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*Only for medical professionals to read and refer to 10 points to fully grasp the difference between clopidogrel and ticagrelor! As we all know, blood vessels are like water pipes.
Only when they are unobstructed, can they guarantee the needs of all aspects.
If a blood vessel is blocked, just like a water pipe is blocked, life will "collapse"! Today we are going to talk about two "pipeline" drugs.
Clopidogrel and ticagrelor are P2Y12 receptor antagonists, which selectively inhibit the binding of adenosine diphosphate (ADP) to its platelet P2Y12 receptor and the secondary ADP-mediated glycoprotein GPⅡb/Ⅲa complex Activation to inhibit platelet aggregation.
Both are commonly used clinical antiplatelet drugs, which can be used to prevent thrombotic events in patients with chronic stable angina, acute coronary syndrome, and ischemic stroke.
So, what is the difference between the two? 1.
The onset time of ticagrelor is faster.
For patients with acute coronary syndrome, it can quickly act to inhibit platelet aggregation, while clopidogrel has a relatively slow onset.
2.
The half-life of frequent dose clopidogrel is 6 hours, while the half-life of ticagrelor is 7.
2 hours.
However, the active metabolite of clopidogrel binds irreversibly to the P2Y12 receptor, while ticagrelor binds reversibly to the P2Y12 receptor.
Therefore, clopidogrel is taken once a day, while ticagrelor needs to be taken twice a day.
3.
Antiplatelet effect Ticagrelor has a stronger antiplatelet effect.
Studies have shown that ticagrelor has a higher incidence of cardiovascular death and myocardial infarction than the clopidogrel group, but there is no difference in stroke.
Based on the benefits of ticagrelor treatment for patients with acute coronary syndrome (ACS), relevant domestic and foreign guidelines recommend that ticagrelor be used for antiplatelet therapy in patients with ACS.
In the two authoritative guidelines of the European Society of Cardiology [The Guidelines for the Management of Patients with Non-persistent ST-segment Elevation Acute Coronary Syndrome (NSTE-ACS) published by the European Society of Cardiology in 2011 and Acute ST-segment The STEMI guidelines] point out that clopidogrel can only be used in patients who cannot receive ticagrelor treatment.
4.
Bleeding risk The bleeding risk of long-term use of ticagrelor is slightly higher than that of clopidogrel, but the bleeding rate of short-term use of the two is similar.
A KAMIR-NIH study based on East Asian populations showed that ticagrelor has a significantly higher risk of TIMI bleeding in patients ≥75 years of age than clopidogrel.
Therefore, for ACS patients ≥75 years of age, it is recommended to choose clopidogrel as the preferred P2Y12 inhibitor on the basis of aspirin.
For antiplatelet therapy in patients with low platelet counts, ticagrelor should also be avoided.
5.
Other adverse reactions Among patients treated with ticagrelor, the most frequently reported adverse reactions were dyspnea, contusion and nose bleeding.
The incidence of these events was higher than that of patients in the clopidogrel group.
6.
Drug interaction Clopidogrel is a prodrug, which is partially metabolized by CYP2C19 to its active metabolite.
Taking drugs that inhibit the activity of this enzyme may reduce the level of clopidogrel converted into active metabolites.
Therefore, it is not recommended to use strong or moderate CYP2C19 inhibitors, such as omeprazole, esomeprazole, fluconazole, voriconazole, fluoxetine, fluvoxamine, ciprofloxacin, carbamazepine equality.
Ticagrelor is mainly metabolized by CYP3A4, and a small part is metabolized by CYP3A5.
Combined use of CYP3A inhibition can increase the peak concentration (Cmax) and area under the drug-time curve (AUC) of ticagrelor.
Therefore, ticagrelor and strong CYP3A inhibitors such as ketoconazole and itraconazole should be avoided , Voriconazole, clarithromycin and other combined use.
The combined use of CYP3A inducers can reduce the Cmax and AUC of ticagrelor, respectively.
Therefore, the use of strong CYP3A inducers such as dexamethasone, phenytoin sodium, phenobarbital and carbamazepine should be avoided. 7.
Regarding antiplatelet therapy for patients with renal insufficiency PLATO In a study of ACS patients with renal insufficiency, the proportion of serum creatinine in the ticagrelor group was significantly higher than that in the clopidogrel group; in the combined use of blood vessels Further analysis of patients with tensin II receptor antagonist (ARB) found that compared with clopidogrel treatment group, the proportion of serum creatinine increased by >50%, renal-related adverse events, and renal function-related adverse events in the ticagrelor group were all Significantly higher.
