Nalbuphine
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Chetan Lokhande, M.B.B.S [2]
Disclaimer
WikiDoc MAKES NO GUARANTEE OF VALIDITY. WikiDoc is not a professional health care provider, nor is it a suitable replacement for a licensed healthcare provider. WikiDoc is intended to be an educational tool, not a tool for any form of healthcare delivery. The educational content on WikiDoc drug pages is based upon the FDA package insert, National Library of Medicine content and practice guidelines / consensus statements. WikiDoc does not promote the administration of any medication or device that is not consistent with its labeling. Please read our full disclaimer here.
Overview
Nalbuphine is an analgesic opioid that is FDA approved for the {{{indicationType}}} of general anesthesia; Adjunct, pain (moderate to severe), pain (moderate to severe), including preoperative, postoperative, and obstetrical analgesia.. Common adverse reactions include dermatologic: diaphoresis (up to 9% ), gastrointestinal: nausea and vomiting (6% ), xerostomia (4% ), neurologic: dizziness (up to 5% ), headache (3% ), sedated (36% ), vertigo (up to 5% ).
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
- General anesthesia; Adjunct: induction, 0.3-3 mg/kg IV over 10-15 min.
- General anesthesia; Adjunct: maintenance, 0.25-0.5 mg/kg in single IV administrations, as needed.
- Pain (Moderate to Severe): 10 mg subQ, IM or IV for a 70 kg individual repeated every 3 Bold textto 6 hours as needed; max single dose is 20 mg/dose; MAX total daily dose is 160 mg/day.
* Pain (Moderate to Severe), Including preoperative, postoperative, and obstetrical analgesia: 10 mg subQ, IM or IV for a 70 kg individual repeated every 3 to 6 hours as needed; max single dose is 20 mg/dose; MAX total daily dose is 160 mg/day.
- Shivering, Postanesthesia: 0.08 mg/kg IV
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information about Off-Label Guideline-Supported Use of Nalbuphine in adult patients.
Non–Guideline-Supported Use
There is limited information about Off-Label Non–Guideline-Supported Use of Nalbuphine in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
- Safety and effectiveness not established in patients under 18 years of age
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information about Off-Label Guideline-Supported Use of Nalbuphine in pediatric patients.
Non–Guideline-Supported Use
There is limited information about Off-Label Non–Guideline-Supported Use of Nalbuphine in pediatric patients.
Contraindications
Nalbuphine hydrochloride injection should not be administered to patients who are hypersensitive to nalbuphine hydrochloride, or to any of the other ingredients in nalbuphine hydrochloride injection.
Warnings
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 respiratory effects of potent opioids.
Naloxone hydrochloride injection, resuscitative and intubation equipment and oxygen should be readily available.
Drug Abuse
Caution should be observed in prescribing nalbuphine for emotionally unstable patients, or for individuals with a history of opioid abuse. Such patients should be closely supervised when long term therapy is contemplated (see DRUG ABUSE AND DEPENDENCE).
Use in Ambulatory Patients
Nalbuphine may impair the mental or physical abilities required for the performance of potentially dangerous tasks such as driving a car or operating machinery. Therefore, nalbuphine hydrochloride injection should be administered with caution to ambulatory patients who should be warned to avoid such hazards.
Use in Emergency Procedures
Maintain patient under observation until recovered from nalbuphine effects that would affect driving or other potentially dangerous tasks.
Use in Pregnancy (Other Than Labor)
Severe fetal bradycardia has been reported when nalbuphine 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. This drug should be used in pregnancy only if clearly needed, if the potential benefit outweighs the risk to the fetus, and if appropriate measures such as fetal monitoring are taken to detect and manage any potential adverse effect on the fetus.
