Butorphanol (injection): Difference between revisions

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__NOTOC__
{{XXXXX}}
{{CMG}}; {{AE}} {{PB}}
'''''For patient information about XXXXX, click [[XXXXX (patient information)|here]].'''''
{{SB}} <sup>®</sup>,
==Overview==
{{drugbox |
{{drugbox |
|image=Butorphanol.svg
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==Overview==
'''Butorphanol''' ([[International Nonproprietary Name|INN]]) is a [[morphinan]]-type synthetic [[opioid]] [[analgesic]] marketed in the U.S. under the trade name '''Stadol'''.  It is most closely structurally related to [[dextromethorphan]].  Butorphanol is available only as butorphanol tartrate in injectable and intranasal spray formulations.
'''Butorphanol''' ([[International Nonproprietary Name|INN]]) is a [[morphinan]]-type synthetic [[opioid]] [[analgesic]] marketed in the U.S. under the trade name '''Stadol'''.  It is most closely structurally related to [[dextromethorphan]].  Butorphanol is available only as butorphanol tartrate in injectable and intranasal spray formulations.
==Category==
==FDA Package Insert==
'''  [[XXXXX indications and usage|Indications and Usage]]'''
'''| [[XXXXX dosage and administration|Dosage and Administration]]'''
'''| [[XXXXX dosage forms and strengths|Dosage Forms and Strengths]]'''
'''| [[XXXXX contraindications|Contraindications]]'''
'''| [[XXXXX warnings and precautions|Warnings and Precautions]]'''
'''| [[XXXXX adverse reactions|Adverse Reactions]]'''
'''| [[XXXXX drug interactions|Drug Interactions]]'''
'''| [[XXXXX use in specific populations|Use in Specific Populations]]'''
'''| [[XXXXX overdosage|Overdosage]]'''
'''| [[XXXXX description|Description]]'''
'''| [[XXXXX clinical pharmacology|Clinical Pharmacology]]'''
'''| [[XXXXX nonclinical toxicology|Nonclinical Toxicology]]'''
'''| [[XXXXX clinical studies|Clinical Studies]]'''
'''| [[XXXXX how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[XXXXX patient counseling information|Patient Counseling Information]]'''
'''| [[XXXXX labels and packages|Labels and Packages]]'''


== Mechanism of action ==
==Mechanism of Action==
Butorphanol exhibits partial agonist and [[Opioid antagonist|antagonist]] activity at the [[Opioid receptor#The μ-opioid receptor|μ]] [[Opioid receptor|opioid receptor]] and agonist activity at the [[Opioid receptor#The κ-opioid receptor|κ]] opioid receptor.<ref name=gear>{{cite journal | first = RW | last = Gear | coauthors = Miaskowski C, Gordon NC, Paul SM, Heller PH, Levine JD | year = 1999 | month = November | title = The kappa opioid nalbuphine produces gender- and dose-dependent analgesia and antianalgesia in patients with postoperative pain | journal = Pain | volume = 83 | issue = 2 | pages = 339-45 | id = PMID 10534607 | accessdate = 2007-02-12}}</ref>  Stimulation of these receptors on [[central nervous system]] [[neuron]]s causes an intracellular [[enzyme inhibitor|inhibition]] of [[adenylate cyclase]], closing of influx membrane [[voltage-dependent calcium channel|calcium channel]]s, and opening of membrane [[potassium channel]]s.  This leads to hyperpolarization of the cell [[membrane potential]] and suppression of action potential transmission of ascending pain pathways.
Butorphanol exhibits partial agonist and [[Opioid antagonist|antagonist]] activity at the [[Opioid receptor#The μ-opioid receptor|μ]] [[Opioid receptor|opioid receptor]] and agonist activity at the [[Opioid receptor#The κ-opioid receptor|κ]] opioid receptor.<ref name=gear>{{cite journal | first = RW | last = Gear | coauthors = Miaskowski C, Gordon NC, Paul SM, Heller PH, Levine JD | year = 1999 | month = November | title = The kappa opioid nalbuphine produces gender- and dose-dependent analgesia and antianalgesia in patients with postoperative pain | journal = Pain | volume = 83 | issue = 2 | pages = 339-45 | id = PMID 10534607 | accessdate = 2007-02-12}}</ref>  Stimulation of these receptors on [[central nervous system]] [[neuron]]s causes an intracellular [[enzyme inhibitor|inhibition]] of [[adenylate cyclase]], closing of influx membrane [[voltage-dependent calcium channel|calcium channel]]s, and opening of membrane [[potassium channel]]s.  This leads to hyperpolarization of the cell [[membrane potential]] and suppression of action potential transmission of ascending pain pathways.
Because of its κ-agonist activity, at analgesic doses butorphanol increases pulmonary arterial pressure and cardiac work.  Additionally, κ-agonism can cause [[dysphoria]] at therapeutic or supertherapeutic doses; this gives butorphanol a lower potential for abuse than other opioid drugs.
Because of its κ-agonist activity, at analgesic doses butorphanol increases pulmonary arterial pressure and cardiac work.  Additionally, κ-agonism can cause [[dysphoria]] at therapeutic or supertherapeutic doses; this gives butorphanol a lower potential for abuse than other opioid drugs.
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Butorphanol can cross the placenta, and it will be present in the milk of lactating mares who are given the drug.
Butorphanol can cross the placenta, and it will be present in the milk of lactating mares who are given the drug.


