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Medication Safety Issues
Sound-alike/look-alike issues:
Stadol® may be confused with Haldol®, sotalol
High alert medication: The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes which have a heightened risk of causing significant patient harm when used in error.
Pronunciation
(byoo TOR fa nole)
U.S. Brand Names
Index Terms
Generic Available
Yes
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Parenteral: Management of moderate-to-severe pain; preoperative medication; supplement to balanced anesthesia; management of pain during labor
Nasal spray: Management of moderate-to-severe pain, including migraine headache pain
Restrictions
C-IV
Pregnancy Risk Factor
C/D (prolonged use or high doses at term)
Lactation
Enters breast milk/use caution (AAP rates “compatible”)
Contraindications
Hypersensitivity to butorphanol or any component of the formulation; avoid use in opiate-dependent patients who have not been detoxified, may precipitate opiate withdrawal; pregnancy (prolonged use or high doses at term)
Warnings/Precautions
Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
• Hypotension: May cause hypotension; use with caution in patients with hypovolemia, cardiovascular disease (including acute MI), or drugs which may exaggerate hypotensive effects (including phenothiazines or general anesthetics).
Disease-related concerns:
• Abdominal conditions: May obscure diagnosis or clinical course of patients with acute abdominal conditions.
• Adrenal insufficiency: Use with caution in patients with adrenal insufficiency, including Addison's disease.
• Biliary tract impairment: Use with caution in patients with biliary tract dysfunction; acute pancreatitis may cause constriction of sphincter of Oddi.
• CNS depression/coma: Use with caution in patients with CNS depression or coma.
• Drug abuse: Use with caution in patients with a history of drug abuse or acute alcoholism; potential for drug dependency exists. Tolerance, psychological and physical dependence may occur with prolonged use.
• Head trauma: Use with extreme caution in patients with head injury, intracranial lesions, or elevated intracranial pressure; exaggerated elevation of ICP may occur.
• Hepatic impairment: Use with caution in patients with hepatic impairment.
• Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia and/or urinary stricture.
• Obesity: Use with caution in patients who are morbidly obese.
• Renal impairment: Use with caution in patients with renal impairment.
• Respiratory disease: Use with caution in patients with pre-existing respiratory compromise (hypoxia and/or hypercapnia), COPD or other obstructive pulmonary disease, and kyphoscoliosis or other skeletal disorder which may alter respiratory function; critical respiratory depression may occur, even at therapeutic dosages.
• Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Concurrent drug therapy issues:
• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
• Sumatriptan nasal spray: Concurrent use of sumatriptan nasal spray and butorphanol nasal spray may increase risk of transient high blood pressure.
Special populations:
• Debilitated patients: Use with caution in debilitated patients; there is a greater potential for critical respiratory depression, even at therapeutic dosages.
• Elderly: Use with caution in the elderly; may be more sensitive to adverse effects. Decrease initial dose.
• Pediatrics: Safety and efficacy have not been established in children.
Other warnings/precaution:
• Abuse/misuse/diversion: Healthcare provider should be alert to problems of abuse, misuse, and diversion.
• Optimal regimen: An opioid-containing analgesic regimen should be tailored to each patient's needs and based upon the type of pain being treated (acute versus chronic), the route of administration, degree of tolerance for opioids (naive versus chronic user), age, weight, and medical condition. The optimal analgesic dose varies widely among patients; doses should be titrated to pain relief/prevention.
• Withdrawal: Concurrent use of agonist/antagonist analgesics may precipitate withdrawal symptoms and/or reduced analgesic efficacy in patients following prolonged therapy with mu opioid agonists. Abrupt discontinuation following prolonged use may also lead to withdrawal symptoms.