Use During Labor and Delivery
The placental transfer of nalbuphine is high, rapid, and variable with a maternal to fetal ratio ranging from 1:0.37 to 1:6. Fetal and neonatal adverse effects that have been reported following the administration of nalbuphine to the mother during labor include fetal bradycardia, respiratory depression at birth, apnea, cyanosis, and hypotonia. Some of these events have been life-threatening. Maternal administration of naloxone during labor has normalized these effects in some cases. Severe and prolonged fetal bradycardia has been reported. Permanent neurological damage attributed to fetal bradycardia has occurred. A sinusoidal fetal heart rate pattern associated with the use of nalbuphine has also been reported. Nalbuphine should be used during labor and delivery only if clearly indicated and only if the potential benefit outweighs the risk to the infant. Newborns should be monitored for respiratory depression, apnea, bradycardia and arrhythmias if nalbuphine has been used.
Head Injury and Increased Intracranial Pressure
The possible respiratory depressant effects and the potential of potent analgesics to elevate cerebrospinal fluid pressure (resulting from vasodilation following CO2 retention) may be markedly exaggerated in the presence of head injury, intracranial lesions or a pre-existing increase in intracranial pressure. Furthermore, potent analgesics can produce effects which may obscure the clinical course of patients with head injuries. Therefore, nalbuphine hydrochloride injection should be used in these circumstances only when essential, and then should be administered with extreme caution.
Impaired Respiration: At the usual adult dose of 10 mg/70 kg, nalbuphine hydrochloride causes some respiratory depression approximately equal to that produced by equal doses of morphine. However, in contrast to morphine, respiratory depression is not appreciably increased with higher doses of nalbuphine. Respiratory depression induced by nalbuphine can be reversed by naloxone hydrochloride when indicated. Nalbuphine hydrochloride injection should be administered with caution at low doses to patients with impaired respiration (e.g., from other medication, uremia, bronchial asthma, severe infection, cyanosis or respiratory obstructions).
Impaired Renal or Hepatic Function: Because nalbuphine is metabolized in the liver and excreted by the kidneys, nalbuphine hydrochloride should be used with caution in patients with renal or liver dysfunction and administered in reduced amounts.
Myocardial Infarction: As with all potent analgesics, nalbuphine hydrochloride should be used with caution in patients with myocardial infarction who have nausea or vomiting.
Biliary Tract Surgery: As with all opioid analgesics, nalbuphine hydrochloride should be used with caution in patients about to undergo surgery of the biliary tract since it may cause spasm of the sphincter of Oddi.
Cardiovascular System: During evaluation of nalbuphine hydrochloride injection, in anesthesia, a higher incidence of bradycardia has been reported in patients who did not receive atropine pre-operatively.
Adverse Reactions
Clinical Trials Experience
The most frequent adverse reaction in 1066 patients treated 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. Other allergic-type reactions reported include stridor, bronchospasm, wheezing, edema, rash, pruritus, nausea, vomiting, diaphoresis, weakness, and shakiness.
Postmarketing Experience
Due to the nature and limitations of spontaneous reporting, causality has not been established for the following adverse events received for nalbuphine hydrochloride injection: abdominal pain, pyrexia, depressed level or loss of consciousness, somnolence, tremor, anxiety, pulmonary edema, agitation, seizures, and injection site reactions such as pain, swelling, redness, burning, and hot sensations. Death has been reported from severe allergic reactions to nalbuphine hydrochloride treatment. Fetal death has been reported where mothers received nalbuphine hydrochloride during labor and delivery.
Drug Interactions
Although nalbuphine possesses opioid antagonist activity, there is evidence that in nondependent patients it will not antagonize an opioid analgesic administered just before, concurrently, or just after an injection of nalbuphine hydrochloride. Therefore, patients receiving an opioid analgesic, general anesthetics, phenothiazines, or other tranquilizers, sedatives, hypnotics, or other CNS depressants (including alcohol) concomitantly with nalbuphine may exhibit an additive effect. When such combined therapy is contemplated, the dose of one or both agents should be reduced.
