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Commonly used urate-lowering drugs, do you really know how to use them?
The prevalence of hyperuricemia in China is 13.
3%, and the prevalence of gout is 1.
1%, which has become another common metabolic disease
after diabetes.
Hyperuricemia can not only lead to gout, kidney stones, chronic kidney disease, but also cardiovascular and cerebrovascular diseases and diabetes
.
Allopurinol, febuxostat and benzbromarone are commonly used urate-lowering drugs in China, what are the differences between these three drugs?
Urate-lowering drug selection strategies
Febuxostat is only approved for the long-term treatment of hyperuricemia in patients with gout and is not recommended for asymptomatic hyperuricemia
.
In addition, considering the potential cardiovascular risks of febuxostat, the 2019 edition of the Chinese Guidelines for the Diagnosis and Treatment of Hyperuricemia and Gout does not recommend febuxostat for asymptomatic hyperuricemia patients
.
1.
Patients with asymptomatic hyperuricemia
First-line urate-lowering agents: allopurinol or benzbromarone
.
2.
Patients who have been diagnosed with gout
First-line urate-lowering drugs: allopurinol, febuxostat, or benzbromarone
.
In order to reduce the frequency of gout attacks, prevent the formation of tophi, prevent bone destruction, and reduce the risk of death, patients with gout need to control blood uric acid within the target range (<360 μmol/ml)</b11> for life,
Source: Center for Drug Evaluation
, one is the increase in uric acid synthesis in the body, and the other is the decrease
in uric acid excretion.
Source: Center for Drug Evaluation
1.
Allopurinol
Allopurinol is a hypoxanthine analogue; The active metabolite oxypurinol is a xanthine analogue
.
Allopurinol and oxypurinol can reduce uric acid synthesis
by inhibiting xanthine oxidase (reduction).
2.
Febuxostat
Febuxostat is a non-purine analogue
.
Febuxostat, which can inhibit both reduced xanthine oxidase and oxidative xanthine oxidase
.
Therefore, febuxostat inhibits uric acid synthesis more than allopurinol
.
3.
Benzbromarone
By inhibiting tubular uric acid transporter-1, benzbromarone inhibits uric acid reabsorption, promotes uric acid excretion, and reduces blood uric acid levels
.
.
03Allopurinol: additional benefits and medication risks
1.
Additional benefits
Studies at home and abroad have found that allopurinol can improve vascular endothelial function, improve exercise tolerance in angina patients, and reduce the morbidity and mortality
of heart failure.
A meta-analysis of 10 clinical studies showed that allopurinol reduced systolic blood pressure by an average of 3.
3 mmHg and diastolic blood pressure by 1.
3 mmHg
.
Allopurinol has also been found to lower serum creatinine and increase creatinine clearance in patients with chronic kidney disease
.
2.
Medication risks
Allopurinol can cause hypersensitivity syndromes
such as fatal exfoliative dermatitis.
Positive HLA-B*5801 gene is a risk factor
for allopurinol hypersensitivity.
The positive rate of HLA-B*5801 gene in Han Chinese is 6%~8%, while that of whites is only 2%.
.
04 Advantages and risks of febuxostat
1.
Advantages
Febuxostat has the strongest
urate-lowering effect.
Compared with allopurinol and benzbromarone, febuxostat is mainly cleared by the liver and hardly affects renal function, and patients with Clcr≥30ml/min do not need to adjust the dose
.
2.
Risks
Compared with allopurinol, febuxostat increases the risk of
death from cardiovascular events in patients with gout.
Allopurinol is the first-line treatment for patients with gout with severe cardiovascular disease (history of myocardial infarction or stroke, or unstable angina) [NICE gout guidelines (2022)].
Source: NICE Gout Guidelines (2022)
Allopurinol and febuxostat are xanthine oxidase inhibitors, and when combined with drugs metabolized by xanthine oxidase, such as theophylline, aminophylline, azathioprine, mercaptopurine, etc.
, significant interactions
can occur.
It should be noted that
allopurinol combined with amoxicillin, the incidence of rash can increase; In combination with captopril, there have been reports
of the development of fatal Stevens-Johnson syndrome.
Source: Drug Evaluation Center 06 Drug
Submission
Source: Drug evaluation center
1.
Drink more water benzbromarone is a uric acid excretion drug, in order to prevent the formation of uric acid crystals, the daily water
intake should not be less than 1.
5~2 liters
.
Although allopurinol and febuxostat do not increase uric acid concentrations in the urine, they do increase subxanthine and xanthine concentrations
in the urine.
To prevent the formation of xanthine stones, during the period of taking allopurinol and febuc, water intake should be increased
.
2.
Pay attention to the rash
allopurinol can cause fatal exfoliative dermatitis and other hypersensitivity syndromes
.
The rash may precede a severe allergic reaction, and the drug should be discontinued and seen if
the rash develops.
3.
Detection of liver function
allopurinol, febuxostat, benzbromarone are hepatotoxic, if there is malaise, loss of appetite, greasy, dark yellow urine, etc.
immediately seek medical attention
.
4.
Be alert to cardiovascular events Febuxostat can increase the risk of cardiovascular events
, if chest pain, shortness of breath, rapid or irregular heartbeat, dizziness, difficulty speaking, sudden severe headache occur during medication, Seek immediate medical attention
.
Where to see more rheumatology clinical knowledge? Come to the "Doctor Station" and take a look 👇
at the source of this articleDrug Review CenterGCPLIVE Responsible editorCassette
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This article is reprinted Welcome to forward the circle of friends
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Recent advances in imaging and treatment of Sjogren syndrome
..
.
.
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