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Phenylbutazone

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Product Overview

Phenylbutazone is a non-steroidal anti-inflammatory drug (NSAID) of the pyrazolone class, primarily used as an analgesic and antipyretic in veterinary medicine. Its use in human medicine has been restricted due to potential adverse effects.

Basic Physicochemical Properties

PropertySpecificationTest Method
Chemical Name4-Butyl-1.2-diphenylpyrazolidine-3.5-dioneIUPAC nomenclature
Molecular FormulaC₁₉H₂₀N₂O₂Elemental analysis
Molecular Weight308.37 g/molMass spectrometry
AppearanceWhite or yellowish crystalline powderVisual inspection
Melting Point104-107°CUSP <741>
SolubilityPractically insoluble in water (0.04 mg/mL), soluble in ethanolUSP <911>

Pharmacological Profile

ParameterValue/DescriptionReference Standard
MechanismNon-selective COX inhibitorFDA veterinary guidelines
Bioavailability98% (oral)Animal studies
Protein Binding98%In vitro studies
Half-lifeSpecies dependent: 3-6 hours (dogs), 24-48 hours (horses)Veterinary PK data
MetabolismHepatic (CYP450)EMA assessment

Veterinary Applications & Dosage

SpeciesIndicationDosage RegimenTreatment Duration
HorsesMusculoskeletal inflammation2.2-4.4 mg/kg IV or PO q12hMax 5 days
DogsPain management15-20 mg/kg PO q24hMax 7 days
CattleAnti-inflammatory4-8 mg/kg IV single doseOne-time only

Safety & Regulatory Status

ParameterSpecification
Human use statusBanned in most countries (risk of aplastic anemia)
Veterinary restrictionsNot for food-producing animals in many jurisdictions
Withdrawal period18 months (horses intended for human consumption)
Major adverse effectsGI ulcers, renal toxicity, blood dyscrasias
Pregnancy categoryContraindicated in late pregnancy

Storage & Handling

ParameterRequirement
Storage conditions15-30°C in tightly closed container
Shelf life36 months from manufacture
Light sensitivityProtect from light
Packaging1kg foil-lined bags or 25kg fiber drums
DisposalIncineration or hazardous waste facility

Important Notes

Strictly for veterinary use under professional supervision

Never administer to animals intended for human consumption

Monitor for signs of toxicity (melena, pale mucous membranes)

Alternative NSAIDs preferred for chronic conditions

Always use lowest effective dose for shortest duration

Phenylbutazone is a drug that acts on the central nervous system and belongs to pyrazolone derivatives. It has weak antipyretic and analgesic effects and strong anti-inflammatory effects. It has good effects on inflammatory pain and can promote the excretion of uric acid.

Phenylbutazone is a non-steroidal anti-inflammatory drug (NSAID) that has been used in both human and veterinary medicine. Below is an overview of Phenylbutazone:

1. Definition and Classification

– Phenylbutazone belongs to the class of drugs known as pyrazolones, which are NSAIDs.

– It was initially developed for human use but is now more commonly employed in veterinary settings due to its potential side effects in humans.

2. Mechanism of Action

– Phenylbutazone inhibits cyclooxygenase (COX) enzymes, reducing the production of prostaglandins that cause inflammation, pain, and fever.

– This mechanism makes it effective for treating inflammatory conditions and alleviating associated discomfort.

3. Uses

– Veterinary Medicine: Widely used in horses and other large animals to manage conditions like arthritis, laminitis, and soft tissue inflammations.

– Human Medicine (Historical): Previously prescribed for rheumatoid arthritis and gout; however, its use has declined due to safety concerns.

4. Dosage and Administration

– The dosage varies depending on the species, weight, and condition being treated.

– In horses, it is typically administered orally or intravenously under veterinary supervision.

5. Side Effects and Risks

– Gastrointestinal Issues: Can cause ulcers, bleeding, and perforation due to its effect on stomach lining.

– Hematological Concerns: Associated with bone marrow suppression, leading to conditions such as aplastic anemia and leukopenia.

– Renal and Hepatic Toxicity: Prolonged use may damage kidneys and liver.

– Due to these risks, careful monitoring is essential when administering Phenylbutazone.

6. Contraindication

– Should not be used in patients with hypersensitivity to Phenylbutazone or other NSAIDs.

– Contraindicated in cases of gastrointestinal ulcers, bleeding disorders, severe liver or kidney disease, and during pregnancy or lactation unless deemed necessary by a veterinarian.

7. Interactions

– Phenylbutazone can interact with other medications, including anticoagulants, increasing the risk of bleeding.

– Concurrent use with other NSAIDs should be avoided to prevent additive toxic effects.

8. Regulatory Status

– In many countries, Phenylbutazone is strictly regulated for use in food-producing animals due to residue concerns.

– For racehorses, its use is controlled to ensure fair competition and animal welfare.

In summary, Phenylbutazone remains a valuable tool in veterinary practice despite its limitations. Its potent anti-inflammatory properties must be balanced against its significant risks through proper administration and monitoring.

,Disclaimer: The above content is for reference and communication only among industry insiders, and does not guarantee its accuracy or completeness. According to relevant laws and regulations and the regulations of this website, units or individuals who purchase related items should obtain valid qualifications and qualification conditions.

Declaration: The products displayed on this website are intended exclusively for industrial applications or scientific research. They are not intended for medical, pharmaceutical, or food use. In accordance with applicable laws and regulations, purchasing organizations must hold valid qualifications and approvals.

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