Butorphanol

  • Generic Name or Active Ingridient: Butorphanol
Drug Class: Butorphanol > Fully Synthetic Opioid > Opioids > Opioid Agonist > Analgesic.

Uses

Doctors prescribe butorphanol to treat headaches and pain due to surgery or other causes. The most common use for butorphanol is to reduce migraines using a nasal spray formula. It is used to control moderate to severe pain, a supplement to anesthesia and for the management of pain during labor. Learn More About Butorphanol Uses

Administration/Dosage

Butorphanol is available by prescription only, in a tablet, as an injectable liquid or as a nasal spray. A nurse administers the injectable liquid intravenously or into a muscle. The nasal spray is administered in a metered dose, absorbed through the lining in your nose.

Each ml of injectable butorphanol solution contains 1 or 2 mg of butorphanol. Each dose of butorphanol spray contains 1 mg of butorphanol. The usual administration for butorphanol spray is one spray per nostril; do not spray into both nostrils unless directed to do so by your physician. Before using, a pharmacist or healthcare provider will prime the spray unit. If you do not use the unit for 48 hours or longer, the unit will need to be re-primed.

In human studies, scientists noted sedation at doses of 0.5 mg or more. Unconsciousness, or narcosis, may be achieved with doses of 10 to 12 mg of butorphanol administered intravenously over 15 minutes. Doses of 1 mg or more may cause nausea.

Medical research has not yet established safety and efficacy of administering butorphanol to children under the age of 18 years. Administer butorphanol to a child only under the close supervision of a pediatrician.

Older patients may be more sensitive to the effects of butorphanol, including dizziness, drowsiness, lightheadedness, nausea, stuffy nose and vomiting. As a person ages, he is more likely to experience decreased kidney function. Because of this, butorphanol does not clear from the body of a person over the age of 65 as it does for younger individuals, so the medicine stays in an older person's body longer. Older patients face an increased risk for toxic reactions to butorphanol. The initial dose for elderly patients should be half the recommended dose for other adults.

If your doctor has instructed you to take butorphanol on a regular schedule and you miss a dose, take the missed dose as soon as you can. If it is nearly time to take another dose, skip the missed dose and resume your normal schedule. Never double up on doses in an effort to make up for missed doses.

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Action

Butorphanol is an opioid analgesic. It binds to pain receptors in your central nervous system, or CNS, and brain to interrupt pain signals and change the way you perceive pain. More specifically, butorphanol binds to the mu and kappa receptors. While binding to the mu receptors provides analgesia and sedation, binding to kappa receptors may cause hallucinations, delusions and other unwanted psychotomimetic effects.

Pain relief begins within a few minutes after receiving butorphanol in an IV; it takes about 15 minutes to feel relief from pain after an intramuscular injection, commonly known as an IM. Peak analgesic effect takes place 30 to 60 minutes after IV and IM administration. Duration varies but the analgesic effects of butorphanol typically last three to four hours. Analgesia duration of butorphanol is similar to other opioids, including morphine.

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Precautions

Do not use butorphanol if you are allergic to it or to any ingredient in a butorphanol preparation, including the preservative benzethonium chloride. An allergic reaction is a serious medical condition that may worsen suddenly into a life-threatening emergency. Discontinue butorphanol and seek professional help immediately upon first onset of symptoms of an allergic reaction. Symptoms of an allergic reaction include hives, trouble breathing or swelling of the face, lips or tongue.

Do not use butorphanol if you have a history of a head injury or increased intracranial pressure. Doing so may cause complications such as carbon dioxide retention and an increase in cerebrospinal fluid pressure, pinpoint pupils and an alteration in mental state. Butorphanol may cause respiratory depression, a condition where breathing is insufficient to provide adequate gas exchange, characterized by slow and shallow breathing. This is especially true in patients receiving other drugs that act on the central nervous system and people suffering from CNS impairment or other breathing problems.

The prescribing physician may reduce your dosage of butorphanol to half the normal dose or suggest a different medication to ease your pain if you have liver or kidney problems. Doctors calculate the frequency of repeated doses of butorphanol based on how well these patients tolerate the medicine rather than at fixed time intervals, but these patients should not take butorphanol more frequently than every 6 hours.

