Author: Jiang Juan Deng Ang Li Liren
Friends who have watched " I am not a God of Medicine " are probably very impressed by Indian medicine. In this magical country of India, in addition to Gleevec, the life-saving drug for chronic myeloid leukemia in the play, another anti-gout drug ZURIG®80, which is advertised as the " special effect" and is also very popular among gout friends and has always been popular in the purchasing agent market.
The Chinese common name of this medicine is febulista . In the past, many friends purchased this medicine from Japan, and now our country also has this medicine. Febulista tablets have good effect in reducing uric acid, and were once considered a blessing for gout patients.
However, in reality, there are many friends who frequently suffer from gout taking the purchasing agent version of anti-gout drugs. They find it very strange. says that this drug is effective in treating gout. Why does taking it worsen your gout?
Also, in recent years, due to cardiovascular risks, febulista has also attracted much attention from drug regulatory authorities. On February 21, 2019, the U.S. Food and Drug Administration (FDA) released a black box warning based on the latest research results: the anti-gout drug febuxstat increases the risk of cardiovascular death in patients.
This black box warning made many people fear the use of febustat.
Is febulista an angel or a demon? Today we will talk about the right and wrong of Feibulista. Before talking about medicines with
, let’s briefly learn about gout. Gout is medically a type of hyperuricemia (HUA). Hyperuricemia is a metabolic disease caused by excessive production or reduced uric acid excretion in the body.
Some patients with hyperuricemia have increased their blood uric acid levels and urate crystals are deposited in multiple tissues or organs such as joints, synovial membranes, tendons, kidneys and connective tissues, forming gout stones, causing acute and chronic inflammation and tissue damage, leading to multiple system damage such as arthritis, urinary tract stones and kidney diseases. This is the gout we are well known. About 5%-12% of hyperuricemia patients eventually develop gout.
Clinically, hyperuricemia is divided into three types:
► Poor uric acid excretion type
► Excessive uric acid production type
► Hyper-uric acid production type
► Mixed type
Commonly used drugs to lower uric acid include two types of drugs: inhibit uric acid production and promote uric acid excretion. Drugs that inhibit uric acid production such as allopurinol and febulista, and drugs that promote uric acid excretion such as benbromalon.
Which uric acid-lowering drug should be chosen for a patient? It usually needs to be comprehensively considered and evaluated and decided after comprehensive consideration and evaluation based on the patient's cause, comorbidities, liver and renal function and disease typing.
The individualized medication choices will also be different for different patients.
What medicine is febusterat?
Febuxstat (also known as febuxostat) is a novel xanthine oxidase inhibitor that reduces blood uric acid levels by reducing uric acid production.
In February 2009, febulista was approved by the US FDA for the treatment of adult gout. The product name is Uloric. In 2013, febuxstat was launched in China. Currently, there are three main types of febuxstat that are popular in the domestic purchasing agent market, namely the Japanese Imperial Edition (specials are 10mg, 20mg, and 40mg), the Indian Edition (ZURIG®80, specifications are 80mg), and the Taiwanese Edition (Fuyu Pain, specifications are 80mg).
There are also many regular pharmaceutical factories in China that produce febulista tablets, with specifications ranging from 40mg and 80mg. The biggest difference between them is the price.
Therefore, we think there is no need for everyone to buy this medicine overseas, and choosing domestic products is the most cost-effective.
2016 edition of the "China Gout Diagnosis and Treatment Guide" has recommended febulista to moderately.
who are febuxlist suitable for?
Febulista is suitable for long-term use in patients with a history of gout or in patients with persistent hyperuricemia. It is also recommended to use anti-inflammatory drugs in the acute phase of gout onset and lowering uric acid.
However, China's instructions and guidelines consensus does not recommend it for patients with hyperuricemia without clinical symptoms.
FDA only recommends it for patients whose treatment with allopurinol is ineffective or whose use of allopurinol has serious adverse reactions.How to take
? What should I pay attention to?
Febulista has a variety of specifications of 10mg, 20mg, 40mg and 80mg. Before taking , be careful to check which specifications you are taking.
recommended initial dose is 40mg once a day (the recommended starting dose is 20mg once a day for some foreign instructions). After taking the medicine for 2 to 5 weeks, the dosage will be gradually increased according to the blood uric acid value, and the amount will be increased by 20mg each time, and the maximum daily dose will be 80 mg. After the blood uric acid value reaches the standard, the minimum effective dose is maintained. Food and antacids have no effect on taking medication.
In the early stage of treatment, the rapid decrease in blood uric acid value may cause more urate deposits in the tissue to be mobilized, resulting in an increase in the frequency of gout attacks.
The patient mentioned at the beginning was an acute attack of gout caused by taking too much dose (80mg) and lowering uric acid too quickly.
To prevent gout attacks in the early stages of treatment, it is recommended to gradually increase the dosage from a small dose, and use colchicine and non-steroidal anti-inflammatory drugs (such as ibuprofen , etc.) under the guidance of a doctor.
Patients with acute gout attacks must first control gout symptoms before using febulistat. If gout occurs during febustat treatment, there is no need to discontinue febustat treatment. Gout should be treated according to the specific circumstances of the attack.
