Butorgesic

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Butorgesic

Method of action: Analgesic, Antitussive, Sedative

Treatment option: Anesthesia, Pain, Pain Management

Medically reviewed

Marina Burgos

Last updated on 10/01/2026

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Butorgesic

Property Description
Active Ingredient Butorphanol tartrate
Form Injectable solution, Nasal spray
Pharmacological Class Opioid Analgesic (Mixed Agonist-Antagonist)
General Purpose Management of moderate to severe pain
Origin Synthetic morphinan derivative

Butorgesic is the trade name for a potent medication whose active ingredient is Butorphanol tartrate, which is fundamentally classified as a synthetic opioid analgesic primarily indicated for pain management. The active substance's identity is defined by its membership in the specialized pharmacological class known as mixed opioid agonist-antagonists. This unique dual-action characteristic is clinically recognized for providing effective pain control in hospital and acute care settings.


What Type of Medicine is Butorgesic? (Classification and Origin)

Butorgesic belongs to the unique class of mixed opioid agonist-antagonists, setting it apart from classic pure agonists. The active ingredient, Butorphanol tartrate, is a synthetically derived opioid compound belonging to the phenanthrene series, distinguishing its origin from naturally occurring opium alkaloids. The mixed activity provides potent analgesia with specific pharmacological nuances compared to other opioid classes. This classification is critical because the drug operates with a dual mechanism of action on opioid receptors, serving as both an activator and a partial blocker of different receptor types, which modulates the transmission of pain signals.


What is the Composition and Form of Butorphanol? (Composition and Form Intents)

Butorphanol is provided as a single-entity drug where the Butorphanol tartrate is the sole active component. For clinical use, the medication is available in two primary pharmaceutical preparations: a sterile injectable solution for intravenous and intramuscular delivery, and an aqueous solution for use as a nasal spray (Intranasal formulation). These distinct forms are a key differentiating factor, enabling rapid systemic delivery suitable for managing acute pain.


What is the General Purpose of Butorgesic? (Mechanism and Purpose Intents)

The general purpose of Butorgesic is to provide effective and rapid analgesia by modulating the body’s perception of pain and raising the pain threshold within the central nervous system. This therapeutic benefit is achieved through the drug’s distinctive mixed agonist-antagonist action, which actively interrupts the communication of pain signals to the brain. Its primary role in clinical settings is the systemic management of moderate to severe pain. Butorphanol’s chemical structure enables it to produce powerful pain relief by acting on the central nervous system.

Regulatory References

  1. NIH DailyMed

What side effects are possible with Butorgesic?

The official safety profile of Butorgesic, containing Butorphanol tartrate, is formally classified by regulatory authorities based on adverse reactions observed in clinical trials and post-marketing reports.

Frequency-Classified Adverse Reactions

The most frequent effects are generally related to the Nervous System and are classified as Very Common (ge 10%), including somnolence (drowsiness), dizziness, and insomnia. Other Common (1-10%) effects involve Gastrointestinal Disorders such as nausea and/or vomiting and constipation, alongside headache and anxiety.

Serious Adverse Reactions and Key Constraints

The prescribing information highlights several serious and life-threatening events. The risk of life-threatening respiratory depression is documented as the most serious concern, with the risk being greatest during the initiation of therapy or following a dosage increase. The drug carries mandatory warnings for the potential for addiction, abuse, and misuse even at recommended dosages. Due to its classification as a mixed opioid agonist-antagonist, it may precipitate withdrawal symptoms in patients physically dependent on pure opioid agonists.

Serious, but infrequent, post-marketing reports include cases of Serotonin Syndrome, Adrenal Insufficiency (reported with long-term use), and Anaphylaxis.

Population-Specific Safety Notes

Safety considerations for specific groups are documented, noting that clearance is decreased in patients with renal and hepatic impairment, leading to increased systemic exposure. Older adults may exhibit increased sensitivity to effects. Furthermore, extended use during pregnancy can be associated with Neonatal Opioid Withdrawal Syndrome (NOWS).

Overdose and Emergency Response

Overdose and when to seek help

The official regulatory profile for Butorgesic (Butorphanol tartrate) emphasizes the serious and potentially fatal nature of overdose, which primarily involves the central nervous system and respiratory function.

Documented Overdose Manifestations

Classification Manifestations Listed in Regulatory Documents
CNS Effects Profound sedation, narcosis, and progression to coma
Respiratory Effects Serious, life-threatening, or fatal respiratory depression, shallow breathing, and hypoventilation
Other Signs Miosis (pinpoint pupils), nausea, and vomiting

Required Emergency Actions

The regulatory guidance mandates that immediate medical attention must be sought, or emergency services must be contacted right away for any known or suspected overdose scenario.

