Nalbuphine

Nalbuphine is an agonist at kappa opioid receptors and an antagonist at mµ opioid receptors.

• Nalbuphine Hydrochloride Injection is indicated for the management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate. Nalbuphine Hydrochloride Injection can also be used as a supplement to balanced anesthesia, for preoperative and postoperative analgesia, and for obstetrical analgesia during labor and delivery.

• Nalbuphine Hydrochloride Injection is contraindicated in patients with: Significant respiratory depression [see WARNINGS ] Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment [see WARNINGS ] Known or suspected gastrointestinal obstruction, including paralytic ileus [see WARNINGS ] Hypersensitivity to nalbuphine or to any of the other ingredients in Nalbuphine Hydrochloride Injection.contraindicated

Important Dosage and Administration Instructions Nalbuphine Hydrochloride Injection should be administered as a supplement to general anesthesia only by persons specifically trained in the use of intravenous anesthetics and management of the respiratory effects of potent opioids. Naloxone, resuscitative and intubation equipment, and oxygen should be readily available. Use the lowest effective dosage for the shortest duration of time ‎consistent with individual patient treatment goals [see WARNINGS ]. ‎Because the risk of overdose increases as opioid doses increase, reserve ‎titration to higher doses of Nalbuphine Hydrochloride Injection ‎for patients in whom lower ‎doses are insufficiently effective and in whom the expected benefits of ‎using a higher dose opioid clearly outweigh the substantial risks.‎ There is variability in the opioid analgesic dose and duration needed to ‎adequately manage pain due both to the cause of pain and to individual ‎patient factors. Initiate the dosing regimen for each patient individually, taking into account the patient's severity of pain, patient response, prior analgesic treatment experience, and risk factors for addiction, abuse, and misuse [see WARNINGS ]. Respiratory depression can occur at any time during opioid therapy, ‎especially when initiating and following dosage increases with ‎Nalbuphine Hydrochloride Injection‎.

Life-Threatening Respiratory Depression Serious, life-threatening, or fatal respiratory depression has been reported with the use of opioids, even when used as recommended. Respiratory depression, if not immediately recognized and treated, may lead to respiratory arrest and death. Management of respiratory depression may include close observation, supportive measures, and use of opioid antagonists, depending on the patient's clinical status [see OVERDOSAGE ]. Carbon dioxide (CO 2 ) retention from opioid-induced respiratory depression can exacerbate the sedating effects of opioids. While serious, life-threatening, or fatal respiratory depression can occur at any time during the use of Nalbuphine Hydrochloride Injection, the risk is greatest during the initiation of therapy or following a dosage increase. Monitor patients closely for respiratory depression, especially within the first 24 to 72 hours of initiating therapy with and following dosage increases of Nalbuphine Hydrochloride Injection. To reduce the risk of respiratory depression, proper dosing and titration of Nalbuphine Hydrochloride Injection is essential [see DOSAGE AND ADMINISTRATION ]. Overestimating the Nalbuphine Hydrochloride Injection dosage when converting patients from another opioid product can result in a fatal overdose with the first dose. Opioids can cause sleep-related breathing disorders including central sleep apnea (CSA) and sleep-related hypoxemia. Opioid use increases the risk of CSA in a dose-dependent fashion.

The most frequent adverse reaction in 1066 patients treated in clinical studies with Nalbuphine Hydrochloride Injection was sedation 381 (36%). Less frequent reactions were: sweaty/clammy 99 (9%), nausea/vomiting 68 (6%), dizziness/vertigo 58 (5%), dry mouth 44 (4%), and headache 27 (3%). Other adverse reactions which occurred (reported incidence of 1% or less) were: CNS Effects: Nervousness, depression, restlessness, crying, euphoria, floating, hostility, unusual dreams, confusion, faintness, hallucinations, dysphoria, feeling of heaviness, numbness, tingling, unreality. The incidence of psychotomimetic effects, such as unreality, depersonalization, delusions, dysphoria and hallucinations has been shown to be less than that which occurs with pentazocine. Cardiovascular: Hypertension, hypotension, bradycardia, tachycardia. Gastrointestinal: Cramps, dyspepsia, bitter taste. Respiratory: Depression, dyspnea, asthma. Dermatologic: Itching, burning, urticaria. Miscellaneous: Speech difficulty, urinary urgency, blurred vision, flushing and warmth. Allergic Reactions: Anaphylactic/anaphylactoid and other serious hypersensitivity reactions have been reported following the use of nalbuphine and may require immediate, supportive medical treatment. These reactions may include shock, respiratory distress, respiratory arrest, bradycardia, cardiac arrest, hypotension, or laryngeal edema. Some of these allergic reactions may be life-threatening.