Therefore, for patients with renal insufficiency, clopidogrel + aspirin should be the first choice.
8.
The results of antiplatelet therapy studies on patients with gout/hyperuricemia show that long-term use of ticagrelor can increase the risk of gout.
Gout is a common side effect in ticagrelor treatment, which may be related to the effect of ticagrelor's active metabolites on the metabolism of uric acid.
Therefore, clopidogrel is the preferred antiplatelet therapy for patients with gout/hyperuricemia.
9.
Antiplatelet therapy before coronary artery bypass graft surgery (CABG) For patients who are planning to undergo CABG and are taking low-dose aspirin (75mg~100mg), there is no need to stop the drug before surgery; patients who are receiving P2Y12 inhibitor therapy should Consider discontinuing ticagrelor for at least 3 days before surgery and clopidogrel for at least 5 days.
10.
The hyporesponsiveness of clopidogrel.
The hyporesponsiveness of platelets to clopidogrel may lead to the occurrence of ischemic time.
In order to overcome the hyporesponsiveness of clopidogrel, increasing the dose of clopidogrel or changing to ticagrelor is Common choice.
In summary, ticagrelor has a faster onset and stronger platelet inhibitory effect.
In the treatment of ACS, its antithrombotic effect is better, which can further reduce the mortality rate, but its bleeding risk is higher, and it is difficult to breathe and contusion.
, Bradycardia, gout and other adverse reactions are also higher than clopidogrel. References: [1] Instructions for clopidogrel and ticagrelor [2] "Chinese Expert Consensus on Antiplatelet Therapy for Special Populations of Acute Coronary Syndrome".
Association of Cardiovascular Physicians of the Chinese Medical Doctor Association.
2018.
Source of this article: Yi Sin pharmacy V author: Chen Chuxiong Sun Yat-sen Memorial hospital Pharmacy editor: Mr.
Lu Li copyright Notice This article is reproduced welcome to forward circle of friends - End - Call for Papers Call for Papers to channel-mail: yxjsjbx@yxj.
org.
cn please specify: [ Contributions】Hospital + department + name Contributions are in the form of word documents, and the remuneration is favorable.
Edit WeChat: chenaFF0911
Only when they are unobstructed, can they guarantee the needs of all aspects.
If a blood vessel is blocked, just like a water pipe is blocked, life will "collapse"! Today we are going to talk about two "pipeline" drugs.
Clopidogrel and ticagrelor are P2Y12 receptor antagonists, which selectively inhibit the binding of adenosine diphosphate (ADP) to its platelet P2Y12 receptor and the secondary ADP-mediated glycoprotein GPⅡb/Ⅲa complex Activation to inhibit platelet aggregation.
Both are commonly used clinical antiplatelet drugs, which can be used to prevent thrombotic events in patients with chronic stable angina, acute coronary syndrome, and ischemic stroke.
So, what is the difference between the two? 1.
The onset time of ticagrelor is faster.
For patients with acute coronary syndrome, it can quickly act to inhibit platelet aggregation, while clopidogrel has a relatively slow onset.
2.
The half-life of frequent dose clopidogrel is 6 hours, while the half-life of ticagrelor is 7.
2 hours.
However, the active metabolite of clopidogrel binds irreversibly to the P2Y12 receptor, while ticagrelor binds reversibly to the P2Y12 receptor.
Therefore, clopidogrel is taken once a day, while ticagrelor needs to be taken twice a day.
3.
Antiplatelet effect Ticagrelor has a stronger antiplatelet effect.
Studies have shown that ticagrelor has a higher incidence of cardiovascular death and myocardial infarction than the clopidogrel group, but there is no difference in stroke.
Based on the benefits of ticagrelor treatment for patients with acute coronary syndrome (ACS), relevant domestic and foreign guidelines recommend that ticagrelor be used for antiplatelet therapy in patients with ACS.
In the two authoritative guidelines of the European Society of Cardiology [The Guidelines for the Management of Patients with Non-persistent ST-segment Elevation Acute Coronary Syndrome (NSTE-ACS) published by the European Society of Cardiology in 2011 and Acute ST-segment The STEMI guidelines] point out that clopidogrel can only be used in patients who cannot receive ticagrelor treatment.
4.
Bleeding risk The bleeding risk of long-term use of ticagrelor is slightly higher than that of clopidogrel, but the bleeding rate of short-term use of the two is similar.