Adverse Reactions
>10%:
Central nervous system: Drowsiness (43%), dizziness (19%), insomnia (Stadol® NS)
Gastrointestinal: Nausea/vomiting (13%)
Respiratory: Nasal congestion (Stadol® NS)
1% to 10%:
Cardiovascular: Vasodilation, palpitation
Central nervous system: Lightheadedness, headache, lethargy, anxiety, confusion, euphoria, somnolence
Dermatologic: Pruritus
Gastrointestinal: Anorexia, constipation, xerostomia, stomach pain, unpleasant aftertaste
Neuromuscular & skeletal: Tremor, paresthesia, weakness
Ocular: Blurred vision
Otic: Ear pain, tinnitus
Respiratory: Bronchitis, cough, dyspnea, epistaxis, nasal irritation, pharyngitis, rhinitis, sinus congestion, sinusitis, upper respiratory infection
Miscellaneous: Diaphoresis increased
<1%: Bradycardia or tachycardia, hypertension, paradoxical CNS stimulation, hallucinations, mental depression, malaise, restlessness, nightmares, CNS depression, urination decreased, rash, stomach cramps, painful urination, blurred vision, tinnitus, weakness, dyspnea, respiratory depression, dependence with prolonged use, difficulty speaking (transient), hypotension, syncope, agitation, dysphoria, hostility, vertigo, withdrawal symptoms, hives.
<1% (Stadol® NS): Edema, chest pain, hypertension, tachycardia, convulsions, delusions, depressions, apnea, shallow breathing
Drug Interactions
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Alvimopan: Analgesics (Opioid) may enhance the adverse/toxic effect of Alvimopan. This is most notable for patients receiving long-term (i.e., more than 7 days) opiates prior to alvimopan initiation. Management: Alvimopan is contraindicated in patients receiving therapeutic doses of opioids for more than 7 consecutive days immediately prior to alvimopan initiation. Risk D: Consider therapy modification
Ammonium Chloride: May increase the excretion of Analgesics (Opioid). Risk C: Monitor therapy
Amphetamines: May enhance the analgesic effect of Analgesics (Opioid). Risk C: Monitor therapy
Antipsychotic Agents (Phenothiazines): May enhance the hypotensive effect of Analgesics (Opioid). Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy
Desmopressin: Analgesics (Opioid) may enhance the adverse/toxic effect of Desmopressin. Risk C: Monitor therapy
Pegvisomant: Analgesics (Opioid) may diminish the therapeutic effect of Pegvisomant. Risk C: Monitor therapy
Selective Serotonin Reuptake Inhibitors: Analgesics (Opioid) may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Risk C: Monitor therapy
Succinylcholine: May enhance the bradycardic effect of Analgesics (Opioid). Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid or limit ethanol (may increase CNS depression). Watch for sedation.
Herb/Nutraceutical: Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).
Storage
Store at room temperature; protect from freezing.
Compatibility
Y-site administration: Compatible: Allopurinol, amifostine, aztreonam, cefepime, cisatracurium, cladribine, docetaxel, doxorubicin liposome, enalaprilat, esmolol, etoposide, filgrastim, fludarabine, gatifloxacin, gemcitabine, granisetron, labetalol, linezolid, melphalan, paclitaxel, piperacillin/tazobactam, propofol, remifentanil, sargramostim, teniposide, thiotepa, vinorelbine. Incompatible: Amphotericin B cholesteryl sulfate complex, midazolam.
Compatibility in syringe: Compatible: Atropine, chlorpromazine, cimetidine, diphenhydramine, droperidol, fentanyl, hydroxyzine, meperidine, methotrimeprazine, metoclopramide, midazolam, morphine, pentazocine, perphenazine, prochlorperazine, promethazine, scopolamine, thiethylperazine. Incompatible: Dimenhydrinate, pentobarbital.
Mechanism of Action
Mixed narcotic agonist-antagonist with central analgesic actions; binds to opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; produces generalized CNS depression
Pharmacodynamics/Kinetics
Onset of action: I.M.: 5-10 minutes; I.V.: <10 minutes; Nasal: Within 15 minutes
Peak effect: I.M.: 0.5-1 hour; I.V.: 4-5 minutes
Duration: I.M., I.V.: 3-4 hours; Nasal: 4-5 hours
Absorption: Rapid and well absorbed
Protein binding: 80%
Metabolism: Hepatic
Bioavailability: Nasal: 60% to 70%
Half-life elimination: 2.5-4 hours
Excretion: Primarily urine
Dosage
Note: These are guidelines and do not represent the maximum doses that may be required in all patients. Doses should be titrated to pain relief/prevention. Butorphanol has an analgesic ceiling.
