Butorphanol

Medically reviewed by Patricia Weiser, PharmD on May 25, 2023
Written by Sarah Lewis, PharmD

Specifically, the Food and Drug Administration (FDA) has approved butorphanol to:

• provide pain relief during anesthesia
• be given before surgery or anesthesia
• relieve pain during labor
• treat severe pain

These approved uses differ based on the form of butorphanol your doctor prescribes.

This article describes butorphanol’s uses and dosage, ways to save on cost, and more. Below you’ll find some coupon options for butorphanol.

Boxed warnings

Butorphanol has boxed warnings about the following risks. Boxed warnings are serious warnings from the FDA. These include:

• addiction and misuse,with all forms of butorphanol
• neonatal opioid withdrawal syndrome,with all forms of butorphanol
• serious respiratory depression,with all forms of butorphanol
• accidental ingestion, with butorphanol nasal (nose) spray
• harm if administered with benzodiazepines or alcohol, with all forms of butorphanol
• harm if administered with certain other medications, with butorphanol nasal spray

For details, see the “Interactions and warnings for butorphanol” section below.

Below you’ll find answers to a few commonly asked questions about butorphanol.

Can butorphanol be prescribed for dogs?

Yes, veterinarians may recommend butorphanol for dogs and other animals for pain relief and other uses. That said, you should never administer this medication or any others to a pet without your veterinarian’s recommendation. Doing so could be harmful.

For more information about butorphanol for dogs, talk with your vet.

Is butorphanol a controlled substance?

Yes, butorphanol is a controlled substance. This means it carries the risks of misuse and addiction. Misuse refers to using a drug in a way other than how a doctor prescribes it. Addiction refers to feeling unable to stop using a drug, even though it may be causing harm.

In fact, butorphanol has a boxed warning about the risks of misuse and addiction. Boxed warnings are serious warnings from the Food and Drug Administration (FDA). To learn more, see the “Interactions and warnings for butorphanol” section below.

If you have concerns about treatment with a controlled substance, or misuse or addiction with butorphanol, talk with your doctor or pharmacist.

Does butorphanol have a reversal process?

Yes, similar to other opioids, the effects of butorphanol can be reversed. This can be done with a drug called an opioid antagonist. Naloxone is an example of an opioid antagonist.

Talk with your doctor or pharmacist to learn more about using an opioid antagonist to reverse butorphanol’s effects.

How does butorphanol work? And how long does it take to start working?

Butorphanol works by binding to sites in the brain and spinal cord called opioid receptors. This causes the pain-relieving effects of the drug.

How quickly butorphanol starts to work depends on how it’s administered. For the nasal (nose) spray, pain relief usually starts within 15 minutes of administering a dose. It’ll also start working within 15 minutes when you receive it as an injection into a muscle. An injection into a vein will start working within a few minutes.

To find out more about what you can expect with butorphanol, ask your doctor or pharmacist.

Butorphanol may cause mild or serious side effects (also known as adverse effects). More common mild side effects of butorphanol and its serious side effects are listed below. This article doesn’t include all possible side effects of the drug. Side effects can vary based on your age and overall health and any other medications you take.

To learn more about butorphanol’s side effects, talk with your doctor or pharmacist. You can also read the prescribing information* for butorphanol.

* To view butorphanol’s prescribing information, see the “Article resources” section below.

Mild side effects

More common mild side effects reported with some forms of butorphanol are listed below. These side effects may differ based on the form of butorphanol you’re prescribed.

This article doesn’t include all possible mild side effects of the drug. To learn more about butorphanol’s side effects based on the form, see the prescribing information* for butorphanol.

With many drugs, mild side effects may go away within a few days or a couple of weeks. If the side effects are bothersome, tell your doctor or pharmacist. They may be able to suggest ways to manage them.

Butorphanol nasal (nose) spray’s mild side effects include:

• dizziness
• nausea or vomiting
• sleepiness
• stuffy nose
• mild allergic reaction*

Butorphanol liquid solution for injection’s mild side effects include:

• dizziness
• nausea or vomiting
• sleepiness
• mild allergic reaction*

* For details about this side effect, see the “Warnings for butorphanol” section below.

Serious side effects

Serious side effects of butorphanol are listed below. These side effects may differ based on the form of butorphanol you’re prescribed.

This article doesn’t include all possible serious side effects of the drug. To learn more about butorphanol’s side effects based on form, see the prescribing information* for butorphanol.

With many drugs, serious side effects are possible but not common. If you have serious side effects from this drug, call your doctor right away. If you’re having severe symptoms or a medical emergency, call 911 or a local emergency number.

In general, butorphanol’s serious side effects include:

• hallucinations (seeing or hearing things that aren’t there)
• adrenal insufficiency (a condition in which the adrenal glands don’t make enough of the hormone cortisol)
• seizures
• serotonin syndrome (a condition in which too much of the chemical serotonin is in your body)
• severe high blood pressure
• severe low blood pressure that leads to fainting
• boxed warnings for addiction and misuse, with all forms of butorphanol†
• boxed warning for neonatal opioid withdrawal syndrome,with all forms of butorphanol†
• boxed warning for serious respiratory depression,with all forms of butorphanol†
• boxed warning for accidental ingestion, with butorphanol nasal spray†
• boxed warning for harm if administered with benzodiazepines or alcohol, with all forms of butorphanol†
• boxed warning for harm if administered with certain other medications, with butorphanol nasal spray†
• severe allergic reaction†

* To view butorphanol’s prescribing information, see the “Article resources” section below.
† For details about this side effect, see the “Interactions and warnings for butorphanol” section below.

