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Nalbuphine Hydrochloride
Overview
What is Nalbuphine Hydrochloride?
Nalbuphine hydrochloride is a synthetic opioid agonist-antagonist analgesic of the phenanthrene series. It is chemically related to both the widely used opioid antagonist, naloxone, and the potent opioid analgesic, oxymorphone. Chemically nalbuphine hydrochloride is 17-(cyclobutylmethyl)-4,5α-epoxymorphinan-3,6α,14-triol hydrochloride. Nalbuphine hydrochloride molecular weight is 393.91 and is soluble in HO (35.5 mg/mL at 25ºC) and ethanol (0.8%); insoluble in CHCl and ether. Nalbuphine hydrochloride has pKa values of 8.71 and 9.96. The molecular formula is CHNO • HCl. The structural formula is:
Nalbuphine Hydrochloride Injection is a sterile, nonpyrogenic solution of nalbuphine hydrochloride in water for injection. This product may be administered by subcutaneous, intramuscular or intravenous injection.
Each milliliter (mL) contains nalbuphine hydrochloride 10 mg or 20 mg; sodium citrate, dihydrate 0.47 mg and citric acid, anhydrous 0.63 mg added as buffers and may contain sodium hydroxide and/or hydrochloric acid for pH adjustment; pH 3.7 (3.0 to 4.5). Contains sodium chloride for tonicity adjustment.
Multiple-dose vials contain 1.8 mg/mL methylparaben and 0.2 mg/mL propylparaben added as preservatives. Single-dose products contain no bacteriostat or antimicrobial agent and unused portions must be discarded.
What does Nalbuphine Hydrochloride look like?
What are the available doses of Nalbuphine Hydrochloride?
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What should I talk to my health care provider before I take Nalbuphine Hydrochloride?
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How should I use Nalbuphine Hydrochloride?
Nalbuphine hydrochloride is indicated for the relief of moderate to severe pain. Nalbuphine hydrochloride can also be used as a supplement to balanced anesthesia, for preoperative and postoperative analgesia, and for obstetrical analgesia during labor and delivery.
The usual recommended adult dose is 10 mg for a 70 kg individual administered subcutaneously, intramuscularly, or intravenously; this dose may be repeated every 3 to 6 hours as necessary. Dosage should be adjusted according to the severity of the pain, physical status of the patient, and other medications which the patient may be receiving (see ). In nontolerant individuals, the recommended single maximum dose is 20 mg with a maximum total daily dose of 160 mg.
The use of nalbuphine hydrochloride injection as a supplement to balanced anesthesia requires larger doses than those recommended for analgesia. Induction doses of nalbuphine hydrochloride range from 0.3 mg/kg to 3 mg/kg intravenously to be administered over a 10 to 15 minute period with maintenance doses of 0.25 to 0.5 mg/kg in single intravenous administrations as required. The use of nalbuphine hydrochloride injection may be followed by respiratory depression which can be reversed with the opioid antagonist naloxone hydrochloride.
Patients Dependent on Opioids:
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit.
What interacts with Nalbuphine Hydrochloride?
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.
What are the warnings of Nalbuphine Hydrochloride?
Prolonged use of corticosteroids may produce posterior subcapsular cataracts, glaucoma with possible damage to the optic nerves, and may enhance the establishment of secondary ocular infections due to fungi or viruses.
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 ).
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.
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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 CO 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.
Interaction With Other Central Nervous System Depressants
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.
What are the precautions of Nalbuphine Hydrochloride?
General
Impaired Respiration:
Impaired Renal or Hepatic Function:
Myocardial Infarction:
Biliary Tract Surgery:
Cardiovascular System:
Information for Patients
Patients should be advised of the following information:
Laboratory Tests
Nalbuphine hydrochloride may interfere with enzymatic methods for the detection of opioids depending on the specificity/sensitivity of the test. Consult the test manufacturer for specific details.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Carcinogenesis:
Mutagenesis:
Impairment of Fertility:
Usage in Pregnancy
Teratogenic Effects:
Pregnancy Category B:
Non-teratogenic 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.
Use During Labor and Delivery
See .
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.
What are the side effects of Nalbuphine Hydrochloride?
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:
Cardiovascular:
Gastrointestinal:
Respiratory:
Dermatologic:
Miscellaneous:
Allergic Reactions:
Events Observed during Post-marketing Surveillance of Nalbuphine Hydrochloride Injection
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.
What should I look out for while using Nalbuphine Hydrochloride?
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.
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.
What might happen if I take too much Nalbuphine Hydrochloride?
The immediate intravenous administration of an opiate antagonist such as naloxone or nalmefene is a specific antidote. Oxygen, intravenous fluids, vasopressors and other supportive measures should be used as indicated.
The administration of single doses of 72 mg of nalbuphine hydrochloride subcutaneously to eight normal subjects has been reported to have resulted primarily in symptoms of sleepiness and mild dysphoria.
