperone, regardless of body weight). After administration, time ...

Abstract	Chemical immobilization is widely used by wildlife and veterinary professionals for the safe handling of animals. A combination of nalbuphine (40 mg/mL), azaperone (10 mg/mL), and medetomidine (10 mg/mL), known as NAM, is a low-volume combination with field immobilization practicality and fewer regulations restricting its use in the US than some other drug combinations. We evaluated the safety and effectiveness of NAM as an immobilizing agent for raccoons (Procyon lotor). From May 2021 to February 2022, 16 adult raccoons were captured in cage traps and immobilized with 0.3 mL NAM intramuscularly (12 mg nalbuphine, 3 mg medetomidine, and 3 mg azaperone, regardless of body weight). After administration, time to sedation was measured; body temperature, heart rate, respiratory rate, and oxygen saturation were monitored and recorded every 5 min for 20 min. Each raccoon was weighed; the dose administered was calculated (range 2.2-4.1 mg/kg, mean 3 mg/kg). Mean induction time was 6 min (4-17 min); time to recovery following administration of 15 mg atipamezole, 7.5 mg naltrexone for reversal, was 10 min (6-18 min). Heart rate, oxygen saturation, and respiration rate remained steady during immobilization. Rectal temperature steadily declined. Overall, NAM appeared to be a practical option for raccoon immobilization, providing rapid induction and reversal as well as adequate sedation for short-term handling and minimally invasive sampling.
MeSH term(s)	Animals ; Medetomidine/pharmacology ; Azaperone/pharmacology ; Raccoons ; Nalbuphine/pharmacology ; Hypnotics and Sedatives/pharmacology ; Immobilization/veterinary ; Heart Rate
Chemical Substances	Medetomidine (MR15E85MQM) ; Azaperone (19BV78AK7W) ; Nalbuphine (L2T84IQI2K) ; Hypnotics and Sedatives
Language	English
Publishing date	2023-05-08
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, Non-P.H.S.
ZDB-ID	410709-3
ISSN	1943-3700 ; 0090-3558
ISSN (online)	1943-3700
ISSN	0090-3558
DOI	10.7589/JWD-D-22-00159
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