Butorphanol: Side Effects, Interactions & Precautions

What Is Butorphanol?

Butorphanol is a synthetic morphine-like pain reliever most commonly used to treat severe pain. Butorphanol is a narcotic or opioid antagonist only available as a generic because the manufacturer discontinued the brand-name version called Stadol. Butorphanol is available as tartrate salt and can be injected, taken as a tablet or used as a nasal spray. The tablet form is only currently used in veterinary medicine because it has a low level of bioavailability in humans. Butorphanol is more effective in reducing pain in women than men.

Butorphanol is a partial agonist and antagonist. It affects the central nervous system, similar to other opioid pain relievers. Some of the possible side effects of butorphanol use can include: 

• Dizziness
• Confusion
• Sedation
• Nausea
• Vomiting
• Agitation
• Mood changes
• Constipation
• Itching
• Loss of appetite
• Sweating

Uniquely, even though butorphanol can activate opioid receptors in a way that allows it to relieve pain, it can also block the effects of opioids. If someone is dependent on opioids and takes butorphanol, they may experience sudden withdrawal symptoms.

What Does Butorphanol Look Like?

When prescribed for outpatient use, butorphanol is a colorless nasal spray that comes in a small bottle labeled with its ingredients, butorphanol tartrate 10 mg/mL. It is used in one nostril, as directed by a physician. In some cases, if the person still has pain 60–90 minutes after the first dose of butorphanol, they may do a second spray in the opposite nostril. Injectable butorphanol is used in a hospital or other medical setting.

How Is Butorphanol Used?

Butorphanol is FDA-approved for people and animals, specifically dogs, cats and horses. It can be prescribed to treat many medical conditions. The drug can be used in a medical setting like a hospital, but the nasal formulation of the drug can also be used in humans in an outpatient setting.

Pain Management

Butorphanol is FDA-approved for pain management. The injectable form of the drug is restricted to use in a hospital setting and is injected into a muscle or by an IV for pain control. In contrast, the nasal spray is available for outpatient use. 

When used in a hospital setting, the typical IV dose of butorphanol is 1 mg every three to four hours as needed. In contrast, the typical intramuscular dose of butorphanol is 2 mg every three to four hours, as needed. 

Anesthesia

Butorphanol is FDA-approved for anesthesia before a procedure and given in a hospital setting. The typical adult dose is 2 mg of butorphanol, given into a muscle 60–90 minutes before surgery. The drug can also be given in a dose of butorphanol 2 mg by IV before a person is put under general anesthesia and/or given in increments of 0.5–1 mg IV during the procedure. 

Treating Migraines

Butorphanol is not FDA-approved for migraines but was previously sometimes prescribed for this reason. However, despite the nasal spray possibly being effective for migraines, it is not recommended for regular use. Instead, newer and safer agents, including triptans, like sumatriptan (Imitrex) and calcitonin gene-related peptide (CGRP) blockers like ubrogepant (Ubrelvy), are more commonly prescribed.

Veterinary Uses of Butorphanol

Veterinarians use oral and injectable butorphanol in dogs and other animals like cats and horses. For dogs, butorphanol is often used for either cough or pain. Meanwhile, in other animals, the drug is usually reserved for pain. The drug can also be prescribed in animals to prevent nausea and vomiting associated with chemotherapy.

How Butorphanol Works

In some ways, butorphanol works similarly to other opioids by binding to opioid receptors in the central nervous system. However, in other ways, butorphanol differs from most other opioids: while many other opioids bind to mu opioid receptors, butorphanol binds to kappa opioid receptors and blocks mu opioid receptors. This impacts the drug’s addiction risk, making it a comparatively less risky Schedule IV controlled substance than Schedule II controlled opioids like oxycodone and hydrocodone.

Drug Interactions With Butorphanol

If you or a loved one take butorphanol, it is important to be aware that it has drug interactions, including:

• Benzodiazepines and other central nervous system depressants, due to the risk of overdose
• Antidepressants and other drugs like MAOIs that increase serotonin levels due to the risk of serotonin syndrome

Pharmacology of Butorphanol

Injectable butorphanol has more studies supporting its exact pharmacology than nasal butorphanol. For example, pain relief occurs within a few minutes for IV butorphanol and within 15 minutes for intramuscular butorphanol, but no specific data is available for nasal butorphanol.

Similarly, when injected, peak pain relief occurs within 30–60 minutes and lasts for about three to four hours; however, data is not available for nasal butorphanol.

Butorphanol Dosage and Administration

When prescribed for outpatient use, butorphanol is given as a 1 mg nasal spray to be used in one nostril only. If additional pain relief is needed, an additional spray may be given within 60–90 minutes. If pain relief is still needed after three to four hours, the person may repeat this. 

In some cases of severe pain, the person can get one 1-mg nasal spray in both nostrils to start. However, the person should not repeat the dose until at least three to four hours have passed.

Butorphanol Side Effects

Butorphanol is a narcotic, which means it can slow the functions of the central nervous system. Such effects on the body can have short and long-term side effects.

Butorphanol side effects can vary from person to person, based on many factors, so no single person’s experience will look exactly like another’s. The risk of serious side effects increases if you take butorphanol with other substances, such as alcohol or other opioids. If you experience any of the following side effects, it is important to seek medical attention immediately.

Short-Term Side Effects

Butorphanol can lead to many side effects, including:

• Drowsiness
• Dizziness
• Nausea and vomiting
• Blurred vision
• Headache
• Constipation
• Sleep disturbances
• Sweating
• Dry mouth
• Changes in mood or behavior
• Confusion
• Lethargy
• Heart palpitations
• Serious Side Effects

In addition to these common side effects, butorphanol can also cause more serious side effects, such as:

• Respiratory depression
• Overdose
• Addiction
• Dependence
• Withdrawal symptoms

Long-Term Side Effects

One long-term effect of butorphanol is increased pain sensitivity. The brain and body become used to the presence of the drug, so a person will have more pain sensitivity when they’re not using it. This can make it difficult to stop using butorphanol, even if the pain is no longer as severe.

Another long-term effect of butorphanol is physical dependence. The longer someone uses butorphanol, the more likely they will become dependent and struggle with withdrawal symptoms if they try to stop using it. Withdrawal symptoms can be very unpleasant and include: 

• Nausea
• Vomiting
• Diarrhea
• Anxiety
• Insomnia

Long-term use of butorphanol can also have negative effects on the cardiac system, affecting heart rate and blood pressure, and it can also cause damage to the respiratory system. For some people, the long-term use of butorphanol can lead to the misuse of other opioids, such as heroin or other powerful drugs.

Precautions for Butorphanol Use

Doctors carefully prescribe butorphanol because it is a Schedule IV controlled substance, which carries some risk for abuse, addiction and dependence. However, some people have additional risk factors, including different medical conditions, that make butorphanol a poor choice or mean they need to be monitored more closely than normal while taking the drug.

When Not To Use Butorphanol

Most people can take butorphanol without a problem. However, people who should avoid butorphanol entirely include those with an allergy to butorphanol or benzethonium chloride, an ingredient in the drug’s injectable and nasal spray forms.

Considerations Prior To Use

Doctors must weigh the risks and benefits of butorphanol in some people and prescribe the drug more cautiously and with closer monitoring to those with certain medical risk factors. This includes those:

• With a history of addiction to other substances
• With a history of lung or breathing problems
• Currently taking other opioids, as butorphanol may block these opioids and send the person into withdrawal
• Currently taking benzodiazepines or other central nervous system depressants

Butorphanol Addiction

Is Butorphanol Addictive?

Butorphanol comes with a black box warning about its addictive potential and the possibility of dependence. Therefore, physicians should assess the patient’s drug misuse and addiction risk factors before prescribing it. The structure of butorphanol is similar to drugs like morphine, oxycodone and heroin. 

Butorphanol is both an opioid antagonist and an agonist and can have the same effects as other commonly misused opioid drugs since it interacts with the central nervous system. While the risk of misuse and addiction is possible with butorphanol, these risks are lower than with other opioid analgesics. However, someone who uses butorphanol for a period and stops using it suddenly may go through withdrawal. 

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Butorphanol Overdose

Butorphanol is a partial opioid agonist that can cause respiratory depression and brain stem dysfunction. This can lead to complications such as brain damage, coma or death.

Risk factors for butorphanol overdose include:

• Misusing butorphanol
• Taking butorphanol for the first time
• Mixing butorphanol with other central nervous system depressants
• Having preexisting breathing problems or asthma
• A history of lung disease
• Being an older adult

Signs and symptoms of a butorphanol overdose include:

• Slow, shallow or stopped breathing
• Dizziness
• Vomiting
• Blue colored lips
• Extreme drowsiness
• Inability to be woken up
• Weak pulse
• Feeling lightheaded or faint
• Confusion

If you think someone is experiencing a butorphanol overdose, call 911 immediately. An antidote may be administered if the overdose is caught early.

It is important to remember that butorphanol overdoses are often the result of combining the drug with other central nervous system depressants. It is imperative to avoid mixing butorphanol with alcohol, tranquilizers or benzodiazepines.

If you are prescribed butorphanol, taking it exactly as prescribed is important. If you have any concerns about taking butorphanol, talk to your doctor.

Butorphanol Withdrawal and Detox

Butorphanol withdrawal symptoms can be unpleasant and make it difficult to function. They typically start within a few hours of the last dose and peak within about 48 hours. Some of the most common symptoms include:

• Physical symptoms: These can include fever, chills, sweating, nausea, vomiting, diarrhea, muscle aches and cramps.
• Psychological symptoms: These can include anxiety, irritability, restlessness, insomnia and depression.
• Cravings: People withdrawing from butorphanol may have intense cravings for the drug.

The severity of withdrawal symptoms can vary depending on how long the drug was used and the dosage. In most cases, the symptoms will start to lessen after about a week. However, some symptoms may persist for longer.

Butorphanol Withdrawal Timeline

Most people will experience withdrawal symptoms within a few hours of the last dose. The initial withdrawal phase can include symptoms similar to the flu, such as headache, fever, chills, cramps, aches and pain, nausea and vomiting. Diarrhea and emotional and psychological symptoms, such as anxiety and irritability, can also occur.

For most people, withdrawal symptoms peak about 48 hours after the last dose. After this, the symptoms will start to lessen. However, some symptoms, such as mild anxiety, cravings and mild aches or pain, may persist for longer. For most people, the symptoms of butorphanol withdrawal should end within a week.

Butorphanol Withdrawal Management

There are a few ways to manage the symptoms of butorphanol withdrawal. One option is to gradually taper the dosage of butorphanol over time. This can help reduce or alleviate withdrawal symptoms. Another option is to undergo a medical detox. A medical detox provides a structured, monitored environment that can be helpful for people who have been using butorphanol heavily or for a long time.

Butorphanol Detox

Butorphanol detox is the process of withdrawing from butorphanol in a safe and supervised environment. It can be done in a standalone facility, on an outpatient basis or as part of an addiction treatment program.

Detoxing from butorphanol can be uncomfortable and even dangerous, so it is important to do it under the care of a medical professional. A medical detox can help reduce the risk of medical complications and ensure the withdrawal process is as safe and comfortable as possible.

In addition to providing medical care, a medical detox can offer support and counseling to help people cope with withdrawal’s emotional and psychological challenges. This support can be essential for preventing relapse.

If you are considering butorphanol detox, it is important to talk to your doctor about your best option. They can help you assess your needs and ensure you receive the necessary care. You can also contact The Recovery Village for help. 

Treatment for Butorphanol Addiction

Treatment options include medical detox programs and many inpatient and outpatient rehabs.

Inpatient Butorphanol Rehab

Inpatient butorphanol rehab is a treatment that provides a safe and structured environment for people struggling with butorphanol addiction. Inpatient rehab typically involves living in a residential facility for a period, and your days and activities are highly scheduled. 

There are many benefits to inpatient butorphanol rehab, including: 

• Provides a sense of supervision and stability: This can be especially beneficial for people whose home lives are chaotic or unstable. 
• Offers a regimented daily schedule: This can help people break out of old patterns and establish new, healthier habits.
• Includes therapy sessions throughout the day: This can include individual, group and family therapy to help people understand their addiction and develop coping mechanisms to avoid relapse.

Outpatient Butorphanol Rehab

Outpatient butorphanol rehab is a type of treatment that allows people to continue living at home while they receive treatment for their addiction. Outpatient rehab typically involves attending therapy sessions several times a week, and sessions usually last for a few hours each.

There are many benefits to outpatient butorphanol rehab, which can include: 

• Allows people to continue going to school or work: This can be important for those who need to maintain their employment or education to support themselves or their families while receiving treatment. 
• Often less expensive than inpatient rehab: This is helpful for those struggling to afford the cost of treatment.
• Includes therapy sessions: This can include individual, group and family therapy to help people understand their addiction and develop coping mechanisms to avoid relapse.

If you are interested in learning more about recovery programs for yourself or a loved one, we would be happy to speak with you to help you navigate your options.

How Long Does Butorphanol Stay In Your System?

Butorphanol has a half-life of about 18 hours, which is how long it takes the body to metabolize half of a dose. It usually takes five half-lives for a drug to be fully eliminated from the body, meaning it takes about 90 hours for a full dose of butorphanol to be eliminated.

However, many factors can affect how long butorphanol stays in your system. These include:

• Liver function: People with liver impairment may have a longer half-life for butorphanol.
• Overall health: People with other health conditions may have a longer half-life for butorphanol.
• Age: Older people may have a longer half-life for butorphanol.
• Other drugs: If you are taking other medications, these may interact with butorphanol and prolong its half-life.
• Weight and size: Larger people may have a shorter half-life for butorphanol than smaller people.

Talk to your doctor if you are concerned about how long butorphanol will stay in your system. They can help you determine how long the drug will last based on your individual factors.

Here are some additional things to keep in mind:

• The half-life of butorphanol can be affected by other factors, such as diet and exercise.
• If you take butorphanol regularly, it may accumulate in your system over time, resulting in lingering traces remaining even longer once you taper off butorphanol.

Mixing Butorphanol and Alcohol

Mixing alcohol and butorphanol can be dangerous and fatal. Even in small amounts, these two substances can cause side effects such as nausea, vomiting, dizziness, drowsiness and short-term memory loss. Butorphanol and alcohol are central nervous system depressants, which can slow breathing. When combined, they can cause serious respiratory depression or even death.

There is no safe way to mix alcohol and butorphanol. If you are prescribed butorphanol, talk to your doctor about the risks of mixing it with alcohol. If you are concerned about someone who is mixing alcohol and butorphanol, please seek help immediately.

The risks of mixing alcohol and butorphanol include:

• Respiratory depression
• Nausea and vomiting
• Dizziness and drowsiness
• Short-term memory loss
• Addiction and dependence
• Fatal overdose

If you experience symptoms after mixing alcohol and butorphanol, seek medical attention immediately.

Help for Butorphanol Addiction

If you or a loved one struggles with butorphanol, it can be hard to know where to turn. However, help is available. At The Recovery Village, we believe the best way to help you through an addiction is to support you every step of the way. That’s why we’ve designed a full continuum of care to help you overcome butorphanol, from medical detox to help wean you off butorphanol to rehab to help keep you off the drug for good. Don’t wait: contact us today to learn more.

Editor – Theresa Valenzky

Theresa Valenzky graduated from the University of Akron with a Bachelor of Arts in News/Mass Media Communication and a certificate in psychology. She is passionate about providing genuine information to encourage and guide healing in all aspects of life. Read more

Medically Reviewed By – Dr. Jessica Pyhtila, PharmD

Dr. Jessica Pyhtila is a Clinical Pharmacy Specialist based in Baltimore, Maryland with practice sites in inpatient palliative care and outpatient primary care at the Department of Veteran Affairs. Read more