azapropazone

Action and Spectrum

Actions and Spectrum: 

Actions: 

azapropazone exerts its effects primarily by inhibiting the synthesis of prostaglandins. Prostaglandins are substances in the body that play a role in the inflammatory process, pain perception, and fever. azapropazone helps reduce inflammation, relieve pain, and lower fever by inhibiting its production. 

Spectrum: 

azapropazone’s spectrum refers to the range of conditions for which the drug is used. It is primarily indicated for treating rheumatoid arthritis, osteoarthritis, and other inflammatory joint conditions. It may also be prescribed for certain musculoskeletal disorders and soft tissue injuries accompanied by inflammation and pain. 

Drug Interaction

Adverse Reaction

Frequency not defined 

nervousness 

depression 

headache 

dizziness 

vertigo 

tinnitus 

drowsiness 

insomnia 

photosensitivity 

fluid retention 

hypertension haematuria 

blood disorders 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity 
• Severe renal impairment 
• Severe hepatic impairment 
• History of GI bleeding 

Cautions: 

• Gastrointestinal issues 
• Cardiovascular disease 
• Asthma 
• Elderly children 
• Lactation 

Pregnancy / Lactation

Pregnancy consideration:  

It is contraindicated during pregnancy. 

Breastfeeding warnings:  

No data is available. 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data for the drug under this category is available. 

Pharmacology

Pharmacology: 

azapropazone exerts its pharmacological effects primarily by inhibiting the enzyme cyclooxygenase (COX). COX converts arachidonic acid into prostaglandins, lipid mediators involved in the inflammatory process, pain perception, and fever. 

Pharmacodynamics: 

COX enzymes convert arachidonic acid into prostaglandins, lipid mediators involved in various physiological processes, including inflammation, pain perception, and fever. 

By inhibiting COX, azapropazone reduces the production of prostaglandins. This leads to decreased inflammation, pain relief, and fever reduction, making it useful in conditions such as rheumatoid arthritis and osteoarthritis. 

Pharmacokinetics: 

Absorption 

azapropazone is administered orally in the form of tablets or capsules. After oral ingestion, the drug is absorbed from the gastrointestinal tract into the bloodstream. The rate and extent of absorption can be influenced by various factors, including the drug’s formulation, food intake, and individual patient characteristics. 

Distribution 

Once absorbed into the bloodstream, azapropazone is distributed throughout the body. It can cross cell membranes and enter tissues, including those affected by inflammation. The drug’s distribution may be influenced by factors such as blood flow to specific tissues, protein binding in the bloodstream, and the presence of any other drugs that may compete for binding sites. 

Metabolism 

azapropazone undergoes metabolism primarily in the liver. Hepatic enzymes metabolize the drug into various metabolites. The specific metabolic pathways and the identities of the primary metabolites are less extensively studied or well-known than some other NSAIDs. 

Elimination and Excretion 

The metabolites of azapropazone, along with a small portion of the unchanged drug, are excreted mainly through the urine. The kidneys play a significant role in eliminating azapropazone and its metabolites from the body. Renal function can affect the drug’s clearance, and caution is needed when prescribing azapropazone to individuals with impaired kidney function. 

Adminstartion

Administration: 

azapropazone is typically administered orally in the form of tablets or capsules. The dosing instructions and frequency may vary depending on the specific medical condition, like the patient’s age, weight, and other factors. It is essential to follow the healthcare provider’s instructions and the medication’s prescribing information for the correct dosage and administration. 

Patient Information Leaflet

Patient information leaflet 

Generic Name:  azapropazone 

Why do we use azapropazone? 

azapropazone is an NSAID. It treats pain, inflammation, gout, and rheumatoid arthritis.