Nalbuphine


Generic Medicine Info
Indications and Dosage
Intravenous
Adjunct in balanced anaesthesia
Adult: Induction: 0.3-3 mg/kg over 10-15 min. Maintenance: 0.25-0.5 mg/kg as single admin if required.

Parenteral
Moderate to severe pain
Adult: IM/IV/SC: 10-20 mg 3-6 hrly as required. Non-opioid-tolerant patients: Max single dose: 20 mg. Max daily dose: 160 mg.
Renal Impairment
Reduce dose.
Hepatic Impairment
Reduce dose.
Incompatibility
Y-site: Allopurinol, amphotericin B cholesteryl sulfate complex, cefepime, docetaxel, methotrexate, nafcillin, piperacillin/tazobactam, pemetrexed, sargramostim, Na bicarbonate. Syringe: Diazepam, dimenhydrinate, ketorolac, pentobarbital.
Special Precautions
Emotionally unstable patients. Patient w/ MI who exhibit nausea and vomiting, history of opiate abuse, impaired respiration due to other drugs, uraemia, bronchial asthma, severe infection, cyanosis or resp obstruction; about to undergo biliary tract surgery; head injury, intracranial lesions or pre-existing increased intracranial pressure. Renal or hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Sedation, dizziness, vertigo, miosis, headache; depression, restlessness, nervousness, crying, drunkenness, euphoria, floating, hostility, confusion, unusual dreams, faintness, feeling of heaviness, tingling, numbness; nausea, vomiting, dry mouth; bradycardia, tachycardia, HTN, hypotension, pulmonary oedema; itching, burning, urticaria; resp depression, dyspnoea, asthma; speech difficulty, urinary urgency, blurred vision, flushing, warmth, sweatiness, clamminess.
Potentially Fatal: Anaphylactic or anaphylactoid and other serious hypersensitivity reactions (e.g. shock, resp distress or arrest, bradycardia, cardiac arrest, hypotension, laryngeal oedema).
IM/Parenteral/SC: B (Prolonged use may cause neonatal opioid withdrawal syndrome.
); IV: B (Prolonged use may cause neonatal opioid withdrawal syndrome.)
Patient Counseling Information
This drug may cause drowsiness and dizziness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor relief of pain, resp and mental status, BP.
Overdosage
Symptoms: Resp depression, CV effects, other CNS effects, sleepiness, mild dysphoria. Management: Supportive treatment. Immediate IV admin of an opiate antagonist (e.g. naloxone or nalmefene) as specific antidote. Admin of oxygen, IV fluids and vasopressors as necessary.
Drug Interactions
Additive CNS depressant effects w/ other CNS depressants (e.g. general anaesth, phenothiazines, other tranquilisers, sedatives, hypnotics).
Food Interaction
Additive CNS depression w/ alcohol.
Action
Description: Nalbuphine is a phenanthrene derivative w/ mixed opioid agonist and antagonist activity (agonist at kappa opiate receptor; partial antagonist at μ receptor). It inhibits the ascending pain pathways, alters the perception of and response to pain by binding to opiate receptors in the CNS. It also produces generalised CNS depression.
Onset: 2-3 min (IV); <15 min (IM/SC).
Duration: 3-6 hr.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: 30 min (IM).
Distribution: Crosses the placenta and distributed in breast milk (small amounts). Plasma protein binding: Approx 50%.
Metabolism: Undergoes extensive first-pass metabolism in GI mucosa and liver.
Excretion: Via urine and faeces (as unchanged drug and conjugates). Elimination half-life: 5 hr.
Chemical Structure

Chemical Structure Image
Nalbuphine

Source: National Center for Biotechnology Information. PubChem Database. Nalbuphine, CID=5311304, https://pubchem.ncbi.nlm.nih.gov/compound/Nalbuphine (accessed on Jan. 22, 2020)

Storage
Store between 15-30°C. Protect from light.
MIMS Class
Analgesics (Opioid)
ATC Classification
N02AF02 - nalbuphine ; Belongs to the class of morphinan derivative opioids. Used to relieve pain.
References
Anon. Nalbuphine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 09/11/2015.

Buckingham R (ed). Nalbuphine Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/11/2015.

McEvoy GK, Snow EK, Miller J et al (eds). Nalbuphine Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com . Accessed 09/11/2015.

Nalbuphine Hydrochloride Injection Solution (Hospira, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 09/11/2015.

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