Prasugrel

Prasugrel is a medication used to treat patients with acute coronary syndrome (ACS), which includes two types of heart attacks, ST-elevation myocardial infarction (STEMI) that is traceable in the ECG and non-ST elevation myocardial infarction (NSTEMI), and unstable angina, which is chest pain that occurs without exertion and is associated with heart attack and impaired blood flow to the heart.

Heart attacks occur when blood supply to the heart muscles is interrupted or blocked due to coronary arteries being clogged with fat and cholesterol deposits (plaques). If a plaque ruptures, a blood clot forms and blocks blood flow to the heart, resulting in acute coronary syndrome. Prasugrel prevents blood clot formation and reduces the risk of further cardiovascular events in patients with ACS.

Acute coronary syndrome is primarily treated with percutaneous coronary intervention (PCI), a minimally invasive procedure used to unclog the artery, place a stent, and restore blood flow to the heart muscles. Prasugrel is part of the initial therapy to prevent clot formation in the coronary arteries, including in the newly placed stent.

Prasugrel is an antiplatelet drug that inhibits the activation and aggregation of platelets. Platelets are blood cells that play a major role in the blood clotting process, which is necessary for preventing excessive bleeding.

During a heart attack, when a plaque ruptures, platelets become activated, release blood-clotting substances, and clump together to form clots. Prasugrel binds to the P2Y12 receptor, a protein molecule on platelets responsible for platelet aggregation, and irreversibly blocks its activity.

Prasugrel is also being investigated for use in sickle cell disease, an inherited blood disorder that causes red blood cells to become sickle-shaped and break down.

Warnings

Prasugrel can cause significant, sometimes fatal, bleeding.

• Do not start prasugrel in patients with active pathological bleeding such as peptic ulcer or intracranial hemorrhage, a history of transient ischemic attack (TIA) or stroke, or who are likely to undergo urgent coronary artery bypass graft surgery (CABG).
• Avoid use in patients with a body weight of less than 60 kg, propensity to bleed, or concurrent use of other drugs that can increase bleeding risk.
• Do not use in patients with hypersensitivity to prasugrel or any of its components.
• Prasugrel can cause thrombotic thrombocytopenic purpura (TTP), a blood disorder that causes clotting in small blood vessels all over the body. Discontinue prasugrel in case of active bleeding, elective surgery, TIA, or stroke.
• In patients with stent placement after acute coronary syndrome, premature discontinuation of prasugrel increases the risk of clot formation in the stent, heart attacks, and death.

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Side effects of prasugrel

Common side effects of prasugrel include high blood pressure, high cholesterol/lipids in the blood, headache, back pain, shortness of breath, nausea, diarrhea, dizziness, cough, low blood pressure, fatigue, noncardiac chest pain, rapid and irregular rhythm in the atria, slow heart rate, low white blood cell count, low red blood cell count, rash, fever, swelling of extremities, and pain in extremity.

Serious side effects of prasugrel include major or minor bleeding events such as nasal bleeding, gastrointestinal hemorrhage, coughing up blood, bleeding under the skin, bleeding in the abdominal cavity, bleeding in the membrane-bound space around the heart, and retinal hemorrhage.

Less common side effects of prasugrel include abnormal liver function tests, swelling under the skin and mucous membrane, and severe hypersensitivity reaction.

This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug. Consult your doctor or the FDA for more information.

Dosages of prasugrel

Tablet

Acute Coronary Syndrome

Adult:

Reduction of thrombotic cardiovascular events in patients with ACS managed by means of PCI who have either unstable angina or non-ST-elevation MI (NSTEMI) or ST-elevation MI (STEMI) when managed with primary or delayed PCI.

• 60 mg orally once as loading dose, then 10 mg/day orally in combination with aspirin 81-325 mg/day.
• If patient is below 60 kg, consider 5 mg/day orally.

Dosing Modifications

• No dosage adjustment necessary.
• End-stage renal disease: Limited experience; higher bleeding risk.
• Mild-to-moderate (Child-Pugh Class A or B): No dosage adjustment necessary.
• Severe (Child-Pugh Class C): Not studied.

Dosing in low-weight patients

• Patients under 60 kg have increased exposure to the active metabolite of prasugrel and an increased risk of bleeding with a 10 mg daily maintenance dose. Consider lowering the maintenance dose to 5 mg in patients under 60 kg.
• Same as adult dosing.

75 years and above

• Generally not recommended, except in high-risk patients, for whom effect appears to be greater and use may be considered.

Pediatric:

Overdose

• Prasugrel can cause life-threatening bleeding, and there is no known antidote.
• Platelet transfusion may restore blood clotting ability.

Drug interactions with prasugrel

Inform your doctor of all medications you are currently taking to avoid possible drug interactions.

• Severe interactions of prasugrel include abrocitinib, apixaban, cangrelor, caplacizumab, codeine, heparin, hydromorphone, morphine, oxycodone, oxymorphone, and protamine.
• Other interactions include devil’s claw, ginger, ginkgo biloba, horse chestnut seed, and verteporfin.

For more information on potential interactions, consult the RxList Drug Interaction Checker and discuss with your doctor or healthcare provider.

Always inform your doctor or healthcare provider of all prescription and over-the-counter medications you use, including the dosage for each.

Pregnancy and breastfeeding

• Prasugrel should be used during pregnancy only if the benefits to the mother outweigh potential risks to the fetus.
• It is not known if prasugrel is excreted in breast milk. Use with caution in nursing women after considering the benefits and potential adverse effects.

Other considerations

• Take prasugrel as directed.
• Be cautious to avoid injury, as prasugrel may cause easy bruising or bleeding.
• Seek medical help for excessive or prolonged bleeding, blood in stools or urine, or unexplained symptoms.

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Summary

Prasugrel is a medication used to treat patients with acute coronary syndrome (ACS) and unstable angina. Prasugrel can cause significant, sometimes fatal, bleeding. Common side effects of prasugrel include high blood pressure, high cholesterol/lipids in the blood, headache, back pain, shortness of breath, nausea, diarrhea, dizziness, cough, low blood pressure, fatigue, noncardiac chest pain, rapid and irregular rhythm in the atria, slow heart rate, and others. Consult your doctor if pregnant or breastfeeding.