Pregnancy Risk Summary Use of opioid analgesics for an extended period of time during pregnancy may cause neonatal opioid withdrawal syndrome. Available data with Nalbuphine Hydrochloride Injection in pregnant women are insufficient to inform a drug-associated risk for major birth defects and miscarriage. In animal reproduction studies, nalbuphine decreased pup survival and pup body weights when pregnant female rats were treated late in gestation and throughout lactation at 1.7 times the MRHD and when female and male rats treated either prior to mating and throughout gestation and lactation. No malformations were observed in either rats or rabbits at doses 6.1 and 3.9 times the MRHD, respectively [see Data ]. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2–4% and 15–20%, respectively. Clinical Considerations Fetal/Neonatal Adverse Reactions Severe fetal bradycardia has been reported when nalbuphine hydrochloride is administered during labor. Naloxone may reverse these effects. Although there are no reports of fetal bradycardia earlier in pregnancy, it is possible that this may occur.

Metabolism

The onset of action of Nalbuphine Hydrochloride Injection occurs within 2 to 3 minutes after intravenous administration, and in less than 15 minutes following subcutaneous or intramuscular injection. The plasma half-life of nalbuphine is 5 hours, and in clinical studies the duration of analgesic activity has been reported to range from 3 to 6 hours.

Clinical Presentation Acute overdose with Nalbuphine Hydrochloride Injection alone can be manifested by respiratory depression and dysphoria. Acute overdose with Nalbuphine Hydrochloride Injection and other opioids or CNS depressants can be manifested by respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, and, in some cases, pulmonary edema, bradycardia, hypotension, hypoglycemia, partial or complete airway obstruction, atypical snoring, and death. Marked mydriasis rather than miosis may be seen with hypoxia in overdose situations. Treatment of Overdose In case of overdose, priorities are the reestablishment of a patent and protected airway and institution of assisted or controlled ventilation, if needed. Employ other supportive measures (including oxygen and vasopressors) in the management of circulatory shock and pulmonary edema as indicated. Cardiac arrest or arrhythmias will require advanced life-support measures. The opioid antagonists, naloxone or nalmefene, are specific antidotes to respiratory depression resulting from opioid overdose.

• Feb 3, 1989ANDAANDA070914Hospira
• Feb 3, 1989ANDAANDA070915Hospira
• Feb 3, 1989ANDAANDA070916Hospira
• Feb 3, 1989ANDAANDA070918Hospira
• Sep 19, 2024ANDAANDA216049Somerset Theraps Llc
• Sep 19, 2024ANDAANDA216050Somerset Theraps Llc

1. 1Drug Hypersensitivity3616%
2. 2Off Label Use167.3%
3. 3Drug Ineffective115.0%
4. 4Foetal Exposure During Pregnancy104.5%
5. 5Neonatal Asphyxia104.5%
6. 6Neonatal Epileptic Seizure104.5%
7. 7Pain73.2%
8. 8Pancreatitis Acute73.2%
9. 9Acute Hepatic Failure62.7%
10. 10Encephalopathy62.7%
11. 11Product Package Associated Injury62.7%
12. 12Product Use In Unapproved Indication62.7%
13. 13Pruritus62.7%
14. 14Pyrexia62.7%
15. 15Drug Interaction52.3%

Recent PubMed references pinned to Nalbuphine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Intraoperative remimazolam-nalbuphine infusion reduces visceral traction response during cesarean delivery: a randomised trial.
  BMC anesthesiology · 2026 · Meng J, Deng XS, Han R, et al.
  PMID 42151802DOI 10.1186/s12871-026-03909-6
• Efficacy and safety of extended-release dinalbuphine sebacate in a multimodal analgesic regimen following cesarean section: A prospective observational study.
  Taiwanese journal of obstetrics & gynecology · 2026 · Hou PH, Chung SM, Huang JY, et al.
  PMID 42036188DOI 10.1016/j.tjog.2026.02.003
• The Effects of Different Doses of Nalbuphine and Esketamine on Prevention of Emergence Agitation in Preschool Children Undergoing Tonsillectomy and Adenoidectomy: A Randomized Clinical Trial.
  Drug design, development and therapy · 2026 · Zou Z, Guo H, Xu T, et al.
  PMID 42007395DOI 10.2147/DDDT.S597263
• Nalbuphine as a Bridge to Delayed Epidural Analgesia: A Randomized Trial on First-Stage Labor Duration.
  Drug design, development and therapy · 2026 · Xu Y, Song C, Xu Y, et al.
  PMID 41908949DOI 10.2147/DDDT.S574810
• Appropriate Combination of Nalbuphine Combined With Esketamine for Weakly Opioid Anesthesia in Postlaparoscopic Cholecystectomy Analgesia: A Randomized Controlled Trial.
  Pain research & management · 2026 · Zhang M, Wu H, Zheng H, et al.
  PMID 41788429DOI 10.1155/prm/5086518
• Comparison of Ciprofol-Nalbuphine and Propofol-Nalbuphine Sedation During Painless Gastrointestinal Endoscopy: A Randomized Controlled Trial.
  Medical science monitor : international medical journal of experimental and clinical research · 2026 · Zhang Z, Jiang W, Zheng L, et al.
  PMID 41580889DOI 10.12659/MSM.951195
• Oral Nalbuphine in Idiopathic Pulmonary Fibrosis-Associated Cough: The CORAL Randomized Clinical Trial.
  JAMA · 2026 · Molyneaux PL, Mogulkoc N, Gunen H, et al.
  PMID 41569557DOI 10.1001/jama.2025.26179
• Comparison of effects of 0.5 % levobupivacaine with buprenorphine and nalbuphine in ultrasound-guided supraclavicular brachial plexus block- A Randomised Control Trial.
  F1000Research · 2025 · Podder S, Shetty D, Sinha S, et al.
  PMID 41509102DOI 10.12688/f1000research.164457.2

