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Butorphanol

 
Drug Info: Butorphanol
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Brand names: Stadol®, Stadol® NS®

Chemical formula:



Butorphanol Tartrate Solution for injection

What is this medicine?

BUTORPHANOL is a pain reliever. It is used to treat moderate to severe pain. It is also used to prevent pain before surgery and during child birth.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

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

They need to know if you have any of these conditions:
• brain tumor
• drug abuse or addiction
• head injury
• heart disease
• if you frequently drink alcohol containing drinks
• kidney disease
• liver disease
• lung or breathing disease, like asthma
• an allergic reaction to butorphanol, benzethonium chloride, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I use this medicine?

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

If you get this medicine at home, you will be taught how to prepare and give this medicine. Use exactly as directed. Take your medicine at regular intervals. Do not take your medicine more often than directed.

It is important that you put your used needles and syringes in a special sharps container. Do not put them in a trash can. If you do not have a sharps container, call your pharmacist or healthcare provider to get one.

Talk to your pediatrician regarding the use of this medicine in children. This medicine is not approved for use in children.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
• buprenorphine
• nalbuphine
• pentazocine

This medicine may also interact with the following medications:
• alcohol
• antihistamines for allergy, cough and cold
• barbiturates, like phenobarbital
• medicines for depression, anxiety, or psychotic disturbances
• medicines for pain like tramadol and propoxyphene
• medicines for sleep

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Tell your doctor or health care professional if your pain does not go away, if it gets worse, or if you have new or a different type of pain. You may develop tolerance to the medicine. Tolerance means that you will need a higher dose of the medicine for pain relief. Tolerance is normal and is expected if you take the medicine for a long time.

Do not suddenly stop taking your medicine because you may develop a severe reaction. Your body becomes used to the medicine. This does NOT mean you are addicted. 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. Your doctor will tell you how much medicine to take. If your doctor wants you to stop the medicine, the dose will be slowly lowered over time to avoid any side effects.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• anxiety, nervousness, agitation
• breathing problems
• changes in vision
• confusion
• feeling faint or lightheaded, falls
• irregular or pounding heartbeat
• ringing in the ears

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
• difficulty sleeping at night
• dizziness
• drowsiness
• dry mouth
• loss of appetite
• nausea, vomiting
• pain at site where injected

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children. This medicine can be abused. Keep your medicine in a safe place to protect it from theft. Do not share this medicine with anyone. Selling or giving away this medicine is dangerous and against the law.

If you are using this medicine at home, you will be instructed on how to store this medicine. Throw away any unused medicine after the expiration date on the label.

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.

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Wikipedia: Butorphanol
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Home > Library > Miscellaneous > Wikipedia
Butorphanol
Systematic (IUPAC) name
17-cyclobutylmethyl-morphinan-3,14-diol
Identifiers
CAS number 42408-82-2
ATC code N02AX02 QR05DA90
PubChem 5361092
DrugBank APRD00835
Chemical data
Formula C21H29NO2 
Mol. mass 327.473 g/mol
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. Brand name Stadol was recently discontinued by the manufacturer. It is now only available in its generic formulations, manufactured by Novex, Mylan, Apotex and Roxane. Butorphanol is most closely structurally related to levorphanol. Butorphanol is available only as butorphanol tartrate in injectable and intranasal spray formulations.

Contents

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 may be combined with tranquilizers such as alpha-2 agonists (medetomidine (Domitor)), benzodiazepines, or phenothiazines (acepromazine) in dogs, cats and exotic animals. It is frequently combined with xylazine or 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 and Beforal (Brand name Stadol no longer available in the US); 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 procedures.

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.

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

In addition to horses, butorphanol with or without acepromazine is frequently used in veterinary settings for post-operative and accident-related pain in small mammals such as dogs, cats, ferrets, coatis, raccoons, mongooses, various marsupials, some rodents and perhaps some larger birds both in the operating suite and as a regular prescription medication for home use for management of moderate to severe pain. The efficacy of opioids (as well as other drugs that slow down the system like anaesthetics) in treating reptiles is a question about which there is currently not a lot of data.

Notes

  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. doi:10.1016/S0304-3959(99)00119-0. PMID 10534607. 
  2. ^ NOAH Compendium of Data Sheets for Animal Medicines 2005

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
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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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Butorphanol Tartrate Solution for injection
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