No

Analgesic, Narcotic

Management of moderate to severe pain

C-IV

C/D (if used for prolonged periods or in high doses at term)

Hypersensitivity to butorphanol or any component; avoid use in opiate-dependent patients who have not been detoxified, may precipitate opiate withdrawal

Use with caution in patients with hepatic/renal dysfunction, may elevate CSF pressure, may increase cardiac workload; tolerance of drug dependence may result from extended use

>10%:

Central nervous system: Drowsiness(43%), dizziness (19%), insomnia (Stadol ® NS)

Respiratory: Nasal congestion (Stadol ® NS)

Gastrointestinal: Nausea/vomiting (13%)

1% to 10%:

Cardiovascular: Vasodilation, palpitations

Central nervous system: Lightheadedness, headache, lethargy, anxiety, confusion, euphoria, somnolence

Gastrointestinal: Anorexia, constipation, xerostomia, stomach pain, unpleasant aftertaste (Stadol ® NS)

Neuromuscular & skeletal: Tremor (Stadol ® NS), paresthesia, weakness

Dermatologic: Pruritus

Ocular: Blurred vision

Otic: Ear pain (Stadol ® NS), tinnitus (Stadol ® NS)

Respiratory: (Stadol ® NS)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, shortness of breath, 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

Symptoms of overdose include respiratory depression, cardiac and CNS depression

Treatment of an overdose includes support of the patient's airway, establishment of an I.V. line and administration of naloxone 2 mg I.V. (0.01 mg/kg for children) with repeat administration as necessary up to a total of 10 mg

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

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

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

Onset of action: I.M.: 5-10 minutes; I.V.: <10 minutes; Nasal: Within 15 minutes

Peak effect: I.M.: Within 0.5-1 hour; I.V.: Within 4-5 minutes

Duration: I.M., I.V.: 3-4 hours; Nasal: 4-5 hours

Absorption: Rapidly and well absorbed

Protein binding: 80%

Metabolism: In the liver

Half-life: 2.5-4 hours

Elimination: Primarily in urine

Adults:

I.V.: 0.5-2 mg every 3-4 hours as needed

Nasal spray: Headache: 1 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 (each spray gives ~1 mg of butorphanol); may repeat in 3-4 hours after the last dose as needed

Dosing adjustment in renal impairment:

Cl_cr 10-50 mL/minute: Administer 75% of dose

Cl_cr <10 mL/minute: Administer 50% of dose

Alcohol: Additive CNS effects, avoid or limit use; watch for sedation

Pain relief, respiratory and mental status, blood pressure

0.7-1.5 ng/mL

Drowsiness is common; may rarely produce CNS stimulation or depression, hallucinations, and confusion

Contraindicated in opiate dependent patients; may precipitate opiate withdrawal; concurrent use with psychotropic may produce additive sedation

No information available to require special precautions

No effects or complications reported

If self-administered, use exactly as directed (do not increase dose or frequency); 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; difficulty breathing 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 be pregnant. If you are breast-feeding, take dose immediately after breast-feeding or 3-4 hours prior to next feeding.

Observe for excessive sedation or confusion, respiratory depression; raise bed rails; aid with ambulation

Injection, as tartrate: 1 mg/mL (1 mL); 2 mg/mL (1 mL, 2 mL, 10 mL)

Spray, nasal, as tartrate: 10 mg/mL [14-15 doses] (2.5 mL)

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, 1998, 40(1033):79-84.

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.

Pachter IJ and Evens RP, "Butorphanol," Drug Alcohol Depend, 1985, 14(3-4):325-38.

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, Igwenezue KB, Hainsworth JD, et al, "Lack of Pharmacokinetic Interaction Between Butorphanol Tartrate Nasal Spray and Sumatriptan Succinate," J Clin Pharmacol, 1995, 35(4):432-7.

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.