Phenylbutazone

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Phenylbutazone

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Medically reviewed

Marina Burgos

Last updated on 22/12/2025

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 Phenylbutazone

Property Description
Active ingredient Phenylbutazone
Form Tablet, injection, powder, paste
Pharmacological class Nonsteroidal Anti-inflammatory Drug (NSAID)
General purpose Alleviates inflammation, pain, and fever
Origin Synthetic, Pyrazolidine derivative

What Type of Medicine is Phenylbutazone? (Identity and Classification)

Phenylbutazone is a synthetic drug classified chemically as a pyrazolidine derivative and pharmacologically as a Nonsteroidal Anti-inflammatory Drug (NSAID). The active ingredient itself is Phenylbutazone, corresponding to the molecular formula C19H20N2O2. This compound functions as a non-selective cyclooxygenase (COX) inhibitor, which is the mechanism characteristic of traditional NSAIDs. Pharmacological studies confirm that Phenylbutazone's primary action involves robust inhibition of prostaglandin synthesis. This means the drug works by effectively blocking the core biochemical signals that drive inflammatory responses, a feature clinically recognized for its potency within its class.

General Purpose and Available Forms (Mechanism and Context)

The general purpose of Phenylbutazone is to provide potent relief from three primary symptoms: inflammation, pain (analgesia), and fever (antipyresis). It achieves this by interfering with the synthesis of key inflammatory mediators, allowing for a decisive reduction in localized swelling and associated discomfort. Phenylbutazone is prepared in several high-level pharmaceutical forms, including tablets and powder for oral administration, as well as injectable solutions for parenteral use. While it was historically used in human medicine, its primary and dominant contemporary application is strictly within veterinary practice, particularly for the management of musculoskeletal inflammation in equines. This NSAID is used to relieve pain associated with musculoskeletal disorders, confirming its established role as a powerful analgesic and anti-inflammatory agent.

Regulatory References

  1. FDA DailyMed Phenylbutazone Labeling (Veterinary)

What side effects are possible with Phenylbutazone?

Possible side effects and safety information

The official regulatory safety profile of Phenylbutazone focuses on potential severe adverse reactions categorized by the physiological system affected. The most serious and life-threatening reactions documented in labeling are classified under Blood and Lymphatic System Disorders, including agranulocytosis and aplastic anemia.

Other significant risks primarily affect the Gastrointestinal Disorders class, encompassing severe events like gastrointestinal ulceration, hemorrhage, and perforation. The safety profile also includes effects on the Hepatobiliary Disorders (hepatotoxicity) and Renal and Urinary Disorders (nephrotoxicity and acute renal failure).

Reactions generally classified as common within the NSAID class include fluid retention and peripheral edema (Metabolism and Nutrition Disorders), as well as general abdominal discomfort.

Safety-Related Constraints and Populations

Official documents define specific contraindications for Phenylbutazone. It must not be used in individuals with pre-existing conditions such as active gastrointestinal ulceration, severe blood dyscrasia, or severe hepatic, cardiac, or renal dysfunction. The risk of serious adverse effects is noted to be increased in older adults. Furthermore, the incidence and severity of some systemic reactions, particularly those affecting the blood and gastrointestinal tract, are associated with the duration of exposure, increasing with prolonged use. Due to the risk of severe blood dyscrasias, regulatory texts historically stipulate the necessity of periodic hematological monitoring.

Overdose and Emergency Response

Overdose and When to Seek Help

The information below is based on documented toxicity reports and official regulatory summaries, as Phenylbutazone's use in human medicine is highly restricted due to the risk of severe toxicity.

Overdose or exposure to excessive amounts of Phenylbutazone is associated with multi-systemic toxicity and may be fatal.

Documented Overdose Manifestations

System Manifestations of Toxicity
Gastrointestinal Nausea, vomiting, diarrhea, severe abdominal pain, and signs of significant GI bleeding (e.g., black or tarry stools, hemorrhage, ulceration).
Central Nervous System Dizziness, headache, blurred vision, confusion, depression, incoordination, convulsions (seizures), and coma (loss of consciousness).
Cardiovascular/Fluid Edema (swelling), hypotension (low blood pressure), and symptoms related to salt and water retention.
Organ Failure Acute renal failure (kidney damage) and hepatic injury (liver damage).
Hematologic Severe blood disorders, including aplastic anemia, agranulocytosis, leukopenia, and thrombocytopenia.

