Stroke, coronary heart disease, peripheral arterial disease, etc. are all closely related to atherosclerosis. The primary and secondary prevention of these diseases are inseparable from antiplatelet drugs, and sometimes even two drugs may be required. Double-antibody therapy. The most clinically used antiplatelet drugs to prevent stroke, coronary heart disease, and peripheral arterial disease are aspirin and clopidogrel, but some patients will experience gastrointestinal damage, bleeding, uric acid and other adverse reactions when they are treated with these two drugs . For such patients, today we introduce a drug that can be used as an alternative to aspirin: indobufen.
Difference between indobufen and aspirin
Indobufen is not a new drug, it has been It was listed in Italy in 1984 and in my country in 2005.
Like aspirin, it also inhibits the production of thromboxane A2 by inhibiting the synthesis of cyclooxygenase, thereby inhibiting platelet aggregation. However, aspirin irreversibly inhibits the synthesis of cyclooxygenase, and the recovery of platelet function requires the formation of new platelets, and this cycle takes 5-7 days; while indobufen inhibits cyclooxygenase 1 with high selectivity and reversibility. Low inhibition of prostacyclin production, platelet function can be restored within 24 hours.
Therefore, aspirin has wider indications and is in the first-line position in the antiplatelet therapy for cardiovascular and cerebrovascular diseases such as stroke, coronary heart disease, etc., but the probability of concurrent adverse reactions is high; It has fewer gastrointestinal reactions, and has better tolerance and safety when used to inhibit platelet aggregation. It is more suitable for patients with elective surgery, and surgery can be performed 24 hours before surgery.
Indobufen and clopidogrel resistance
In addition to aspirin, clopidogrel It is also a commonly used antiplatelet drug. However, about 50% of aspirin-resistant patients have clopidogrel resistance at the same time, showing low response, slow onset of action, and the onset of effects on the 5th day with conventional doses. Moreover, clopidogrel is metabolized by the cytochrome CYP2C19 enzyme in the liver, and many drugs will affect its metabolism, such as omeprazole, which will affect the effect of clopidogrel.
Therefore, in the “Chinese Guidelines for Clinical Management of Cerebrovascular Diseases” (2019), it is recommended to use indobufen for prevention of ischemic stroke patients with gastrointestinal reactions or aspirin allergy and high bleeding risk.
Indobufen: both antiplatelet and anticoagulant effects
Indobufen has antiplatelet effects at low doses, At high doses, it can inhibit platelet factor and coagulation factors II, X, and play an anticoagulant role. Therefore, the instructions recommend it for ischemic cardiovascular disease, ischemic cerebrovascular disease, and venous thrombosis caused by arteriosclerosis; it can also be used to prevent thrombosis during hemodialysis. Take orally after meals, 100-200 mg each time, twice a day; for elderly patients over 65 years old and patients with renal insufficiency, the dose is halved, and 100-200 mg per day is appropriate.
Conclusion
Aspirin is currently the first choice for primary and secondary prevention of cardiovascular and cerebrovascular diseases. However, indobufen is also a good option for patients with aspirin intolerance or contraindications. It is believed that with the development of medicine, more drugs with better safety and better effect will be developed.
References:
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2.Chinese Medical Association, Chinese Medical Association Journal, Chinese Medical Association Branch of Chinese Medicine, Chinese Medical Association “Chinese Journal of General Practitioners” editorial committee, expert group for the preparation of guidelines for primary diagnosis and treatment of neurological diseases. Guidelines for primary diagnosis and treatment of ischemic stroke (2021) [J]. Chinese Journal of General Practitioners, 2021, 20(9):927-946.
3. Wen Jili, Cui Xiaoying. The application of indobufen in the prevention of coronary restenosis after PCI [J]. Journal of Hunan University of Traditional Chinese Medicine, 2012,32(010):29-30.
4. Yang Xia, Liu Wei, Chen Ken, et al. Efficacy and safety of indobufen tablets in the prevention and treatment of ischemic cardiovascular and cerebrovascular diseases Meta-analysis of sexuality[J].Chinese Journal of Clinical Pharmacology,2017(4).