Adults:
Parenteral:
Acute pain (moderate to severe):
I.M.: Initial: 2 mg, may repeat every 3-4 hours as needed; usual range: 1-4 mg every 3-4 hours as needed
I.V.: Initial: 1 mg, may repeat every 3-4 hours as needed; usual range: 0.5-2 mg every 3-4 hours as needed
Preoperative medication: I.M.: 2 mg 60-90 minutes before surgery
Supplement to balanced anesthesia: I.V.: 2 mg shortly before induction and/or an incremental dose of 0.5-1 mg (up to 0.06 mg/kg), depending on previously administered sedative, analgesic, and hypnotic medications
Pain during labor (fetus >37 weeks gestation and no signs of fetal distress):
I.M., I.V.: 1-2 mg; may repeat in 4 hours
Note: Alternative analgesia should be used for pain associated with delivery or if delivery is anticipated within 4 hours
Nasal spray:
Moderate to severe pain (including migraine headache pain): Initial: 1 spray (?1 mg per spray) in 1 nostril; if adequate pain relief is not achieved within 60-90 minutes, an additional 1 spray in 1 nostril may be given; may repeat initial dose sequence in 3-4 hours after the last dose as needed
Alternatively, an initial dose of 2 mg (1 spray in each nostril) may be used in patients who will be able to remain recumbent (in the event drowsiness or dizziness occurs); additional 2 mg doses should not be given for 3-4 hours
Note: In some clinical trials, an initial dose of 2 mg (as 2 doses 1 hour apart or 2 mg initially - 1 spray in each nostril) has been used, followed by 1 mg in 1 hour; side effects were greater at these dosages
Elderly:
I.M., I.V.: Initial dosage should generally be 1/2 of the recommended dose; repeated dosing must be based on initial response rather than fixed intervals, but generally should be at least 6 hours apart
Nasal spray: Initial dose should not exceed 1 mg; a second dose may be given after 90-120 minutes
Dosage adjustment in renal impairment:
I.M., I.V.: Initial dosage should generally be 1/2 of the recommended dose; repeated dosing must be based on initial response rather than fixed intervals, but generally should be at least 6 hours apart
Nasal spray: Initial dose should not exceed 1 mg; a second dose may be given after 90-120 minutes
Dosage adjustment in hepatic impairment:
I.M., I.V.: Initial dosage should generally be 1/2 of the recommended dose; repeated dosing must be based on initial response rather than fixed intervals, but generally should be at least 6 hours apart
Nasal spray: Initial dose should not exceed 1 mg; a second dose may be given after 90-120 minutes
Administration: Inhalation
See Dosing.
Administration: Other
Intranasal: Consider avoiding simultaneous intranasal migraine sprays; may want to separate by at least 30 minutes
Administration: I.V. Detail
pH: 3.0-5.5
Monitoring Parameters
Pain relief, respiratory and mental status, blood pressure
Reference Range
0.7-1.5 ng/mL
Patient Education
If self-administered, use exactly as directed; do not increase dose or frequency. Drug may cause physical and/or psychological dependence. While using this medication, do not use alcohol and other prescription or OTC medications (especially sedatives, tranquilizers, antihistamines, or pain medications) without consulting prescriber. May cause dizziness, drowsiness, confusion, or blurred vision (use caution when driving, climbing stairs, or changing position - rising from sitting or lying to standing, or when engaging in tasks requiring alertness until response to drug is known); nausea or vomiting, or loss of appetite (frequent mouth care, small frequent meals, sucking lozenges, or chewing gum may help). Report unresolved nausea or vomiting; respiratory difficulty or shortness of breath; restlessness, insomnia, euphoria, or nightmares; excessive sedation or unusual weakness; facial flushing, rapid heartbeat, or palpitations; urinary difficulty; or vision changes. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. If you are breast-feeding, take dose immediately after breast-feeding or 3-4 hours prior to next feeding.
Nasal administration: Do not use more frequently than prescribed. Blow nose prior to administering. Follow directions on package insert. Insert nozzle of applicator gently into one nostril and exhale. With next breath, squeeze applicator once firmly and quickly once as you breath in. If adequate relief from headache is not achieved within 60-90 minutes, an additional 1 spray may be given. May be repeated in 3-4 hours following last dose, as needed. Alternatively: Two sprays may be given - one spray in each nostril, if you are able to remain lying down (in the event of drowsiness or dizziness). Additional doses should not be taken for 3-4 hours. Avoid using simultaneously with intranasal migraine sprays. Separate by at least 30 minutes.
