• Management of moderate to severe pain.
• Analgesia during labor.
• Sedation before surgery.
• Supplement in balanced anesthesia.

Contraindicated in:

• Hypersensitivity
• Patients physically dependent on opioids (may precipitate withdrawal).

Use Cautiously in:

• Personal or family history of substance use disorder or mental illness
• Head trauma
• ↑intracranial pressure
• Severe renal, hepatic, or pulmonary disease (↑ interval to every 6–8 hr initially in hepatic/renal impairment)
• Hypothyroidism
• Adrenal insufficiency
• Alcoholism
• Undiagnosed abdominal pain
• Prostatic hyperplasia
• OB: Avoid chronic use; prolonged use of opioids during pregnancy can result in neonatal opioid withdrawal syndrome
• Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant
• Pedi: Safety and effectiveness not established in children
• Geri: ↓usual dose by 50% in older adults (administer at an extended interval).

CV: hypertension, hypotension, palpitations.

Derm: sweating, clammy feeling.

EENT: blurred vision, diplopia, miosis (high doses).

GI: nausea, constipation, dry mouth, ileus, vomiting.

GU: urinary retention.

Neuro: confusion, dysphoria, hallucinations, sedation, euphoria, floating feeling, headache, unusual dreams.

Resp: RESPIRATORY DEPRESSION (INCLUDING CENTRAL SLEEP APNEA AND SLEEP-RELATED HYPOXEMIA).
Misc: allodynia, opioid-induced hyperalgesia, physical dependence, psychological dependence, tolerance.

Drug-Drug:

• Use with extreme caution in patients receiving MAO inhibitors (may produce severe, potentially fatal reactions — ↓ initial dose of butorphanol to 25% of usual dose).
• Additive CNS depression with alcohol, antidepressants, antihistamines, and sedative/hypnotics.
• May precipitate withdrawal in patients who are physically dependent on opioids and have not been detoxified.
• May ↓ effects of concurrently administered opioids.
• Drugs that affect serotonergic neurotransmitter systems, including tricyclic antidepressants, SSRIs, SNRIs, MAO inhibitors, TCAs, tramadol, trazodone, mirtazapine, 5-HT₃ receptor antagonists, linezolid, methylene blue, and triptans, ↑ risk of serotonin syndrome.

Drug-Natural Products:

• Concomitant use of kava-kava, valerian, chamomile, or hops can ↑ CNS depression.

(Generic available)

• Solution for injection: 1 mg/mL; 2 mg/mL;
• Intranasal solution: 10 mg/mL, in 2.5-mL metered-dose spray pump (14–15 doses; 1 mg/spray);

• IM (Adults): 2 mg every 3–4 hr as needed (range 1–4 mg).
• IV (Adults): 1 mg every 3–4 hr as needed (range 0.5–2 mg).
• IM, IV (Geriatric Patients): 1 mg every 4–6 hr; ↑ as necessary.
• Intranasal (Adults): 1 mg (one spray in one nostril) initially. An additional dose may be given 60–90 min later. This sequence may be repeated in 3–4 hr. If pain is severe, an initial dose of 2 mg (one spray in each nostril) may be given. May be repeated in 3–4 hr.
• Intranasal (Geriatric Patients): 1 mg (one spray in one nostril) initially. An additional dose may be given 90–120 min later. This sequence may be repeated in 3–4 hr.

Stadol

• Binds to opiate receptors in the CNS.
• Alters the perception of and response to painful stimuli while producing generalized CNS depression.
• Has partial antagonist properties that may result in opioid withdrawal in physically dependent patients.

• Decreased severity of pain.

Therapeutic Classification: opioid analgesics

Pharmacologic Classification: opioid agonists antagonists

Absorption: Well absorbed from IM sites and nasal mucosa.

Distribution: Extensively distributed to tissues.

Metabolism/Excretion: Mostly metabolized by the liver; 11–14% excreted in the feces. Minimal renal excretion.

Half-life: 3–4 hr.

Schedule IV (C-IV)

(analgesia)

• REMS: Instruct patient in how and when to ask for and take pain medication. Discuss safe use, risks, and proper storage and disposal of opioid analgesics with patients and caregivers with each Rx. The Patient Counseling Guide is available at OpioidAnalgesicREMSPCG. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
• Instruct patient on how and when to ask for pain medication.
• Advise patient that butorphanol is a drug with known abuse potential. Protect it from theft, and never give to anyone other than the individual for whom it was prescribed. Store out of sight and reach of children, and in a location not accessible by others.
• Educate patients and caregivers on how to recognize respiratory depression and emphasize the importance of calling 911 or getting emergency medical help right away in the event of a known or suspected overdose. Inform patients and caregivers about various ways to obtain naloxone as permitted by individual state naloxone dispensing and prescribing requirements or guidelines (by prescription, directly from a pharmacist, or as part of a community-based program).
• Medication may cause drowsiness or dizziness. Advise patient to call for assistance when ambulating and to avoid driving or other activities requiring alertness until response to the medication is known.
• Encourage patients on bedrest to turn, cough, and breathe deeply every 2 hr to prevent atelectasis.
• Instruct patient to change positions slowly to minimize orthostatic hypotension.
• Caution patient to avoid concurrent use of alcohol or other CNS depressants with this medication.
• Advise patient that good oral hygiene, frequent mouth rinses, and sugarless gum or candy may decrease dry mouth.
• Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Inform patient of potential for neonatal opioid withdrawal syndrome with prolonged use during pregnancy. Monitor neonate for signs and symptoms of withdrawal symptoms (irritability, hyperactivity and abnormal sleep pattern, high-pitched cry, tremor, vomiting, diarrhea, and/or failure to gain weight); usually occur the first days after birth.
• Intranasal: Instruct patient on proper use of nasal spray. See package insert for detailed instructions. Instruct patient to replace protective clip and clear cover after use and to store the unit in the child resistant container. Caution patient that medication should not be used by anyone other than the person for whom it was prescribed. Excess medication should be disposed of as soon as it is no longer needed. To dispose of, unscrew cap, rinse bottle and pump with water, and dispose of in waste can.
  • If 2-mg dose is prescribed, administer additional spray in other nostril. May cause dizziness and dysphoria. Patient should remain recumbent after administration of 2-mg dose until response to medication is known.

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