Butorphanol (injection)

Butorphanol (injection)
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

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

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Overview

Butorphanol (injection) is an opioid agonist-opioid antagonist, analgesic that is FDA approved for the treatment of management of pain when the use of an opioid analgesic is appropriate.. Common adverse reactions include nausea, vomiting, dizziness, Insomnia, Sedation, Somnolence, nasal congestion and a long-term use of intranasal product.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Factors to be considered in determining the dose are age, body weight, physical status, underlying pathological condition, use of other drugs, type of anesthesia to be used, and surgical procedure involved. Use in the elderly and in patients with hepatic or renal disease requires extra caution. The following doses are for patients who do not have impaired hepatic or renal function and who are not on CNS active agents:

Management of Pain

• Dosage:
  • The usual recommended dose for initial nasal administration of butorphanol tartrate nasal solution is 1 mg (1 spray in one nostril). Adherence to this dose reduces the incidence of drowsiness and dizziness. If adequate pain relief is not achieved within 60 to 90 minutes, an additional 1 mg dose may be given.
  • The initial dose sequence outlined above may be repeated in 3 to 4 hours as required after the second dose of the sequence.
  • Depending on the severity of the pain, 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. In such patients single additional 2 mg doses should not be given for 3 to 4 hours.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Butorphanol in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Butorphanol in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding Butorphanol (injection) FDA-Labeled Indications and Dosage (Pediatric) in the drug label.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Butorphanol in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Butorphanol in pediatric patients.

Contraindications

Butorphanol tartrate nasal solution is contraindicated in patients hypersensitive to butorphanol tartrate or the preservative benzethonium chloride.

Warnings

Patients Dependent on Narcotics

Because of its opioid antagonist properties, butorphanol is not recommended for use in patients dependent on narcotics. Such patients should have an adequate period of withdrawal from opioid drugs prior to beginning butorphanol therapy. In patients taking opioid analgesics chronically, butorphanol has precipitated withdrawal symptoms such as anxiety, agitation, mood changes, hallucinations, dysphoria, weakness and diarrhea.

Because of the difficulty in assessing opioid tolerance in patients who have recently received repeated doses of narcotic analgesic medication, caution should be used in the administration of butorphanol to such patients.

Drug Abuse and Dependence

Drug Abuse: Butorphanol tartrate, by all routes of administration, has been associated with episodes of abuse. Of the cases received, there were more reports of abuse with the nasal solution formulation than with the injectable formulation.

Physical Dependence, Tolerance and Withdrawal

Prolonged, continuous use of butorphanol tartrate may result in physical dependence or tolerance (a decrease in response to a given dose). Abrupt cessation of use by patients with physical dependence may result in symptoms of withdrawal.

Note: Proper patient selection, dose and prescribing limitations, appropriate directions for use, and frequent monitoring are important to minimize the risk of abuse and physical dependence (see DRUG ABUSE AND DEPENDENCE).

Adverse Reactions

Clinical Trials Experience

A total of 2446 patients were studied in premarketing clinical trials of butorphanol. Approximately half received butorphanol tartrate injection with the remainder receiving butorphanol tartrate nasal solution. In nearly all cases the type and incidence of side effects with butorphanol by any route were those commonly observed with opioid analgesics.

The adverse experiences described below are based on data from short-term and long-term clinical trials in patients receiving butorphanol by any route. There has been no attempt to correct for placebo effect or to subtract the frequencies reported by placebo-treated patients in controlled trials. The most frequently reported adverse experiences across all clinical trials were somnolence (43%), dizziness (19%), nausea and/or vomiting (13%). In long-term trials with butorphanol tartrate nasal solution only, nasal congestion (13%) and insomnia (11%) were frequently reported.