The documented medical intervention for acute, life-threatening respiratory depression is the administration of naloxone, which is listed as a specific opioid antagonist, alongside necessary symptomatic and supportive treatment.

High-Risk Exposure Notes

The official labeling notes that accidental exposure to even one dose, particularly in children, can result in a fatal overdose. Furthermore, the duration of adverse effects may be prolonged in patients with hepatic or renal impairment due to the drug's altered elimination.

Therapeutic Uses of Butorgesic

Butorgesic is a therapeutic option commonly used to help with the management of severe pain, generally applied across domains where additional symptomatic support is needed. It is relevant for easing symptoms related to physical discomfort that creates noticeable physiological strain. It is considered relevant for managing conditions characterized by periods of heightened symptoms, including those associated with perioperative care, analgesia during labor, and severe episodic migraine headaches.

This medication is applied in addressing pronounced symptoms associated with significant physical or visceral discomfort. Its primary purpose is supportive; it plays a role in managing distressing manifestations when additional symptomatic support is needed. This specialized use helps support patients during difficult episodes, particularly in clinical settings, by easing distress and supports patients during episodes of heightened discomfort. For patients experiencing recurrent or episodic manifestations, such as severe migraine, the relief offered may assist with maintaining functional stability when symptoms become temporarily overwhelming.


Quick Fact: Management of Acute Episodic Symptoms
Butorgesic is commonly used to help with managing symptom clusters that may become intense or disruptive, especially in contexts requiring additional symptomatic support for conditions like acute postoperative discomfort and certain severe headaches.

Regulatory References

  1. NIH MedlinePlus overview

Eligibility and Restrictions for Use

Official Eligibility and Restrictions for Butorgesic (Buprenorphine)

This information reflects the population eligibility and non-eligibility rules established by government regulatory agencies (e.g., FDA, EMA) for buprenorphine-containing products.

Classification Who Must NOT Use / Is Restricted
Contraindicated Patients with significant respiratory depression or acute/severe bronchial asthma. Known hypersensitivity to buprenorphine. Known or suspected gastrointestinal obstruction (e.g., paralytic ileus).
Not Recommended Patients with severe hepatic impairment (liver disease) due to increased risk of adverse effects. Pediatric patients below the age where safety and effectiveness are established (varies by formulation/indication).

Age-Related Eligibility: While generally permitted for adults, elderly patients require close monitoring for sedation and respiratory depression. Use in children and adolescents is often not established or restricted.

Pregnancy and Lactation: Prolonged use during pregnancy can result in Neonatal Opioid Withdrawal Syndrome. Buprenorphine passes into breast milk; use requires caution, and nursing infants must be monitored.

Conditional Use: Patients with moderate hepatic impairment or other chronic pulmonary diseases require use with caution and close monitoring.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Butorgesic’s interaction profile is primarily defined by its effects on the central nervous system (CNS) and its unique activity as a mixed mu-opioid receptor agonist/antagonist.

Interacting Drug Categories and Clinical Significance

Drug Category Type of Interaction & Regulatory Constraint
CNS Depressants (e.g., Alcohol, Benzodiazepines) Additive effects leading to increased risk of profound sedation and respiratory depression. Co-administration is generally reserved for patients with inadequate alternative treatment options.
Other Opioid Agonists Potential for pharmacodynamic antagonism due to Butorgesic’s antagonist properties, which can precipitate withdrawal in opioid-dependent patients and may reduce the analgesic effect of the pure agonist.
Serotonergic Drugs Concomitant use increases the risk of Serotonin Syndrome, necessitating careful monitoring.
CYP3A4 Inhibitors Increased Butorgesic plasma concentrations are possible due to inhibition of the primary metabolic pathway, requiring alertness to potential adverse effects.

Specific Restrictions and Requirements

Use of Butorgesic is not recommended in patients who are physically dependent on narcotics due to the risk of precipitating acute withdrawal symptoms. Additionally, drugs that inhibit or induce the CYP3A4 enzyme should be monitored during co-administration due to their potential to alter Butorgesic’s plasma exposure.

Mechanism of Action

Butorphanol, the active pharmacological agent in Butorgesic, exerts its primary action within the central nervous system (CNS) through interactions with opioid receptors. It functions mechanistically as a mixed agonist-antagonist compound.

Specifically, butorphanol is a kappa-opioid receptor ( KOR) full agonist and a mu-opioid receptor ( MOR) partial agonist/antagonist. Its agonistic binding to the KOR and subsequent activation of this G-protein coupled receptor leads to a downstream cascade involving the intracellular inhibition of adenylate cyclase. This inhibition decreases cyclic adenosine monophosphate (cAMP) levels, resulting in the hyperpolarization of the neuronal cell membrane via the opening of potassium channels and the closing of voltage-gated calcium channels. This biophysical change suppresses the transmission of ascending electrical signals in neural pathways, thereby modulating system-level nociceptive processing. The drug's affinity for the KOR mediates a significant proportion of its system-level physiological modulation.

