Butorphanol

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What is Butorphanol?[edit | edit source]

  • Butorphanol (Stadol) is an opioid agonist-antagonist of the phenanthrene series used to relieve moderate to severe pain.
  • Butorphanol is available as the tartrate salt in injectable, tablet, and intranasal spray formulations.
  • The tablet form is only used in dogs, cats and horses due to low bioavailability in humans.
  • Butorphanol Tartrate Nasal Spray (Stadol NS) is indicated for the management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate.
  • Butorphanol injection is also used to relieve pain during labor and to prevent pain and decrease awareness before or during surgery.
  • Butorphanol has a lower potential for physical and psychological dependency than morphine, fentanyl and oxycodone and is classified as a Schedule IV drug, indicating that it has medical usefulness, and only a low potential for physical and psychological dependency and abuse.
Butorphanol structure
Butorphanol molecule ball
Butorphanol2DCSD



What are the uses of this medicine?[edit | edit source]

Butorphanol (Stadol) Injection is indicated:


How does this medicine work?[edit | edit source]

  • Butorphanol (bue tor’ fa nol) is a fully synthetic opioid that has both partial agonist and partial antagonist activity to the µ type opiate receptors, as well as antagonist and partial agonist activity at the ĸ opioid receptor.
  • Engagement of the opiate receptors results in inhibition of intracellular adenylate cyclase, decrease in calcium influx and hyperpolarization of neurons with suppression of action potentials.
  • These actions lead to typical analgesic effects of the opioids.
  • The partial agonist-antagonist activity of butorphanol causes it to antagonize the effects of fully agonist opioids such as morphine and fentanyl, and higher doses of butorphanol do not provide the euphoria typical of full agonists.


Who Should Not Use this medicine ?[edit | edit source]

This medicine cannot be used in patients with:

Limitations of use:

  • Indications for the parenteral forms of butorphanol include moderate-to-severe pain that is not responsive to nonnarcotic analgesia.


What drug interactions can this medicine cause?[edit | edit source]

  • Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:


Is this medicine FDA approved?[edit | edit source]

  • Butorphanol was first approved for use in the United States in 1978.
  • It remains available as a solution for injection as well as nasal spray (typically for migraine headaches).


How should this medicine be used?[edit | edit source]

Recommended dosage: Use for Pain:

  • Intravenous: The usual recommended single dose for IV administration is 1 mg repeated every 3 to 4 hours as necessary. The effective dosage range, depending on the severity of pain, is 0.5 to 2 mg repeated every 3 to 4 hours.
  • Intramuscular: The usual recommended single dose for IM administration is 2 mg in patients who will be able to remain recumbent, in the event drowsiness or dizziness occurs. This may be repeated every 3 to 4 hours, as necessary. The effective dosage range depending on the severity of pain is 1 to 4 mg repeated every 3 to 4 hours. There are insufficient clinical data to recommend single doses above 4 mg.

Use as Preoperative/Preanesthetic Medication:

  • The usual adult dose is 2 mg IM, administered 60 to 90 minutes before surgery.
  • This is approximately equivalent in sedative effect to 10 mg morphine or 80 mg meperidine.

Use in Balanced Anesthesia:

  • The usual dose of Butorphanol Tartrate Injection is 2 mg IV shortly before induction and/or 0.5 mg to 1 mg IV in increments during anesthesia.

Labor:

  • In patients at full term in early labor a 1 to 2 mg dose of Butorphanol Tartrate Injection IV or IM may be administered and repeated after 4 hours.
  • Alternative analgesia should be used for pain associated with delivery or if delivery is expected to occur within 4 hours.
  • When a patient who has been taking Butorphanol Tartrate Injection regularly and may be physically dependent no longer requires therapy with Butorphanol Tartrate Injection, taper the dose gradually, by 25% to 50% every 2 to 4 days, while monitoring carefully for signs and symptoms of withdrawal.

Administration:

  • Butorphanol injection comes as a liquid to be injected into a muscle or vein.
  • When butorphanol injection is used to relieve pain, it is usually given once every 3 to 4 hours as needed.
  • When butorphanol injection is used to relieve pain during surgery, it may be given 60 to 90 minutes before surgery and then as needed during the surgery. When butorphanol injection is used to relieve pain during labor, it may be given once every 4 hours but should not be given less than 4 hours before delivery is expected.
  • You may receive butorphanol injection in a hospital, or you may be given the medication to use at home.
  • If you have been told to administer butorphanol injection at home, it is very important that you use the medication exactly as directed.
  • If you have been told to use butorphanol injection at home, do not stop using the medication without talking to your doctor.
  • If you suddenly stop using butorphanol injection, you may experience withdrawal symptoms such as nervousness, agitation, shakiness, diarrhea, chills, sweats, difficulty falling asleep or staying asleep, confusion, loss of coordination, or hallucinations (seeing things or hearing voices that do not exist).
  • Your doctor will probably decrease your dose gradually.


