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. Nalbuphin exerts its effects by binding to specific opiate receptors present in the central nervous system, functions as an antagonist at the µ-receptor, however it has agonist action at ?-receptor, Nalbuphine is also an agonist at the d-receptor, but Nalbuphine (HCl) is nalbuphine''s action at the ?-receptor that provides analgesia. Actions at the ?-receptors are believed to produce alterations in the perception of pain as well as the emotional response to pain, possibly by altering the release of neurotransmitters from afferent nerves sensitive to painful stimuli.'


Adult Dose
Dose: 10 to 20 mg
Single Dose: 15 (15)
Frequency: 12 hourly
Route: IM,IV,SC
Instructions: For Pain. Frequency may be increased to 3 times if needed.
Neonatal
Paedriatic
Dose: 0.1 to 0.15 mg/kg
Single Dose: 0.12 (0.125)
Frequency: 6 hourly
Route: Intra Muscular
Instructions: -
Characteristics
Nalbuphine, Nalbuphine are the derivatives of Nalbuphine (HCl). It is of Synthetic origin and belongs to Alkaloid. It belongs to OPIATE agonist pharmacological group on the basis of mechanism of action and also classified in Analgesics and Anti-inflammatory Agents pharmacological group.The Molecular Weight of Nalbuphine (HCl) is 393.90. Its pKa is 8.71.
Contraindications
Nalbuphine (HCl) is contraindicated in conditions like Respiratory depression,Hypersensitivity,Raised intracranial pressure,Opioid dependence.
Effects
The severe or irreversible adverse effects of Nalbuphine (HCl), which give rise to further complications include Sinus tachycardia, Urticaria, Hypotension, 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, VertigoX, Sedation, SweatingX, Flushing, Nausea and vomiting, Euphoria, Urinary urgency, Xerostomia, Dry mouth, dizziness.
Indications
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-anaesthetic medication.
Interactions
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.
Interfrence
Interfere with enzymatic methods for the detection of opioids
Risks
Drug should not be given to Pregnant Mothers, patients suffering from Liver Malfunction, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Inj Store Below 40°C. Protect from Sunlight, Moisture and Heat.
Warnings
Nalbufine should be used with caution and in low doses in patients with respiratory depression, kidney or liver disease, patients undergoing biliary tract surgery. Patients should observe caution while driving or performing tasks requiring alertness, because it may cause drowsiness.
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