what is the action of clopidogrel

Precautions

There is no proven risk in humans during pregnancy. Clopidogrel 75 mg (base) is not a controlled substance under the Controlled Substances Act (CSA). Note: Inactive ingredients may vary. Get help with Imprint Code FAQs.

Is clopidogrel a controlled substance?

For decades, aspirin and warfarin have been the predominant antiplatelet and anticoagulant alternatives. Beginning with the introduction of the antiplatelet agent clopidogrel in 2002, several more potent oral antiplatelet and oral anticoagulant agents have been approved for use.

Is clopidogrel an anticoagulant?

Clopidogrel only comes in the form of a tablet you take by mouth. Clopidogrel is used to prevent blood clots if you have chest pain, peripheral artery disease (poor circulation in your legs), a heart attack, or stroke. This drug may be used as part of a combination therapy. That means you may need to take it with other drugs.

What is clopidogrel prescribed for?

Usual Adult Dose for Peripheral Arterial Disease: 75 mg orally once a day. Uses: Prevention of atherothrombotic events in patients with a history of recent myocardial infarction, recent stroke, or established peripheral arterial disease. Detailed Clopidogrel dosage information.

What is clopidogrel 75 mg prescribed for?

What is clopidogrel mechanism of action?

Mechanism Of Action Clopidogrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets.

What is the major side effect of clopidogrel?

Easy bleeding/bruising, stomach upset/pain, diarrhea, and constipation may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly. Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects.

What class of drugs is clopidogrel?

Clopidogrel is in a class of medications called antiplatelet medications. It works by preventing platelets (a type of blood cell) from collecting and forming clots that may cause a heart attack or stroke.

What is clopidogrel used for and side effects?

Clopidogrel is a platelet inhibitor. It reduces the chance that a harmful blood clot will form by preventing platelets from clumping together in the blood. Clopidogrel may also increase the chance of serious bleeding in some people. This medicine is available only with your doctor's prescription.

How long should you stay on clopidogrel?

The standard recommendation is typically at least 12 months of Plavix.

When is the best time to take clopidogrel?

You can take clopidogrel at whatever time of day you find easiest to remember, but take your doses at the same time of day each day. Most people prefer to take it in the morning, as they find this helps them to remember to take it regularly. You can take the tablet either before or after a meal.

What happens when you stop taking clopidogrel?

Feb. 5, 2008 -- Heart attack survivors and other heart patients may be more likely to die or suffer a heart attack in the first three months after stopping the drug Plavix, new research shows. Plavix is an antiplatelet drug.

Which is better aspirin or clopidogrel?

In the original, large-scale Clopidogrel versus Aspirin in Patients at Risk of Ischaemic Events (CAPRIE) trial,13 clopidogrel alone was found to be superior to aspirin alone in reducing the risk of ischemic stroke, myocardial infarction, or death from vascular causes.

Does clopidogrel reduce blood pressure?

Arterial hypertension is associated with platelet activation, increased sCD40L levels and endothelial dysfunction suggesting that inhibition of platelet-derived sCD40L release may improve endothelial function and lower blood pressure (BP)....Effects of Clopidogrel on Blood Pressure.Last Update Posted:April 28, 2010Last Verified:April 20105 more rows

What medications should not be taken with clopidogrel?

Clopidogrel may interact with other medicationsDiabetes drug. In most cases, repaglinide should not be taken with clopidogrel. ... Stomach acid drugs (proton pump inhibitors) ... Nonsteroidal anti-inflammatory drugs (NSAIDs) ... Blood thinners.Drugs used to treat depression. ... Salicylates (aspirin) ... Opioids.

What foods should I avoid while taking clopidogrel?

Foods to avoid when taking heart medicationsAsparagus.Broccoli.Brussels sprouts.Cauliflower.Green onions.Kale.Parsley.Spinach.

Does clopidogrel affect the kidneys?

Conclusions. In summary, among patients hospitalized with ACS and treated with clopidogrel, lower levels of kidney function were associated with a greater risk of death, hospitalization for AMI, and major bleeding.

What foods should I avoid when taking clopidogrel?

Foods to avoid when taking heart medicationsAsparagus.Broccoli.Brussels sprouts.Cauliflower.Green onions.Kale.Parsley.Spinach.

What happens when you stop taking clopidogrel?

Feb. 5, 2008 -- Heart attack survivors and other heart patients may be more likely to die or suffer a heart attack in the first three months after stopping the drug Plavix, new research shows. Plavix is an antiplatelet drug.

How long do clopidogrel side effects last?