Because butorphanol binds with kappa receptors, this opioid may increase the heart's workload, especially in the pulmonary circuit between the heart and the lungs. Patients with a history of certain types of heart disease or heart attack should limit use of butorphanol to situations where the benefits clearly outweigh the risks.

Discuss your medical history with the prescribing physician. Butorphanol may worsen your condition or interfere with treatment. Your illness may change the way butorphanol works in your body. Your doctor may alter the dosage of butorphanol, request medical laboratory tests or suggest a different medication based on your medical history.

Tell your physician about any significant illnesses or conditions, including:

  • Brain Tumor, Head Injuries or Increased Pressure in the Head.
  • Breathing Problems such as COPD, Cor Pulmonale or Hypoxia.
  • Central Nervous System Disease.
  • Drug dependence.
  • Heart Attack.
  • Heart or Blood Vessel Problems.
  • High Blood Pressure.
  • Kidney Disease.
  • Liver Disease.

Butorphanol may cause dizziness or drowsiness and may impair your mental and physical capabilities, especially within the first hour after taking butorphanol. Do not operate heavy machinery, drive a motor vehicle, engage in risky behavior, participate in behaviors that require you make fast decisions or have fast reflexes for at least one hour after taking butorphanol.

Do not use butorphanol if you drink alcohol.

Butorphanol, like other opioids, can be habit forming, especially if you take large doses or use this analgesic for a long time. To avoid developing a drug habit, take butorphanol exactly as prescribed by your doctor and stop taking butorphanol when directed to do so.

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Warnings

Butorphanol may cause severe high blood pressure. If your blood pressure rises, your doctor may discontinue butorphanol use and administer anti-hypertensive drugs. If you are not physically dependent on opioids, your doctor may give you naloxone to reduce your blood pressure. Tell your doctor if you think you are physically dependent on opioids, as taking naloxone may cause unpleasant symptoms of withdrawal in opioid-dependent individuals.

Butorphanol crosses placental barriers and into human milk. This means a woman who takes butorphanol during her pregnancy can pass butorphanol to her unborn child. Tell your doctor if you are pregnant or plan to become pregnant while taking butorphanol. Doctors may safely administer butorphanol during delivery to ease the pain of childbirth. A nursing baby can be exposed to butorphanol while breastfeeding. Do not breastfeed while taking butorphanol.

Do not stop taking butorphanol suddenly unless directed to do so by a healthcare professional. Abrupt cessation may cause uncomfortable symptoms of opioid withdrawal. When it is nearly time to stop using butorphanol, take successively smaller doses less frequently to reduce the level of butorphanol in your blood. Contact your doctor or consult with a rehabilitation clinic if debilitating withdrawal symptoms prevent you from discontinuing butorphanol.

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Drug Interactions

Butorphanol may interact with other drugs in unsafe or unfavorable ways. Give the prescriber and druggist filling the order a complete list of all your medications, including prescript and non-prescription drugs, herbal remedies, vitamins and dietary supplements. Do not start, stop or change the way you take any medication or remedy while you are taking butorphanol without first consulting with a physician.

Butorphanol increases your risk for experiencing side effects associated with sodium oxybate, commonly known as GHB. Nasal decongestants can delay the time it takes for butorphanol to work. Cimetidine increases the risk for side effects associated with butorphanol. Naltrexone or rifamycins, especially rifampin, may decrease butorphanol's effectiveness.

Consult with your physician before using medications that cause drowsiness, such as sleep aides or muscle relaxers, while taking butorphanol. Butorphanol can add to their effects. Talk with a pharmacist before taking over-the-counter cough and cold preparations.

Tell your doctor and pharmacist if you are taking any of the following medications:

  • Alfentanil
  • Alphaprodine
  • Codeine
  • Dihydrocodeine
  • Fentanyl
  • Fospropofol
  • Hydrocodone
  • Hydromorphone
  • Levorphanol
  • Meperidine
  • Methadone
  • Morphine
  • Morphine Sulfate Liposome
  • Oxycodone
  • Oxymorphone
  • Propoxyphene
  • Sufentanil
  • Tapentadol

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Side effects

Patients have reported side effects associated with butorphanol use. Most of the common side effects are not serious and disappear after a few days. If you experience common side effects while taking butorphanol, continue taking the medication but contact the prescribing physician if your non-serious side effects become intolerable or do not go away on their own.

