Nalbuphine (HCl)

Nalbuphine (HCl) is a synthetic opiate agonist/antagonist that is chemically related to both naloxone, a narcotic antagonist, and oxymorphone, a potent narcotic analgesic. Used to treat moderate to severe pain associated with acute and chronic medical disorders such as cancer, renal or biliary colic, migraine or vascular headaches, and surgical pain. Another clinical use is obstetrical analgesia during labor and delivery. Some evidence suggests that nalbuphine's respiratory depressant effects do not increase proportionately with increasing doses, thus making this drug safer in patients at risk from respiratory depression. It was approved by the FDA in 1979. Nalbuphine is a mixed agonist/antagonist opioid modulator. Specifically, it acts as a moderate-efficacy partial agonist or antagonist of the μ-opioid receptor (MOR) and as a high-efficacy partial agonist of the κ-opioid receptor (KOR), whereas it has relatively low affinity for the δ-opioid receptor (DOR) and sigma receptors.

Nalbuphine (HCl) is primarily indicated in conditions like Adjunct to prevent relapse, Long term management of hereditary angioedema, Moderate to severe pain, and can also be given in adjunctive therapy as an alternative drug of choice in All forms of epilepsy, Anesthesia, Myoclonus, Post-operative pain, Pre-anesthetic medication.

Nalbuphine (HCl) is contraindicated in conditions like Respiratory depression, Hypersensitivity, Raised intracranial pressure, Opioid dependence, Diarrhea associated with toxins, GI obstruction, IBS.

The severe or irreversible adverse effects of Nalbuphine (HCl), which give rise to further complications include Sinus tachycardia, Urticaria, Hypotension, Orthostatic hypotension, Hypertension, Depression, Sinus bradycardia, Syncope, Respiratory depression. The symptomatic adverse reactions produced by Nalbuphine (HCl) are more or less tolerable and if they become severe, they can be treated symptomatically, these include Dizziness, Headache, Dyspnea, Dry mouth, Blurred vision, Pruritus, Vertigo, Sedation, Sweating, Flushing, Nausea and vomiting, Euphoria, Urinary urgency, Xerostomia.

