Dosing & Uses
Dosage Forms & Strengths
injectable solution: Schedule IV
- 1mg/mL
- 2mg/mL
nasal spray: Schedule IV
- 10 mg/mL (1mg/spray)
Pain
Indicated for pain when use of opioid analgesic is appropriate
IV: 1 mg IV q3-4hr PRN; dosage range 0.5-2 mg q3-4hr
IM: 2 mg IM q3-4 hr; dosage range 1-4 mg q3-4hr
Intranasal
- Initial: 1 mg (1 spray in 1 nostril); may repeat once after 60-90 min if inadequate pain relief
- Depending on pain severity, by give initial dose of 2 mg (1 spray in each nostril); patient must remain recumbant; do not repeat this dose
- Maintenance: 1 mg (1 spray in 1 nostril) q3-4hr prn
Balanced Anesthesia
2 mg IV before induction and/or 0.5-1 mg increments during anesthesia (higher dose may be required, up to 0.06 mg/kg, or 4 mg/70 kg)
Total cumulative dose varies; typically ranges between 4-12.5 mg (0.06-0.18 mg/kg)
Labor Pain
Indicated for labor pain in full-term (37 weeks gestation or more) women without fetal distress in early labor
1-2 mg/dose IV/IM; may repeat PRN q4hr
Decrease dose if concomitantly used with other analgesics or CNS depressants
Do not administer within 4 hr of anticipated delivery
Preoperative & Preanesthesia
2 mg IM 60-90 minutes preop
This dose is approximately equipotent to morphine 10 mg or meperidine 80 mg
Renal & Hepatic Impairment
Decrease initial dose by 50% (0.5 mg IV and 1 mg IM)
Increase dose interval from q4hr to q6hr
Intranasal
- 1 mg (1 spray in 1 nostril) initially, may repeat once after 90-120 minutes if inadequate pain control
- Maintenance: 1 mg (1 spray in 1 nostril) q4-6hr prn
<18 years old: Not recommended
Pain
Decrease initial dose by 50% (0.5 mg IV and 1 mg IM)
Increase dose interval from q4hr to q6hr
Intranasal
- 1 mg (1 spray in 1 nostril) initially, may repeat once after 90-120 minutes if inadequate pain control
- Maintenance: 1 mg (1 spray in 1 nostril) q4-6hr prn
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Sedation (43%)
Dizziness (19%)
Nasal congestion (13%)
Nausea and/or vomiting (13%)
Insomnia (11%)
1-10%
Anorexia
Anxiety
Blurred vision
Bronchitis
Confusion
Constipation
Cough
Dizziness
Dry mouth
Dyspnea
Ear pain
Epistaxis
Euphoria
Floating feeling
Headache
Lethargy
Nasal irritation
Nervousness
Paresthesia
Palpitations
Pharyngitis
Pruritis
Rhinitis
Sensation of heat
Sinus congestion
Sinusitis
Stomach pain
Sweating/clammy
Taste abnormalities
Tinnitus
Tremor
URI
Vasodilation
<1%
Apnea
Increased/decreased BP
Bradycardia
Chest pain
Respiratory depression
Tachycardia
Warnings
Contraindications
Absolute: opioid dependence, respiratory depression, respiratory failure
Relative: cardiac arrhythmias, cardiovascular disease, coronary insufficiency, myocardial infarction, toxin-mediated diarrhea
Cautions
Drug abuse, emotional lability, head injury, hepatic/renal impairment, incr ICP, GI/urinary obstruction, BPH, hypothyroidism
Less risk of respiratory sedation than with pure opioid agonist
May produce withdrawal in opioid dependent pts
Avoid alcohol
Pregnancy & Lactation
Pregnancy Category: C; D if used for prolonged periods or near term
Lactation: excreted in breast milk, but infant likely exposed to insignificant amounts (AAP Committee states compatible w/ nursing)
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Narcotic agonist-analgesic of kappa opiate receptors and partial agonist of mu opiate receptors; inhibits ascending pain pathways, which causes alteration in response to pain; produces analgesia, respiratory depression, and sedation
Pharmacokinetics
Half-life: 4.6 hr
Onset: <10 min (IV); 5-10 min (IM); within 15 min (nasal)
Duration: 3-4 hr (IV/IM); 4-5hr (nasal);
Peak effect: 0.5-1hr (IM); 4-5min (IV)
Bioavailability: 60-70% (nasal)
Protein Bound: 80%
Vd: 487 L (range: 305-901 L)
Metabolites: hydroxybutorphanol; N-dealkylation & conjugation of butorphanol & its metabolites)
Metabolism: Liver (hydroxylation)
Excretion: Urine (primarily)
Administration
IV Compatibilities
Syringe: (partial list) atropine, diphenhydramine, fentanyl, hydroxyzine, meperidine, metoclopramide, midazolam, prochlorperazine, promethazine
Y-site: (partial list) allopurinol, bivalirudin, labetalol, linezolid, propofol
IV Incompatibilities
Syringe: dimenhydrinate, pentobarbital
Y-site: amphotericin B cholesteryl SO4, midazolam
IV Administration
pH: 3.0-5.5
IM/IV injection
Storage
Store at room temp
Protect from freezing
Images
Patient Handout
Formulary
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To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
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- Compare formulary status to other drugs in the same class.
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