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- Clopidogrel vs. Effient: What's the difference?
- What is clopidogrel? What is Effient?
- What are the side effects of clopidogrel and Effient?
- What is the dosage of clopidogrel vs. Effient?
- What drugs interact with clopidogrel and Effient?
- Are clopidogrel and Effient safe to use while pregnant or breastfeeding?
Clopidogrel vs. Effient: What's the difference?
- Clopidogrel and Effient (prasugrel) are antiplatelet drugs used for preventing strokes, heart attacks, and death in individuals who have had a previous stroke, unstable angina, heart attack, or have peripheral arterial disease (PAD).
- A brand name for clopidogrel is Plavix.
- Side effects of clopidogrel and Effient that are similar include diarrhea, rash, headache, chest pain, dizziness, and increased bleeding.
- Side effects of clopidogrel that are different from Effient include itching, abdominal pain, muscle aches, allergic reactions, pancreatitis, and liver failure.
- Side effects of Effient that are different from clopidogrel include back pain, tired feeling, fatigue, nausea, cough, high or low blood pressure (hypertension or hypotension), shortness of breath, slow heart rate, fever, and swelling or pain in the extremities.
What is clopidogrel? What is Effient?
Clopidogrel is an anti-platelet drug used to prevent heart attacks, strokes, and death in patients who have had a previous stroke, unstable angina (chest pain), heart attack, or have peripheral arterial disease (PAD). Clopidogrel prevents blood clots by binding to the P2Y12 receptor on platelets, preventing adenosine diphosphate (ADP) from activating platelets. It belongs to a class of drugs called P2Y12 inhibitors, which also includes prasugrel (Effient) and ticagrelor (Brilinta). Clopidogrel is similar to ticlopidine (Ticlid) in chemical structure and in the way it works.
Effient (prasugrel) is an antiplatelet drug that prevents the platelets in the bloodstream from aggregating and forming blood clots, used to prevent blood clots in people with acute coronary syndrome who are undergoing a procedure after a recent heart attack or stroke, and in people with certain disorders of the heart or blood vessels.
What are the side effects of clopidogrel and Effient?
The tolerability of clopidogrel is similar to that of aspirin. The more common side effects of clopidogrel are:
- Abdominal pain
- chest pain,
- muscle aches,
- severe bleeding,
- allergic reactions,
- pancreatitis, and
- liver failure.
Ticlopidine (Ticlid) is an antiplatelet medication quite similar to clopidogrel. It has been associated with a severe reduction in white blood cell count in between 0.8% and 1% of persons. The risk of this dangerous side effect with clopidogrel is about 0.04%, much less than with ticlopidine but twice that of aspirin.
Clopidogrel rarely causes a condition called thrombotic thrombocytopenic purpura (TTP) in one out of every 250,000 people. TTP is a serious condition in which blood clots form throughout the body. Blood platelets, which participate in clotting, are consumed, and the result can be bleeding because enough platelets are no longer left to allow blood to clot normally. For comparison, the related drug, ticlodipine (Ticlid), causes TTP 17-50 times more frequently than clopidogrel.
General Risk of Bleeding
Thienopyridines, including Effient, increase the risk of bleeding. With the dosing regimens used in TRITON-TIMI 38, TIMI (Thrombolysis in Myocardial Infarction) Major (clinically overt bleeding associated with a fall in hemoglobin ≥ 5 g/dL, or intracranial hemorrhage) and TIMI Minor (overt bleeding associated with a fall in hemoglobin of ≥ 3 g/dL but < 5 g/dL) bleeding events were more common on Effient than on clopidogrel.
- Age ≥ 75 years. Because of the risk of bleeding (including fatal bleeding) and uncertain effectiveness in patients ≥75 years of age, use of Effient is generally not recommended in these patients, except in high-risk situations (patients with diabetes or history of myocardial infarction) where its effect appears to be greater and its use may be considered.
- CABG or other surgical procedure.
- Body weight < 60 kg. Consider a lower (5 mg) maintenance dose.
- Propensity to bleed (e.g., recent trauma, recent surgery, recent or recurrent gastrointestinal (GI) bleeding, active peptic ulcer disease, or severe hepatic impairment).
- Medications that increase the risk of bleeding (e.g., oral anticoagulants, chronic use of non-steroidal anti-inflammatory drugs [NSAIDs], and fibrinolytic agents). Aspirin and heparin were commonly used in TRITON-TIMI 38.
Thienopyridines inhibit platelet aggregation for the lifetime of the platelet (7-10 days), so withholding a dose will not be useful in managing a bleeding event or the risk of bleeding associated with an invasive procedure.
