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Butorphanol Tartrate

Butorphanol tartrate is a prescription medication primarily used to manage moderate to severe pain. It is an opioid analgesic with mixed agonist-antagonist properties, meaning it activates certain opioid receptors in the brain while blocking others. This unique mechanism makes butorphanol effective for pain relief while also reducing some of the risks associated with full opioid agonists, such as respiratory depression. Butorphanol is available in both injectable and nasal spray forms and is often used in situations where other pain relief methods are inadequate.

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Frequently Asked Questions

How long does it take for Butorphanol tartrate to start working?
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Butorphanol typically begins to relieve pain within 15 minutes when administered intravenously, 30 minutes when administered intramuscularly, and within 15 to 60 minutes when administered via the nasal spray.

Can Butorphanol tartrate be used for chronic pain?
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Butorphanol is generally not recommended for long-term use or chronic pain due to the risks of dependence and tolerance. It is typically reserved for short-term management of acute pain.

What should I do if I miss a dose of Butorphanol tartrate?
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Butorphanol is usually taken on an as-needed basis for pain, so missed doses are uncommon. If you are on a scheduled dosing regimen, take the missed dose as soon as you remember, but if it is almost time for your next dose, skip the missed dose and resume your regular schedule. Do not double the dose to make up for the missed one.

Is Butorphanol tartrate safe to use during pregnancy?
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Butorphanol should be used during pregnancy only if the potential benefits justify the potential risks to the fetus. It may cause withdrawal symptoms in newborns if used long-term during pregnancy. Pregnant women should consult their healthcare provider before using this medication.

Can Butorphanol tartrate cause dependence or withdrawal symptoms?
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Yes, butorphanol can cause physical dependence with prolonged use, and abrupt discontinuation may lead to withdrawal symptoms. It is important to follow your healthcare provider’s instructions on tapering the dose if needed.

Comprehensive Drug Guide

How Does Butorphanol Tartrate Work?

Butorphanol tartrate works by binding to the kappa opioid receptors and partially agonizing the mu opioid receptors in the brain. Its action on the kappa receptors provides effective pain relief, while its partial agonism at the mu receptors helps limit the risks associated with respiratory depression and euphoria typically seen with full opioid agonists. This dual action makes butorphanol a useful option for pain management in various clinical settings.

What is Butorphanol Tartrate Used For?

  • Management of Moderate to Severe Pain: Often used for pain relief after surgery, during labor, or for migraine headaches.
  • Preoperative or Preanesthetic Medication: Used to provide analgesia and sedation before surgery.

Common Dosages

Butorphanol tartrate is available in injectable form (usually administered in a hospital setting) and as a nasal spray for at-home use.

Administration:

  • Injectable Form: Administered intravenously or intramuscularly by healthcare professionals, typically in a hospital setting.
  • Nasal Spray: Used at home or in a clinical setting for the management of acute pain. The patient should be instructed on proper use to ensure effective dosing.

Duration of Use: Butorphanol is generally used for short-term pain relief due to its potential for tolerance, dependence, and side effects.


Typical Dosing

FDA Approved Indications

The typical dosage of butorphanol tartrate depends on the form used and the severity of the pain:

For Injectable Form:

  • Initial Dose: 1 mg to 2 mg administered intravenously or intramuscularly, repeated every 3 to 4 hours as needed.

For Nasal Spray:

  • Initial Dose: One spray (1 mg) in one nostril, which may be repeated in 60 to 90 minutes if needed. For severe pain, one spray in each nostril may be used.

Who Shouldn't Take Butorphanol Tartrate?

Butorphanol tartrate is contraindicated in patients with:

  • Hypersensitivity to butorphanol or any of the other components of the formulation.
  • Significant respiratory depression, particularly in unmonitored settings or without resuscitative equipment.
  • Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment.
  • Known or suspected gastrointestinal obstruction, including paralytic ileus.

Advice From The Pharmacist

Patients using butorphanol tartrate should be advised to:

  • Use the medication exactly as prescribed and not exceed the recommended dose, particularly with the nasal spray form, to avoid serious side effects.
  • Avoid alcohol and other central nervous system depressants, as these can enhance the sedative and respiratory depressant effects of butorphanol.
  • Report any signs of respiratory depression, severe drowsiness, or confusion to their healthcare provider immediately.
  • Be cautious when performing activities that require alertness, such as driving or operating machinery, as butorphanol can cause dizziness, drowsiness, and impaired judgment.
  • Discuss with their healthcare provider any history of substance use disorder, as butorphanol can be habit-forming.

Side Effects of Butorphanol Tartrate

Common Side Effects

  • Drowsiness or dizziness
  • Nausea or vomiting
  • Sweating
  • Headache
  • Dry mouth

Uncommon/Severe Side Effects

Serious side effects can include:

  • Respiratory Depression: Particularly in opioid-naive patients or at high doses.
  • Dependency and Withdrawal: Long-term use can lead to physical dependence and withdrawal symptoms if the medication is abruptly discontinued.
  • Allergic Reactions: Such as rash, itching, swelling, or difficulty breathing.

Risks and Warnings of Butorphanol Tartrate

  • Respiratory Depression: Butorphanol has the potential to cause life-threatening respiratory depression, particularly when used in higher doses or in combination with other CNS depressants.
  • Dependency and Abuse: Although butorphanol has a lower potential for abuse compared to other opioids, it can still be habit-forming, especially with prolonged use.
  • Impaired Mental and Physical Abilities: Patients should be warned about the potential for butorphanol to impair cognitive and motor skills, which can affect their ability to drive or operate heavy machinery.

Interactions with Butorphanol Tartrate

Common Drug Interactions

Butorphanol tartrate may interact with other medications, including:

  • CNS Depressants: Such as benzodiazepines, opioids, and alcohol, which can enhance the sedative and respiratory depressant effects.
  • MAO Inhibitors: Concomitant use may increase the risk of serotonin syndrome or other serious side effects.
  • Serotonergic Drugs: Such as SSRIs, SNRIs, or triptans, which can increase the risk of serotonin syndrome.

Patients should inform their healthcare provider of all medications and supplements they are taking to avoid potential interactions.


Alternatives to Butorphanol Tartrate

Alternative treatments for moderate to severe pain include:

  • Other Opioid Analgesics: Such as morphine, oxycodone, or hydromorphone, depending on the patient’s needs and the clinical situation.
  • Non-Opioid Analgesics: Such as NSAIDs, acetaminophen, or adjuvant therapies like anticonvulsants for specific types of pain.
  • Regional Anesthesia: For specific types of pain, such as nerve blocks or epidurals.

The choice of treatment depends on the type and severity of pain, patient preferences, and the presence of any co-existing health conditions.