Plavix is estimated to be cleared from your body in about 33 hours. A single, oral dose of Plavix (clopidogrel) 75 mg has a half-life of approximately 6 hours. It takes 5.5 x half-life of a medicine for a drug to leave the body, therefore most of the Plavix should be eliminated from your system in 5.5 x 6 = 33 hours.

What should you not take with clopidogrel?

Interactions with other medicines There is an increased risk of bleeding when clopidogrel is taken with some other medications, including: aspirin. non-steroidal anti-inflammatory painkillers (NSAIDs) – like diclofenac, ibuprofen and naproxen. dipyridamole – another type of antiplatelet.

Before Taking This Medicine

You should not use clopidogrel if you are allergic to it, or if you have: 1. any active bleeding; or 2. a stomach ulcer or bleeding in the brain (s...

How Should I Take Clopidogrel?

Follow all directions on your prescription label and read all medication guides or instruction sheets. Use these medicines exactly as directed.Clop...

What Happens If I Miss A Dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What Happens If I Overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. Overdose can cause excessive bleeding.

What Should I Avoid While Taking Clopidogrel?

Avoid alcohol. It can increase your risk of stomach bleeding.Avoid activities that may increase your risk of bleeding or injury. Use extra care to...

Clopidogrel Dosing Information

Usual Adult Dose for Acute Coronary Syndrome:Unstable Angina (UA)/Non-ST-Elevation Myocardial Infarction (NSTEMI):-Loading dose: 300 mg orally once...

What Other Drugs Will Affect Clopidogrel?

Certain other medicines may increase your risk of bleeding, including aspirin. Avoid taking aspirin unless your doctor tells you to.Tell your docto...

Which drug class is clopidogrel?

The search for active antiplatelet drugs within the original chemical class of the thienopyridines, led to the discovery of clopidogrel, a novel ADP-selective agent whose antiaggregating properties are several times higher than those of ticlopidine. The antiaggregating properties of this compound ar …

Is clopidogrel an ADP?

The antiaggregating properties of this compound are well known and, very recently, new results have clarified its mechanism of action. Clopidogrel is active only after intravenous or oral administration, and no circulating activity has been found in the plasma of treated animals or human volunteers. Experiments in rats have demonstrated that the antiaggregating activity was caused by a shortlasting metabolite generated in the liver by a cytochrome P450-dependent pathway. The antiaggregating property of clopidogrel is caused by an inhibition of the binding of ADP to its platelet receptors, and more specifically to the low affinity receptors, the high affinity binding sites being unaffected by clopidogrel. Several events in the ADP activation process, including adenylyl cyclase down-regulation, protein tyrosine phosphorylation, activation of the GPIIb-IIIa complex, fibrinogen binding, aggregation and release, were inhibited by clopidogrel and indicate their close relationship with the activation of a low affinity receptor by ADP. In contrast, binding of ADP to its high affinity binding sites (clopidogrel-resistant receptors) induced shape change, cytosolic calcium increase and phosphorylations of several other proteins, some events which were clopidogrel-sensitive. Thus, clopidogrel not only constitutes a potent antithrombotic drug in humans but also a good tool to study the effect of ADP on platelets.

How long does clopidogrel stay in your system?

However, platelet function can begin to return as new platelets turn over, and a return of full function is often seen within 5 days. Given this factor, clopidogrel should be held at least 5 days before any surgical procedure. It should be noted this decision should not occur in isolation, especially in high-risk patients (e.g., patients with recent stenting for ACS). Thus, in these situations, it is imperative to consult with the primary prescriber for the clopidogrel. [8]

Can you overdose on Clopidogrel?

Overdose following clopidogrel administration may result in bleeding complications. Based on animal studies, a single dose of 1500 to 2000 mg/kg was lethal to mice and rats, and 3000 mg/kg was lethal to baboons.

Does clopidogrel inhibit platelet activity?

Clopidogrel is an inactive prodrug that requires enzymatic activation via a variety of CYP enzymes, including the CYP2C19 and CYP3A4 enzymes, through a two-step process of bioactivation. Genetic polymorphisms to these enzymes can influence response to therapy. The most commonly discussed genetic polymorphism related to clopidogrel is that of one or both alleles of the CYP2C19 enzyme. Patients with any loss of function allele will not effectively metabolize clopidogrel, leading to the inability to inhibit platelet activity . For example, patients who are homozygous for these non-functioning alleles often demonstrate the poorest metabolism and subsequent activation of clopidogrel, as indicated by high on-treatment platelet reactivity via platelet function testing. [7]

Is clopidogrel FDA approved?