Because the half-life of prasugrel’s active metabolite is short relative to the lifetime of the platelet, it may be possible to restore hemostasis by administering exogenous platelets; however, platelet transfusions within 6 hours of the loading dose or 4 hours of the maintenance dose may be less effective.
Coronary Artery Bypass Graft Surgery-Related Bleeding
The risk of bleeding is increased in patients receiving Effient who undergo CABG. If possible, Effient should be discontinued at least 7 days prior to CABG. Of the 437 patients who underwent CABG during TRITON-TIMI 38, the rates of CABG-related TIMI Major or Minor bleeding were 14.1% in the Effient group and 4.5% in the clopidogrel group.
The higher risk for bleeding events in patients treated with Effient persisted up to 7 days from the most recent dose of study drug. For patients receiving a thienopyridine within 3 days prior to CABG, the frequencies of TIMI Major or Minor bleeding were 26.7% (12 of 45 patients) in the Effient group, compared with 5.0% (3 of 60 patients) in the clopidogrel group.
For patients who received their last dose of thienopyridine within 4 to 7 days prior to CABG, the frequencies decreased to 11.3% (9 of 80 patients) in the prasugrel group and 3.4% (3 of 89 patients) in the clopidogrel group. Do not start Effient in patients likely to undergo urgent CABG.
CABG-related bleeding may be treated with transfusion of blood products, including packed red blood cells and platelets; however, platelet transfusions within 6 hours of the loading dose or 4 hours of the maintenance dose may be less effective.
Discontinuation of Effient
Discontinue thienopyridines, including Effient, for active bleeding, elective surgery, stroke, or TIA. The optimal duration of thienopyridine therapy is unknown. In patients who are managed with PCI and stent placement, premature discontinuation of any antiplatelet medication, including thienopyridines, conveys an increased risk of stent thrombosis, myocardial infarction, and death. Patients who require premature discontinuation of a thienopyridine will be at increased risk for cardiac events. Lapses in therapy should be avoided, and if thienopyridines must be temporarily discontinued because of an adverse event(s), they should be restarted as soon as possible.
Thrombotic Thrombocytopenic Purpura
Thrombotic thrombocytopenic purpura (TTP) has been reported with the use of Effient. TTP can occur after a brief exposure (< 2 weeks). TTP is a serious condition that can be fatal and requires urgent treatment, including plasmapheresis (plasma exchange). TTP is characterized by thrombocytopenia, microangiopathic hemolytic anemia (schistocytes [fragment red blood cells] seen on peripheral smear), neurological findings, renal dysfunction, and fever.
Hypersensitivity Including Angioedema
Hypersensitivity including angioedema has been reported in patients receiving Effient, including patients with a history of hypersensitivity reaction to other thienopyridines.
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What is the dosage of clopidogrel vs. Effient?
Clopidogrel bisulfate usually is taken once daily. It can be taken with or without food. Clopidogrel is activated by enzymes in the liver to its active form. Individuals who have reduced activity of liver enzymes that activate clopidogrel due to liver disease may not adequately respond to clopidogrel. Alternative treatments should be used for these patients. The recommended dose for treating unstable angina or heart attack is 300 mg initially followed by 75 mg daily in combination with 75-325 mg of aspirin. Peripheral arterial disease or recent stroke is treated with 75 mg daily.
Initiate Effient treatment as a single 60 mg oral loading dose and then continue at 10 mg orally once daily. Patients taking Effient should also take aspirin (75 mg to 325 mg) daily.
Effient may be administered with or without food.
What drugs interact with clopidogrel and Effient?
The combination of clopidogrel with nonsteroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen (Motrin, Advil, Nuprin), naproxen (Naprosyn, Aleve), diclofenac (Voltaren), etodolac (Lodine), nabumetone (Relafen), fenoprofen (Nalfon), flurbiprofen (Ansaid), indomethacin (Indocin), ketoprofen (Orudis; Oruvail), oxaprozin (Daypro), piroxicam (Feldene), sulindac (Clinoril), tolmetin (Tolectin), and mefenamic acid (Ponstel) may increase the risk of stomach and intestinal bleeding.
Clopidogrel is converted to its active form by enzymes in the liver. Drugs that reduce the activity of these enzymes, for example, omeprazole (Prilosec, Zegerid) or esomeprazole (Nexium) may reduce the activity of clopidogrel and should not be used with clopidogrel. Other drugs that also may react with clopidogrel in a similar fashion include fluoxetine (Prozac, Sarafem), cimetidine (Tagamet), fluconazole (Diflucan), ketoconazole (Nizoral, Extina, Xolegel, Kuric), voriconazole (Vfend), ethaverine (Ethatab, Ethavex), felbamate (Felbatol), and fluvoxamine (Luvox).
