Patient Information on ULORIC (febuxostat)

 Manufacturing company: Takeda Pharmaceuticals America, Inc.

What is Uloric? It is a uric acid lowering agent used for the treatment of gout. It is not to be confused with Xyloric.

Alterations or switch from the normal metabolic formation and excretion of the uric acid leads to an accumulation of increased levels of urate in the joints which causes severe pain and if left untreated can result in tophy i.e. deformation of the bones and joints.

What is its dosage form? It is marketed in a form of tablets with different potencies. The 40mg tablet is round whereas an 80mg tablet is tear-shaped.

What should you know about Uloric?

  • Do not confuse it with Xyloric which sounds alike but has a different active agent.
  • You can take it before or after the meal. Swallow it whole. Do not break or chew the tablets.
  • You can use Uloric irrespective of the gender.
  • After two weeks of starting the treatment with Uloric, you will need to have your uric acid levels tested.
  • Not only the increased levels, but the decrease and fluctuation and movement of the urate can cause pain and inflammation termed as gouty flares. Your doctor will prescribe you NSAIDs (analgesics) for the prophylactic purposes against the gouty flares. Although Uloric can be taken on an empty stomach, do not take NSAIDs empty stomached.
  • Along with medication, you will also require dietary modification in gout such as reduced use of meat, dairy products, fizzy drinks etc. Consult a dietician in this respect.

Can Uloric be used in different patient populations?

In pregnancy: it is placed under the category C because no adequate and well-structured tests have been conducted in this regard. It should be used with great care in such women, only when truly needed.

In nursing mothers: test on rats have revealed the presence of Uloric in the milk but it is not yet known if the case is same in humans. However, it should be used by breast-feeding mothers with caution and on the advice of the doctor.

In children: it is not for use in children under 18 years.

In geriatrics: it is safe to be used by elderly.

In liver injuries: Uloric can be easily used in mildly damaged liver but not in severe hepatic impairments.

In kidney failure: Uloric does not require any specific considerations in moderately affected kidney function, but should not be taken if your kidneys are majorly compromised.

In asymptomatic hyperuricemia:  Uloric is not used if you have high levels of uric acid in your body but have no apparent symptoms yet.

In secondary hyperuricemia: if the raised uric levels are result to an organ transplant, Uloric can be used only if guided by professional medical personnel.

What are its contra-signs or precautions?

  • Uloric can cause varying cardiovascular symptoms, talk to your doctor if you experience any chest pains, breathlessness, fatigue, palpitations.
  • Uloric can also lead to liver failure. If you develop any signs of weight loss, loss of appetite, extreme tiredness, yellowing of the skin, upper abdominal pain, dark colored urine, consult your doctor and have your liver functioning tests. Your doctor may ask you to stop Uloric until and unless any other cause of the liver abnormality is discovered.
  • Uloric is highly forbidden if you are undergoing chemo treatment with mercaptopurine or azathioprine.
  • Uloric on initial treatment stages can produce bouts of inflammation and pain in the joint which is managed by the use of NSAIDs as prescribed.

What are its various drug-interactions?

Mercaptopurine and azathioprine: Uloric is never to be used concomitantly with these high alert medications as it increases their levels by affecting their metabolism in the body.

Theophylline: it changes the metabolic processes of theophylline because theophylline is metabolized via xanthine oxidase and Uloric inhibits the enzyme.

Others: Uloric has no effect with warfarin, desipramine, indomethacin, hydrochlorothiazide, colchicine, and naproxen.

 What are its side effects?

Uloric gives following adverse effects; Abnormal levels of liver enzymes, nausea, rashes on the skin, painful muscles, muscle protein breakdown, anaphylaxis, aggression, inflammation of nephrons, eruptions on the skin.

What are the components present in the tablets? It has febuxostat, microcrystalline cellulose, silicon dioxide, hydroxypropyl cellulose, sodium croscarmellose, lactose monohydrate, and magnesium stearate.

What are its storage requirements? Place the tablets at a room temperature in a place where it is protected from the direct light.

What is the toxicology report of Uloric? When the rats and mice were given 25 times the human dose of Uloric, it caused bladder cancer in female rats and epithelial tumor in male rats. It had no effect on their reproductive functions but came out positive for chromosomal mutation tests.

What should you inform your doctor about?

Before starting Uloric tell your doctor if you have any;

Kidney, liver, heart disease, cancer or taking anti-cancer medications, a history of stroke.

What is its mode of action?

It is an inhibitor of enzyme xanthine oxidase. This enzyme is involved in uric acid synthesis by transforming hypoxanthine to xanthine and then finally to uric acid. On inhibition of this enzyme by Uloric, more uric acid is not formed.

What is its absorption, distribution, metabolism and excretion profile?

Absorption: it reaches its full plasma concentrations after 1-2 hours.

Distribution: almost whole drug gets bind with the proteins in the plasma which helps in its transportation. It has a distribution volume of 50L.

Metabolism: it is metabolized by both CYP450 enzymes and non-cytochrome enzymes.

Excretion: it is removed from both urine and feces.

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