febuxostat

Action and Spectrum

Actions and Spectrum: 

febuxostat is a medication used to lower uric acid levels in the blood. High levels of uric acid can lead to a condition called gout, which is characterized by painful inflammation in the joints

Drug Interaction

Adverse Reaction

1-10%: 

Rash (0.5-1.6%) 

Arthralgia (0.7-1.1%) 

Liver function abnormalities (4.6-6.6%) 

Nausea (1.1-1.3%) 

>1%: 

Thrombocytopenia 

Anemia 

Blurred vision 

Pain  

Thirst 

Fatigue 

Edema 

Herpes zoster 

Contusion 

Anorexia 

Hyperglycemia 

Dyspepsia 

Ulceration 

Vertigo 

Peptic ulcer 

Black Box Warning

Black Box Warning: 

It is essential to follow the dosage and administration instructions for febuxostat carefully

Contraindication / Caution

Contraindication/Caution: 

febuxostat should not be used in people hypersensitive to the drug itself. 

Pregnancy / Lactation

Pregnancy consideration:  

Limited data is available regarding the use of febuxostat in pregnant women. 

Breastfeeding warnings:  

No data is available regarding the presence of drugs in human breast milk. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.        
• 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 available 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: No data is available for the drug under this category. 

Pharmacology

Pharmacology 

febuxostat is a medication that belongs to a class of drugs called xanthine oxidase inhibitors. It works by inhibiting the activity of the enzyme xanthine oxidase, which is responsible for the production of uric acid in the body. By reducing the production of uric acid, febuxostat can lower uric acid levels in the blood, which can help reduce gout symptoms. 

Pharmacodynamics: 

The main therapeutic effect of febuxostat is the reduction of serum uric acid levels. This effect is dose-dependent, meaning that the higher the drug dose, the more significant the reduction in uric acid levels. 

Pharmacokinetics: 

When febuxostat is taken orally, it is rapidly and almost completely absorbed from the gastrointestinal tract, with peak concentrations of the drug in the blood typically occurring within 1 to 2 hours of taking the medication. The bioavailability of febuxostat is about 45%. 

Absorption 

After absorption, febuxostat is distributed throughout the body and is known to cross the blood-brain barrier. The drug is metabolized in the liver by the enzymes CYP2C9 and UGT1A1 and is then eliminated primarily by the kidneys. The drug’s half-life is about 17 hours, meaning it takes about 17 hours for half of the drug to be eliminated from the body. 

Distribution 

The volume of distribution of febuxostat is 50 L. The concentration of bound protein is 99.2%. 

Metabolism 

febuxostat is metabolized in the liver by UGT1A1, UGT1A3, UGT1A9, and UGT2B7 enzymes. CYP1A2, CYP2C8, and CYP2C9 enzymes oxidize them.  

Elimination and excretion 

The elimination half-life of febuxostat is 5-8 hours. It is eliminated in urine and feces. 

Adminstartion

Administration: 

febuxostat is administered through the oral route. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: febuxostat 

Pronounced: fe-BUX-oh-stat 

Why do we use febuxostat? 

febuxostat helps to treat chronic gout.