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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.
| Property | Specification | Test Method |
|---|---|---|
| Chemical Name | 4-Butyl-1.2-diphenylpyrazolidine-3.5-dione | IUPAC nomenclature |
| Molecular Formula | C₁₉H₂₀N₂O₂ | Elemental analysis |
| Molecular Weight | 308.37 g/mol | Mass spectrometry |
| Appearance | White or yellowish crystalline powder | Visual inspection |
| Melting Point | 104-107°C | USP <741> |
| Solubility | Practically insoluble in water (0.04 mg/mL), soluble in ethanol | USP <911> |
| Parameter | Value/Description | Reference Standard |
|---|---|---|
| Mechanism | Non-selective COX inhibitor | FDA veterinary guidelines |
| Bioavailability | 98% (oral) | Animal studies |
| Protein Binding | 98% | In vitro studies |
| Half-life | Species dependent: 3-6 hours (dogs), 24-48 hours (horses) | Veterinary PK data |
| Metabolism | Hepatic (CYP450) | EMA assessment |
| Species | Indication | Dosage Regimen | Treatment Duration |
|---|---|---|---|
| Horses | Musculoskeletal inflammation | 2.2-4.4 mg/kg IV or PO q12h | Max 5 days |
| Dogs | Pain management | 15-20 mg/kg PO q24h | Max 7 days |
| Cattle | Anti-inflammatory | 4-8 mg/kg IV single dose | One-time only |
| Parameter | Specification |
|---|---|
| Human use status | Banned in most countries (risk of aplastic anemia) |
| Veterinary restrictions | Not for food-producing animals in many jurisdictions |
| Withdrawal period | 18 months (horses intended for human consumption) |
| Major adverse effects | GI ulcers, renal toxicity, blood dyscrasias |
| Pregnancy category | Contraindicated in late pregnancy |
| Parameter | Requirement |
|---|---|
| Storage conditions | 15-30°C in tightly closed container |
| Shelf life | 36 months from manufacture |
| Light sensitivity | Protect from light |
| Packaging | 1kg foil-lined bags or 25kg fiber drums |
| Disposal | Incineration or hazardous waste facility |
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:
– 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.
– 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.
– 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.
– The dosage varies depending on the species, weight, and condition being treated.
– In horses, it is typically administered orally or intravenously under veterinary supervision.
– 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.
– 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.
– 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.
– 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.
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