Clopidogrel is FDA approved for the medical management of unstable angina (UA)/non-ST-segment elevation myocardial infarction (NSTEMI), ST- segment elevation myocardial infarction (STEMI) in patients receiving fibrinolytic therapy, and for secondary prevention in recent myocardial infarction (MI), recent stroke, and peripheral arterial disease. There also a number of other FDA-approved uses. This activity reviews the mechanism of action, adverse event profile, toxicity, dosing, pharmacodynamics, and monitoring of clopidogrel, pertinent for members of the interprofessional team where this agent is indicated.

Is clopidogrel contraindicated?

Clopidogrel is contraindicated in patients who have had anaphylaxis to clopidogrel or its components or have active bleeding. [11]

Does Clopidogrel cause rash?

Other options to manage these patients or scenarios include desensitization and switching to an alternative agent with a different structure (e.g., ticagrelor). Rarely, clopidogrel has correlations with thrombotic thrombocytopenia (TTP). A patient who develops TTP while on clopidogrel should receive urgent plasmapheresis.

Is Clopidogrel safe for pregnancy?

It is not known if clopidogrel is secreted into breast milk. At the moment, the expert recommendation is to stop nursing or stop the drug in these situations.

What is a clopidogrel used for?

Clopidogrelis used to prevent heart attacksand strokes in persons with heart disease(recent heart attack), recent stroke, or bloodcirculation disease (peripheral vascular disease). It is also used with aspirinto treat new/worsening chest pain(new heartattack, unstable angina) and to keep blood vessels open and prevent blood clotsafter certain procedures (such as cardiac stent).Clopidogrel works by blocking platelets from sticking together and prevents them from forming harmful clots. It is an antiplatelet drug. It helps keep blood flowing smoothly in your body.

Can Clopidogrel cause allergic reactions?

Precautions. Before taking clopidogrel, tell your doctor or pharmacist if you are allergic to it; or to similar antiplatelet drugs (thienopyridines such as prasugrel); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems.

Does clopidogrel slow down the removal of other drugs?

Clopidogrel can slow down the removal of other drugs from your body, which may affect how they work. Examples of affected drugs include dasabuvir, repaglinide, among others.

What is clopidogrel used for?

Clopidogrel should be administered in conjunction with aspirin.

How is clopidogrel metabolized?

Clopidogrel is extensively metabolized by two main metabolic pathways: one mediated by esterases and leading to hydrolysis into an inactive carboxylic acid derivative (85% of circulating metabolites) and one mediated by multiple cytochrome P450 enzymes.

How long does clopidogrel inhibit platelet aggregation?

After repeated doses of 75 mg Clopidogrel per day for 10 days in patients with severe hepatic impairment, inhibition of ADP-induced platelet aggregation was similar to that observed in healthy subjects.

What enzymes are involved in clopidogrel?

Clopidogrel must be metabolized by CYP450 enzymes to produce the active metabolite that inhibits platelet aggregation. The active metabolite of Clopidogrel selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet P2Y 12 receptor and the subsequent ADP-mediated activation of the glycoprotein GPIIb/IIIa complex, thereby inhibiting platelet aggregation. This action is irreversible. Consequently, platelets exposed to Clopidogrel's active metabolite are affected for the remainder of their lifespan (about 7 to 10 days). Platelet aggregation induced by agonists other than ADP is also inhibited by blocking the amplification of platelet activation by released ADP.

How long does clopidogrel stay in your system?

After a single, oral dose of 75 mg, Clopidogrel has a half-life of approximately 6 hours.

How old are people who take clopidogrel?

Of the total number of subjects in the CAPRIE and CURE controlled clinical studies, approximately 50% of patients treated with Clopidogrel were 65 years of age and older, and 15% were 75 years and older. In COMMIT, approximately 58% of the patients treated with Clopidogrel were 60 years and older, 26% of whom were 70 years and older.

Is clopidogrel contraindicated for peptic ulcers?

Clopidogrel is contraindicated in patients with active pathological bleeding such as peptic ulcer or intracranial hemorrhage.

How does clopidogrel work?

Clopidogrel works by preventing platelets, which is a type of blood cell, from forming clots. A blood clot which forms inside a blood vessel can cut off blood supply to the heart or brain which would cause a heart attack or stroke. Common side effects associated with clopidogrel are headache, dizziness, nausea, vomiting, ...

What is clopidogrel?

Bob has never heard of this medication and asked the doctor for more information. The doctor stated that clopidogrel is an antiplatelet medication and sometimes called a ''blood thinner''. He said it is used to prevent strokes, heart attacks, and other heart problems. The more common name for clopidogrel is Plavix.