How should I store and handle Nalbuphine Hydrochloride?
Store at 20°-25°C (68°-77°F) (see USP Controlled Room Temperature). PROTECT FROM LIGHT. KEEP TIGHTLY CLOSED. Sarafem is a registered trademark of Eli Lilly and Company. Nalbuphine Hydrochloride Injection 1 mL (20 mg) is supplied as follows:1 ampul packaged in a pouch NDC 63739-466-215 pouches (NDC 63739-466-21) packaged in a carton NDC 63739-466-05Nalbuphine Hydrochloride Injection 1 mL (20 mg) is supplied as follows:1 ampul packaged in a pouch NDC 63739-466-215 pouches (NDC 63739-466-21) packaged in a carton NDC 63739-466-05Nalbuphine Hydrochloride Injection 1 mL (20 mg) is supplied as follows:1 ampul packaged in a pouch NDC 63739-466-215 pouches (NDC 63739-466-21) packaged in a carton NDC 63739-466-05
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Nalbuphine hydrochloride is a potent analgesic. Its analgesic potency is essentially equivalent to that of morphine on a milligram basis. Receptor studies show that nalbuphine hydrochloride binds to mu, kappa, and delta receptors, but not to sigma receptors. Nalbuphine hydrochloride is primarily a kappa agonist/partial mu antagonist analgesic.
The onset of action of nalbuphine hydrochloride 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.
The opioid antagonist activity of nalbuphine is one-fourth as potent as nalorphine and 10 times that of pentazocine.
Nalbuphine hydrochloride may produce the same degree of respiratory depression as equianalgesic doses of morphine. However, nalbuphine hydrochloride exhibits a ceiling effect such that increases in dose greater than 30 mg do not produce further respiratory depression in the absence of other CNS active medications affecting respiration.
Nalbuphine hydrochloride by itself has potent opioid antagonist activity at doses equal to or lower than its analgesic dose. When administered following or concurrent with mu agonist opioid analgesics (e.g., morphine, oxymorphone, fentanyl), nalbuphine hydrochloride may partially reverse or block opioid-induced respiratory depression from the mu agonist analgesic. Nalbuphine hydrochloride may precipitate withdrawal in patients dependent on opioid drugs. Nalbuphine hydrochloride should be used with caution in patients who have been receiving mu opioid analgesics on a regular basis.
Non-Clinical Toxicology
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.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.
Reports suggest that NSAIDs may diminish the antihypertensive effect of ACE-inhibitors. This interaction should be given consideration in patients taking NSAIDs concomitantly with ACE-inhibitors.
When nabumetone in administered with aspirin, its protein binding is reduced, although the clearance of free nabumetone is not altered. The clinical significance of this interaction is not known; however, as with other NSAIDs, concomitant administration of nabumetone and aspirin is not generally recommended because of the potential of increased adverse effects.
Clinical studies, as well as post marketing observations, have shown that nabumetone can reduce the natriuretic effect of furosemide and thiazides in some patients. This response has been attributed to inhibition of renal prostaglandin synthesis. During concomitant therapy with NSAIDs, the patient should be observed closely for signs of renal failure (see ), as well as to assure diuretic efficacy.
NSAIDs have produced an elevation of plasma lithium levels and a reduction in renal lithium clearance. The mean minimum lithium concentration increased 15% and the renal clearance was decreased by approximately 20%. These effects have been attributed to inhibition of renal prostaglandin synthesis by the NSAID. Thus, when NSAIDs and lithium are administered concurrently, subjects should be observed carefully for signs of lithium toxicity.
NSAIDs have been reported to competitively inhibit methotrexate accumulation in rabbit kidney slices. This may indicate that they could enhance the toxicity of methotrexate. Caution should be used when NSAIDs are administered concomitantly with methotrexate.
The effects of warfarin and NSAIDs on GI bleeding are synergistic, such that users of both drugs together have a risk of serious GI bleeding higher than users of either drug alone.
In vitro studies have shown that, because of its affinity for protein, 6MNA may displace other protein-bound drugs from their binding site. Caution should be exercised when administering Nabumetone with warfarin since interactions have been seen with other NSAIDs.
Concomitant administration of an aluminum-containing antacid had not significant effect on the bioavailability of 6MNA. When administered with food or milk, there is more rapid absorption; however, the total amount of 6MNA in the plasma is unchanged (see ).
Impaired Respiration:
Impaired Renal or Hepatic Function:
Myocardial Infarction:
Biliary Tract Surgery:
Cardiovascular System:
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:
Cardiovascular:
Gastrointestinal:
Respiratory:
Dermatologic:
Miscellaneous:
Allergic Reactions:
Events Observed during Post-marketing Surveillance of Nalbuphine Hydrochloride Injection
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.
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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