The following adverse experiences were reported at a frequency of 1% or greater in clinical trials, and were considered to be probably related to the use of butorphanol:

Body as a Whole

• Asthenia/lethargy
• Headache
• Sensation of heat

Cardiovascular

• Vasodilation
• Palpitations

Digestive

• Anorexia
• Constipation
• Dry mouth
• Nausea and/or vomiting
• Stomach pain

Nervous

• Anxiety
• Confusion
• Dizziness
• Euphoria
• Floating feeling
• Insomnia
• Nervousness
• Paresthesia
• Somnolence
• Tremor

Respiratory

• Bronchitis
• Cough
• Dyspnea
• Epistaxis
• Nasal congestion
• Nasal irritation
• Pharyngitis
• Rhinitis
• Sinus congestion
• Sinusitis
• Upper respiratory infection

Skin and Appendages

• Sweating/clammy
• Pruritus

Special Senses

• Blurred vision
• Ear pain
• Tinnitus
• Unpleasant taste

The following adverse experiences were reported with a frequency of less than 1% in clinical trials, and were considered to be probably related to the use of butorphanol:

Cardiovascular

• Hypotension
• Syncope

Nervous

• Abnormal dreams
• Agitation
• Dysphoria
• Hallucinations
• Hostility
• Withdrawal symptoms

Skin and Appendages

• Rash/hives

Urogenital: impaired urination

Postmarketing Experience

There is limited information regarding Butorphanol (injection) Postmarketing Experience in the drug label.

Drug Interactions

There is limited information regarding Butorphanol (injection) Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): There is no FDA guidance on usage of Butorphanol (injection) in women who are pregnant.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Butorphanol (injection) in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Butorphanol (injection) during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Butorphanol (injection) in women who are nursing.

Pediatric Use

There is no FDA guidance on the use of Butorphanol (injection) in pediatric settings.

Geriatic Use

There is no FDA guidance on the use of Butorphanol (injection) in geriatric settings.

Gender

There is no FDA guidance on the use of Butorphanol (injection) with respect to specific gender populations.

Race

There is no FDA guidance on the use of Butorphanol (injection) with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Butorphanol (injection) in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Butorphanol (injection) in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Butorphanol (injection) in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Butorphanol (injection) in patients who are immunocompromised.

Administration and Monitoring

Administration

There is limited information regarding Butorphanol (injection) Administration in the drug label.

Monitoring

There is limited information regarding Butorphanol (injection) Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Butorphanol (injection) and IV administrations.

Overdosage

There is limited information regarding Butorphanol (injection) overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.

Pharmacology

There is limited information regarding Butorphanol (injection) Pharmacology in the drug label.

Mechanism of Action

There is limited information regarding Butorphanol (injection) Mechanism of Action in the drug label.

Structure

There is limited information regarding Butorphanol (injection) Structure in the drug label.

Pharmacodynamics

There is limited information regarding Butorphanol (injection) Pharmacodynamics in the drug label.

Pharmacokinetics

There is limited information regarding Butorphanol (injection) Pharmacokinetics in the drug label.

Nonclinical Toxicology

There is limited information regarding Butorphanol (injection) Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Butorphanol (injection) Clinical Studies in the drug label.

How Supplied

There is limited information regarding Butorphanol (injection) How Supplied in the drug label.

Storage

There is limited information regarding Butorphanol (injection) Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Butorphanol (injection) Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Butorphanol interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Butorphanol (injection) Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Butorphanol (injection) Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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. [3]; Associate Editor(s)-in-Chief: Pratik Bahekar, MBBS [4]

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	C/D (U.S.)
Routes of administration	IV, intranasal
ATC code	N02AX02 (WHO)
Legal status
Legal status	US: Schedule IV
Pharmacokinetic data
Bioavailability	Nasal: 60-70%
Metabolism	Hepatic hydroxylated & glucuronidated
Elimination half-life	4-7 hours
Excretion	Renal, 75% Biliary, 11-14% Fecal, 15%
Identifiers
IUPAC name 17-cyclobutylmethyl- morphinan-3,14-diol
CAS Number	42408-82-2
PubChem CID	5361092
DrugBank	APRD00835
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C21H29NO2
Molar mass	327.473

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.

BUTORPHANOL TARTRATE spray

| 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. 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.

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. Normal 0 false false false EN-US X-NONE X-NONE Normal 0 false false false EN-US X-NONE X-NONE

References

• 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