oxyphenbutazone

Action and Spectrum

Actions and spectrum: 

Action:  

oxyphenbutazone’s action is primarily related to its ability to inhibit cyclooxygenase (COX), which is involved in the production of prostaglandins. The Prostaglandins are substances that play a role in inflammation, pain, and fever. By inhibiting COX, oxyphenbutazone reduces the synthesis of prostaglandins, leading to decreased inflammation, pain relief, and reduced fever. 

Spectrum:  

• Arthritis: It was used to manage symptoms of inflammatory arthritis, like rheumatoid arthritis and osteoarthritis. 
• Gout: oxyphenbutazone was sometimes prescribed to manage pain and inflammation associated with gout attacks. 
• Other Painful Conditions: It was occasionally used for other painful conditions, such as musculoskeletal pain and certain types of chronic pain. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Nausea 

Vomiting 

GI bleeding 

Stomatitis 

GI disturbances 

Ulcer 

Rash 

hypersensitivity reactions 

Photosensitivity 

Nephrotoxicity 

hepatitis 

Black Box Warning

Black Box Warning: 

oxyphenbutazone carries a black box warning due to its serious and life-threatening adverse effects, including gastrointestinal bleeding, ulcers, bone marrow suppression, and agranulocytosis. Its use is associated with significant risks, and safer alternatives are recommended for pain and inflammation management. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: Individuals with a known hypersensitivity or allergic reaction to oxyphenbutazone should avoid its use. 
• Gastrointestinal Ulcers: oxyphenbutazone can exacerbate or worsen existing gastrointestinal ulcers, making it unsuitable for individuals with active ulcers. 
• Bone Marrow Suppression: Individuals with a history of bone marrow suppression, which can lead to reduced blood cell production, should not use oxyphenbutazone due to the risk of exacerbating this condition. 
• Agranulocytosis: oxyphenbutazone is contraindicated in individuals with a history of agranulocytosis, a severe reduction in white blood cell count. 
• Coagulation Disorders: Individuals with bleeding disorders or coagulation abnormalities are advised against using oxyphenbutazone due to the increased risk of bleeding. 
• Severe Hepatic Impairment: oxyphenbutazone can affect liver function, and its use is contraindicated in individuals with severe hepatic impairment. 
• Pregnancy and Lactation: oxyphenbutazone is contraindicated during pregnancy and breastfeeding due to potential harm to the fetus and nursing infant.

Caution: 

• Gastrointestinal Effects: oxyphenbutazone can cause gastrointestinal irritation, ulcers, and bleeding. Individuals with a history of gastrointestinal issues, such as ulcers or bleeding, should use oxyphenbutazone cautiously and be monitored for any signs of gastrointestinal complications. 
• Renal Effects: oxyphenbutazone can impair kidney function and lead to kidney damage. Individuals with pre-existing kidney problems, such as renal insufficiency, should use oxyphenbutazone with caution and regular monitoring of kidney function. 
• Cardiovascular Risk: NSAIDs, including oxyphenbutazone, may increase the risk of heart attack & stroke, especially with long-term use or in individuals with pre-existing cardiovascular conditions. 
• Hypertension: oxyphenbutazone can lead to elevated blood pressure. Individuals with hypertension or cardiovascular disease should use the medication cautiously and have blood pressure monitored regularly. 
• Bleeding Risk: oxyphenbutazone can interfere with blood clotting, increasing the risk of bleeding. Individuals on anticoagulant therapy or with bleeding disorders should exercise caution and be monitored for signs of bleeding.

Comorbidities: 

• Gastrointestinal Disorders: Individuals with a history of gastrointestinal ulcers, bleeding, or inflammatory bowel disease are at increased risk of exacerbation of these conditions due to oxyphenbutazone’s potential to cause gastrointestinal irritation and ulcers. 
• Renal Impairment: oxyphenbutazone can cause kidney damage and worsen renal function. Individuals with pre-existing renal impairment are at greater risk of experiencing kidney-related adverse effects. 
• Hypertension: oxyphenbutazone can elevate blood pressure, which may be problematic for individuals with hypertension. 
• Asthma: People with aspirin-sensitive asthma are more likely to experience exacerbation of their asthma symptoms when using oxyphenbutazone. 
• Bleeding Disorders: oxyphenbutazone’s effects on blood clotting can be concerning for individuals with bleeding disorders or those taking anticoagulant medications. 
• Liver Disease: Individuals with liver impairment may experience worsened liver function while using oxyphenbutazone. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into breast milk: unknown   

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• <b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

oxyphenbutazone is a non-steroidal anti-inflammatory drug (NSAID) that exerts its pharmacological effects by inhibiting the enzyme cyclooxygenase (COX), particularly COX-1 and COX-2. This inhibition reduces the production of prostaglandins, which are inflammatory mediators involved in pain, fever, and inflammation.

