Butorphanol

Pronunciation

(byoo TOR fa nole)

U.S. Brand Names

Stadol®; Stadol® NS [DSC]

Synonyms

Butorphanol Tartrate

Generic Available

Yes

Canadian Brand Names

Apo-Butorphanol®; PMS-Butorphanol; Stadol® NS

Use

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

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. May cause CNS depression, which may impair physical or mental abilities. Effects with other sedative drugs or ethanol may be potentiated. Use with caution in patients with hepatic/renal dysfunction. Tolerance or drug dependence may result from extended use. Concurrent use of sumatriptan nasal spray and butorphanol nasal spray may increase risk of transient high blood pressure.

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, decreased urination, 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

Overdosage/Toxicology

Symptoms of overdose include respiratory depression, cardiac and CNS depression. Treatment is supportive. Naloxone, 2 mg I.V. with repeat administration as necessary up to a total of 10 mg, can also be used to reverse toxic effects of the opiate.

Drug Interactions

Increased toxicity: CNS depressants, phenothiazines, barbiturates, skeletal muscle relaxants, alfentanil, guanabenz, MAO inhibitors

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).

Stability

Store at room temperature, protect from freezing; incompatible when mixed in the same syringe with diazepam, dimenhydrinate, methohexital, pentobarbital, secobarbital, thiopental

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

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:

Nasal spray: Initial dose should not exceed 1 mg; a second dose may be given after 90-120 minutes

Elderly:

Nasal Spray: Initial dose should not exceed 1 mg; a second dose may be given after 90-120 minutes

Administration

Intranasal: Consider avoiding simultaneous intranasal migraine sprays; may want to separate by at least 30 minutes

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.

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. Alternately: 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.

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.

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

Dosage Forms

Injection, solution, as tartrate [preservative free] (Stadol®): 1 mg/mL (1 mL); 2 mg/mL (1 mL, 2 mL)

Injection, solution, as tartrate [with preservative] (Stadol®): 2 mg/mL (10 mL)

Solution, intranasal spray, as tartrate: 10 mg/mL (2.5 mL) [14-15 doses]

Stadol® NS [DSC]: 10 mg/mL (2.5 mL)

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.

Carr DB, Jacox AK, Chapman RC, et al, "Acute Pain Management," Guideline Technical Report, No. 1. Rockville, MD: U.S Department of Health and Human Services, Public Health Service, Agency for Health Care Policy and Research. AHCPR Publication No. 95-0034. February 1995.

"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 Biol Fate Chem , 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," 4th ed, Glenview, IL: American Pain Society, 1999.

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

Apo-Butorphanol® (CA); Beforal® (CZ); Moradol® (RO, YU); PMS-Butorphanol (CA); Stadol NS™ (CA); Stadol NS® (CL)

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