It is necessary to remind everyone that febulista can control gout but cannot cure gout. Treatment for lowering uric acid in gout patients is a long-term process. After the blood uric acid drops to meet the standards, you cannot stop the medication at will. You must reduce the dosage or stop the medication according to the doctor's instructions according to the uric acid level.
Discontinuation of uric acid-lowering drugs without authorization can easily cause blood uric acid to return to the pre-treatment level, which can not only cause gout attacks again, but also cause long-term failure of blood uric acid to meet the standards of kidneys and cardiovascular and cerebrovascular risks.
Drug treatment is an important measure for the treatment of gout, but lifestyle changes are also essential.
Changes in lifestyle include: reduce the intake of high-purine foods, drink more water for people with normal heart and kidney function (preferably more than 2,000 ml per day), quit smoking at the same time, and ban beer and liquor. If you have to drink, you can use the appropriate amount of red wine. You also need to control your weight.
The following table is the dietary advice for patients with hyperuricemia.
Who is not suitable for using febulista?
► Patients with a history of allergic to fobulista tablets.
► Patients who are using thiopurine or azathioprine because febulista may cause increased blood concentrations of azathioprine, thiopurine and theophylline and increased toxicity.
► Febulista has not been studied in patients with secondary hyperuricemia, so it is not recommended for patients with secondary hyperuricemia.
► It is not recommended for asymptomatic hyperuricemia patients. What are the important adverse reactions of
febustat?
will not have an inhibitory effect on enzymes other than xanthine oxidase, so it is relatively safe, but you should also pay attention to its adverse reactions. Common adverse reactions include:
► Liver function impairment: incidence rate is 2% to 3%, manifested as fatigue, loss of appetite, discomfort at the upper right abdomen, soy sauce urine, jaundice, diarrhea, etc.
Countermeasures: Before using febulista for the first time, patients should check liver function as baseline level. When the above symptoms of liver function damage occur during medication, liver function should be checked.
liver enzyme is slightly elevated (2 times lower than the upper limit of the normal reference value) and can be followed up and observed, and most of them can gradually return to normal. When liver enzymes increase by 2 times the upper limit of the normal reference value, it is recommended to provide liver protection treatment. When it exceeds 3 times the upper limit of the normal reference value, the dosage or stop the medication as appropriate. Generally, after quitting the drug or liver protection treatment, the symptoms of liver function damage can be relieved.
► Skin reaction: There have been clinical reports at home and abroad, manifested as skin allergic reactions, rashes, itching, blisters, peeling, etc.
Countermeasures: If you suspect a serious skin reaction, you should stop using febulista and seek medical treatment in a timely manner. If patients have reported similar skin reactions when using allopurinol, febulista should be used with caution.
► Cardiovascular disease-related death: Studies have shown that compared with allopurinol, febulista causes an increase in cardiovascular-related death. This is the black box warning mentioned above. The purpose of the black box warning is to remind doctors and patients to use the drug more reasonably, and it does not completely deny its efficacy. It is also the reason why the FDA restricts it from only being used for patients whose treatment is ineffective or whose allopurinol has serious adverse reactions.
Countermeasures: should be fully evaluated when deciding to use febulista, patients with a history or risk factors should be used with caution, and patients should be followed up and monitored to be vigilant against the occurrence of cardiovascular thrombosis events.
For patients with a history of heart disease or stroke, the risks and benefits need to be carefully weighed. If a patient has a history of heart disease or stroke, he/she should tell the medical staff.
If you experience chest pain, shortness of breath, rapid or irregular heartbeat, numbness or weakness on one side of the body, dizziness, difficulty speaking, sudden and severe headache, etc. during the period of taking febustat, you should seek medical attention immediately.
Can febulista be used in special groups?
FDA Pregnancy safety classification is C: There has been no adequate controlled study in pregnant women. Febulista can only be used during pregnancy if the potential benefit is confirmed to outweigh the risk to the fetus.
The safety grading of febulista during breastfeeding is L3. Studies on rats have found that febuxstat can be excreted through milk. But it is not yet known whether febustat can be excreted through human breasts.
Since many drugs can be secreted into milk, lactating women should use this product with caution. Lactating women should stop breastfeeding during the administration of this product.
has not yet been determined the safety and effectiveness of febulista in patients under 18 years of age, and is not recommended for children under 418 years of age.
Elderly patients do not need to adjust the dose.
Does febuxstat damage the liver and kidneys?
Febulista is mainly metabolized in the liver. The metabolized inactive substances are excreted through the kidneys, feces and bile through multiple pathways. It has high safety in patients with renal insufficiency and renal transplantation. Dosage adjustment is not required for patients with mild and moderate renal insufficiency (eGFR≥30ml/min).
For patients with severe renal insufficiency (eGFR30 ml/min), several studies have shown the effectiveness and safety of febulista. The recommended starting dose is 20 mg once a day.
Do not need to adjust the dose for patients with mild or moderate (Child-Pugh Grade A and B) liver insufficiency, and there is no sufficient study data for severe liver insufficiency (Child-Pugh Grade C). Such patients should use it with caution.
Acknowledgement: Thank you to the pharmacist team for writing this article by Jiang Juan, a clinical pharmacist in the endocrine department of the pharmacist team. Thank you to the endocrine department of the pharmacist Deng Ang and Li Liren, for independently reviewing the content of this article.