Possible respiratory depression. Administer with caution and in low doses in patients with impaired respiration caused by other drugs, uremia, bronchial asthma, severe infection, cyanosis, or respiratory obstruction. Should be administered as a supplement to general anesthesia only by individuals who are experienced in the use of parenteral anesthetics and in the maintenance of an adequate airway and respiratory support. Facilities and personnel necessary for intubation, administration of oxygen, and assisted or controlled respiration should be readily available; an opiate antagonist (e.g., naloxone) should also be readily available. Routinely discuss availability of the opiate antagonist naloxone with all patients receiving new or reauthorized prescriptions for opiate analgesics. Consider prescribing naloxone for patients receiving opiate analgesics who are at increased risk of opiate overdosage (e.g., those receiving concomitant therapy with benzodiazepines or other CNS depressants, those with history of opiate or substance use disorder, those with medical conditions that could increase sensitivity to opiate effects, those who have experienced a prior opiate overdose) or who have household members, including children, or other close contacts who are at risk for accidental ingestion or overdosage. Even if patients are not receiving an opiate analgesic, consider prescribing naloxone if the patient is at increased risk of opiate overdosage (e.g., those with current or past diagnosis of opiate use disorder [OUD], those who have experienced a prior opiate overdose). Concomitant use of opiate agonists or opiate partial agonists, including nalbuphine, and benzodiazepines or other CNS depressants (e.g., anxiolytics, sedatives, hypnotics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, other opiates, alcohol) may result in profound sedation, respiratory depression, coma, and death. Substantial proportion of fatal opiate overdoses involve concurrent benzodiazepine use. Reserve concomitant use of nalbuphine and other CNS depressants for patients in whom alternative treatment options are inadequate. (See Specific Drugs and Laboratory Tests under Interactions.) Performance of activities requiring mental alertness and physical coordination may be impaired. When used in emergency procedures, keep the patient under observation until recovery from the drug’s effects that would affect driving or other potentially hazardous tasks has occurred. Concurrent use of other CNS depressants may potentiate CNS depression and may result in profound sedation, respiratory depression, coma, or death. (See Concomitant Use with Benzodiazepines or Other CNS Depressants under Cautions.) Adrenal insufficiency reported in patients receiving opiate agonists or opiate partial agonists. Manifestations are nonspecific and may include nausea, vomiting, anorexia, fatigue, weakness, dizziness, and hypotension. If adrenal insufficiency is suspected, perform appropriate laboratory testing promptly and provide physiologic (replacement) dosages of corticosteroids; taper and discontinue the opiate agonist or partial agonist to allow recovery of adrenal function. If the opiate agonist or partial agonist can be discontinued, perform follow-up assessment of adrenal function to determine if corticosteroid replacement therapy can be discontinued. In some patients, switching to a different opiate improved symptoms. Potential for elevation of CSF pressure as a result of vasodilation following carbon dioxide retention. Opiate effects may obscure the existence, extent, or course of intracranial pathology. Use in patients with head injury, other intracranial lesions, or preexisting elevation in intracranial pressure only if the potential benefits justify the possible risks. Possible tolerance, psychologic dependence, and physical dependence. Prescribe cautiously for patients who are emotionally unstable or have a history of opiate abuse; closely supervise these patients when long-term therapy is contemplated. Avoid unnecessary increases in dose or frequency of administration; avoid use in anticipation of pain. Anaphylactic or anaphylactoid and other serious hypersensitivity reactions, including shock, respiratory distress, respiratory arrest, bradycardia, cardiac arrest, hypotension, and laryngeal edema, reported. Some formulations contain sodium metabisulfite, which may cause allergic-type reactions (including anaphylaxis and life-threatening or less severe asthmatic episodes) in certain susceptible individuals. Use with caution in patients who have been chronically receiving opiate agonists; nalbuphine does not suppress the abstinence syndrome in these patients; high doses may precipitate withdrawal symptoms (e.g., abdominal cramps, nausea, vomiting, lacrimation, rhinorrhea, anxiety, restlessness, increased temperature, piloerection) as a result of opiate antagonist effect. (See Patients Tolerant to Opiate Agonists under Dosage and Administration.) Possible spasm of Oddi’s sphincter; use with caution in patients about to undergo biliary tract surgery. Use with caution in patients with MI who exhibit nausea and vomiting. During studies evaluating nalbuphine as a supplement to balanced anesthesia, increased incidence of bradycardia reported in patients who did not receive atropine preoperatively. Hypogonadism or androgen deficiency reported in patients receiving long-term opiate agonist or opiate partial agonist therapy; causality not established. Manifestations may include decreased libido, impotence, erectile dysfunction, amenorrhea, or infertility. Perform appropriate laboratory testing in patients with manifestations of hypogonadism. Category B. Safe use during pregnancy (except during labor and delivery) not established. Administration during labor and delivery may result in fetal bradycardia or respiratory depression, apnea, cyanosis, and hypotonia in neonates at birth. Adverse effects may resolve in some cases following maternal administration of naloxone during labor. Fetal bradycardia may be severe and prolonged; permanent neurological damage associated with fetal bradycardia reported. In addition, a sinusoidal fetal heart rate pattern associated with maternal use of nalbuphine. Use with caution in women during labor and delivery, especially in those delivering premature infants; monitor neonates for respiratory depression, apnea, bradycardia, and cardiac arrhythmias. Distributed into milk. Caution if used in nursing women. Safety and efficacy not established in children <18 years of age. Use with caution and in reduced dosage. Use with caution and in reduced dosage.

