Pronunciation:

(byoo TOR fa nole)

U.S. Brand Names:

Synonyms:

Generic Available:

Canadian Brand Names:

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:

Pregnancy Risk Factor:

Lactation:

Contraindications:

Warnings/Precautions:

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:

Drug Interactions:

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:

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:

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:

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:

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

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

Administration:

Monitoring Parameters:

Reference Range:

Patient Education:

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:

Dental Health: Effects on Dental Treatment:

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

Mental Health: Effects on Mental Status:

Mental Health: Effects on Psychiatric Treatment:

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)

International Brand Names: