Butorphanol Injection
Butorphanol injection is an opioid pain reliever used to manage severe pain, as a preoperative or anesthetic supplement, and for pain relief during labor.
🧬 Where this information comes from Click to expand
The clinical label records used on this page are FDA-filed Structured Product Labeling (SPL) retrieved through openFDA. We identified 2 clinical label sets within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. Forms, routes, brands, labelers, strengths, and NDC product-record counts are built separately from matching FDA National Drug Code Directory records. The linked DailyMed document is a representative official source for verification, not the page’s only clinical source. View the linked label on DailyMed →
⚠️ FDA Boxed Warning — the FDA’s strongest safety alert ▾
Butorphanol Tartrate Injection carries serious FDA boxed warnings that every patient and caregiver should know about.
Addiction and misuse: Like all opioids, butorphanol can be misused or lead to addiction, even when taken exactly as prescribed. Overdose from opioids can be fatal.
Life-threatening breathing problems: Butorphanol can cause breathing to slow dangerously or stop — especially when you first start using it or after a dose increase. This risk is greatest in elderly, frail, or debilitated patients and those with lung disease.
Neonatal opioid withdrawal syndrome: If used for a prolonged time during pregnancy, the newborn may go through opioid withdrawal after birth. This can be life-threatening if not recognized and treated right away.
Dangerous combinations: Taking butorphanol with benzodiazepines (like Valium or Xanax), alcohol, or other sedating substances can cause extreme sedation, stopped breathing, coma, or death. This combination should only be used when there is no safer option, and only under close medical supervision.
📖 Butorphanol Injection: Patient Information Guide
A plain-language walkthrough of Butorphanol Injection — what it treats, how it works, how it’s taken, side effects, warnings and interactions. Tap any section to expand it.
🎯What it's used for▾
Butorphanol injection is an opioid analgesic (pain reliever) used in several specific medical situations:
- Managing pain that is severe enough to require an opioid and for which non-opioid alternatives are inadequate
- As a preoperative or pre-anesthetic medication given before surgery
- As a supplement to balanced anesthesia during a surgical procedure
- Relieving pain during early labor in patients at full term — not intended for use close to the time of delivery
⚙️How it works▾
Butorphanol binds to two types of opioid receptors in the brain and spinal cord: it partially activates mu receptors and fully activates kappa receptors. This combination produces strong pain relief (analgesia). It also directly affects the brain's respiratory control centers, which is why breathing must be monitored closely — especially at higher doses or when combined with other sedating drugs.
Kappa receptor activation can sometimes cause unusual perceptual effects (psychotomimetic effects) such as dysphoria or hallucinations in some people. Butorphanol also slows movement in the gut, which can cause constipation, and can affect hormone levels with longer-term use.
💊How it's taken▾
Butorphanol Tartrate Injection is always administered by a healthcare professional — never self-injected at home. It can be given into a vein (IV) or into a muscle (IM), and the route chosen affects how quickly it works. For pain management, it is typically given every three to four hours as needed. Elderly patients and those with liver or kidney problems require longer intervals between doses and lower starting amounts.
- IV administration: pain relief begins within a few minutes; peak effect at 30–60 minutes
- IM administration: absorption is rapid; peak effect at 30–60 minutes; pain relief generally lasts 3–4 hours
- Dosing for surgery, anesthesia, and labor has specific timing — always managed by your medical team
Your dose is always tailored to your situation. Never adjust it on your own.
🤒Side effects — in detail▾
The most common side effects reported with Butorphanol Tartrate Injection include:
- Drowsiness or somnolence (very common)
- Dizziness
- Nausea and/or vomiting
- Headache
- Sweating
- Constipation
- Dry mouth
- Blurred vision
- Feelings of floating, euphoria, or confusion
- Anxiety or nervousness
Serious reactions that require immediate medical attention include dangerously slow or stopped breathing, extreme drowsiness or difficulty waking up, signs of serotonin syndrome (agitation, fast heartbeat, muscle rigidity, high temperature), signs of adrenal insufficiency (prolonged fatigue, dizziness, low blood pressure, nausea), or severe allergic reactions such as anaphylaxis.
⚠️Warnings & precautions▾
- Respiratory depression: Butorphanol can cause life-threatening slowing or stopping of breathing. Risk is highest when starting the drug, after dose increases, and when combined with other sedating substances. Elderly, frail, or debilitated patients and those with lung disease are at the greatest risk.
- Addiction, misuse, and abuse: As a controlled opioid, butorphanol carries real risk of addiction even when used correctly. Personal or family history of substance use disorder increases this risk.
- Dangerous drug combinations: Combining butorphanol with benzodiazepines, alcohol, sleep aids, muscle relaxants, antipsychotics, or other opioids dramatically increases the risk of coma and death from respiratory failure.
- Neonatal opioid withdrawal syndrome: Prolonged use in pregnancy can cause the newborn to go through withdrawal after birth — a potentially life-threatening condition requiring specialized neonatal care.
- Cardiovascular effects: Butorphanol increases the workload on the heart; use in patients with heart attack, ventricular dysfunction, or coronary insufficiency requires careful benefit-risk assessment.
- Do not stop suddenly: In people who have used butorphanol regularly, abrupt discontinuation can trigger withdrawal. Doses should be tapered gradually under medical supervision.
- Opioid-induced hyperalgesia: Rarely, opioids can paradoxically increase pain sensitivity — tell your provider if your pain seems to worsen despite treatment.
🔀What it interacts with▾
Butorphanol Tartrate Injection can interact seriously with several types of drugs and substances:
- Benzodiazepines (e.g., diazepam, lorazepam, alprazolam) — combined use can cause profound sedation, stopped breathing, coma, or death
- Alcohol — greatly increases sedation and breathing risk; avoid completely
- Other CNS depressants (sleep aids, anti-anxiety medications, muscle relaxants, antipsychotics, gabapentin, pregabalin) — additive sedation and respiratory depression
- Other opioids — increased overdose risk; butorphanol is a mixed agonist-antagonist and may trigger withdrawal if combined with a full opioid agonist
- Serotonergic drugs (SSRIs, SNRIs, tricyclic antidepressants, triptans, tramadol, mirtazapine, trazodone, MAO inhibitors, linezolid) — risk of serotonin syndrome, a potentially life-threatening reaction
- MAO inhibitors — no safe guidance exists for this combination; avoid
- Drugs that affect liver metabolism (e.g., erythromycin, theophylline) — may change how butorphanol is processed; dose adjustments may be needed
This is not a complete list of interactions. Always talk with your doctor or pharmacist before starting, stopping, or changing any medication.
📋Before taking it▾
- People with significant respiratory depression, severe or unmonitored asthma, or low blood oxygen — butorphanol is contraindicated in these situations
- People with COPD, cor pulmonale (right heart strain from lung disease), or other chronic lung conditions — at high risk of dangerous breathing slowdown
- People with known or suspected bowel obstruction, including paralytic ileus (stopped bowel movement) — butorphanol is contraindicated
- Anyone with a hypersensitivity or allergic reaction to butorphanol tartrate or benzethonium chloride (a preservative in the multi-dose vial) — do not use
- People with liver or kidney disease — require lower doses and longer dosing intervals
- Older adults — more sensitive to respiratory and sedating effects; need closer monitoring and dose adjustment
- People with a history of seizure disorders — butorphanol may worsen seizure control
- People with increased intracranial pressure (pressure inside the skull), brain tumors, or head injury — use with caution; drug may worsen these conditions and mask symptoms
- Pregnant women — prolonged use can cause neonatal opioid withdrawal syndrome; discuss risks and birth plan with your provider
- Breastfeeding women — butorphanol passes into breast milk; discuss with your provider
- People with a personal or family history of addiction or mental illness — at higher risk; requires close monitoring
🚑If you take too much▾
Taking too much butorphanol can cause dangerously slow or stopped breathing, extreme drowsiness progressing to stupor or coma, limpness of muscles, cold or clammy skin, pinpoint pupils, very low blood pressure, and in severe cases, death. If overdose is suspected, emergency care is needed immediately. The opioid reversal agent naloxone can reverse butorphanol's effects, though larger doses may be needed because of butorphanol's mixed opioid action — and monitoring must continue even after reversal since butorphanol may outlast the antidote.
📡Pharmacodynamics — effects in the body▾
After injection, butorphanol produces analgesia (pain relief) with an onset of a few minutes via IV and within about 15 minutes via IM injection. Peak pain-relieving effect occurs within 30 to 60 minutes with either route, and pain relief generally lasts 3 to 4 hours with IM or IV dosing. Butorphanol also slows gut motility — meaning digestion is slowed and constipation is common — and it can affect cardiovascular function by increasing pulmonary artery pressure and cardiac workload, which is important in patients with heart conditions. Like other opioids, it can affect hormone systems with longer-term use, potentially reducing levels of sex hormones.
🔬Pharmacokinetics — how your body processes it▾
After intramuscular injection, butorphanol is rapidly absorbed and reaches peak blood levels in about 20 to 40 minutes. It is approximately 80% bound to proteins in the blood and is extensively metabolized in the liver. The drug crosses into the brain, across the placenta, and into breast milk. The average half-life (time for blood levels to fall by half) is about 4.5 hours in younger adults and about 5.6 hours in older adults, meaning the drug stays active for several hours. Because the major metabolite, hydroxybutorphanol, has a much longer half-life of about 18 hours, it can accumulate with repeated dosing — a key reason dose and interval adjustments matter, especially in elderly patients and those with liver or kidney impairment.
📦How to store it▾
Store at 20°C to 25°C (68°F to 77°F). Protect from light.
📄 Written from Butorphanol Injection’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Every point is grounded in that labeling — nothing is invented. How we use AI →
Supplements & herbs that interact with Butorphanol Injection
100 supplements and herbal products have documented interactions with Butorphanol Injection in the licensed clinical database we use. Most are manageable — but your pharmacist should know about everything you take, including vitamins and herbals.
- Major · 7
- Moderate · 78
- Minor · 15
Educational information from a licensed clinical database (Natural Medicines) — see our data sources & update cadence. Not medical advice: an interaction being documented does not mean it will happen to you; do not start or stop medications or supplements without professional guidance.
🩺 Pharmacist Counseling Corner
Quick, plain-English answers to the questions patients ask most about Butorphanol Injection — the kind of thing our pharmacy team would talk through with you at the counter.
What is butorphanol injection actually used for? ▾
How fast does butorphanol injection work, and how long does it last? ▾
What side effects should I expect, and which ones should make me call for help right away? ▾
Can I drink alcohol or take other medications while receiving butorphanol? ▾
Is butorphanol safe to use during pregnancy or while breastfeeding? ▾
What happens if I've been using butorphanol regularly and want to stop? ▾
Is Butorphanol Injection available over the counter? ▾
Is Butorphanol Injection a controlled substance? ▾
When was Butorphanol Injection first available? ▾
Who makes Butorphanol Injection? ▾
💬 Answers drafted from Butorphanol Injection’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Grounded in that labeling — nothing is made up. How we use AI →
🧰 Keep exploring
💊 How Butorphanol Injection comes
Butorphanol Injection is available in 1 form. Different forms and brands can have different approved uses, doses, schedules, and directions. Follow the instructions for your exact product, and do not switch forms without guidance from your prescriber or pharmacist.
Injection
How this form is used
- Butorphanol Tartrate Injection is used to manage severe pain requiring an opioid when other treatments are inadequate
- Butorphanol Tartrate Injection is used as a preoperative or pre-anesthetic medication before surgery
- Butorphanol Tartrate Injection is used as a supplement to balanced anesthesia during surgical procedures
- Butorphanol Tartrate Injection is used to relieve pain during early labor in patients at full term
- Butorphanol Tartrate Injection is given by a healthcare professional either into a vein (IV) or into a muscle (IM)
- For pain, Butorphanol Tartrate Injection is typically given every three to four hours as needed; elderly or patients with kidney or liver impairment require adjusted dosing intervals
- For labor pain, Butorphanol Tartrate Injection (IV or IM) may be repeated after 4 hours, but an alternative should be used if delivery is expected within 4 hours
- Butorphanol Tartrate Injection should be inspected visually for particles or discoloration before use
📊 Butorphanol Injection across the U.S. market
How Butorphanol Injection appears in the FDA’s National Drug Code Directory — including its dosage forms, strengths, brand names, manufacturers, and FDA-listed product records. These are directory records, not sales or prescription volume.
Share of FDA-listed product records by manufacturer — FDA National Drug Code Directory. Record counts are not sales or prescription volume.
📈 How widely Butorphanol Injection is used
A general measure of how commonly Butorphanol Injection is prescribed, based on Medicaid — one of the largest public drug programs. The figure below is prescriptions filled in Q1–Q4 2025, summed across every form and brand of the drug.
Think of this as a proxy for how widely Butorphanol Injection is used, drawn from freely available public data. Medicaid is just one program — these numbers don’t include Medicare, other government coverage, or commercial and cash-pay prescriptions, so real-world use is higher than what’s shown here.
How commonly is Butorphanol Injection prescribed? Of the 1,597 medications we measure, Butorphanol Injection ranks #1,289 by Medicaid prescriptions — more than 19% of them.
Utilization by Butorphanol Injection product
Pick a product to see its own Medicaid numbers. Each chip is one clinical product — a specific strength & dosage form as defined by RxNorm — with brand-name and generic versions combined.
1 ML butorphanol tartrate 2 MG/ML Injection Most dispensed
Summed across the 1 of 3 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 1728351
1 ML butorphanol tartrate 1 MG/ML Injection
Summed across the 1 of 3 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 886627
Shares are of the Medicaid prescriptions shown here. Product grouping follows RxNorm (the National Library of Medicine’s drug terminology), so “one product” means one strength & dosage form regardless of manufacturer. Dollar figures are gross Medicaid reimbursement before mandatory rebates — rebates (often large, especially for brand-name drugs) are confidential, so actual net cost to Medicaid is lower than shown.
Source: Medicaid State Drug Utilization Data (CMS), aggregated by generic ingredient — summed across every NDC (all brands, strengths, salt forms and dosage forms) of Butorphanol Injection, and across all states and both fee-for-service and managed-care claims. A general popularity signal; it excludes Medicare, commercial insurance and cash prescriptions, so it is not total U.S. use. Based on the 2 of 6 listed Butorphanol Injection NDCs with Medicaid activity.
🔍 Compare Butorphanol Injection products
A representative set of FDA-listed product records for Butorphanol Injection — across manufacturers, strengths, and dosage forms, grouped by form with each product’s manufacturer and how the FDA approved it. The same medicine may be made and packaged by different companies, so a single drug can have many directory entries. (It’s also why a refill can look different — a new shape, color, or box — even though it contains the same medication.)
| Strength | Route | Manufacturer / Labeler | Category ⓘ | Details |
|---|---|---|---|---|
| 💊Injection | ||||
| 1 mg/mL | Intramuscular, Intravenous | Hikma Pharmaceuticals USA Inc. | ANDA | View NDC → |
| 1 mg/mL | Intramuscular; Intravenous | Hikma Pharmaceuticals USA Inc. | ANDA | View NDC → |
| 2 mg/mL | Intramuscular, Intravenous | Hikma Pharmaceuticals USA Inc. | ANDA | View NDC → |
| 2 mg/mL | Intramuscular; Intravenous | Hikma Pharmaceuticals USA Inc. | ANDA | View NDC → |
| 1 mg/mL | Intramuscular, Intravenous | Hospira, Inc. | ANDA | View NDC → |
| 1 mg/mL | Intramuscular; Intravenous | Hospira, Inc. × 2 listings | ANDA | View NDC → |
| 2 mg/mL | Intramuscular, Intravenous | Hospira, Inc. | ANDA | View NDC → |
| 2 mg/mL | Intramuscular; Intravenous | Hospira, Inc. × 2 listings | ANDA | View NDC → |
Showing 10 of 10 products — FDA National Drug Code Directory. See every product, package size and price: browse all 10 Butorphanol Injection NDCs →
📈 What people report — real-world data (FDA FAERS)
After a medicine reaches the market, patients, doctors and drugmakers can send the FDA reports of problems they think may be linked to it. Here’s what’s been reported for Butorphanol Injection — a signal of what to watch for, not proof the drug caused it.
Source: openFDA, from the FDA Adverse Event Reporting System (FAERS). These are voluntary reports — they don’t prove the drug caused the effect, and counts reflect how often something was reported, not how often it actually happens. Reports also often name the very problem the medicine is taken for — a common reason to file one is that the drug didn’t help — so for a pain reliever you may see “pain” high on the list; that points to why the report was filed, not to the drug causing the symptom. This counts every report that lists Butorphanol Injection in any role, so the total runs higher than the FDA’s official dashboard, which counts only cases where the drug is the suspect. For the authoritative figures, see the FDA FAERS Public Dashboard. Always talk to your pharmacist or doctor.
🏛️ The road to your pharmacy
How Butorphanol Injection went from FDA review to the pharmacy shelf — the key milestones in its regulatory journey.
Source: Drugs@FDA.
🚨 Recall history
A recall is when a specific batch of a medicine is pulled from the market — usually a manufacturing issue, not a problem with the drug itself. Class I is most serious, Class III least.
Source: openFDA drug enforcement (recall) reports.
RxNorm Concept Web — From Ingredient to Every Form and Strength
This page starts with one ingredient concept (IN). The branches below show its dose-form concepts (SCDF), then the available clinical drug and strength concepts (SCD). Combination products remain separate concepts with their own pages.
RxCUI 1841 3 dose forms · 6 strengths
-
Dose form (SCDF) Injectable Solution RxCUI 371174In current FDA listingsClinical drug / strength (SCD) tartrate 2 MG/MLRxCUI 88662210 MG/MLRxCUI 1302739 -
Dose form (SCDF) Injection RxCUI 1728350In current FDA listingsClinical drug / strength (SCD) 1 ML butorphanol tartrate 1 MG/MLRxCUI 8866271 ML butorphanol tartrate 2 MG/MLRxCUI 17283512 ML butorphanol tartrate 2 MG/MLRxCUI 1728355 -
Dose form (SCDF) Metered Dose Nasal Spray RxCUI 2201634No current FDA listingClinical drug / strength (SCD) tartrate 1 MG/ACTUATRxCUI 886634
Look up RxCUI 1841 in the RxCUI Atlas →
RxNorm is the U.S. National Library of Medicine’s normalized drug vocabulary. Its concept hierarchy can include forms that are not currently marketed; the status on each branch compares that concept with current FDA listings. RxCUIs identify vocabulary concepts, not individual packages or manufacturers.
📦 Supply & shortage status
Whether Butorphanol Injection is in short supply in the U.S. right now, plus any shortage history the FDA has on record. A shortage usually reflects a manufacturing or demand issue — not a safety problem with the drug.
Source: openFDA, from the FDA Drug Shortages database.
🏷️ Sold under these brand names
🏭 Manufacturers & labelers
RxNorm drug class
Butorphanol Injection belongs to the Opioid Agonist/Antagonist class.
Classified by RxNorm RxClass — the U.S. National Library of Medicine's standardized drug-classification service (Established Pharmacologic Class from the FDA, the ATC drug family from the WHO, and mechanism of action). Reference only, not medical advice.
🔬 Where this comes from
Core label, product, RxNorm, safety, and utilization data on this page come from the sources identified below. AI-written, editorial, and licensed sections are labeled separately.
How we combine label and product data
HelloPharmacist combines public FDA and NLM records; we don’t author the underlying clinical facts. We identified 2 FDA-filed SPL label sets within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. The representative label is the starting point for the displayed reference monograph; the 12 largest stored in-scope SPL records, which may include that representative, are compared section by section, and the longest available version of each section is retained. Forms, routes, brands, labelers, product-listed strengths, and product-record counts are aggregated separately from ingredient-matched FDA NDC Directory records; package records listed above are associated with the linked SPL; and the normalized concept hierarchy comes from NLM RxNorm.
Where a section is identified as AI-written, its plain-language text is generated from bounded label evidence. New draft drug pages remain in the admin review queue before first publication. Hospira, Inc. is the representative DailyMed label linked for verification and dates; it is not the sole source used for the page.
This is general education, not medical advice — always consult your doctor or pharmacist about your medications and any medical condition. For the exact wording of the linked representative label, view that label on DailyMed; some displayed composite sections may come from other in-scope SPL labels. Learn how we use AI and our data sources & update cadence.