The dosage of butorphanol your doctor prescribes may vary based on your condition and certain other factors. Talk with your doctor about the dosage you should follow.

Taking and receiving butorphanol

Butorphanol nasal (nose) spray is administered by spraying it into a nostril.

Butorphanol liquid solution for injection is given as an injection into a muscle or vein.

Your doctor will talk with you about how to administer butorphanol nasal spray. They’ll explain how much to spray and how often. Always follow your doctor’s recommendation.

Your doctor will explain how butorphanol injection will be given to you and where you’ll receive it. They’ll also explain how much you’ll receive and how often.

Overdose of butorphanol

You should not administer more butorphanol than your doctor prescribes. For some drugs, doing so may lead to serious side effects or overdose.

If you think you’ve administered too much butorphanol, call your doctor or pharmacist right away. Or you could call 800-222-1222 to speak with someone at America’s Poison Centers. You can also use its online resource. If you have concerning symptoms, call 911 or a local emergency number immediately. You can also go to the closest emergency room.

Below, you’ll find information about butorphanol’s possible interactions and warnings.

Interactions of butorphanol

For some medications, certain things may affect how the drug works. These include getting vaccines, consuming alcohol or certain foods, or taking the drug with other medications. This effect is called a drug interaction.

Before starting butorphanol, ask your doctor to check for possible interactions. They can check for interactions these items may cause with butorphanol. Be sure to tell them about any of the following you take or use:

• prescription drugs
• over-the-counter medications
• vitamins, herbs, or supplements

To learn about drug-condition interactions, see the “Warnings for butorphanol” section below.

Warnings for butorphanol

Butorphanol should not be administered to or should be administered cautiously by certain people.

Boxed warnings

Butorphanol has boxed warnings about the following risks. Boxed warnings are serious warnings from the Food and Drug Administration (FDA).

To learn more about these warnings, read below. You can also talk with your doctor or pharmacist.

Risk of addiction and misuse. With misuse, you use the drug in a way other than how a doctor prescribes it. This can lead to addiction. Addiction means continuing to use a drug even though it may be causing harm. It’s unknown how often these side effects were reported in studies* of butorphanol.

If you have concerns about treatment with butorphanol, tell your doctor. They’ll likely recommend ways to get help with misuse or addiction.

Risk of neonatal opioid withdrawal syndrome. With neonatal opioid withdrawal syndrome, withdrawal symptoms can occur in your baby if you were treated with butorphanol for a long time during pregnancy. (Withdrawal symptoms are side effects that can occur when you stop taking a drug that your body has become dependent on.) It’s unknown how often this side effect was reported in studies* of butorphanol.

Symptoms may include a high pitched cry, tremor, vomiting, and diarrhea in the newborn. These and other withdrawal symptoms can be life threatening.

If you become pregnant while taking butorphanol, tell your doctor. They’ll help you decide whether you should continue treatment with the drug.

Risk of serious respiratory depression. With serious respiratory depression, you have slowed or stopped breathing. This can be life threatening or fatal. This side effect was rarely reported in studies* of butorphanol.

The risk is highest when you first start treatment with butorphanol and after dosage increases. The risk is also higher for older adults (ages 65 years or over).

If you experience slowed or stopped breathing, seek immediate medical care or have someone call 911 for you.

Risk of serious accidental ingestion. With serious accidental ingestion, you can overdose on butorphanol. This can be life threatening. Accidentally ingesting butorphanol can be very dangerous in children.

Symptoms may include very small eye pupils, slow or shallow breathing, limp muscles, extreme sleepiness, or coma.

If you or someone else experiences accidental ingestion, seek immediate medical care or call 911.

Risk of harm if administered with benzodiazepines. If you administer benzodiazepines with butorphanol, you are at risk of coma and death. Benzodiazepines are central nervous system (CNS) depressants. This means they slow down your brain function. Other CNS depressants carry this same risk of harm if you use them with butorphanol. These CNS depressants include alcohol, other opioid pain relievers, and several other medications, such as zolpidem.

It’s unknown how often this side effect was reported in studies* of butorphanol. Symptoms may include slowed or stopped breathing, losing consciousness, and coma. In some cases, these symptoms can lead to death.

If you take benzodiazepines or drink alcohol, tell your doctor. They’ll likely recommend you stop taking benzodiazepines or stop consuming alcohol during butorphanol treatment.

Risk of harm if administered with certain other medications. With certain other medications, there is a risk of dangerous drug interactions. This includes drugs that affect the way your body processes and gets rid of butorphanol. Certain drugs can cause a high level of butorphanol in the body and increase the risk of serious side effects.

