Butorphanol

STADOL

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Pronunciation: byoo-TOR-fa-noel

Butorphanol ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Butorphanol ballicule

Butorphanol STADOL mascot mnemonic cartoon — Visual mnemonic: Butorphanol mascot
**“Butter fan’s all ‘Stay, doll’”**

What it isKappa-opioid agonist and partial mu agonist; moderate-to-severe pain, including migraine.

Why this oneThe nasal spray gives rapid analgesia without injection, while partial mu activity limits but does not eliminate respiratory depression.

What limits itIt can precipitate withdrawal in opioid-dependent patients; kappa agonism causes dysphoria, and dependence still develops.

Butorphanol molecular structure (skeletal formula) — Molecular structure: Butorphanol

FDA-approved for

pain (~1978)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Opioid addiction/abuse/misuse; life-threatening respiratory depression; accidental exposure (esp. children) can be fatal; profound sedation/coma/death with benzodiazepines or other CNS depressants; neonatal opioid withdrawal syndrome with prolonged use in pregnancy; opioid REMS; CYP3A4 inhibitors (or stopping inducers) may raise levels and cause fatal respiratory depression

FDA dosing	Population	Start	Target	Max
Pain severe enough to require an opioid, alternatives inadequate	Adults	1 mg (1 spray, one nostril); if inadequate relief in 60-90 min, may give additional 1 mg; sequence may repeat q3-4h PRN	1-2 mg q3-4h PRN (lowest dose achieving analgesia)	2 mg/dose (1 spray each nostril) only if patient can remain recumbent; no additional 2 mg dose for 3-4 h

Renal Initial sequence limited to 1 mg, repeat 1 mg in 90-120 min if needed; subsequent doses generally no less than q6h

Hepatic Initial sequence limited to 1 mg, repeat 1 mg in 90-120 min if needed; subsequent doses generally no less than q6h

Elderly: same reduced sequence as renal/hepatic impairment (1 mg, repeat in 90-120 min; then generally no less than q6h)

Instructions

Use lowest effective dose for shortest duration
Do not abruptly discontinue in physically dependent patients - taper gradually (risk of withdrawal, uncontrolled pain, suicide)
Discuss access to an opioid overdose reversal agent (naloxone/nalmefene)
Conservative dosing when converting from other opioids (agonist-antagonist; underestimate 24-h dose)
Not recommended in labor or for balanced anesthesia (not studied intranasally)

Available strengths

nasal spray 1 mg/spray
inj 1, 2 mg/mL

Contraindications

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

Cautions

Addiction, abuse, and misuse (Schedule IV) - assess risk before prescribing and reassess regularly
Life-threatening respiratory depression - greatest at initiation and after dose increase
Sleep-related breathing disorders incl. central sleep apnea (dose-dependent) - consider opioid taper
Profound sedation/respiratory depression/coma/death with benzodiazepines, alcohol, or other CNS depressants - reserve for inadequate alternatives
Neonatal opioid withdrawal syndrome with extended use in pregnancy (may be life-threatening)
CYP3A4 inhibitors (or discontinuing inducers) may increase butorphanol levels - fatal respiratory depression possible; inducers may reduce efficacy/precipitate withdrawal
Opioid-induced hyperalgesia and allodynia - consider dose decrease or opioid rotation
Extra caution in elderly and hepatic or renal disease

Adverse reactions

Somnolence (49%)
Dizziness (23%)
Nausea and/or vomiting (8%)
Nasal congestion (13%, long-term use)
Insomnia (11%, long-term use)
Asthenia/lethargy
Headache
Sweating
Nasal irritation/epistaxis

Pregnancy No adequate human studies; use only if benefit justifies fetal risk; extended use can cause neonatal opioid withdrawal syndrome (may be life-threatening); higher stillbirth/postimplantation loss in animals

Lactation Present in milk (est. 4 mcg/L with 2 mg IM QID - probably clinically insignificant); monitor breastfed infant for excess sedation and respiratory depression

Cost

Butorphanol (STADOL)

Strength		#/mo	CostPlus
1 mg/mL	inj	per unit	not offered
2 mg/mL	inj	per unit	not offered
1 mg/spray	nasal spray	per unit	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Butorphanol is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry1997

⚠ BOXED WARNINGS

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

Principal riskPrecipitated withdrawal; dysphoria from kappa agonism

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.

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Memory aids: interaction avatars

CYP3A4 substrate

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