A KAMIR-NIH study based on East Asian populations showed that ticagrelor has a significantly higher risk of TIMI bleeding in patients ≥75 years of age than clopidogrel.
Therefore, for ACS patients ≥75 years of age, it is recommended to choose clopidogrel as the preferred P2Y12 inhibitor on the basis of aspirin.
For antiplatelet therapy in patients with low platelet counts, ticagrelor should also be avoided.
5.
Other adverse reactions Among patients treated with ticagrelor, the most frequently reported adverse reactions were dyspnea, contusion and nose bleeding.
The incidence of these events was higher than that of patients in the clopidogrel group.
6.
Drug interaction Clopidogrel is a prodrug, which is partially metabolized by CYP2C19 to its active metabolite.
Taking drugs that inhibit the activity of this enzyme may reduce the level of clopidogrel converted into active metabolites.
Therefore, it is not recommended to use strong or moderate CYP2C19 inhibitors, such as omeprazole, esomeprazole, fluconazole, voriconazole, fluoxetine, fluvoxamine, ciprofloxacin, carbamazepine equality.
Ticagrelor is mainly metabolized by CYP3A4, and a small part is metabolized by CYP3A5.
Combined use of CYP3A inhibition can increase the peak concentration (Cmax) and area under the drug-time curve (AUC) of ticagrelor.
Therefore, ticagrelor and strong CYP3A inhibitors such as ketoconazole and itraconazole should be avoided , Voriconazole, clarithromycin and other combined use.
The combined use of CYP3A inducers can reduce the Cmax and AUC of ticagrelor, respectively.
Therefore, the use of strong CYP3A inducers such as dexamethasone, phenytoin sodium, phenobarbital and carbamazepine should be avoided. 7.
Regarding antiplatelet therapy for patients with renal insufficiency PLATO In a study of ACS patients with renal insufficiency, the proportion of serum creatinine in the ticagrelor group was significantly higher than that in the clopidogrel group; in the combined use of blood vessels Further analysis of patients with tensin II receptor antagonist (ARB) found that compared with clopidogrel treatment group, the proportion of serum creatinine increased by >50%, renal-related adverse events, and renal function-related adverse events in the ticagrelor group were all Significantly higher.
Therefore, for patients with renal insufficiency, clopidogrel + aspirin should be the first choice.
8.
The results of antiplatelet therapy studies on patients with gout/hyperuricemia show that long-term use of ticagrelor can increase the risk of gout.
Gout is a common side effect in ticagrelor treatment, which may be related to the effect of ticagrelor's active metabolites on the metabolism of uric acid.
Therefore, clopidogrel is the preferred antiplatelet therapy for patients with gout/hyperuricemia.
9.
Antiplatelet therapy before coronary artery bypass graft surgery (CABG) For patients who are planning to undergo CABG and are taking low-dose aspirin (75mg~100mg), there is no need to stop the drug before surgery; patients who are receiving P2Y12 inhibitor therapy should Consider discontinuing ticagrelor for at least 3 days before surgery and clopidogrel for at least 5 days.
10.
The hyporesponsiveness of clopidogrel.
The hyporesponsiveness of platelets to clopidogrel may lead to the occurrence of ischemic time.
In order to overcome the hyporesponsiveness of clopidogrel, increasing the dose of clopidogrel or changing to ticagrelor is Common choice.
In summary, ticagrelor has a faster onset and stronger platelet inhibitory effect.
In the treatment of ACS, its antithrombotic effect is better, which can further reduce the mortality rate, but its bleeding risk is higher, and it is difficult to breathe and contusion.
, Bradycardia, gout and other adverse reactions are also higher than clopidogrel. References: [1] Instructions for clopidogrel and ticagrelor [2] "Chinese Expert Consensus on Antiplatelet Therapy for Special Populations of Acute Coronary Syndrome".
Association of Cardiovascular Physicians of the Chinese Medical Doctor Association.
2018.
Source of this article: Yi Sin pharmacy V author: Chen Chuxiong Sun Yat-sen Memorial hospital Pharmacy editor: Mr.
Lu Li copyright Notice This article is reproduced welcome to forward circle of friends - End - Call for Papers Call for Papers to channel-mail: yxjsjbx@yxj.
org.
cn please specify: [ Contributions】Hospital + department + name Contributions are in the form of word documents, and the remuneration is favorable.
Edit WeChat: chenaFF0911
