STADOL PRESERVATIVE FREE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for STADOL PRESERVATIVE FREE (STADOL PRESERVATIVE FREE).

How it works

Butorphanol is a synthetic agonist-antagonist opioid analgesic that exerts its effects primarily through binding to kappa-opioid receptors and, to a lesser extent, mu-opioid receptors, producing analgesia and sedation. It also has partial antagonist activity at mu receptors.

What the body does with it

Metabolism	Primarily metabolized in the liver to hydroxylbutorphanol via CYP3A4 and other enzymes.
Excretion	Primarily hepatic metabolism (glucuronidation) to inactive metabolites; renal excretion accounts for <5% unchanged drug. Approximately 70% of dose excreted in urine as metabolites, 20% in feces.
Half-life	Terminal elimination half-life is 2.5–3.3 hours in adults; prolonged to 4–6 hours in elderly or hepatic impairment.
Protein binding	Approximately 76–80% bound to serum proteins, primarily albumin and α1-acid glycoprotein.
Volume of Distribution	Volume of distribution is 1.2–1.7 L/kg, indicating extensive tissue distribution.
Bioavailability	Intramuscular: 70–80%; Subcutaneous: similar to IM. Oral: <5% due to extensive first-pass metabolism.
Onset of Action	Intravenous: 2–3 minutes; Intramuscular: 10–15 minutes.
Duration of Action	IV: 3–4 hours; IM: 4–6 hours. Duration may be shorter with rapid IV administration due to redistribution.

Classification & Brands

Dosing & administration

0.5–2 mg intravenously or intramuscularly every 3–4 hours as needed for pain. Alternatively, 1–2 mg as a single dose, may repeat in 30–60 minutes if needed.

Dosage form	INJECTABLE
Renal impairment	For GFR 15–29 mL/min: reduce dose by 50% or increase dosing interval to every 6–8 hours. For GFR <15 mL/min: use with caution, reduce dose by 75% or administer every 8–12 hours. Hemodialysis: no supplemental dosing; not dialyzable.
Liver impairment	Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce dose by 50% or extend interval to every 6 hours. Child-Pugh Class C: avoid use; if necessary, reduce dose by 75% and monitor closely.
Pediatric use	Children ≥12 years: 0.5–2 mg intravenously or intramuscularly every 3–4 hours as needed. Children 2–12 years: 0.1–0.2 mg/kg/dose intravenously or intramuscularly every 3–4 hours as needed (max single dose 2 mg). Children <2 years: not recommended.
Geriatric use	Elderly patients (≥65 years): initiate at 0.5 mg intravenously or intramuscularly every 4–6 hours; increase cautiously based on response and tolerability. Reduce total daily dose by 25–50% compared to younger adults.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for STADOL PRESERVATIVE FREE (STADOL PRESERVATIVE FREE).

Breastfeeding	Excreted in human milk in low concentrations; M/P ratio not established. American Academy of Pediatrics considers butorphanol compatible with breastfeeding. Caution with high doses or prolonged use due to potential for neonatal drowsiness or withdrawal.
Teratogenic Risk	Pregnancy Category C. First trimester: No adequate studies; potential risk based on animal data at 2.5-5 times human dose. Second trimester: Same as first; prolonged use may lead to neonatal opioid withdrawal syndrome. Third trimester: Risk of neonatal respiratory depression if administered near term; may cause opioid withdrawal in newborn after chronic use.

Warnings & precautions

■ FDA Black Box Warning

Risk of opioid addiction, abuse, and misuse; life-threatening respiratory depression; accidental ingestion; neonatal opioid withdrawal syndrome; risks from concomitant use with benzodiazepines or other CNS depressants; and risk of abuse and dependence.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Known hypersensitivity to butorphanol or any component","Patients with significant respiratory depression","Acute or severe bronchial asthma in an unmonitored setting or without resuscitative equipment","Known or suspected gastrointestinal obstruction, including paralytic ileus","Concurrent use of monoamine oxidase inhibitors (MAOIs) or within 14 days of such therapy"]

Clinical Precautions

Precautions

["Concomitant use with CNS depressants (e.g., benzodiazepines) increases risk of sedation, respiratory depression, coma, and death","Risk of respiratory depression, especially in elderly, cachectic, or debilitated patients","Physical and psychological dependence with chronic use","May increase intracranial pressure in patients with head injury","Risk of hypotension in hypovolemic patients","May impair ability to perform hazardous tasks","Use in renal or hepatic impairment requires dose adjustment"]

Clinical Tips & Counseling

Drug interactions

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STADOL PRESERVATIVE FREE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for STADOL PRESERVATIVE FREE (STADOL PRESERVATIVE FREE).

How it works

What the body does with it

Metabolism	Primarily metabolized in the liver to hydroxylbutorphanol via CYP3A4 and other enzymes.
Excretion	Primarily hepatic metabolism (glucuronidation) to inactive metabolites; renal excretion accounts for <5% unchanged drug. Approximately 70% of dose excreted in urine as metabolites, 20% in feces.
Half-life	Terminal elimination half-life is 2.5–3.3 hours in adults; prolonged to 4–6 hours in elderly or hepatic impairment.
Protein binding	Approximately 76–80% bound to serum proteins, primarily albumin and α1-acid glycoprotein.
Volume of Distribution	Volume of distribution is 1.2–1.7 L/kg, indicating extensive tissue distribution.
Bioavailability	Intramuscular: 70–80%; Subcutaneous: similar to IM. Oral: <5% due to extensive first-pass metabolism.
Onset of Action	Intravenous: 2–3 minutes; Intramuscular: 10–15 minutes.
Duration of Action	IV: 3–4 hours; IM: 4–6 hours. Duration may be shorter with rapid IV administration due to redistribution.

Classification & Brands

Dosing & administration

0.5–2 mg intravenously or intramuscularly every 3–4 hours as needed for pain. Alternatively, 1–2 mg as a single dose, may repeat in 30–60 minutes if needed.

Dosage form	INJECTABLE
Renal impairment	For GFR 15–29 mL/min: reduce dose by 50% or increase dosing interval to every 6–8 hours. For GFR <15 mL/min: use with caution, reduce dose by 75% or administer every 8–12 hours. Hemodialysis: no supplemental dosing; not dialyzable.
Liver impairment	Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce dose by 50% or extend interval to every 6 hours. Child-Pugh Class C: avoid use; if necessary, reduce dose by 75% and monitor closely.
Pediatric use	Children ≥12 years: 0.5–2 mg intravenously or intramuscularly every 3–4 hours as needed. Children 2–12 years: 0.1–0.2 mg/kg/dose intravenously or intramuscularly every 3–4 hours as needed (max single dose 2 mg). Children <2 years: not recommended.
Geriatric use	Elderly patients (≥65 years): initiate at 0.5 mg intravenously or intramuscularly every 4–6 hours; increase cautiously based on response and tolerability. Reduce total daily dose by 25–50% compared to younger adults.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for STADOL PRESERVATIVE FREE (STADOL PRESERVATIVE FREE).

Breastfeeding	Excreted in human milk in low concentrations; M/P ratio not established. American Academy of Pediatrics considers butorphanol compatible with breastfeeding. Caution with high doses or prolonged use due to potential for neonatal drowsiness or withdrawal.
Teratogenic Risk	Pregnancy Category C. First trimester: No adequate studies; potential risk based on animal data at 2.5-5 times human dose. Second trimester: Same as first; prolonged use may lead to neonatal opioid withdrawal syndrome. Third trimester: Risk of neonatal respiratory depression if administered near term; may cause opioid withdrawal in newborn after chronic use.