Possible respiratory depression. Administer with caution and in low doses in patients with impaired respiration caused by other drugs, uremia, bronchial asthma, severe infection, cyanosis, or respiratory obstruction. Should be administered as a supplement to general anesthesia only by individuals who are experienced in the use of parenteral anesthetics and in the maintenance of an adequate airway and respiratory support. Facilities and personnel necessary for intubation, administration of oxygen, and assisted or controlled respiration should be readily available; an opiate antagonist (e.g., naloxone) should also be readily available. Routinely discuss availability of the opiate antagonist naloxone with all patients receiving new or reauthorized prescriptions for opiate analgesics. Consider prescribing naloxone for patients receiving opiate analgesics who are at increased risk of opiate overdosage (e.g., those receiving concomitant therapy with benzodiazepines or other CNS depressants, those with history of opiate or substance use disorder, those with medical conditions that could increase sensitivity to opiate effects, those who have experienced a prior opiate overdose) or who have household members, including children, or other close contacts who are at risk for accidental ingestion or overdosage. Even if patients are not receiving an opiate analgesic, consider prescribing naloxone if the patient is at increased risk of opiate overdosage (e.g., those with current or past diagnosis of opiate use disorder [OUD], those who have experienced a prior opiate overdose). Concomitant use of opiate agonists or opiate partial agonists, including nalbuphine, and benzodiazepines or other CNS depressants (e.g., anxiolytics, sedatives, hypnotics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, other opiates, alcohol) may result in profound sedation, respiratory depression, coma, and death. Substantial proportion of fatal opiate overdoses involve concurrent benzodiazepine use. Reserve concomitant use of nalbuphine and other CNS depressants for patients in whom alternative treatment options are inadequate. (See Specific Drugs and Laboratory Tests under Interactions.) Performance of activities requiring mental alertness and physical coordination may be impaired. When used in emergency procedures, keep the patient under observation until recovery from the drug’s effects that would affect driving or other potentially hazardous tasks has occurred. Concurrent use of other CNS depressants may potentiate CNS depression and may result in profound sedation, respiratory depression, coma, or death. (See Concomitant Use with Benzodiazepines or Other CNS Depressants under Cautions.) Adrenal insufficiency reported in patients receiving opiate agonists or opiate partial agonists. Manifestations are nonspecific and may include nausea, vomiting, anorexia, fatigue, weakness, dizziness, and hypotension. If adrenal insufficiency is suspected, perform appropriate laboratory testing promptly and provide physiologic (replacement) dosages of corticosteroids; taper and discontinue the opiate agonist or partial agonist to allow recovery of adrenal function. If the opiate agonist or partial agonist can be discontinued, perform follow-up assessment of adrenal function to determine if corticosteroid replacement therapy can be discontinued. In some patients, switching to a different opiate improved symptoms. Potential for elevation of CSF pressure as a result of vasodilation following carbon dioxide retention. Opiate effects may obscure the existence, extent, or course of intracranial pathology. Use in patients with head injury, other intracranial lesions, or preexisting elevation in intracranial pressure only if the potential benefits justify the possible risks. Possible tolerance, psychologic dependence, and physical dependence. Prescribe cautiously for patients who are emotionally unstable or have a history of opiate abuse; closely supervise these patients when long-term therapy is contemplated. Avoid unnecessary increases in dose or frequency of administration; avoid use in anticipation of pain. Anaphylactic or anaphylactoid and other serious hypersensitivity reactions, including shock, respiratory distress, respiratory arrest, bradycardia, cardiac arrest, hypotension, and laryngeal edema, reported. Some formulations contain sodium metabisulfite, which may cause allergic-type reactions (including anaphylaxis and life-threatening or less severe asthmatic episodes) in certain susceptible individuals. Use with caution in patients who have been chronically receiving opiate agonists; nalbuphine does not suppress the abstinence syndrome in these patients; high doses may precipitate withdrawal symptoms (e.g., abdominal cramps, nausea, vomiting, lacrimation, rhinorrhea, anxiety, restlessness, increased temperature, piloerection) as a result of opiate antagonist effect. (See Patients Tolerant to Opiate Agonists under Dosage and Administration.) Possible spasm of Oddi’s sphincter; use with caution in patients about to undergo biliary tract surgery. Use with caution in patients with MI who exhibit nausea and vomiting. During studies evaluating nalbuphine as a supplement to balanced anesthesia, increased incidence of bradycardia reported in patients who did not receive atropine preoperatively. Hypogonadism or androgen deficiency reported in patients receiving long-term opiate agonist or opiate partial agonist therapy; causality not established. Manifestations may include decreased libido, impotence, erectile dysfunction, amenorrhea, or infertility. Perform appropriate laboratory testing in patients with manifestations of hypogonadism. Category B. Safe use during pregnancy (except during labor and delivery) not established. Administration during labor and delivery may result in fetal bradycardia or respiratory depression, apnea, cyanosis, and hypotonia in neonates at birth. Adverse effects may resolve in some cases following maternal administration of naloxone during labor. Fetal bradycardia may be severe and prolonged; permanent neurological damage associated with fetal bradycardia reported. In addition, a sinusoidal fetal heart rate pattern associated with maternal use of nalbuphine. Use with caution in women during labor and delivery, especially in those delivering premature infants; monitor neonates for respiratory depression, apnea, bradycardia, and cardiac arrhythmias. Distributed into milk. Caution if used in nursing women. Safety and efficacy not established in children <18 years of age. Use with caution and in reduced dosage. Use with caution and in reduced dosage.

10 to 20 mg (15 (15)) 12 hourly IM,IV,SC — For Pain. Frequency may be increased to 3 times if needed. 10 to 30 mg (20 (20)) 12 hourly Slow IV — For Myocardial Infarction. Frequency may be increased to 3 times if needed.

0.1 to 0.15 mg/kg (0.12 (0.125)) 6 hourly Intra Muscular — - 0.1 to 0.15 mg/kg (0.12 (0.125)) 6 hourly Intra Venous — - 0.1 to 0.15 mg/kg (0.12 (0.125)) 6 hourly Subcutaneous — -

No neonatal dosage information is recorded for this medicine yet.

Nalbuphine (HCl) is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAlcoholAlfentanil (HCl)Fentanyl (Citrate)Naloxone (HCl) These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Inj Store Below 40°C. Protect from Sunlight, Moisture and Heat.