Butorphanol (injection)

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Butorphanol
BUTORPHANOL TARTRATE spray® 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
Butorphanol tartrate (butorphanol tartrate) injection, solution® 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
Clinical Trials on Butorphanol
ClinicalTrials.gov

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

For patient information about Butorphanol, click here.

Synonyms / Brand Names: BUTORPHANOL TARTRATE(butorphanol tartrate )solution [Apotex Corp.]®,Butorphanol tartrate (butorphanol tartrate injection, solution [Apotex Inc.]®, BUTORPHANOL TARTRATE injection, solution [West-ward Pharmaceutical Corp]®

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}}
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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

BUTORPHANOL TARTRATE spray Normal 0 false false false EN-US X-NONE X-NONE

FDA Package Insert

| 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

Butorphanol tartrate (butorphanol tartrate) injection, solution

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.[2] Normal 0 false false false EN-US X-NONE X-NONE [3] Normal 0 false false false EN-US X-NONE X-NONE

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)
  2. ↑ "BUTORPHANOL TARTRATE SPRAY [MYLAN PHARMACEUTICALS INC.]".
  3. ↑ "Butorphanol tartrate (butorphanol tartrate INJECTION, SOLUTION [APOTEX INC.]".
  • 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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