Generic
Nalbuphine Hydrochloride
12 brands available in the market
At a glance
Nalbuphine Hydrochloride is an opioid analgesic used for moderate to severe pain. It blocks transmission of pain signals to the brain to lower pain perception.
Description
Nalbuphine Hydrochloride is a synthetic potent analgesic. Its analgesic potency is essentially equivalent to that of morphine on a milligram basis. Receptor studies show that Nalbuphine binds to mu, kappa, and delta receptors, but not to sigma receptors. Nalbuphine is primarily a kappa agonist/partial mu antagonist analgesic. Onset of action occurs within 2-3 minutes after IV administration and less than 15 minutes following SC or IM injection.
Indications
- Moderate to severe pain
- Pain associated with myocardial infarction
- Supplement to balanced anesthesia
- Preoperative and postoperative analgesia
- Obstetrical analgesia during labor
Therapeutic class
Opioid Analgesics
Pharmacological class
Kappa Agonist/Partial Mu Antagonist
Pharmacology
Nalbuphine binds to opioid receptors to alter pain perception. It acts primarily as a kappa agonist and partial mu antagonist.
Mechanism of action
Alters pain perception and provides pain relief by activating opioid receptors.
Dosage
Adult Dose (Parenteral):
- Moderate-severe pain: IM/IV/SC: 10-20 mg 3-6 hrly; non-opioid-tolerant patients max single dose 20 mg; max daily 160 mg
- Anesthesia supplement: Induction: 0.3-3 mg/kg over 10-15 min; Maintenance: 0.25-0.5 mg/kg
- Myocardial infarction: Slow IV 10-20 mg, repeat after 30 min if needed
Pediatric Dose (18 months-15 years): 0.2 mg/kg IV/IM, 4-6 hrly
Administration
- Administered by doctor or nurse IV/IM/SC; do not self-administer
- IV: Administer slowly over 4-5 minutes
Missed dose
Not generally applicable (scheduled administration); consult doctor if needed.
Side effects
Common Side Effects:
- Sedation
- Sweating
- Nausea, vomiting
- Dizziness, vertigo
- Dry mouth
- Headache
- Respiratory depression
- Dyspnea and asthma
Precautions & warnings
- Caution in patients with impaired respiratory function
- Caution in renal and hepatic impairment
- Caution in biliary tract surgery, myocardial infarction and hypotension
- Caution when driving or doing activities requiring concentration (may cause drowsiness and dizziness)
- Avoid alcohol
Contraindications
- Hypersensitivity
- Diarrhea associated with toxins
- Pseudomembranous colitis
- Respiratory depression (<12 breaths/min)
- Acute asthma
- Bradycardia
- Inflammatory bowel disease
- Respiratory impairment
Drug interactions
- Additive CNS depression with other CNS depressants (alcohol, anaesthetics, anxiolytics, hypnotics, TCAs, antipsychotics)
Food interactions
Alcohol may cause excessive drowsiness.
Use in pregnancy
Use in Pregnancy: Nalbuphine is safe during pregnancy (Category B); placental transfer is high and rapid. Use only if clearly needed.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Nalbuphine is excreted in breast milk in small amounts (<1% of dose); clinically insignificant effect. Use with caution.
Pediatric use
Safety not established in children under 1 year; dose established for children over 1 year.
Geriatric use
Elderly may require dose adjustment.
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; dose reduction may be needed.
Hepatic Impairment: Caution in liver disease; dose reduction may be needed.
Overdose effects
Overdose: Sleepiness and mild dyspnea; naloxone or nalmefene as antidote; oxygen, IV fluids, vasopressors and supportive measures.
Storage conditions
Store below 30°C; protect from light; keep out of reach of children.
Chemical structure
Nalbuphine Hydrochloride