An elderly friend who suffers from coronary heart disease told Huazi that he has been taking aspirin to prevent myocardial infarction, but his gastrointestinal function is not very good and he feels more uncomfortable after taking aspirin. Can he switch to clopidogrel? Hua Zi said that aspirin and clopidogrel are both commonly used drugs for antiplatelet aggregation, and both can prevent myocardial infarction and cerebral infarction. During use, aspirin causes greater damage to the digestive tract mucosa, and people who cannot tolerate the adverse reactions of aspirin can consider using clopidogrel as a substitute. But there are some issues that need attention when using clopidogrel. 1. Clopidogrel requires biotransformation to be effective Clopidogrel is an inactive drug itself, but after being absorbed by the human body, it will be metabolized by the liver enzyme CYP2C19 and release active thiol metabolites. In other words, clopidogrel is a prodrug that needs to be biotransformed by the human body to exert its antiplatelet activity. In the process of clopidogrel biotransformation, the activity of CYP2C19 enzyme plays a decisive role. However, there are genetic differences in enzyme activity. In China, about 13% of people have CYP2C19 enzyme in a "slow metabolism" state, which may affect the efficacy of clopidogrel. However, some studies have pointed out that although there are genetic differences, clopidogrel still has a good preventive effect on cardiovascular and cerebrovascular diseases and can replace the effect of aspirin. 2. It cannot be used in combination with the hypoglycemic drug repaglinide. People with diabetes who are taking repaglinide to control blood sugar are not recommended to take clopidogrel, because after absorption, only 15% of clopidogrel will be converted into active thiol metabolites, and the remaining 85% will be converted into inactive carboxylic acid metabolites, but carboxylic acid metabolites will inhibit the CYP2C8 enzyme. CYP2C8 enzyme is the main metabolic enzyme of repaglinide. Once it is inhibited, repaglinide will accumulate in the human body, stimulate insulin secretion, and increase the risk of hypoglycemia. Therefore, it is not recommended for those using repaglinide to use clopidogrel. Clopidogrel can be replaced with ticaglinide, or repaglinide can be adjusted to nateglinide or mitiglinide. 3. Choose the appropriate "prazole" drug. Clopidogrel has less adverse gastrointestinal reactions than aspirin, but it may also damage the digestive tract. People with digestive tract risks can use antacids to protect the digestive tract when using clopidogrel. It should be noted that when using proton pump inhibitors (various "prazole" drugs) to reduce gastric acid secretion, omeprazole and esomeprazole should be avoided. Because the two drugs need to be metabolized by the CYP2C19 enzyme, they compete with clopidogrel, resulting in a decrease in the production of active metabolites and reduced inhibition of platelets. If it is necessary to use it in combination with a proton pump inhibitor, drugs such as rabeprazole, lansoprazole, and pantoprazole can be selected, which will not affect the activation process of clopidogrel. 4. Clopidogrel is more suitable to be taken after meals. In the drug instructions, clopidogrel can be taken "with or without food", implying that the effect of the drug is not affected by food. However, in the "Chinese Journal of Pharmacy", a related research article pointed out that when clopidogrel is taken after meals, although the time to reach the peak concentration of the drug will be prolonged, the peak concentration is higher, the bioavailability is better, and the possibility of clopidogrel resistance is lower. Therefore, it is recommended that clopidogrel be taken within 15 minutes after a meal to increase the effectiveness of the drug. The conventional dose of clopidogrel is 75 mg once a day, and regular medication should be maintained. If a dose is missed, take a supplementary dose immediately if it is discovered within 12 hours; if a dose is missed after more than 12 hours, take the normal dose next time and do not double the dose. In summary, people with poor digestive function can use clopidogrel instead of aspirin to reduce damage to the digestive tract. However, when taking the medicine, you need to pay attention to the interaction with other drugs and the choice of specific medication time. The medicine should be used under the guidance of a doctor. If you have any questions about the use of the medicine, please consult a doctor or pharmacist. I am pharmacist Huazi, welcome to follow me and share more health knowledge. |
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