By decreasing prostaglandin synthesis, oxyphenbutazone provides pain relief, reduces fever, and mitigates inflammation. However, its use is associated with significant risks, including gastrointestinal ulcers, bleeding, and adverse effects on the cardiovascular and renal systems. Due to these risks, oxyphenbutazone’s use has been discontinued, and safer alternatives are preferred for managing pain and inflammation.  

Pharmacodynamics: 

• COX Inhibition: oxyphenbutazone is a non-selective inhibitor of both COX-1 and COX-2 enzymes, which are responsible for converting arachidonic acid into prostaglandins. COX-1 is constitutively present and involved in maintaining normal physiological functions, while COX-2 is induced during inflammation and contributes to pain and inflammation. 
• Prostaglandin Reduction: By inhibiting COX enzymes, oxyphenbutazone reduces the prostaglandins production, which are chemical messengers that mediate pain, fever, and inflammation. 
• Pain Relief: oxyphenbutazone’s ability to lower prostaglandin levels contributes to pain relief, making it effective in conditions where pain is caused by inflammation, such as arthritis and other inflammatory disorders. 
• Anti-Inflammatory Effects: By dampening the production of inflammatory prostaglandins, oxyphenbutazone helps mitigate the inflammatory response. This can lead to reduced swelling, redness, and other symptoms associated with inflammation. 
• Fever Reduction: The suppression of prostaglandins involved in fever regulation can lead to lower body temperature, making oxyphenbutazone useful in managing fever.

Pharmacokinetics: 

Absorption 

oxyphenbutazone is well-absorbed from the gastrointestinal tract after oral administration. However, its absorption can be variable, and food intake may affect its absorption rate. Peak plasma concentrations are usually reached within a few hours after ingestion. 

Distribution 

oxyphenbutazone has a large volume of distribution, which suggests that it can penetrate various body tissues. It crosses the blood-brain barrier and may also accumulate in synovial fluid. 

Metabolism 

oxyphenbutazone undergoes extensive metabolism in the liver. It is metabolized by various enzymes, including the cytochrome P450 system, into multiple metabolites. Some of these metabolites are pharmacologically active, contributing to the drug’s effects. 

Elimination and excretion 

oxyphenbutazone and its metabolites are primarily excreted through the urine. The elimination half-life of oxyphenbutazone can vary among individuals due to its metabolism and other factors. The half-life can range from several hours to more than a day. 

Adminstartion

Administration: 

• Dosage: The dosage of oxyphenbutazone varies based on the individual’s condition, age, and other factors. It is crucial to follow the healthcare provider’s instructions and the prescribed dosage. 
• Route of Administration: oxyphenbutazone is typically administered orally in the form of tablets or capsules. It should be taken with a full glass of water and can be taken with or without food. However, taking it with food might help reduce potential gastrointestinal irritation. 
• Frequency: The dosing frequency can vary but is usually taken multiple times per day. Follow the prescribed dosing schedule carefully. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: oxyphenbutazone 

Pronounced: (ok-see-fen-BYOO-tuh-zohn)  

Why do we use oxyphenbutazone? 

• Arthritis: oxyphenbutazone was prescribed to manage symptoms of rheumatoid arthritis and osteoarthritis. Its anti-inflammatory properties were aimed at reducing pain and swelling in joints. 
• Musculoskeletal Pain: The drug was occasionally used to alleviate musculoskeletal pain, such as that caused by injuries, strains, or other orthopedic conditions. 
• Gout: oxyphenbutazone was sometimes employed to help manage the pain & inflammation associated with gout attacks, which results from deposition of uric acid crystals. 
• Fever: Like other NSAIDs, oxyphenbutazone was used to reduce fever, particularly in cases where fever was related to inflammation.