- Coadministration of Effient and warfarin increases the risk of bleeding
- Non-Steroidal Anti-Inflammatory Drugs
- Coadministration of Effient and NSAIDs (used chronically) may increase the risk of bleeding.
- Other Concomitant Medications
- Effient can be administered with drugs that are inducers or inhibitors of cytochrome P450 enzymes.
- Effient can be administered with aspirin (75 mg to 325 mg per day), heparin, GPIIb/IIIa inhibitors, statins, digoxin, and drugs that elevate gastric pH, including proton pump inhibitors and H2 blockers.
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Are clopidogrel and Effient safe to use while pregnant or breastfeeding?
There are no adequate studies of clopidogrel in pregnant women.
Studies in rats have shown that clopidogrel appears in breast milk; however, it is not known whether it also appears in human breast milk. Because of a potential for side effects in the nursing infant, the physician must weigh the potential benefits and possible risks before prescribing clopidogrel to nursing mothers.
There are no adequate and well-controlled studies of Effient use in pregnant women. Reproductive and developmental toxicology studies in rats and rabbits at doses of up to 30 times the recommended therapeutic exposures in humans (based on plasma exposures to the major circulating human metabolite) revealed no evidence of fetal harm; however, animal studies are not always predictive of a human response. Effient should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.
In embryo fetal developmental toxicology studies, pregnant rats and rabbits received prasugrel at maternally toxic oral doses equivalent to more than 40 times the human exposure. A slight decrease in pup body weight was observed; but, there were no structural malformations in either species. In prenatal and postnatal rat studies, maternal treatment with prasugrel had no effect on the behavioral or reproductive development of the offspring at doses greater than 150 times the human exposure.
It is not known whether Effient is excreted in human milk; however, metabolites of Effient were found in rat milk. Because many drugs are excreted in human milk, prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
Plavix (clopidogrel) and Effient (prasugrel) are antiplatelet drugs used for preventing strokes, heart attacks, and death in individuals who have had a previous stroke, unstable angina, heart attack, or have peripheral arterial disease (PAD).
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Blood Clots (in the Leg)
Blood clots can form in the heart, legs, arteries, veins, bladder, urinary tract, and uterus. Risk factors include high blood pressure and cholesterol, diabetes, smoking, and family history. Symptoms and treatment depend on the location of the clot.
A stroke is an interruption of the blood supply to part of the brain caused by either a blood clot (ischemic) or bleeding (hemorrhagic). Symptoms of a stroke may include weakness, numbness, double vision or vision loss, confusion, vertigo, difficulty speaking, or understanding speech. A physical exam, imaging tests, neurological exam, and blood tests may be used to diagnose a stroke. Treatment may include administration of clot-busting drugs, supportive care, and in some instances, neurosurgery. The risk of stroke can be reduced by controlling high blood pressure, high cholesterol, diabetes, and stopping smoking.
14 Warning Signs and Symptoms of a Stroke FAST
Stroke is a serious medical condition. If you think you or someone you know is having a stroke call 911 immediately. There are two main types of strokes, hemorrhagic and ischemic (the most common type). A hemorrhagic stroke occurs due to a blood vessel rupture in the brain. An ischemic stroke occurs when a blood clot becomes lodged in a blood vessel in the brain, which causes a loss of blood supply to the brain, possibly causing brain tissue death. FAST is an acronym that helps people identify stroke signs and symptoms so they can act fast and call 911. Face drooping, Arm weakness, and Speech difficulty are indicators that a person may be having a stroke and it is Time to seek emergency medical treatment. Additional signs and symptoms of stroke may include weakness, difficulty walking, blurred vision, dizziness, headache, confusion, difficulty speaking, and loss of sensation. Stroke is a major cause of death and disability in the U.S. Early identification and treatment of stroke helps reduce the risk of morbidity and mortality.
Stroke vs. Mini-Stroke (TIA) Differences
A stroke occurs when a blood clot or artery ruptures within the brain. The rupture or clot causes brain cell damage or death. A mini-stroke (TIA, transient ischemic attack) is caused by brain cells that become dysfunctional over a short period. Stroke and mini-stroke warning signs of stroke and mini-stroke are the same, and include, speech problems, weakness, numbness, and facial droop. Side effects of stroke may be permanent and you may never regain full function of the parts of the body affected. Mini-stroke side effects usually resolve within minutes to a couple of days. A transient ischemic attack (mini-stroke) is a precursor for stroke because 40% of individuals who have a mini-stroke will have a stroke within a year. Treatment of stroke depends upon the type and parts of the body affected.