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA): B Pregnancy Category B: Reproduction studies have been performed in rats by subcutaneous administration of nalbuphine up to 100 mg/kg/day, or 590 mg/m2/day which is approximately 6 times the MRHD, and in rabbits by intravenous administration of nalbuphine up to 32 mg/kg/day, or 378 mg/m2/day which is approximately 4 times the MRHD. The results did not reveal evidence of developmental toxicity, including teratogenicity, or harm to the fetus. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Non-teratogenenic Effects:
Neonatal body weight and survival rates were reduced at birth and during lactation when
nalbuphine was subcutaneously administered to female and male rats prior to mating and throughout gestation and lactation or to pregnant rats during the last third of gestation and throughout lactation at doses approximately 4 times the maximum recommended human dose.
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Nalbuphine in women who are pregnant.
Labor and Delivery
The placental transfer of nalbuphine is high, rapid, and variable with a maternal to fetal ratio ranging from 1:0.37 to 1:6. Fetal and neonatal adverse effects that have been reported following the administration of nalbuphine to the mother during labor include fetal bradycardia, respiratory depression at birth, apnea, cyanosis, and hypotonia. Some of these events have been life-threatening. Maternal administration of naloxone during labor has normalized these effects in some cases. Severe and prolonged fetal bradycardia has been reported. Permanent neurological damage attributed to fetal bradycardia has occurred. A sinusoidal fetal heart rate pattern associated with the use of nalbuphine has also been reported. Nalbuphine should be used during labor and delivery only if clearly indicated and only if the potential benefit outweighs the risk to the infant. Newborns should be monitored for respiratory depression, apnea, bradycardia and arrhythmias if nalbuphine has been used.
Nursing Mothers
Limited data suggest that nalbuphine hydrochloride is excreted in maternal milk but only in a small amount (less than 1% of the administered dose) and with a clinically insignificant effect. Caution should be exercised when nalbuphine hydrochloride is administered to a nursing woman.
Pediatric Use
Safety and effectiveness in pediatric patients below the age of 18 years have not been established.
Geriatic Use
There is no FDA guidance on the use of Nalbuphine in geriatric settings.
Gender
There is no FDA guidance on the use of Nalbuphine with respect to specific gender populations.
Race
There is no FDA guidance on the use of Nalbuphine with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Nalbuphine in patients with renal impairment.
Hepatic Impairment
There is no FDA guidance on the use of Nalbuphine in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Nalbuphine in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Nalbuphine in patients who are immunocompromised.
Administration and Monitoring
Administration
There is limited information regarding Nalbuphine Administration in the drug label.
Monitoring
There is limited information regarding Nalbuphine Monitoring in the drug label.
IV Compatibility
There is limited information regarding the compatibility of Nalbuphine and IV administrations.
Overdosage
There is limited information regarding Nalbuphine overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.
Pharmacology
There is limited information regarding Nalbuphine Pharmacology in the drug label.
Mechanism of Action
There is limited information regarding Nalbuphine Mechanism of Action in the drug label.
Structure
There is limited information regarding Nalbuphine Structure in the drug label.
Pharmacodynamics
There is limited information regarding Nalbuphine Pharmacodynamics in the drug label.
Pharmacokinetics
There is limited information regarding Nalbuphine Pharmacokinetics in the drug label.
Nonclinical Toxicology
There is limited information regarding Nalbuphine Nonclinical Toxicology in the drug label.
Clinical Studies
There is limited information regarding Nalbuphine Clinical Studies in the drug label.
How Supplied
There is limited information regarding Nalbuphine How Supplied in the drug label.
Storage
There is limited information regarding Nalbuphine Storage in the drug label.
Images
Drug Images
{{#ask: Page Name::Nalbuphine |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}
Package and Label Display Panel
{{#ask: Label Page::Nalbuphine |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}
Patient Counseling Information
There is limited information regarding Nalbuphine Patient Counseling Information in the drug label.
Precautions with Alcohol
Alcohol-Nalbuphine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
There is limited information regarding Nalbuphine Brand Names in the drug label.
Look-Alike Drug Names
There is limited information regarding Nalbuphine Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.