Certain other drugs can cause your butorphanol level to become too low. This could lead to withdrawal side effects and cause the drug not to work as well as it should. When you stop treatment with these types of drugs, the level of butorphanol could increase, raising the risk of serious side effects.

If you take other medications, tell your doctor. They’ll likely recommend changes to your dosage.

* To view butorphanol’s prescribing information, see the “Article resources” section below.

Other warnings

Butorphanol could cause harm to people with certain health conditions. This effect is called a drug-condition interaction. Other factors can also affect whether butorphanol is a safe option for you. These warnings may differ based on the form of butorphanol you’re prescribed.

Ask your doctor about specific warnings for butorphanol, and be sure to tell your doctor about your:

• current health, including any allergies to medications
• past health conditions or surgeries

Allergic reaction

Butorphanol can cause an allergic reaction in some people. Severe allergic reactions are rare but possible.

If you’ve had an allergic reaction to butorphanol or any of its ingredients, your doctor will likely not prescribe butorphanol. They can tell you about medications that are safer options for you.

A mild allergic reaction may cause the following symptoms:

• skin rash
• itchiness
• flushing (temporary warmth, redness, or deepening of skin color)

A severe allergic reaction may cause the following symptoms:

• swelling under your skin, usually in your hands, feet, eyelids, or lips
• swelling of your mouth, throat, or tongue, which can cause breathing problems

If you have an allergic reaction to butorphanol, call your doctor right away. If you have severe symptoms, call 911 or a local emergency number.

Pregnancy or breastfeeding and butorphanol

Information about butorphanol and pregnancy and breastfeeding is described below.

Butorphanol and pregnancy

There are risks associated with butorphanol treatment during pregnancy. But there are also risks associated with having untreated severe pain while pregnant. (Keep in mind that butorphanol is prescribed for treating severe pain.)

If you’re planning a pregnancy or can become pregnant, talk with your doctor about severe pain treatment options during pregnancy. Together, you can discuss the risks and benefits of your treatment options and decide whether you should have butorphanol during pregnancy.

Butorphanol and breastfeeding

It’s not known whether butorphanol treatment is safe while breastfeeding. If you’re currently breastfeeding or planning to do so, talk with your doctor before starting treatment with this medication.

The Food and Drug Administration (FDA) approves prescription drugs such as butorphanol for certain conditions. Approved uses for butorphanol are described below. These uses differ based on the form of butorphanol prescribed.

Use for pain

Doctors may prescribe butorphanol nasal (nose) spray or liquid solution for injection for treating severe pain. The drug is prescribed for this purpose in adults. The nasal spray can be prescribed as a long-term treatment. The injection is usually for short-term treatment.

With severe pain, doctors prescribe butorphanol for a variety of painful conditions that need an opioid pain reliever.

Doctors may not prescribe butorphanol nasal spray or liquid solution for injection in certain situations, such as for:

• people who are at a higher risk of serious respiratory depression
• people who have or may have a blockage in the digestive system
• people with severe asthma

Use for anesthesia

Doctors may prescribe butorphanol liquid solution for injection to help with anesthesia. It’s prescribed for this purpose in adults. It’s usually prescribed as a short-term treatment.

With anesthesia, doctors administer a combination of drugs. Together, the drugs put you in a deep sleep, relieve your pain, and keep you from remembering the procedure. Butorphanol is a pain reliever doctors can administer for this purpose.

Butorphanol is prescribed together with various other drugs for anesthesia.

Doctors may not prescribe butorphanol nasal spray and liquid solution for injection in certain situations, such as for:

• people who already have serious respiratory depression
• people who have or may have a blockage in the digestive system
• people with severe asthma, if doctors don’t have the right equipment to monitor them

You may be able to save money on your prescription for butorphanol by using our Perks discount coupons. These can be found at the end of this article.

If you have questions about how to pay for butorphanol, talk with your doctor or pharmacist.

Note: Optum Perks coupons cannot be used with insurance copays or benefits.

This article describes butorphanol’s uses and dosage, ways to save on cost, and more. Let your doctor know if you have questions about butorphanol or would like more details about it.

Here’s a list of some possible questions you may want to ask your doctor:

• How does butorphanol compare with other opioid pain relievers?
• What other options would you prescribe for severe pain?
• Is there anything in my medical history that makes me more likely to have side effects from butorphanol?

• Butorphanol tartrate- butorphanol tartrate injection, solution. (2023). https://nctr-crs.fda.gov/fdalabel/services/spl/set-ids/9822ca3f-aee2-46e5-8a96-495400e65d10/spl-doc#
• Butorphanol tartrate- butorphanol tartrate spray, metered. (2022). https://nctr-crs.fda.gov/fdalabel/services/spl/set-ids/5a50d22e-acbe-4b15-9ed6-70713378408a/spl-doc#
• Food and Drug Administration. (2023). Orange Book: Approved drug products with therapeutic equivalence evaluations. https://www.accessdata.fda.gov/scripts/cder/ob/index.cfm

Disclaimer: Optum Perks has made every effort to make certain that all information is factually correct, comprehensive, and up to date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or another healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.