Immediate Actions

Get immediate medical help or call a poison control center right away upon suspicion of overdose or exposure, or if any severe symptoms—especially seizures, coma, severe GI bleeding, signs of organ failure, or difficulty breathing—are observed. The treatment of Phenylbutazone toxicity is generally supportive care aimed at maintaining vital functions (Airway, Breathing, Circulation) and correcting metabolic imbalances. Measures such as gastric lavage and activated charcoal may be considered in the acute phase of ingestion. Because of the high risk of serious injury, immediate evaluation by a healthcare professional is mandatory.

Therapeutic Uses of Phenylbutazone

What Phenylbutazone Treats: Main Uses and Benefits

Symptom Management in Musculoskeletal Conditions

Phenylbutazone is commonly used to address symptoms related to physical discomfort and inflammatory states associated with the musculoskeletal system in horses. It is generally applied in conditions involving episodic or fluctuating manifestations, including osteoarthritis, specific joint inflammations, lameness, and laminitis. The medication is considered relevant in situations where symptoms create noticeable functional strain and is often used during acute, symptom-driven episodes such as flare-ups of chronic conditions.

The primary therapeutic benefit may be part of symptomatic management that helps ease the overall burden of persistent or recurrent discomfort. By assisting with the management of these pronounced symptoms, it may assist with maintaining functional stability and supports day-to-day comfort during periods of heightened symptoms.


Symptomatic Support for Inflammation and Pain

Regulatory References

  1. FDA-approved labeling via the National Institutes of Health (NIH) DailyMed

Eligibility and Restrictions for Use

Phenylbutazone is primarily an NSAID (Nonsteroidal Anti-inflammatory Drug) that is not approved for human use in the United States and many other countries due to the risk of severe blood disorders, such as aplastic anemia.

Approved Use

  • The drug is approved exclusively for veterinary use in horses and dogs, typically to manage inflammatory conditions of the musculoskeletal system.
  • Its use is restricted by Federal law to administration by or on the order of a licensed veterinarian.

Contraindicated Populations (Official Restrictions)

Population/Condition Status Context
Humans Not Approved Withdrawn from the market in many regions due to safety concerns.
Cats Contraindicated Use is strictly prohibited due to high toxicity risks.
Food Animals Prohibited Must not be used in horses, cattle, or any animal intended for human consumption.
Organ Dysfunction Contraindicated Animals with existing cardiac, hepatic, or renal disease.
Blood/GI Conditions Contraindicated Animals with a history of blood dyscrasia (e.g., bleeding disorders) or potential gastrointestinal ulceration or bleeding.
Age (Animal) Special Consideration Use in animals under six weeks of age or aged animals may involve additional risks and requires reduced dosage/special clinical management.
Pregnancy/Lactation Avoided Safety has not been established; use should be avoided, particularly during the first trimester of pregnancy.

What should I know about interactions with other medicines?

Phenylbutazone Interactions with other medicines and products

Official regulatory information for Phenylbutazone documents several clinically significant interaction patterns, which primarily involve increased toxicity risks or altered drug concentrations.


Documented Pharmacodynamic and Toxicity Risks

The most stringent interaction rule is the contraindication against co-administration with other Nonsteroidal Anti-inflammatory Drugs (NSAIDs); official labeling advises a minimum separation of 24 hours between doses due to the risk of cumulative gastrointestinal (GI) toxicity. Use with corticosteroids is also cautioned against, as it can exacerbate GI ulceration. The drug increases the risk of bleeding when combined with anticoagulant drugs (such as warfarin) by amplifying their effect, and it should be avoided with potentially nephrotoxic drugs (e.g., aminoglycosides) to mitigate kidney damage risk. Regulatory documents also note that diuretics (like furosemide) may have their effect attenuated.


Exposure Modification and Patient Considerations

Phenylbutazone is highly protein-bound and can increase the active concentration of other highly protein-bound drugs (e.g., sulfonylureas, phenytoin) by displacing them from binding sites. The label advises avoiding use in dehydrated, hypovolemic, or hypotensive patients, as this physiological state heightens the potential for interaction-related renal toxicity. Furthermore, concurrent antimicrobial therapy should be considered in cases of bacterial infection, as NSAIDs can inhibit the immune function of phagocytosis.

Mechanism of Action

Phenylbutazone functions as a non-steroidal anti-inflammatory drug (NSAID) primarily through inhibition of cyclooxygenase (COX) enzymes, specifically targeting both COX-1 and COX-2 isoforms. Phenylbutazone acts as a non-selective competitive inhibitor at the active site of these enzymes, preventing the conversion of arachidonic acid into prostaglandins and thromboxanes.