Geriatric Considerations
Adjust dose for renal function in the elderly.
Anesthesia and Critical Care Concerns/Other Considerations
Butorphanol is a mixed agonist-antagonist opiate; may precipitate withdrawal in narcotic-dependent patients. Abrupt discontinuation after sustained use (generally >10 days) may cause withdrawal symptoms. This agent can potentially cause hallucinations.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation) and unpleasant aftertaste.
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
Drowsiness is common; may rarely produce CNS stimulation or depression, hallucinations, and confusion
Mental Health: Effects on Psychiatric Treatment
Contraindicated in opiate dependent patients; may precipitate opiate withdrawal; concurrent use with psychotropic may produce additive sedation
Nursing: Physical Assessment/Monitoring
Assess other medications patient may be taking for possible additive or adverse interactions. Monitor for effectiveness of pain relief, signs of overdose, vital signs, and adverse effects at beginning of therapy and at regular intervals with long-term use. For inpatients, implement safety measures. May cause physical and/or psychological dependence. Assess knowledge/teach patient appropriate use (if self-administered), adverse reactions to report, and appropriate interventions to reduce side effects.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution, as tartrate [preservative free]: 1 mg/mL (1 mL); 2 mg/mL (1 mL, 2 mL)
Injection, solution, as tartrate [with preservative]: 2 mg/mL (10 mL)
Solution, intranasal, as tartrate [spray]: 10 mg/mL (2.5 mL) [14-15 doses]
Pricing: U.S. (www.drugstore.com)
Solution (Butorphanol Tartrate)
10 mg/mL (2.5): $56.99
References
Bennie RE, Boehringer LA, Dierdorf SF, et al, “Transnasal Butorphanol Is Effective for Postoperative Pain Relief in Children Undergoing Myringotomy,” Anesthesiology, 1998, 89(2):385-90.
“Drugs for Pain,” Med Lett Drugs Ther, 2000, 42(1085):73-8.
Gaver RC, Vasiljev M, Wong H, et al, “Disposition of Parenteral Butorphanol in Man,” Drug Metab Dispos, 1980, 8(4):230-5.
Melanson SW, Morse JW, Pronchik DJ, et al, “Transnasal Butorphanol in the Emergency Department Management of Migraine Headache,” Am J Emerg Med, 1997, 15(1):57-61.
Mokhlesi B, Leikin JB, Murray P, et al, “Adult Toxicology in Critical Care: Part II: Specific Poisonings,” Chest, 2003, 123(3):897-922.
Pachter IJ and Evens RP, “Butorphanol,” Drug Alcohol Depend, 1985, 14(3-4):325-38.
“Principles of Analgesic Use in the Treatment of Acute Pain and Chronic Cancer Pain,” 5th ed, Glenview, IL: American Pain Society, 2003.
Ramsey R, Higbee M, Maesner J, et al, “Influence of Age on the Pharmacokinetics of Butorphanol,” Acute Care, 1986, 12(Suppl 1):8-16.
Shyu WC, Morgenthien EA, and Barbhaiya RH, “Pharmacokinetics of Butorphanol Nasal Spray in Patients With Renal Impairment,” Br J Clin Pharmacol, 1996, 41(5):397-402.
Srinivas NR, Shyu WC, Upmalis D, et al, “Lack of Pharmacokinetic Interaction Between Butorphanol Tartrate Nasal Spray and Sumatriptan Succinate,” J Clin Pharmacol, 1995, 35(4):432-7.
Vachharajani NN, Shyu WC, Garnett WR, et al, “The Absolute Bioavailability and Pharmacokinetics of Butorphanol Nasal Spray in Patients With Hepatic Impairment,” Clin Pharmacol Ther, 1996, 60(3):283-94.
Vachharajani NN, Shyu WC, Greene DS, et al, “The Pharmacokinetics of Butorphanol and Its Metabolites at Steady State Following Nasal Administration in Humans,” Biopharm Drug Dispos, 1997, 18(3):191-202.
International Brand Names
Lexi-Comp.com
Last full review/revision August 2008
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