Common side effects include:

  • Dizziness.
  • Drowsiness.
  • Dry Mouth.
  • Light-Headedness.
  • Nasal Irritation.
  • Nausea or Vomiting.
  • Runny or Stuffy Nose.
  • Sore Throat.
  • Insomnia.
  • Unpleasant Taste.
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Some side effects are serious, even life threatening. Stop taking butorphanol and contact a medical professional immediately if you experience serious side effects.

Serious side effects:

  • Agitation, Anxiety or Depression.
  • Blurred Vision.
  • Burning, Numbness, or Tingling.
  • Change in the Amount of Urine Produced.
  • Chest Pain.
  • Confusion.
  • Ear Pain.
  • Fainting.
  • Fast, Slow or Irregular Heartbeat.
  • Flushing.
  • Hallucinations.
  • Restlessness.
  • Ringing in the Ears.
  • Seizure.
  • Severe or Persistent Dizziness, Drowsiness or Light-Headedness.
  • Severe or Persistent Headache.
  • Shortness of Breath.
  • Slow, Shallow, or Difficult Breathing.
  • Tremors.
  • Unusual Swelling.

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Overdose

Drug overdose is a growing problem in the United States, especially fatal overdose of prescription painkillers. Approximately 36,000 Americans died from drug overdoses in 2008, most of them from prescription drugs. The numbers of drug overdose tripled in the years between 1990 and 2008. In 2008, more people died from prescription drug overdose than from heroin and cocaine combined. Drug overdose is a serious, life threatening medical emergency. If you suspect you or someone you know has taken too much butorphanol or any other drug, discontinue all medications and contact poison control center at 1-800-222-1222 or go to the emergency room. Overdose symptoms include:

  • Cold, Clammy Skin.
  • Deep Sleep or Loss of Consciousness.
  • Seizure.
  • Severe Drowsiness, Dizziness or Light-Headedness.
  • Slow Heartbeat.
  • Slow, Shallow or Labored Breathing.

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Abuse

Recreational users abuse butorphanol because of the euphoria it causes. There were more reports of abuse with the nasal spray than from the injectable forms of butorphanol. To abuse drugs means to use it in a way other than what the manufacturers intended, either to treat symptoms for which it was not prescribed or to get high.

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Withdrawal

Withdrawal is a normal, predictable outcome of taking large doses of opioids such as butorphanol, or using these drugs for a long time. Anyone can become dependent on opioids, even a person who uses drugs as prescribed by a physician.

Withdrawal symptoms include:

  • Agitation.
  • Anxiety.
  • Depression.
  • Hallucinations.
  • Mood Changes.
  • Weakness and Diarrhea.

Detox

Freeing yourself from opioid dependence requires a complex approach to rehabilitation. First, you must reduce overpowering withdrawal symptoms that prevent you from quitting opioid use in the past while simultaneously detoxifying your body from the effects of butorphanol dependence. During typical drug rehabilitation, doctors administer medications to ease withdrawal symptoms and other drugs to cleanse your system. Despite these medicines, withdrawal is a physically uncomfortable and demoralizing phase of rehabilitation that frequently presents an obstacle to rehabilitation. Withdrawal symptoms can last five or more days.

Rapid detox is a new, humane approach to drug rehabilitation. During rapid detox, specially trained doctors administer anesthesia and sedatives alongside the standard anti-withdrawal and detoxification drugs. You sleep comfortably through the withdrawal process and awaken refreshed, unaware of debilitating symptoms of withdrawal.

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Storage

Keep butorphanol at room temperature, between 59 and 86 degrees Fahrenheit, away from heat, light and moisture. Do not keep butorphanol in your bathroom. When not in use, store butorphanol in a childproof container. Put this medication out of the reach of children and pets. Do not allow adults to access this medication, as butorphanol is a drug of choice for recreational users.

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Miscellaneous information

Butorphanol was initially available in injectable form for human and veterinary use. Butorphanol became a favorite among drug abusers only after manufacturers offered the product in an easy to use nasal spray. Widespread diversion and abuse of butorphanol lead to its classification as a schedule IV drug, which means it carries the same potential for abuse as Darvon or Darvocet. Miscellaneous Information About Butorphanol

Facts

  • Butorphanol

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