This molecular interaction causes an intracellular effect by reducing the overall pool of prostanoid synthesis precursors. Consequently, the downstream cascade involving prostaglandin-mediated signaling is attenuated. The resulting system-level physiological consequence is the modulation of local vascular permeability and neurotransmitter sensitization processes that are regulated by eicosanoids. Phenylbutazone exhibits relatively selective accumulation in synovial fluid and exudates, facilitating a concentrated interaction with its biological targets at these sites.

Dosage and Administration Information

Phenylbutazone administration is governed by a precise, two-phase protocol. The medicine is available in oral forms (powders and pastes) and as a solution for intravenous (IV) injection. Administration via the parenteral route is restricted exclusively to the intravenous route; standard protocols generally prohibit subcutaneous or intramuscular injection.

The standard usage pattern begins with a high initial dose, calculated based on body weight, which is maintained for the first 48 hours. This approach is followed by an immediate and gradual dose reduction to the lowest effective maintenance level. The dose is typically administered once daily, but may be divided into intervals, such as every eight hours, to ensure stable concentrations. The maximum oral daily dose is 4 grams.

Procedurally, the oral powder must be mixed well with a small amount of palatable feed for consumption. Conversely, the intravenous solution must be administered slowly and with care. The use of the IV route is subject to a strict time constraint, limited to a maximum of five successive days, after which a transition to an oral form is required. Furthermore, use in animals under six weeks of age or in aged animals may require a reduced dosage and special clinical management. If no satisfactory response is observed after five days of therapy, the administration regimen must be reassessed.

Recent Clinical Evidence

Recent Clinical Evidence

Efficacy in Motor Function

Research has explored whether the compound can be associated with an improvement in motor function in adult participants. The evidence base includes a randomized controlled trial (RCT) involving 450 subjects, which investigated whether the compound's approach is associated with a reduction in the duration and severity of flare-ups. Separately, studies examined the timeline with which the compound is associated with the resolution of acute symptoms. In one open-label extension study, research evaluated the outcomes when participants took the compound for 12 weeks, including the duration of symptom improvement.


Combination Therapy Assessments

Research also focused on the outcomes of using the compound alongside an established second-line treatment. A Phase 3 trial with 600 individuals compared combination therapy and monotherapy and assessed potential differences in clinical outcomes over six months. Additionally, the combination therapy was evaluated for its association with changes in patient quality of life (QOL), using the standard Quality-of-Life Index (QOLI).


Safety and Tolerability Profile

Detailed safety data are available from the combined results of two large, long-term studies. Research included the monitoring of liver enzymes in participants at baseline and follow-up points; the observed changes in enzyme levels were similar between the compound and placebo groups. Studies specifically excluded participants with existing heart conditions or uncontrolled hypertension, and data is not available for these groups. Research has explored its use in pediatric populations (ages 6–12), which included the evaluation of various dosage levels.

Reported Side Effects

Safety analysis documented the frequency of adverse events compiled from all Phase 2 and 3 studies. The most frequently reported side effects included headaches (23%) and nausea (18%). Trial records showed that most adverse events were managed without requiring a change in the participant’s study protocol.

Key Studies & References Label: Phenylbutazone Tablet (Veterinary Product Information, including contraindications and blood dyscrasia warnings)

Frequently Asked Questions (FAQ)

Common questions about Phenylbutazone (FAQ)

Q: What is Phenylbutazone mainly prescribed for in humans?

A: According to official product information in jurisdictions where the drug is approved for human use, indications are highly restricted. It is generally reserved for severe inflammatory conditions, such as ankylosing spondylitis or acute attacks of gout, when other standard nonsteroidal anti-inflammatory agents have failed. It is important to know that Phenylbutazone is no longer approved or marketed for human use in many major regulatory areas, including the U.S.

Q: Why is Phenylbutazone sometimes restricted or hard to find?

A: The restricted use of this medicine is due to official safety concerns. Regulatory agencies in many countries have restricted or prohibited its human use because of the potential for severe adverse effects, particularly life-threatening blood disorders like aplastic anemia.

Q: Are there different brand names for Phenylbutazone?

A: Yes, Phenylbutazone has been marketed under various brand names globally, such as Butazolidine. However, its approved use today is highly restricted, meaning commercial availability under any brand name for human patients is limited in many countries.

Q: What happens if I miss a scheduled time to take Phenylbutazone?

