Adult: As metered-dose spray: Initially, 1 mg (1 spray in 1 nostril), repeated after 60-90 min if needed; sequence may be repeated after 3-4 hr when necessary. Severe pain: 2 mg (1 spray into each nostril), may only be repeated after 3-4 hr. Elderly: Initially, 1 mg, repeated after 90-120 min if needed. Subsequent doses may be given if necessary at intervals of ≥6 hr.
Parenteral Moderate to severe pain
Adult: 1-4 mg via IM inj or 0.5-2 mg via IV inj, repeated after 3-4 hr if necessary. Elderly: Initiate at half the usual dose. Adjust subsequent doses according to response at intervals of ≥6 hr.
Parenteral Anaesthesia
Adult: As premedication: 2 mg via IM inj 60-90 min prior to surgery. As balanced anaesth: 2 mg via IV inj before induction and/or 0.5-1 mg in increments during anaesth.
Parenteral Obstetric analgesia
Adult: 1-2 mg via IM or IV inj during early labour, may be repeated after 4 hr, if necessary.
Renal Impairment
Moderate to severe pain Parenteral: Initiate at half the usual dose. Adjust subsequent doses according to response at intervals of ≥6 hr. Nasal: Initially, 1 mg, repeated after 90-120 min if needed. Subsequent doses may be given if necessary at intervals of ≥6 hr.
Hepatic Impairment
Moderate to severe pain Parenteral: Initiate at half the usual dose. Adjust subsequent doses according to response at intervals of ≥6 hr. Nasal: Initially, 1 mg, repeated after 90-120 min if needed. Subsequent doses may be given if necessary at intervals of ≥6 hr.
Significant resp depression, unmonitored acute or severe brochial asthma.
Special Precautions
Patient w/ head injury, increased intracranial pressure, acute MI, ventricular dysfunction, coronary insufficiency, adrenal insufficiency, biliary tract dysfunction, CNS depression, prostatic hyperplasia, hypercapnia/hypoxia, COPD, thyroid dysfunction; obese patients and those at risk for drug abuse. Renal and hepatic impairment. Elderly. Pregnancy (may cause neonatal opioid withdrawal syndrome in prolonged use during pregnancy) and lactation.
This drug may cause drowsiness and dizziness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor pain relief, resp and mental status, BP, signs and symptoms of hypogonadism or hypoadrenalism.
Overdosage
Symptoms: Resp depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, and, in some cases, pulmonary oedema, bradycardia, hypotension, partial or complete airway obstruction, atypical snoring. Management: Supportive treatment. Immediate IV admin of an opiate antagonist (e.g. naloxone or nalmefene) as specific antidote. Administer oxygen, IV fluids and vasopressors as necessary.
Drug Interactions
Additive effect w/ other CNS depressants (e.g. general anaesth, phenothiazines or other tranquilizers, sedatives, hypnotics, antihistamines). May increase risk of transient high BP when used w/ sumatriptan nasal spray. Increased conjunctival changes when used w/ pancuronium. Decreased rate of absorption when used w/ oxymetazoline (nasal).
Food Interaction
Additive CNS depressant effect w/ alcohol.
Action
Description: Mechanism of Action: Butorphanol is a phenanthrene derivative w/ mixed opioid agonist and antagonist effect. It causes inhibition of ascending pain pathways, thus alters the perception of and response to pain. It also produces resp depression and sedation similar to opioids. Onset: ≤15 min (IM, nasal). Duration: 3-4 hr (IV, IM); 4-5 hr (nasal). Pharmacokinetics: Absorption: Rapidly and well absorbed. Bioavailability: 60-70% (nasal). Time to peak plasma concentration: 0.5-1 hr (IM, IV); 1-2 hr (nasal). Distribution: Crosses the placenta and enters breast milk. Volume of distribution: 305-901 L. Plasma protein binding: Approx 80%. Metabolism: Metabolised hepatically to hydroxybutorphanol as major metabolite. Excretion: Via urine (approx 70-80%, 5% as unchanged); faeces (approx 15%). Elimination half-life: Approx 2-9 hr (IV, nasal).
Chemical Structure
Butorphanol Source: National Center for Biotechnology Information. PubChem Database. Butorphanol, CID=5361092, https://pubchem.ncbi.nlm.nih.gov/compound/Butorphanol (accessed on Jan. 22, 2020)
N02AF01 - butorphanol ; Belongs to the class of morphinan derivative opioids. Used to relieve pain.
References
Anon. Butorphanol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/09/2016.Buckingham R (ed). Butorphanol Tartrate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/09/2016.Butorphanol Tartrate Injection, Solution (Hospira Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 01/09/2016.Butorphanol Tartrate Solution (Apotex Corp). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 01/09/2016.Butorphanol Tartrate Spray, Metered (Roxane Laboratories, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 01/09/2016.McEvoy GK, Snow EK, Miller J et al (eds). Butorphanol Tartrate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 01/09/2016.
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