Does clopidogrel interact with other medications?

Make sure this medication does not interact with any other medication you may be taking. Clopidogrel is an antiplatelet and is commonly known as Plavix. It is used to prevent strokes, heart attacks, and other heart problems. Clopidogrel works by preventing platelets, which is a type of blood cell, from forming clots.

Does Clopidogrel cause nausea?

Common side effects associated with clopidogrel are headache, dizziness, nausea, vomiting, excessive tiredness and nosebleed. If these become severe or dont go away, one needs to notify their doctor.

Can clopidogrel cause bleeding?

Individuals on clopidogrel should stay away from the following medications which could increase their chances of bleeding: aspirin, heparin, non steroidal anti-inflammatory drugs such as ibuprofen or naproxen, warfarin, and antidepressants such as fluoxetine, paroxetine.

What is clopidogrel used for?

Clopidogrel is used to prevent blood clots if you have chest pain, peripheral artery disease (poor circulation in your legs), a heart attack, or stroke.

Can you stop taking Clopidogrel before a procedure?

Before having any procedures done, you should tell your doctors or dentists that you’re taking clopidogrel. You may need to stop taking this drug for a short time before a procedure to prevent bleeding. Your doctor will let you know when to stop taking this medication and when it’s OK to take it again.

Can clopidogrel cause bleeding?

This drug can cause serious and sometimes fatal bleeding. Clopidogrel may make you bruise and bleed more easily, have nosebleeds, and it will take longer than usual for bleeding to stop. You should tell your doctor about any serious bleeding, such as:

Can you take clopidogrel and opioids together?

Taking an opioid medication with clopidogrel can delay the absorption and reduce the amount of clopidogrel in your body, making it less effective . If you must take these drugs together, your doctor may prescribe an additional medication to help prevent blood clots in certain situations.

Can you take Repaglinide and Clopidogrel together?

In most cases, repaglinide should not be taken with clopidogrel. Taking these drugs together increases the amount of repaglinide in your body, which can result in low blood sugar levels. If you must take these drugs together, your doctor will carefully manage your dosage of repaglinide.

Can you take Clopidogrel if you are allergic to thienopyridine?

For people with an allergy to thienopyridines: If you’ve ever had an allergic reaction to any kind of thienopyridine, you shouldn’t take clopidogrel.

Can you take a genetic test before taking Clopidogrel?

Before starting treatment with clopidogrel, your doctor may do a genetic test to check your CYP2C19 genotype. This genetic test will help your doctor decide if you should take clopidogrel. Some genotypes slow how clopidogrel is broken down. If you have this kind of genotype, this drug may not work for you.

How long does clopidogrel stay in your system?

Oral: 75 mg once daily in combination with aspirin; duration of clopidogrel depends on degree of stenosis. Stenosis of 50% to 69%: Clopidogrel may be added to aspirin for 21 days; after 21 days, discontinue clopidogrel and continue aspirin indefinitely (Ehtisham 2019).

How long after ticagrelor can you take clopidogrel?

Transitioning from ticagrelor: Give a clopidogrel 600 mg loading dose 12 hours after the last dose of ticagrelor, followed by 75 mg once daily (Franchi 2018).

Which agents enhance the antiplatelet effect of other agents?

Agents with Antiplatelet Properties (e.g., P2Y12 inhibitors, NSAIDs, SSRIs, etc.): May enhance the antiplatelet effect of other Agents with Antiplatelet Properties. Monitor therapy

Does clopidogrel reduce platelet activity?

The effectiveness of clopidogrel results from its antiplatelet activity, which is dependent on its conversion to an active metabolite by the cytochrome P450 (CYP-450) system, principally CYP2C19. Clopidogrel at recommended doses forms less of the active metabolite and has a reduced effect on platelet activity in patients who are homozygous ...

Does clopidogrel block ADP?

Clopidogrel requires in vivo biotransformation to an active thiol metabolite. The active metabolite irreversibly blocks the P2Y 12 component of ADP receptors on the platelet surface, which prevents activation of the GPIIb/IIIa receptor complex, thereby reducing platelet aggregation.

Is clopidogrel good for a symptomatic artery?

Based on the American College of Chest Physicians guidelines for antithrombotic therapy in peripheral artery disease, clopidogrel is effective and recommended for patients with symptomatic carotid artery atherosclerosis. Carotid artery stentingc.

How does clopidogrel work?

How it works. Clopidogrel inhibits the way platelets clump together (aggregate) to form clots. Its activity is thought to be due to its active thiol metabolite, which inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor which indirectly inhibits platelet aggregation. This action is irreversible.