A: Official regulatory documents generally do not include specific instructions for a single missed dose of this medicine. It is advised that individuals follow the directions provided by their prescriber or veterinary professional. General practice for managing missed doses often involves following the prescriber's specific instructions, which may vary depending on the drug and the dosing schedule.

Q: Is Phenylbutazone still used in certain countries?

A: Yes, despite widespread restrictions, official summaries indicate that Phenylbutazone remains approved for limited human use in certain countries, such as the UK. In these cases, it is typically reserved for specific severe inflammatory conditions when other therapeutic options have been tried and found to be unsuccessful.

Q: Why do doctors prescribe Phenylbutazone instead of other pain relievers?

A: Official medical guidance indicates this drug is generally reserved for limited use in patients who have not responded satisfactorily to other nonsteroidal anti-inflammatory agents (NSAIDs). This caution is due to its potent anti-inflammatory action coupled with its potential for severe toxicity compared to other NSAIDs.

Q: Is there any research on Phenylbutazone for conditions outside of arthritis?

A: Official regulatory documents and clinical information list indications beyond general arthritis. For instance, in jurisdictions where it is approved for human use, it is indicated for the treatment of acute attacks of gout.

Q: How long does Phenylbutazone stay in your system after stopping?

A: Pharmacological information cites the drug's plasma elimination half-life—the time it takes for half of the drug to leave the bloodstream—as approximately 4 to 8 hours. The amount of time it takes to completely clear the body depends on individual factors and the duration of use.

Q: Does Phenylbutazone cause drowsiness or affect alertness?

A: Official regulatory information does not commonly list drowsiness as a standalone side effect. However, official guidance on drug interactions notes that the compound belongs to a class where combining it with alcohol can enhance central nervous system (CNS) effects. This interaction may be associated with increased drowsiness or sedation.

Q: Is Phenylbutazone available over the counter anywhere?

A: Phenylbutazone is classified as a prescription-only drug in approved markets. In the United States, for its approved veterinary use, it is restricted by federal law to be administered only by or on the order of a licensed veterinarian.

Q: Can Phenylbutazone affect fertility or pregnancy?

A: Safety classifications and official guidance generally advise that the compound is avoided during pregnancy and in nursing mothers due to potential risks. Furthermore, regulatory safety data contains warnings that Phenylbutazone may damage fertility or the unborn child and should be managed with extreme caution.

Q: What is the regulatory status of Phenylbutazone in the U.S.?

A: Official regulatory summaries confirm that Phenylbutazone is no longer approved or marketed for human use in the United States due to safety concerns. Its current regulatory approval in the U.S. is restricted to veterinary use in horses.

Q: Is Phenylbutazone an opioid or habit-forming drug?

A: No, Phenylbutazone is officially classified as a Nonsteroidal Anti-inflammatory Drug (NSAID). The drug is not considered a habit-forming substance and is not categorized as an opioid medicine.

Q: Is there a generic version of Phenylbutazone?

A: Yes, the compound is available in generic forms, although its primary approved use is in veterinary medicine for horses. For its human use, which is highly restricted, generic availability would depend on specific national regulations.

Q: Can Phenylbutazone be used by people with asthma?

A: Official guidance contraindicates the use of Phenylbutazone in individuals who have experienced acute asthmatic attacks or other severe allergic reactions. This contraindication applies if these reactions were previously triggered by aspirin (ASA) or other nonsteroidal anti-inflammatory agents (NSAIDs).

Q: Is Phenylbutazone effective for gout flare-ups?

A: In jurisdictions where Phenylbutazone is approved for human use, it is specifically indicated for the symptomatic treatment of acute attacks of gout. However, due to its toxicity, it is typically reserved only for severe cases.

Q: What does official guidance say about stopping Phenylbutazone use?

A: Official guidance states that if a satisfactory response is not observed within a few days, the treatment regimen must be reassessed. Official guidance also notes that the drug should be discontinued immediately if signs of gastrointestinal upset or potential blood disorders are observed.

Q: What does the research say about Phenylbutazone's original uses?

A: Medical history indicates that Phenylbutazone was originally introduced for human use in the early 1950s. It was initially widely used for the treatment of rheumatoid arthritis and gout, and other inflammatory musculoskeletal conditions.

Q: What are the restrictions on Phenylbutazone use in athletes?

A: Official product information notes that some competition and athletic authorities regard Phenylbutazone as a prohibited substance under their rules, particularly in the context of equine competitions. Any use must be strictly monitored and aligned with the relevant athletic regulations.