The 10 most recently updated of 160 ClinicalTrials.gov registrations naming Nalbuphine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• COMPARISON OF AIRWAY NERVE BLOCK VERSUS NEBULIZED LIDOCAINE ON HEMODYNAMIC RESPONSES DURING AWAKE FIBEROPTIC INTUBATION
  Not yet recruiting · Interventional · 80 enrolled · Mayo Hospital Lahore
  NCT07627100updated 2026-06-04
• Study of PHN131 in Healthy Volunteers
  Completed · Observational · 16 enrolled · PhytoHealth Corporation
  NCT02192151updated 2026-06-01
• Study of PHN131 in Patients After Surgery
  Completed · Phase 2 · Phase 3 · Interventional · 106 enrolled · PhytoHealth Corporation
  NCT02193620updated 2026-06-01
• FASCIA ILIACA BLOCK VERSUS INTRAVENOUS NALBUPHINE AS ANALGESIC METHOD BEFORE POSITIONING FOR SPINAL ANESTHESIA IN PATIENTS UNDERGOING SURGERY FOR HIP FRACTURES
  Active not recruiting · Phase 4 · Interventional · 30 enrolled · Liaquat National Hospital & Medical College
  NCT07613801updated 2026-05-29
• Analgesia Comparison of Nalbuphine and Morphine for Laparoscopic Myomectomy
  Completed · Phase 4 · Interventional · 80 enrolled · Peking University First Hospital
  NCT03288428updated 2026-05-19
• Spinal Nalbuphine for Analgesia in Total Hip Arthroplasty
  Completed · Phase 2 · Interventional · 60 enrolled · Asklepieion Voulas General Hospital
  NCT06577155updated 2026-05-12
• Comparison of Two Drugs ,i.e., Nalbuphine Vs Ketamine at Low Doses for the Peri-Operative Shivering Control in Patients Undergoing Gynaecological Surgery Under Spinal Anaesthesia
  Completed · Interventional · 90 enrolled · Sargodha Medical College
  NCT07543913updated 2026-04-22
• Exploring the Impact of Genetic Variations on The Clinical Efficacy of Nalbuphine in Postoperative Pain Management
  Recruiting · Phase 2 · Phase 3 · Interventional · 263 enrolled · Dr. Asma Abdus Salam
  NCT06996561updated 2026-04-15
• NAL ER IPF Respiratory Function and Safety Study
  Recruiting · Phase 1 · Interventional · 10 enrolled · Trevi Therapeutics
  NCT07036029updated 2026-04-09
• Pharmacokinetics, Pharmacodynamics, and Safety Profile of Understudied Drugs Administered to Children Per Standard of Care (POPS)
  Recruiting · Observational · 5,000 enrolled · Duke University
  NCT04278404updated 2026-04-06

Frequently asked questions

How does Nalbuphine work?

Nalbuphine is an agonist at kappa opioid receptors and an antagonist at mµ opioid receptors.

What is Nalbuphine used for?

According to FDA labeling, Nalbuphine carries indications including: Nalbuphine Hydrochloride Injection is indicated for the management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate. Nalbuphine Hydrochloride Injection can also be used as a supplement to balanced anesthesia, for preoperative and postoperative analgesia, and for obstetrical analgesia during labor and delivery.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Nalbuphine?

Nalbuphine is classified as Morphinan derivatives, Opioid Agonist/Antagonist, Competitive Opioid Antagonists, Opioid Agonists, Partial Opioid Agonists, Analgesia, Decreased Organized Electrical Activity.

What are the contraindications for Nalbuphine?

Nalbuphine labeling lists contraindications including: Nalbuphine Hydrochloride Injection is contraindicated in patients with: Significant respiratory depression [see WARNINGS ] Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment [see WARNINGS ] Known or suspected gastrointestinal obstruction, including paralytic ileus [see WARNINGS ] Hypersensitivity to nalbuphine or to any of the other ingredients in Nalbuphine Hydrochloride Injection.. Always consult the full prescribing information and a clinician.