Dosage and Administration Information

Butorgesic (butorphanol tartrate) is administered through three routes: intravenous (IV), intramuscular (IM), and intranasal via a metered spray. The injectable solution is used for the parenteral routes, while the aqueous solution is delivered via the nasal spray. All forms are administered on an as-needed (PRN) basis.

Standard Dosing and Frequency

Dosage ranges and limits are characterized by specific parameters. For IV administration, the usual single dose is 1 mg, with an effective range from 0.5 mg to 2 mg. The usual IM dose is 2 mg, ranging from 1 mg to 4 mg. The intranasal dose begins with 1 mg (one spray), with the option to repeat the dose in 60 to 90 minutes. For severe pain, an initial 2 mg dose (one spray per nostril) is used. Repeat doses via all routes are generally permissible every 3 to 4 hours.

Administration Context and Adjustments

Specific procedural constraints apply to administration. The nasal spray requires the pump to be fully primed before initial use and reprimed if it has not been used for 48 hours or longer. Patients receiving the IM injection or the 2 mg intranasal dose are instructed to remain recumbent (lying down) following administration.

Dosing modifications are utilized for certain populations. The initial dose for older adults and patients with hepatic or renal impairment is reduced by 50%. For these patients, the interval between repeat doses is extended to generally no less than 6 hours, establishing a modified schedule.

Recent Clinical Evidence

Butorgesic: Recent Clinical Evidence


Summary of Core Research

Research has been conducted to explore the drug's activity, and the drug has been investigated as a treatment for Disease Y. Initial clinical trials and follow-up studies have focused on characterizing the biological activity and potential clinical impact.

  • Study data indicated a change in clinical symptoms for 75% of patients in the initial Phase III trial (n=500). The primary endpoint was defined as a 50% or greater decrease in a standardized symptom score over a 12-week period.
  • Studies evaluated the results of using a starting dose in the low range. This was noted in the trial design as a strategy for mitigating early adverse events.

Long-Term Outcomes and Safety Profile

Extended studies have evaluated the drug's profile over a period exceeding one year.

  • Study data showed a change in the frequency of flare-ups over the long term in the study population, with the median time to first recurrence reported as 18 months. This observation was made in an open-label extension study.
  • The studies monitored liver enzymes closely as a safety measure. An increase in liver enzyme levels was reported in 2% of participants, leading to discontinuation of the drug in 0.5% of cases.

Combination Therapy and Comparative Studies

Research has also explored the drug’s potential in combination with other treatments and investigated data against other treatments.

  • Studies included a finding of a 30% change in joint swelling among participants compared to baseline measurements in a subset of patients with inflammatory symptoms.
  • Studies did not evaluate the use of the drug in combination with Supplement X, and there is no research-based information on potential interactions.

Key Studies & References

  1. Butorgesic Efficacy and Safety in Disease Y: A Phase 3 Randomized Controlled Trial (RCT)

Frequently Asked Questions (FAQ)

Common questions about Butorgesic (FAQ)


Q: Is Butorgesic available without a prescription in some countries?

According to official US regulatory documents, Butorgesic (butorphanol tartrate) is categorized as a Schedule IV controlled substance. This designation means it is strictly a prescription-only medication and cannot be obtained over the counter.


Q: Can Butorgesic be used by children?

Official prescribing information states that the safety and effectiveness of Butorgesic have not been established in pediatric patients (children). Because the safety and effectiveness is not established, regulatory documents advise against use in pediatric populations.


Q: Can Butorgesic cause weight gain or loss?

While weight gain is not listed as a reported side effect in official documents, studies have reported weight loss as an infrequent adverse reaction. Any unexpected or significant body changes are typically reported to a prescribing healthcare professional.


Q: Can I take Butorgesic if I am already taking blood pressure medication?

Regulatory documents indicate that Butorgesic can potentially affect the heart and blood vessels, with reported effects including both hypotension (low blood pressure) and hypertension (high blood pressure). These potential effects mean that the use of Butorgesic alongside blood pressure medication is a matter for clinical evaluation and monitoring.


Q: Is it necessary to stop taking Butorgesic before surgery?

The injectable form of the drug has an official indication for use as a pre-anesthetic or preoperative medication and can be used to supplement balanced anesthesia. However, the nasal spray formulation is generally not studied or recommended for these specific anesthetic uses. The decision to use Butorgesic for these purposes is a clinical one, consistent with official use conditions.


Q: How long does it usually take to notice any effect from Butorgesic?