What are the dosage forms and brand names of this medicine?[edit | edit source]

This medicine is available in fallowing doasage form:

  • As Butorphanol Tartrate Injection, USP

This medicine is available in fallowing brand namesː

  • Stadol


What side effects can this medication cause?[edit | edit source]

The most common side effects of this medicine include:

Less common side effects may include:


What special precautions should I follow?[edit | edit source]

  • As an opioid, Butorphanol Tartrate Injection exposes users to the risks of addiction, abuse, and misuse. Assess each patient’s risk for opioid addiction, abuse, or misuse prior to prescribing Butorphanol Tartrate Injection, and monitor all patients receiving Butorphanol Tartrate Injection for the development of these behaviors or conditions.
  • Serious, life-threatening, or fatal respiratory depression has been reported with the use of opioids, even when used as recommended. Management of respiratory depression may include close observation, supportive measures, and use of opioid antagonists, depending on the patient’s clinical status. Monitor patients closely for respiratory depression, especially within the first 24 to 72 hours of initiating therapy with and following dosage increases of Butorphanol Tartrate Injection. To reduce the risk of respiratory depression, proper dosing and titration of Butorphanol Tartrate Injection are essential.
  • Opioids can cause sleep-related breathing disorders including central sleep apnea (CSA) and sleep-related hypoxemia. In patients who present with CSA, consider decreasing the opioid dosage using best practices for opioid taper.
  • Prolonged use of Butorphanol Tartrate Injection during pregnancy can result in withdrawal in the neonate. Advise pregnant women using opioids for a prolonged period of the risk of neonatal opioid withdrawal syndrome and ensure that appropriate treatment will be available.
  • Profound sedation, respiratory depression, coma, and death may result from the concomitant use of Butorphanol Tartrate Injection with benzodiazepines or other CNS depressants.
  • Life-threatening respiratory depression is more likely to occur in elderly, cachectic, or debilitated patients. Monitor such patients closely, particularly when initiating and titrating Butorphanol Tartrate Injection and when Butorphanol Tartrate Injection is given concomitantly with other drugs that depress respiration.
  • Opioids may also obscure the clinical course in a patient with a head injury. Avoid the use of Butorphanol Tartrate Injection in patients with impaired consciousness or coma.
  • Butorphanol Tartrate Injection is contraindicated in patients with gastrointestinal obstruction, including paralytic ileus.
  • The butorphanol in Butorphanol Tartrate Injection may increase the frequency of seizures in patients with seizure disorders. Monitor patients with a history of seizure disorders for worsened seizure control during Butorphanol Tartrate Injection therapy.
  • When discontinuing Butorphanol Tartrate Injection, gradually taper the dosage. Do not abruptly discontinue Butorphanol Tartrate Injection.
  • Severe hypertension has been reported rarely during butorphanol therapy. In such cases, butorphanol should be discontinued and the hypertension treated with antihypertensive drugs. In patients who are not opioid dependent, naloxone has also been reported to be effective.
  • Butorphanol injection may make you drowsy and dizzy. Do not drive a car or operate machinery for at least one hour after you receive a dose. After one hour has passed, do not drive until you are certain that you are not dizzy, drowsy, or less alert than usual.
  • Inform patients that opioids could cause a rare but potentially life-threatening condition resulting from concomitant administration of serotonergic drugs. Warn patients of the symptoms of serotonin syndrome and to seek medical attention right away if symptoms develop.
  • Inform patients that anaphylaxis has been reported with ingredients contained in Butorphanol Tartrate Injection. Advise patients how to recognize such a reaction and when to seek medical attention
  • Advise nursing mothers to monitor infants for increased sleepiness (more than usual), breathing difficulties, or limpness. Instruct nursing mothers to seek immediate medical care if they notice these signs.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are using butorphanol injection.
  • This medication may decrease fertility in men and women. Talk to your doctor about the risks of using butorphanol.


What to do in case of emergency/overdose?[edit | edit source]

Symptoms of overdosage may include:

Management of overdosage:

  • In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.
  • Overdose related information is also available online at poisonhelp.org/help.
  • In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
  • In case of overdose, priorities are the reestablishment of a patent and protected airway and institution of assisted or controlled ventilation, if needed.
  • Employ other supportive measures (including oxygen and vasopressors) in the management of circulatory shock and pulmonary edema as indicated.
  • Cardiac arrest or arrhythmias will require advanced life-support techniques.
  • The opioid antagonists, naloxone or nalmefene, are specific antidotes to respiratory depression resulting from opioid overdose.
  • In an individual physically dependent on opioids, administration of the recommended usual dosage of the antagonist will precipitate an acute withdrawal syndrome.


Can this medicine be used in pregnancy?[edit | edit source]

  • Prolonged use of Butorphanol Tartrate Injection during pregnancy can result in neonatal opioid withdrawal syndrome, which may be life-threatening if not recognized and treated.
  • Butorphanol Tartrate Injection should be used during pregnancy only if the potential benefit justifies the potential risk to the infant.


Can this medicine be used in children?[edit | edit source]

  • Butorphanol is not recommended for use in patients below 18 years of age because safety and efficacy have not been established in this population.


What are the active and inactive ingredients in this medicine?[edit | edit source]

Active ingredient:

  • BUTORPHANOL TARTRATE

Inactive ingredients:

  • citric acid
  • sodium citrate
  • sodium chloride
  • benzethonium chloride as a preservative


Who manufactures and distributes this medicine?[edit | edit source]

Manufactured by:

Distributed by:


What should I know about storage and disposal of this medication?[edit | edit source]

  • Store at 20º-25°C (68º-77°F).
  • Protect from light.
  • Discard unused portion.
  • Retain in carton until time of use.
  • Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.


Full and partial opiod agonists:

Opiate antagonists:

Butorphanol Resources

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