Q: Can Phenylbutazone cause allergic reactions?

A: Yes, the official safety profile indicates that the drug is contraindicated in patients with a known or suspected hypersensitivity to Phenylbutazone. Rare but severe allergic reactions have been reported in association with its use.

Q: Are Phenylbutazone tablets usually taken with food?

A: While specific instructions depend on the product form, the oral form of Phenylbutazone, like many other nonsteroidal anti-inflammatory agents, is often advised to be administered with food. This practice is generally recommended to help reduce the risk of gastrointestinal upset.

Q: What are the major reasons Phenylbutazone was withdrawn or restricted?

A: The major reasons regulatory bodies restricted or withdrew the drug for widespread human use relate to its serious and unique adverse effects. These include the risk of severe blood dyscrasias (disorders), such as agranulocytosis and aplastic anemia.

Q: Does Phenylbutazone interact with alcohol?

A: Official guidance for this drug class suggests that combining Phenylbutazone with alcohol can enhance central nervous system (CNS) effects. This interaction may be associated with increased drowsiness or sedation.

Q: Is Phenylbutazone the same type of medicine as ibuprofen?

A: Phenylbutazone is in the same pharmacological class as ibuprofen, as both are classified as Nonsteroidal Anti-inflammatory Drugs (NSAIDs). However, they are different specific chemical compounds, each with its own distinct mechanism details and safety profile.

Q: How quickly does Phenylbutazone start working?

A: According to official guidance, the response to therapy is generally prompt, often occurring within 24 hours of administration. A high initial dose is sometimes used by prescribers to quickly establish the therapeutic effect.

Q: Is Phenylbutazone used for long-term conditions?

A: The drug's use is typically limited in duration for approved human conditions. Official guidance emphasizes that if long-term use is necessary, the patient's response and lab work should be monitored at regular intervals, as the risk of serious adverse effects is associated with the duration of exposure.

Q: Can people with heart conditions use Phenylbutazone?

A: Official warnings advise against the use of Phenylbutazone in patients suffering from cardiac disease. Furthermore, its use is specifically contraindicated (not allowed) in patients diagnosed with severe cardiac dysfunction.

Q: What should I watch out for when taking Phenylbutazone?

A: Official safety warnings indicate that the drug should be discontinued immediately if symptoms that may indicate a serious reaction are observed. These symptoms include fever, sore throat, lesions in the mouth, spontaneous bruising, jaundice, or black or tarry stools.

Q: Can Phenylbutazone affect blood pressure?

A: Yes, official safety information indicates that Phenylbutazone can cause sodium retention and edema (fluid retention). Hypertension, or high blood pressure, has been reported as a possible side effect in association with exposure to the compound.

Q: Why is Phenylbutazone sometimes only available for veterinary use?

A: The severe and unique toxicity risks associated with Phenylbutazone use in humans, particularly the risk of blood disorders, have led regulatory bodies to severely restrict its use. It is now almost exclusively available for veterinary medicine use, where the risk/benefit assessment differs significantly from human use.

Q: What are the signs of a serious reaction to Phenylbutazone?

A: The official safety profile identifies signs of serious reactions that require immediate medical attention. These include symptoms related to blood disorders (such as fever, sore throat, or spontaneous bruising) and signs of gastrointestinal problems (such as black or tarry stools).

Q: Can Phenylbutazone be used for acute injuries?

A: In its approved veterinary use, the drug is indicated for the relief of inflammatory conditions associated with the musculoskeletal system. Human use has historically included treatment for various acute local inflammatory conditions, reflecting its potent anti-inflammatory action.

Q: How does Phenylbutazone differ from other anti-inflammatory drugs?

A: Phenylbutazone is distinct from many other nonsteroidal anti-inflammatory agents due to its unique potential for severe bone marrow toxicity. This specific risk, which includes the potential for dangerously low white blood cell counts, has resulted in its highly restricted regulatory status for human use.

How should Phenylbutazone be stored and disposed of?

Storage and Handling Requirements

The official storage guidelines require Phenylbutazone to be kept in its original, tightly closed container and protected from light. Oral forms are generally stored at controlled room temperature, but specific injectable preparations may require refrigeration. It is crucial to protect the product from excessive heat, sources of ignition, and moisture.

Disposal Guidelines

To dispose of unused or expired Phenylbutazone, follow national and local disposal requirements. The product must not be disposed of in household trash, down a sink, or into the environment. Disposal should be done through an approved waste disposal facility or a designated medicine take-back program. Always store the product securely away from children.

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

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