Why is clopidogrel given?

Clopidogrel may be given to reduce the risk of a heart attack or stroke in certain cardiovascular conditions or following a heart attack or ischemic stroke. People who are poor metabolizers at CYP2C19 may not respond very well to clopidogrel. Bleeding is the main side effect of clopidogrel.

How long does clopidogrel last?

Even though the active form of clopidogrel doesn't last for very long in the body, its effect on platelets lasts for the lifetime of the platelet. (7 to 10 days).

How long does it take for clopidogrel to stop bleeding?

Clopidogrel may need to be discontinued up to five days before surgery that carries a major risk of bleeding.

What is the best medicine for angina?

Clopidogrel may be used for the treatment of unstable angina and for certain types of heart attack (myocardial infarction) to reduce the risk of stroke or heart attack. Clopidogrel should be administered in conjunction with aspirin.

What medications interact with Clopidogrel?

Speak to your doctor about how drug interactions should be managed. Common medications that may interact with clopidogrel include: amiodarone. a pixaban. bupropion. calcium channel blockers. corticosteroids, such as prednisone and methylprednisone. dabigatran.

What is TPP in clopidogrel?

May cause a condition called Thrombotic Thrombocytopenic Purpura (TPP) - a blood disorder where blood clots form in the small blood vessels of the body. This can occur anytime during clopidogrel therapy, even after a short exposure (less than 2 weeks).

What is clopidogrel used for?

Clopidogrel is a prodrug of a platelet inhibitor used to reduce the risk of myocardial infarction and stroke. 3, 9 It has a long duration of action as it is taken once daily and a large therapeutic window as it is given in doses of 75-300mg daily. 9. Mechanism of action.

What is the active form of clopidogrel?

3 The active form is a platelet inhibitor that irreversibly binds to P2Y 12 ADP receptors on platelets. 9 This binding prevents ADP binding to P2Y 12 receptors, activation of the glycoprotein GPIIb/IIIa complex, and platelet aggregation. 9. Target.

How long does clopidogrel last?

That half life of clopidogrel is approximately 6 hours following a 75mg oral dose while the half life of the active metabolite is approximately 30 minutes. 9

How much of Clopidogrel is oxidized?

85-90% of an oral dose undergoes first pass metabolism by carboxylesterase 1 in the liver to an inactive carboxylic acid metabolite. 4 about 2% of clopidogrel is oxidized to 2-oxoclopidogrel. 4 This conversion is 35.8% by CYP1A2, 19.4% by CYP2B6, and 44.9% by CYP2C19 4 though other studies suggest CYP3A4, CYP3A5, and CYP2C9 also contribute. 3 2-oxoclopidogrel is further metabolized to the active metabolite. 3, 4 This conversion is 32.9% by CYP2B6, 6.79% by CYP2C9, 20.6% by CYP2C19, and 39.8% by CYP3A4. 3, 4

What is Revital Lifshitz-Liron?

Revital Lifshitz-Liron, "Novel crystal forms III, IV, V, and novel amorphous form of clopidogrel hydrogensulfate, processes for their preparation, processes for the preparation of form I, compositions contain ing the new forms and methods of administering the new forms." U.S. Patent US20030114479, issued June 19, 2003.

What is the apparent volume of distribution of clopidogrel?

The apparent volume of distribution of clopidogrel is 39,240±33,520L. 5

Can clopidogrel be used in combination with Xylometazoline?

Xylometazoline. The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Xylometazoline. Zafirlukast. The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Zafirlukast resulting in a loss in efficacy.

Indications and Usage For Clopidogrel

Clopidogrel Dosage and Administration

Dosage Forms and Strengths

Contraindications

Warnings and Precautions

Adverse Reactions

• The dosage and length of treatment are based on your medical condition and response to treatment. If you are taking this medication to prevent clots after a stent implant or other procedure, take this medication with aspirin for many months to years after the procedure (depending on the procedure/type of stent) as directed by your doctor. Consult y...

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Drug Interactions

Use in Specific Populations

Overdosage

• Acute Coronary Syndrome
  1. Clopidogrel tablet is indicated to reduce the rate of myocardial infarction (MI) and stroke in patients with non-ST-segment elevation ACS (unstable angina [UA]/non-ST-elevation myocardial infarction [NSTEMI]), including patients who are to be managed medically and those who are to …
• Recent MI, Recent Stroke, or Established Peripheral Arterial Disease
  In patients with established peripheral arterial disease or with a history of recent myocardial infarction (MI) or recent stroke Clopidogrel tablet is indicated to reduce the rate of MI and stroke.

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Clopidogrel Description