==References ==
==References ==
{{Reflist|2}}
<div class="references-small">
<div class="references-small">
* Katzung, Bertam G. (Ed.) (2001) ''Basic & Clinical Pharmacology'' (8th ed.). New York: McGraw-Hill. ISBN 0-8385-0598-8.
* Katzung, Bertam G. (Ed.) (2001) ''Basic & Clinical Pharmacology'' (8th ed.). New York: McGraw-Hill. ISBN 0-8385-0598-8.
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</div>
</div>


[[Antimigraine preparations]]
[[Category:Drugs]]
{{Analgesics}}
{{Analgesics}}
[[Category:Anesthesiology]]
[[Category:Anesthesiology]]

Revision as of 17:08, 12 February 2014


Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Pratik Bahekar, MBBS [2]

For patient information about XXXXX, click here.

Synonyms / Brand Names: ®,

Overview

Butorphanol (injection)
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Clinical data
Pregnancy
category
Routes of
administration		IV, intranasal
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityNasal: 60-70%
MetabolismHepatic hydroxylated & glucuronidated
Elimination half-life4-7 hours
ExcretionRenal, 75%
Biliary, 11-14%
Fecal, 15%
Identifiers
CAS Number
PubChem CID
DrugBank
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC21H29NO2
Molar mass327.473

Butorphanol (INN) is a morphinan-type synthetic opioid analgesic marketed in the U.S. under the trade name Stadol. It is most closely structurally related to dextromethorphan. Butorphanol is available only as butorphanol tartrate in injectable and intranasal spray formulations.

Category

FDA Package Insert

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

Mechanism of Action

Butorphanol exhibits partial agonist and antagonist activity at the μ opioid receptor and agonist activity at the κ opioid receptor.[1] Stimulation of these receptors on central nervous system neurons causes an intracellular inhibition of adenylate cyclase, closing of influx membrane calcium channels, and opening of membrane potassium channels. This leads to hyperpolarization of the cell membrane potential and suppression of action potential transmission of ascending pain pathways. Because of its κ-agonist activity, at analgesic doses butorphanol increases pulmonary arterial pressure and cardiac work. Additionally, κ-agonism can cause dysphoria at therapeutic or supertherapeutic doses; this gives butorphanol a lower potential for abuse than other opioid drugs.

Place in therapy

The most common indication for butorphanol is management of migraine using the intranasal spray formulation. It may also be used parenterally for management of moderate-to-severe pain, as a supplement for balanced general anesthesia, and management of pain during labor. Butorphanol is more effective in reducing pain in women than in men.[1]

Adverse effects

As with other opioid analgesics, central nervous system effects (such as sedation, confusion, and dizziness) are considerations with butorphanol. Nausea and vomiting are common. Less common are the gastrointestinal effects of other opioids (mostly constipation).

Proprietary preparations

Butorphanol is available in the U.S. as a generic drug; it is available in various nations under one of any number of trade names, including Moradol, Beforal, Stadol, and Stadol NS; veterinary trade names include Butorphic, Dolorex, Morphasol, Torbugesic, and Torbutrol.

Use in horses

Butorphanol is a commonly used narcotic for pain relief in horses. It is administered either IM or IV, with its analgestic properties beginning to take effect about 15 minutes after injection and lasting 4 hours. It is also commonly paired with sedatives, such as xylazine and detomidine, to make the horse easier to handle during veterinary proceedures.

Side effects, overdose, and precautions

Side effects specific to horses include sedation, CNS excitement (displayed by head pressing or tossing). Overdosing may result in seizures, falling, salivation, constipation, and muscle twitching. If an overdose occurs, a narcotic antagonist, such as naloxone, may be given. Caution should be used if Butorphanol is administered in addition to other narcotics, sedatives, depressants, or antihistamines as it will cause an additive effect.

Butorphanol can cross the placenta, and it will be present in the milk of lactating mares who are given the drug.


References

  1. ↑ 1.0 1.1 Gear, RW (1999). "The kappa opioid nalbuphine produces gender- and dose-dependent analgesia and antianalgesia in patients with postoperative pain". Pain. 83 (2): 339–45. PMID 10534607. Unknown parameter |month= ignored (help); Unknown parameter |coauthors= ignored (help); |access-date= requires |url= (help)
  • Katzung, Bertam G. (Ed.) (2001) Basic & Clinical Pharmacology (8th ed.). New York: McGraw-Hill. ISBN 0-8385-0598-8.
  • DiPiro, Joseph T. et al. (2005) Pharmacotherapy: A Pathophysiologic Approach (6th ed.). New York: McGraw-Hill. ISBN 0-07-141613-7.
  • Stadol NS - monograph
  • Forney, Barbara C, MS, VMD. Equine Medications, Revised Edition.' Blood Horse Publications. Lexington, KY. Copyright 2007.
  • The Merck Manual of Vetrinary Medicine, 2004 edition (English)
  • The Merck Manual, 2004 Edition (German)
  • Mosby's Drug Guide 2004
  • Various Usenet (alt.drugs.hard, alt.drugs.valium and rec.pets.cats) discussions about surgery on cats and a cat who was injured by being hit by am automobile.
  • Surgery-related episode from c.a. June 2004 of "The Crocodile Hunter" television programme, section on doing surgery on a crocodile and shortly thereafter a Fierce Snake -- specifically commentary by Steve Irwin on the dangers that most or all general anaesthetics pose to reptiles and amphibians.


Antimigraine preparations

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