Butorphanol (injection): Difference between revisions
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{{DrugProjectFormSinglePage | |||
|authorTag={{AP}} | |||
|genericName=Butorphanol tartrate | |||
|aOrAn=an | |||
|drugClass=[[opioid agonist]]-[[opioid antagonist]], [[analgesic]] | |||
|indicationType=treatment | |||
|indication=management of [[pain]] when the use of an [[opioid analgesic]] is appropriate. | |||
|adverseReactions=[[nausea]], [[vomiting]], [[dizziness]], [[Insomnia]], [[Sedation]], [[Somnolence]], [[nasal congestion]] and a [[long-term use of intranasal product]] | |||
|blackBoxWarningTitle=<b><span style="color:#FF0000;">What Is The Most Important Information I Should Know About Butorphanol Tartrate Nasal Solution?</span></b> | |||
|blackBoxWarningBody=<i><span style="color:#FF0000;">Condition Name:</span></i> Your doctor has prescribed butorphanol tartrate nasal solution to treat your pain. The medication in butorphanol tartrate nasal solution belongs to a group of medicines that is known to cause dependence and abuse. Butorphanol tartrate nasal solution causes these effects only in a small number of patients. However, because it can have these effects, it is VERY IMPORTANT that you not use butorphanol tartrate nasal solution more often or in larger doses than your doctor has instructed. Also, it is important to have regular checkups with your doctor to ensure that you're using butorphanol tartrate nasal solution correctly. The longer you use butorphanol tartrate nasal solution, the greater your risk of getting dependent on it. | |||
Because butorphanol tartrate nasal solution may make you feel sleepy or dizzy, do not drive or operate dangerous machinery, e.g., automobiles until you can no longer feel the effects of the drug. Also, do not drink alcohol while using butorphanol tartrate nasal solution because it may worsen any side effects. | |||
|fdaLIADAdult=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. | |||
|offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Butorphanol in adult patients. | |||
|offLabelAdultNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of Butorphanol in adult patients. | |||
|offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Butorphanol in pediatric patients. | |||
|offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> 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). | |||
|alcohol=Alcohol-Butorphanol interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication. | |||
}} | |||
__NOTOC__ | __NOTOC__ | ||
{{ Butorphanol}} | {{ Butorphanol}} | ||
Revision as of 17:36, 16 January 2015
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Alberto Plate [2]
Disclaimer
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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
There is limited information regarding Butorphanol (injection) Clinical Trials Experience in the drug label.
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
{{#ask: Page Name::Butorphanol (injection) |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}
Package and Label Display Panel
{{#ask: Label Page::Butorphanol (injection) |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}
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
| Error creating thumbnail: File missing | |
| Clinical data | |
|---|---|
| Pregnancy category |
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| Routes of administration | IV, intranasal |
| ATC code | |
| Legal status | |
| Legal status |
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| 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 | |
| |
| 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 | |
| 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.
Category
FDA Package Insert
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.[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
- ↑ 1.0 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) - ↑ "BUTORPHANOL TARTRATE SPRAY [MYLAN PHARMACEUTICALS INC.]".
- ↑ "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.
- Pages with script errors
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- Drugs
- Anesthesiology