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Drug Info:

Butorphanol

Brand names: Stadol®



Butorphanol injection

What is butorphanol injection?

BUTORPHANOL (Stadol®) relieves moderate to severe pain. Butorphanol decreases the pain of migraine headaches, and labor and delivery. It can help to supplement anesthesia when given before surgery. Do not share this medicine with anyone else. Federal law prohibits the transfer of butorphanol to any person other than the patient for whom it was prescribed. Generic butorphanol injections are available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• If you frequently drink alcohol-containing beverages
• constipation
• head injury
• heart disease
• intestinal disease, such as inflammatory bowel disease or ulcerative colitis
• liver disease
• lung disease, such as asthma or COPD
• kidney disease
• an allergic or unusual reaction to butorphanol, codeine, morphine, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I use this medicine?

Butorphanol is for injection into a muscle or a vein. It is usually given by a health-care professional in a hospital or clinic setting.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What if I miss a dose?

This does not apply.

What drug(s) may interact with butorphanol?

Because butorphanol can cause drowsiness, other medicines that also cause drowsiness may increase this effect of butorphanol. Some medicines that cause drowsiness are:
• alcohol and alcohol-containing medicines
• barbiturates such as phenobarbital
• certain antidepressants, tranquilizers or medications for Parkinson's disease
• muscle relaxants
• certain antihistamines used in cold medicines
Ask your prescriber or health care professional about other medicines that may increase the effect of butorphanol.

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking butorphanol?

Tell your prescriber or health care professional if your pain does not go away, if it gets worse, or if you have new or different type of pain.

Use exactly as directed by your prescriber or health care professional. If you are taking butorphanol on a regular basis, do not suddenly stop taking it. Your body becomes used to the butorphanol, and when you suddenly stop taking it, you may develop a severe reaction. This DOES NOT mean you are "addicted" to butorphanol. Addiction is a behavior related to getting and using a drug for a non-medical reason. If you have pain, you have a medical reason to take pain medicine such as butorphanol to control your pain.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how butorphanol affects you. Do not sit or stand up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol can increase possible drowsiness, dizziness, or confusion and can affect your breathing. Avoid alcohol while receiving butorphanol.

If you are going to have surgery, tell your prescriber or health care professional that you are using butorphanol.

What side effects may I notice from receiving butorphanol?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• anxiety, nervousness, agitation
• chest infection
• cold and clammy skin, increased perspiration
• confusion
• difficulty breathing
• lightheadedness or fainting spells
• irregular heartbeat, palpitations
• ringing in the ears

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• change in taste
• constipation
• difficulty sleeping at night
• dizziness or drowsiness
• dry mouth
• headache
• loss of appetite
• nausea, vomiting
• pain or difficulty passing urine, reduced amount of urine
• pain, swelling or irritation at the injection site
• stomach cramps or pain
• tremor

Where can I keep my medicine?

This does not apply.


Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

 
 
Wikipedia: butorphanol
Butorphanol.svg
Butorphanol
Systematic (IUPAC) name
17-cyclobutylmethyl-
morphinan-3,14-diol
Identifiers
CAS number 42408-82-2
ATC code N02AX02
PubChem 5361092
DrugBank APRD00835
Chemical data
Formula C21H29NO2 
Mol. mass 327.473
Pharmacokinetic data
Bioavailability Nasal: 60-70%
Metabolism Hepatic hydroxylated & glucuronidated
Half life 4-7 hours
Excretion Renal, 75%
Biliary, 11-14%
Fecal, 15%
Therapeutic considerations
Pregnancy cat.

C/D (U.S.)
Legal status

Schedule IV(US)
Routes IV, intranasal

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.

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]

In veterinary use, butorphanol ("Torbugesic") is widely used as a sedative and analgesic in dogs, cats and horses. For sedation, it is often combined with medetomidine(Domitor) in dogs, cats and detomidine (Domosedan etc) in horses[2].

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 xylaxine ad 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, consitipation, 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.

The drug is also prohibited for use in competition by most equestrian organizations, including the FEI, which considers it a class A drug.

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.
  1. ^ a b Gear, RW; Miaskowski C, Gordon NC, Paul SM, Heller PH, Levine JD (November 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. Retrieved on 2007-02-12. 
  2. ^ NOAH Compendium of Data Sheets for Animal Medicines 2005
Analgesics (N02A, N02B)
Opioids Buprenorphine, Butorphanol, Codeine, Dextropropoxyphene, Diamorphine, Dihydrocodeine, Fentanyl, Hydrocodone, Hydromorphone, Ketobemidone, Levorphanol, Methadone, Morphine, Nicomorphine, Opium, Oxycodone, Oxymorphone, Pethidine, Tramadol, Tapentadol
Salicylic acid and derivatives Aspirin (Acetylsalicylic Acid), Diflunisal, Ethenzamide, Salicin, Salicylamide -- See also: NSAIDs
Pyrazolones Aminophenazone, Metamizole, Phenazone
Cannabinoids Cannabis, Tetrahydrocannabinol, AM404
Anilides Paracetamol (acetaminophen), Phenacetin
Others Ziconotide, Ibuprofen, Ketoprofen, Mefenamic Acid, Naproxen, Diclofenac, Flurbiprofen, Diflunisal, Indomethacin, Ketorolac, Meloxicam, Piroxicam

This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)

 
 

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Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Wikipedia. This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Butorphanol".  Read more

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