butorphanol

ROUTE	ONSET	PEAK	DURATION
IM	within 15 min	30–60 min	3–4 hr
IV	within min	4–5 min	2–4 hr
Intranasal	within 15 min	1–2 hr	4–5 hr

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).

Adv. Reactions/Side Effects ⬆ ⬇

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

Interactions ⬆ ⬇

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.

Route/Dosage ⬆ ⬇

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.
(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.
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.

Availability ⬆ ⬇

(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)

Assessment ⬆ ⬇

Assess type, location, and intensity of pain before and 30–60 min after IM, 5 min after IV, and 60–90 min after intranasal administration. When titrating opioid doses, increases of 25–50% should be administered until there is either a 50% reduction in the patient’s pain rating on a numerical or visual analogue scale or the patient reports satisfactory pain relief. A repeat dose can be safely administered at the time of the peak if previous dose is ineffective and side effects are minimal. Patients requiring doses higher than 4 mg should be converted to an opioid agonist. Butorphanol is not recommended for prolonged use or as first-line therapy for acute or cancer pain.
An equianalgesic chart (see Equianalgesic Dosing Guidelines) should be used when changing routes or when changing from one opioid to another.
Assess BP, pulse, and respirations before and periodically during administration. If respiratory rate is <10/min, assess level of sedation. Dose may need to be decreased by 25–50%. Respiratory depression does not increase in severity, only in duration, with increased dose. Monitor for respiratory depression, especially during initiation or following dose increase; serious, life-threatening, or fatal respiratory depression may occur. May cause sleep-related breathing disorders (central sleep apnea, sleep-related hypoxemia).
Monitor patients for opioid-induced hyperalgesia occurs when an opioid paradoxically causes an ↑ in pain or an ↑ in sensitivity to pain. Opioid-induced hyperalgesia differs from tolerance, which is the need for increasing doses of opioids to maintain a defined effect. Symptoms of opioid-induced hyperalgesia include ↑ levels of pain upon opioid dosage ↑, ↓ levels of pain upon opioid dosage ↓, or pain from ordinarily nonpainful stimuli. If opioid-induced hyperalgesia suspected, consider ↓ butorphanol dose.
Assess previous analgesic history. Antagonistic properties may induce withdrawal symptoms (vomiting, restlessness, abdominal cramps, increased BP and temperature) in patients who are physically dependent on opioid agonists.
Butorphanol has a lower potential for dependence than other opioids, but prolonged use may lead to physical and psychological dependence and tolerance. This should not prevent the patient from receiving adequate analgesia. Most patients receiving butorphanol for pain do not develop psychological dependence. If tolerance develops, changing to an opioid agonist may be required to relieve pain.
Assess risk for opioid addiction, abuse, or misuse prior to administration.

Lab Test Considerations:

May cause ↑ serum amylase and lipase levels.

Toxicity and Overdose:

If an opioid antagonist is required to reverse respiratory depression or coma, naloxone is the antidote. Dilute the 0.4-mg ampule of naloxone in 10 mL of 0.9% NaCl and administer 0.5 mL (0.02 mg) by IV push every 2 min. For children and patients weighing <40 kg, dilute 0.1 mg of naloxone in 10 mL of 0.9% NaCl for a concentration of 10 mcg/mL and administer 0.5 mcg/kg every 1–2 min. Titrate dose to avoid withdrawal, seizures, and severe pain.

Implementation ⬆ ⬇

Accidental overdosage of opioid analgesics has resulted in fatalities. Before administering, clarify all ambiguous orders; have second practitioner independently check original order, dose calculations, and route of administration.
Explain therapeutic value of medication before administration to enhance the analgesic effect.
- Regularly administered doses may be more effective than prn administration. Analgesic is more effective if given before pain becomes severe.
- Coadministration with nonopioid analgesics may have additive analgesic effects and permit lower opioid doses.
Butorphanol should be discontinued gradually after long-term use to prevent withdrawal symptoms.
FDA strongly encourages health care professionals to complete a REMS-compliant education program that includes all the elements of the FDA Education Blueprint for Health Care Providers Involved in the Management or Support of Patients with Pain, available at www.fda.gov/OpioidAnalgesicREMSBlueprint. Information on programs can be found at 1-800-503-0784 or www.opioidanalgesicrems.com.
Discuss availability of naloxone for emergency treatment of opioid overdose with the patient and caregiver and assess the potential need for access to naloxone, both when initiating and renewing therapy, especially if patient has household members (including children) or other close contacts at risk for accidental exposure or overdose. Consider prescribing naloxone, based on the patient’s risk factors for overdose, such as concomitant use of CNS depressants, a history of opioid use disorder, or prior opioid overdose. However, the presence of risk factors for overdose should not prevent the proper management of pain in any patient.
IM: Administer IM injections deep into well-developed muscle. Rotate sites of injections.
Administer 1 spray in 1 nostril.

IV Administration:

Diluent: May give IV undiluted.
Rate: Administer over 3–5 min.
Rapid administration may cause respiratory depression, hypotension, and cardiac arrest.

Patient/Family Teaching ⬆ ⬇

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 www.fda.gov/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.
Rep: 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.
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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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