Prasugrel

What is Prasugrel?

• Prasugrel (Effient) is a P2Y12 platelet inhibitor used to decrease the risk of myocardial infarction and stroke in patients with acute coronary syndromes.

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Prasugrel

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Prasugrel Enantiomers Structural Formulae V.1

What are the uses of this medicine?

Prasugrel (Effient) is a prescription medicine used to treat people who:

• have had a heart attack or severe chest pain that happens when your heart does not get enough oxygen, and
• have been treated with a procedure called “angioplasty” (also called balloon angioplasty).

• Effient is used to lower your chance of having another serious problem with your heart or blood vessels, such as another heart attack, a stroke, blood clots in your stent, or death.
• Platelets are blood cells that help with normal blood clotting. Effient helps prevent platelets from sticking together and forming a clot that can block an artery or a stent.

How does this medicine work?

• Prasugrel (pra' soo grel) is a thienopyridine inhibitor of adenosine diphosphate (ADP) receptors (P2Y12) on platelets, and is used as an anticoagulant to decrease the risk of recurrent coronary thromboses in patients who undergo interventions during an acute coronary syndrome.
• Activated platelets release ADP which binds to ADP platelet receptors, causing activation of the intracellular glycoprotein IIb/IIIA complex which triggers platelet adherence and aggregation.
• The aggregation of platelets plays an important role in the growth of atheromatous plaques, which can lead to coronary, cerebral and peripheral arterial occlusions.
• Prasugrel is an irreversible inhibitor of the P2Y12 receptor and its effects last for the life time of the platelet (7 to 10 days).
• In clinical trials, prasugrel therapy during acute coronary events (unstable angina and myocardial infarction) was equivalent or slightly better than clopidogrel in decreasing the frequency of recurrence of myocardial infarction and stent thrombosis.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• currently have abnormal bleeding, such as stomach or intestinal bleeding, or bleeding in your head
• have a history of stroke, or “mini-stroke” (transient ischemic attack or TIA)
• are allergic to prasugrel or any of the ingredients in Effient.

What drug interactions can this medicine cause?

• Coadministration of Effient and warfarin increases the risk of bleeding.
• Coadministration of Effient and NSAIDs (used chronically) may increase the risk of bleeding.

Is this medicine FDA approved?

• Prasugrel was approved for use in the United States in 2009 and has been used in limited numbers of patients for a limited time only.
• Current indications are reduction of recurrent cardiovascular events in patients with acute coronary syndromes.

How should this medicine be used?

Recommended dosage:

• Initiate treatment with a single 60 mg oral loading dose.
• Continue at 10 mg once daily with or without food. Consider 5 mg once daily for patients <60 kg.
• Patients should also take aspirin (75 mg to 325 mg) daily.

Administration:

• Take Effient exactly as prescribed by your doctor.
• Take Effient one time each day.
• You can take Effient with or without food.
• Take Effient with aspirin as instructed by your doctor.
• Your doctor will decide how long you should take Effient. Do not stop taking Effient without first talking to the doctor who prescribed it for you.
• If you miss a dose, take Effient as soon as you remember. If it is almost time for your next dose, skip the missed dose. Just take the next dose at your regular time. Do not take two doses at the same time unless your doctor tells you to.
• If you take too much Effient, call your local emergency room or poison control center right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As 5 mg and 10 mg tablets

This medicine is available in fallowing brand namesː

• Effient

What side effects can this medication cause?

The most common side effects of this medicine include:

• Bleeding
• including life-threatening fatal bleeding

Effient can cause serious side effects, including:

• A blood clotting problem called Thrombotic Thrombocytopenic Purpura (TTP)

What special precautions should I follow?

• Thienopyridines, including Effient, increase the risk of bleeding. Risk increases in patients receiving Effient who undergo Coronary Artery Bypass Graft Surgery-Related Bleeding (CABG).
• Discontinue thienopyridines, including Effient, for active bleeding, elective surgery, stroke, or TIA. The optimal duration of thienopyridine therapy is unknown. Premature discontinuation increases risk of stent thrombosis, MI, and death.
• Thrombotic thrombocytopenic purpura (TTP) has been reported with the use of Effient. TTP is a serious condition that can be fatal and requires urgent treatment, including plasmapheresis (plasma exchange).
• Prasugrel has been linked to mild and transient serum enzyme elevations during therapy and to rare instances of hypersensitivity reactions accompanied by mild liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• Symptoms of acute toxicity in dogs included emesis, increased serum alkaline phosphatase, and hepatocellular atrophy.
• Symptoms of acute toxicity in rats included mydriasis, irregular respiration, decreased locomotor activity, ptosis, staggering gait, and lacrimation.

Management of overdosage:

• Platelet transfusion may restore clotting ability.
• The prasugrel active metabolite is not likely to be removed by dialysis.

Can this medicine be used in pregnancy?

There are no adequate and well-controlled studies of Effient use in pregnant women.

• Effient should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

• Active Ingredient: prasugrel
• Inactive Ingredients: mannitol, hypromellose, croscarmellose sodium, microcrystalline cellulose, and vegetable magnesium stearate. The color coatings contain lactose, hypromellose, titanium dioxide, triacetin, iron oxide yellow, and iron oxide red (only in Effient 10 mg tablet).

Who manufactures and distributes this medicine?

• Manufactured by Eli Lilly and Company, Indianapolis, IN, 46285
• Marketed by Daiichi Sankyo, Inc. and Eli Lilly and Company

What should I know about storage and disposal of this medication?

• Keep Effient at room temperature between 59°F to 86°F (15°C to 30°C).
• Keep Effient in the container it comes in.
• Keep the container closed tightly with the gray cylinder inside.
• Protect Effient from moisture.

• Dailymed label info on Prasugrel
• FDA Prasugrel

Prasugrel Resources
Latest articles Most recent articles Ongoing trials	Wikipedia

• Dailymed label info on Prasugrel
• FDA Prasugrel

Prasugrel Resources
Latest articles Most recent articles Ongoing trials	Wikipedia