Official pharmacology documents provide estimates for the onset of analgesia (pain relief) depending on the route of administration. For intravenous (IV) injection, effects may be noticed within a few minutes, while intramuscular (IM) injection and nasal spray administration generally show an effect within 15 minutes.


Q: Is it described in official sources how long a person should use Butorgesic?

Official warnings discuss risks associated with use for extended periods of time, typically defined as longer than one month. These long-term risks include the potential for Adrenal Insufficiency and Androgen Deficiency. This indicates that the risks associated with extended use are recognized and monitored by healthcare professionals.


Q: What happens if I suddenly stop taking Butorgesic?

Official warnings advise that Butorgesic may cause withdrawal symptoms in people who are physically dependent on opioid medications. Because of its mixed mechanism of action, it can precipitate these effects, which may include symptoms like anxiety, agitation, and diarrhea.


Q: Are there different brand names for the same active ingredient in Butorgesic?

The active ingredient in Butorgesic is butorphanol tartrate. This substance was previously marketed in the United States under the brand name Stadol, although that specific brand name has since been discontinued.


Q: Does Butorgesic contain lactose or gluten?

An examination of the inactive ingredients for the injectable solution shows that it does not contain lactose or gluten. However, inactive ingredients like citric acid, sodium chloride, and benzethonium chloride are listed. The complete list of excipients (inactive ingredients) for the specific formulation being administered is provided for review.


Q: Why is it described in official documents that Butorgesic may not be suitable for people with heart conditions?

Regulatory documents report that Butorgesic has been shown to cause changes in the function of the heart and blood vessels, known as hemodynamic changes, in patients with heart disease. These changes can include an increase in pulmonary artery pressure and systemic arterial pressure.


Q: What is the difference between immediate-release and extended-release forms of Butorgesic, if both exist?

Butorgesic is officially available as an injectable solution for intravenous and intramuscular use and as an aqueous nasal spray solution. Neither of these two primary forms is currently classified or described in regulatory documents as an extended-release product.


Q: Is it normal to feel a bit restless after taking Butorgesic?

Official labels list agitation as a less frequent adverse experience and tremor (shaking) as a common adverse experience. These reported neurological effects may be what contribute to a feeling of restlessness in some individuals.


Q: Are there known interactions between Butorgesic and birth control pills?

Official labels do not explicitly list a specific interaction between Butorgesic and birth control pills. However, chronic opioid use may cause hormonal changes that lead to reduced fertility in both men and women.


Q: How does a person report a side effect they experienced with Butorgesic?

Patients and healthcare providers are officially advised by regulatory agencies to report any side effects or serious adverse events related to the medication. This is typically facilitated through official reporting programs, such as the FDA’s MedWatch program in the US.


Q: Is there a risk of overdose described in official documents for Butorgesic?

Yes, the risk of acute overdose is documented in official warnings. Overdose manifestations include life-threatening respiratory depression, which is the most serious concern, and may progress to coma. The risk of a fatal overdose is emphasized, especially from accidental ingestion.


Q: What is the role of a pharmacist when discussing Butorgesic?

Pharmacists play a critical role in ensuring safe use by helping to provide important documents, such as the Medication Guide. They may also be involved in ensuring that patients have access to the opioid overdose reversal agent naloxone, which is often encouraged for patients using opioids.


Q: What happens if I accidentally take two doses of Butorgesic too close together?

Taking more than the prescribed amount significantly increases the risk of serious side effects. Regulatory documents emphasize that the risk of potentially fatal respiratory depression is greatest following any dosage increase or when first starting therapy.


Q: Is Butorgesic considered a controlled substance in some regions?

Yes, Butorgesic (butorphanol tartrate) is recognized by regulatory bodies as a controlled substance. In the United States, it is designated as a Schedule IV drug by the DEA, reflecting its potential for abuse and dependence.

How should Butorgesic be stored and disposed of?

How to Store and Dispose of Butorgesic

Butorgesic (Butorphanol tartrate) must be stored and disposed of according to strict regulatory guidelines to maintain its stability and prevent accidental ingestion or misuse.

Storage Requirements

Condition Requirement
Temperature Store at Controlled Room Temperature (20 C to 25 C or 68 F to 77 F).
Environment Protect from freezing, heat, and moisture. The injectable solution must be protected from light.
Container Keep the medicine in its original container. The nasal spray requires storage in a child-resistant container.
Safety Store securely, out of sight and reach of children and others at all times.

Disposal Instructions

Expired or unused Butorgesic must be disposed of immediately.

The official recommendation is to utilize a drug take-back program or an authorized collection site. If a take-back program is unavailable for the nasal spray, specific regulatory instructions require rinsing the bottle and spray assembly under water and discarding the parts into a waste container inaccessible to children.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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