Transient Ischemic Attack (TIA, Mini-Stroke)
When a portion of the brain loses blood supply, through a blood clot or embolus, a transient ischemic attack (TIA, mini-stroke) may occur. If the symptoms do not resolve, a stroke most likely has occurred. Learn the symptoms, risk factors, and treatment for a transient ischemic attack.
Deep Vein Thrombosis (DVT, Blood Clot in the Legs)
Deep vein thrombosis (DVT) is a blood clot in the deep veins, and can be caused by broken bones, trauma to a limb, immobility, medications, smoking, cancer, genetic predisposition, and cancer. Symptoms and signs of a deep vein thrombosis in a leg are swelling, tenderness, redness, warmth, and pain. Treatments for DVT include medications and surgery.
Pulmonary Embolism (Blood Clot in the Lung)
A pulmonary embolism (PE) occurs when a piece of a blood clot from deep vein thrombosis (DVT) breaks off and travels to an artery in the lung where it blocks the artery and damages the lung. The most common symptoms of a pulmonary embolism are shortness of breath, chest pain, and a rapid heart rate. Causes of pulmonary embolism include prolonged immobilization, certain medications, smoking, cancer, pregnancy, and surgery. Pulmonary embolism can cause death if not treated promptly.
Heat stroke (heatstroke or sun stroke) is a form of hyperthermia. Heat stroke is a true medical emergency that can be fatal if not promptly and properly treated. Symptoms of heat stroke include high body temperature, absence of sweating, hot red or flushed dry skin, rapid pulse, difficulty breathing, strange behavior, hallucinations, confusion, agitation, disorientation, seizure, and coma. A victim of heat stroke must receive immediate treatment to avoid permanent organ damage.
Heart Attack vs. Stroke Symptoms, Differences, and Similarities
Heart attack usually is caused by a clot that stops blood flow supplying oxygen to an area of heart muscle, which results in heart muscle death. Stroke or "brain attack" is caused by a loss of blood supply to the brain (usually a blood clot) or by hemorrhagic stroke (bleeding within the brain), which results in brain tissue death. Both heart attack and stroke usually come on suddenly, produce similar symptoms, can be disabling, and can be fatal. The classic symptoms and warning signs of heart attack are different. Classic heart attack warning signs are chest pain or discomfort, shortness of breath, pain that radiates to the shoulders, back, arms, belly, jaw, or teeth, sweating, fainting, and nausea and vomiting. Moreover, woman having a heart attack may have additional symptoms like abdominal pain or discomfort, dizziness, clammy skin, and moderate to severe fatigue. The classic symptoms and warning signs that a person is having a stroke are confusion or loss of consciousness, sudden severe headache, speech problems, problems seeing out of one or both eyes, and numbness or weakness of only one side of the body. Moreover, a woman having a stroke may have additional warning symptom and signs like shortness of breath, disorientation, agitation, behavioral changes, weakness, nausea, vomiting, seizures, and hiccups. Recognition of stroke symptoms is vital for emergency treatment. The acronym "FAST" stands for recognition of Facial drooping, Arm weakness, Speech difficulty, and a Time for action. If you experience the symptoms heart attack or stroke (FAST) or see them develop in another person, then contact 911 immediately.
Migraine and Stroke
Migraine headache is a type of headache in which the exact cause is not known; however, they may be inherited, and certain foods and environmental factors can trigger and may contribute them. A stroke (brain attack) happens when a blood vessel in the brain leaks, bursts, or becomes blocked, which can be caused by many other health problems. Both migraines and strokes can can cause severe head pain (migraine pain usually is only on one side of the head). Migraine aura symptoms may mimic or feel like a stroke or mini-stroke (transient ischemic attack, TIA) because they have similar symptoms and signs like severe headache, numbness in the legs, feet, arms, hands, or face, nausea, vomiting, and dizziness. Other migraine aura symptoms include vision problems like flashing lights or blind spots in one eye. The main difference between migraine headache and stroke symptoms and signs is that a migraine headaches usually come on gradually while a stroke symptoms come on suddenly and unexpectedly.
Stroke is the third leading killer in the United States. Some of the warning signs of stroke include sudden confusion, trouble seeing with one or both eyes, dizziness, loss of balance, and more. Stroke prevention and reatable risk factors for stroke include lowering high blood pressure, quit smoking, heart disease, diabetes control and prevention.
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