Nalbuphine

NUBAIN

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What it isKappa agonist and mu antagonist; moderate to severe pain and opioid-induced pruritus.

Why this oneA ceiling on respiratory depression, and its mu antagonism relieves opioid itch without reversing analgesia entirely.

What limits itIt precipitates withdrawal in the opioid-dependent. Dysphoria and sedation from kappa agonism.

FDA-approved for

pain (~1979)

Off-label

opioid-induced pruritus

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Addiction/abuse/misuse; life-threatening respiratory depression; profound sedation, respiratory depression, coma, and death with benzodiazepines or other CNS depressants.

FDA dosing	Population	Start	Target	Max
Pain	adult (~70 kg)	10 mg SC/IM/IV q3–6h PRN		20 mg single dose; 160 mg/day
Supplement to balanced anesthesia	adult	0.3–3 mg/kg IV over 10–15 min (induction); 0.25–0.5 mg/kg IV maintenance PRN

Renal Undefined

Hepatic Undefined

May repeat every 3–6 hours as necessary

Instructions

When discontinuing a physically dependent patient, taper by 25–50% every 2–4 days; do not abruptly discontinue
Have an opioid overdose reversal agent (naloxone/nalmefene) and resuscitative equipment available
Inspect visually before administration

Contraindications

Significant respiratory depression
Acute or severe bronchial asthma in an unmonitored setting or without resuscitative equipment
Known or suspected GI obstruction, including paralytic ileus

Cautions

Respiratory depression
Serotonin syndrome with serotonergic drugs
Adrenal insufficiency
Severe hypotension
Life-threatening anaphylactoid reactions
Fetal bradycardia in labor

Adverse reactions

Sedation
Sweaty/clammy feeling
Nausea/vomiting
Dizziness/vertigo
Dry mouth
Headache

Pregnancy Insufficient data; extended use can cause neonatal opioid withdrawal; severe fetal bradycardia reported in labor

Lactation Excreted in milk in small amounts (<1% of dose), clinically insignificant; monitor infant for sedation/respiratory depression

⚠ BOXED WARNINGS

Addiction, abuse and misuse
Life-threatening respiratory depression
Risk from concomitant use with benzodiazepines

Principal riskPrecipitated withdrawal; dysphoria from kappa agonism

Cost, est. cash$10–$300/month

Generic entry1986

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger4 / 4

Weight-gain liability0 / 4

Sedation liability2 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityRespiratory depression, dependence and overdose; risk rises sharply with sedatives or impaired clearance.

Mechanism of action: Nalbuphine ballicule

Nalbuphine ballicule: receptor binding, kinetics and half-life diagram

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Memory aids: mascots and interaction avatars

Nalbuphine NUBAIN mascot mnemonic cartoon — **“Newbie’s Nail booth”**
Constricted pupils → opioid
IV route
K → kappa agonist; weak mu partial agonist — the non-DEA-controlled opioid

CYP3A4 substrate

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