Febuxostat

BRAND NAMES:

Adenuric- It contains the active ingredients of Febuxostat. It is available in the form of tablets used to treat gout diseases.

Uloric- It contains the active ingredient of Febuxostat. It is available in the form of tablets used to treat gout by decreasing the lowering of uric acid. 

MECHANISM OF ACTION:

It entails inhibiting xanthine oxidase, a key enzyme in uric acid synthesis. Febuxostat inhibits xanthine oxidase, reducing the conversion of xanthine and hypoxanthine into uric acid. This reduces uric acid levels in the circulation, treating the underlying cause of hyperuricemia, a disorder marked by high uric acid levels.

PHARMACOKINETICS:

Absorption: Febuxostat is readily absorbed, reaching maximal plasma levels after 1 to 1.5 hours of oral dosing. Approximately 49% of the oral febuxostat dosage is absorbed.

Distribution: Febuxostat has a steady-state distribution volume of around 50%.

Metabolism: Febuxostat is metabolized by conjugation via UGT enzymes, including UGT1A1, UGT1A3, UGT1A9 and UGT2B7. Febuxostat is metabolized by CYPs1A2, CYP2C8, and non-CYP enzymes. Febuxostat also inhibits breast cancer resistance protein activity. 

Excretion: Febuxostat's apparent elimination half-life is approximately 5 to 8 hours. Metabolites of febuxostat are eliminated by both hepatic and renal routes. The percentage of febuxostat excreted unchanged in the urine is less than 5%.

PHARMACODYNAMICS:

Febuxostat lowered both mean serum uric acid and serum xanthine concentrations, as well as total urine uric acid excretion. Febuxostat, at daily doses of 40-80 mg, lowered 24-hour mean blood uric acid concentrations by 40 to 55%. Febuxostat is linked to gout flares due to the drug's effect on serum uric acid levels and the mobilization of urate crystals in tissue deposits. Because allopurinol and oxypurinol febuxostat are not structurally similar to purine or pyrimidines, they have no inhibitory effects on other enzymes involved in purine and pyrimidine synthesis and metabolism.

DOSAGE AND ADMINISTRATION:

Dosage of high levels of uric acid from gout

Adult dosage –Typically dose starts from 40 mg per day, it is necessary physician may increase the dose to 80mg after 2 weeks, if the uric acid level does not fall below 6 mg/dl. Maximum dose is 80 mg per day. The strength of the febuxostat oral tablets is 40 mg and 80mg.

Febuxostat is available as a tablet that can be taken orally. It is usually taken once per day, with or without food. Take febuxostat every day at roughly the same time. Follow the instructions on your medication label. It relieves gout but does not cure it. Even if you feel better, you should not stop taking febuxostat without consulting your doctor.

DRUG INTERACTIONS:

Febuxostat has the following medication interactions: 

• Azathioprine is used to treat immunological disorders such as rheumatoid arthritis. 

• Mercaptopurine is used to treat cancer and immunological disorders.

• Didanosine is sometimes used in the treatment of HIV.

CONTRAINDICATIONS:

Febuxostat contraindications include patients treated with azathioprine or mercaptopurine. Xanthine oxidase inhibition increases concentrations of azathioprine and mercaptopurine, resulting in serious toxicity that can cause myelosuppression. Febuxostst dormulation contain lactose as an excipient. Use with caution for lactose-intolerant patients.

SIDE EFFECTS:

Side effects of febuxostat include

• Chest pain or pressure

• Fast or abnormal heartbeat

• Trouble breathing

• Pain in your back, jaw, throat, or arm

• Sweating, upset stomach, vomiting, or dizziness

• Sudden and severe headache

• Slurring of speech

• Numbness or weakness on one side of your body

• Sudden blurry vision

Liver damage – 

• Nausea or vomiting

• Stomach or belly pain

• Fever

• Itching

• Loss of appetite

• Dark-colored urine

• Skin reactions

• Painful red or purple skin

• Flat red rash

• Red painful watery eyes

Severe Allergic Reactions

• Racing heart

• Swollen lymph nodes

• Nausea and vomiting

• Inflammation of the face, lips, mouth, tongue or throat

• Dizziness, feeling lightheaded or fainting

• Stomach cramps

• Joint pain

OVERDOSE:

Symptoms of overdose include

• Drowsiness

• Fainting

• Seizures

• Rapid heartbeat

TOXICITY:

There is no known human toxicity with febuxostat treatment. Febuxostat was evaluated in healthy patients in doses of up to 300mg daily for 7 days without evidence of dose-limiting toxicities. Patients who overdose should be given symptomatic and supportive care.

STORAGE:

The recommended room temperature range for the Febuxostat is 68–77 degrees Fahrenheit (20–25 degrees Celsius). Under certain circumstances, like during transit, it may be subjected to temperatures ranging from 59 to 86 Fahrenheit (15 to 30 degrees Celsius). Store with the lid firmly closed in a cold, dry location. Keep out of the light.