Nalbuphine

Dose reduction is required.

Dose reduction is required.

Incompatible with nafcillin Na, diazepam, ketorolac, pentobarbital Na, thiethylperazine maleate.

Significant respiratory depression; acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment; gastrointestinal obstruction (including paralytic ileus).

Patient with CV disease (including patient with MI who has nausea and vomiting), hypovolaemia, history of substance abuse disorder, mental health condition (e.g. depression, anxiety disorder, post-traumatic stress disorder); impaired respiration due to other drugs, uraemia, severe infection, or cyanosis; COPD or cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, pre-existing respiratory depression; biliary tract disease (including acute pancreatitis); head injury, intracranial lesions or pre-existing increased intracranial pressure; history of seizure disorder, adrenal insufficiency (Addison disease), prostatic hyperplasia and/or urinary stricture, sleep-related disorder (e.g. sleep apnoea), thyroid dysfunction. Avoid concomitant use with full opioid agonist analgesic and MAOIs. Avoid abrupt withdrawal in physically dependent patient. Concomitant use with benzodiazepines or other CNS depressants. Cachectic or debilitated patients. Renal and hepatic impairment. Elderly. Pregnancy and lactation.

Significant: Severe hypotension (including orthostatic hypotension and syncope), CNS depression; adrenal insufficiency (more often after >1 month of use); may cause spasm of the sphincter of Oddi, increased serum amylase; increased risk of seizures (particularly in patients with seizure disorders); hypogonadism and androgen deficiency (in patients receiving chronic opiate agonist or partial agonist treatment).
Cardiac disorders: Bradycardia, tachycardia.
Ear and labyrinth disorders: Vertigo.
Eye disorders: Blurred vision.
Gastrointestinal disorders: Nausea, vomiting, dry mouth, dyspepsia, cramps, bitter taste.
General disorders and administration site conditions: Feeling of heaviness, warmth.
Nervous system disorders: Dizziness, headache, speech difficulty, tingling, numbness.
Psychiatric disorders: Depression, restlessness, nervousness, crying, euphoria, floating feeling, hostility, confusion, unusual dreams.
Renal and urinary disorders: Urinary urgency.
Respiratory, thoracic and mediastinal disorders: Dyspnoea, asthma.
Skin and subcutaneous tissue disorders: Sweatiness or clamminess, itching, burning sensation, urticaria.
Vascular disorders: Hypertension, flushing.
Potentially Fatal: Anaphylactic or anaphylactoid and other serious hypersensitivity reactions (e.g. shock, cardiac arrest, laryngeal oedema); respiratory depression (particularly during initiation or after dose increase).

This drug may cause CNS depression which may impair physical or mental abilities, if affected, do not drive or operate machinery.

Monitor respiratory and mental status, blood pressure, and for effectiveness of pain relief. Evaluate each patient's risk for opioid addiction, abuse, or misuse before initiating treatment and re-assess all patients for the development of these conditions and behaviours. Closely monitor patients for respiratory depression, particularly within the 1st 24-72 hours of initiating treatment and after dosage increases. In postoperative patients, monitor for decreased bowel motility.

Symptoms: Respiratory depression, dysphoria, sleepiness progressing to stupor or coma, cold and clammy skin, constricted pupils, and skeletal muscle flaccidity. In some cases, bradycardia, hypotension, partial or complete airway obstruction, pulmonary oedema, and atypical snoring. Marked mydriasis may be seen with hypoxia. Management: Supportive treatment. Opioid antagonists (naloxone or nalmefene) are used as specific antidotes to respiratory depression. Re-establishment of patent and protected airway and institution of controlled or assisted ventilation are considered priorities if needed. Carefully observe patient until spontaneous respiration is reliably re-established. May give an additional antagonist if the response to an opioid antagonist is only brief or is suboptimal. In case a decision is made to treat serious respiratory depression in patients physically dependent on opioids, administration of antagonist must be done with care and titrated with smaller doses than usual. Advanced life support techniques may be required in case of cardiac arrest or arrhythmias. For the management of circulatory shock and pulmonary oedema, employ other supportive measures (including oxygen and vasopressors) as indicated.

Increased risk of serotonin syndrome with other serotonergic agents, including SSRIs, SNRIs, TCAs, triptans, 5-HT₃ receptor antagonists, certain muscle relaxants (e.g. metaxalone, cyclobenzaprine), MAOIs (e.g. phenelzine, tranylcypromine, linezolid), and other serotonin modulators (e.g. mirtazapine, trazodone). May decrease the efficacy of diuretics by inducing the release of antidiuretic hormone. May increase the risk of urinary retention and/or severe constipation with anticholinergic agents, which may result in paralytic ileus.
Potentially Fatal: Concomitant use with benzodiazepines or other CNS depressants (e.g. anxiolytics, non-benzodiazepine sedatives or hypnotics, muscle relaxants, tranquilisers, antipsychotics, general anaesthetics, other opioids) may lead to profound sedation, respiratory depression, and coma.

Concomitant use with alcohol may result in profound sedation, respiratory depression, and coma.

May interfere with enzymatic methods for the detection of opioids (depending on the test sensitivity or specificity).

Description:
Mechanism of Action: Nalbuphine is a phenanthrene derivative with mixed opioid agonist and antagonist activity (agonist at kappa opiate receptors and partial antagonist at μ receptors in the CNS). It inhibits the ascending pain pathways and alters the perception of and response to pain. Additionally, it causes generalised CNS depression.
Onset: 2-3 minutes (IV); <15 minutes (IM/SC).
Duration: 3-6 hours.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: 30 minutes (IM).
Distribution: Crosses the placenta; enters breast milk (small amounts). Plasma protein binding: Approx 50%.
Metabolism: Metabolised in the liver.
Excretion: Via urine (approx 7% as unchanged drug and metabolites) and faeces. Elimination half-life: 5 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5311304, Nalbuphine. https://pubchem.ncbi.nlm.nih.gov/compound/Nalbuphine. Accessed Jan. 25, 2024.

Store between 15-30°C. Protect from light.

Thuốc giảm đau (opioid)

N02AF02 - nalbuphine ; Belongs to the class of morphinan derivative opioids. Used to relieve pain.

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