DrugInfoSys

Prasugrel HCl

Drug #2225

Prasugrel is an anti-platelet agent. The chemical name is 5-[(1RS)-2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]- 4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl acetate hydrochloride corresponding to the molecular formula C20H20FNO3S•HCl. Prasugrel is a prodrug, oxidation by intestinal and hepatic cytochrome P-450 enzymes convert prasugrel into its active metabolite. Its active form binds irreversibly to the adenosine diphosphate (ADP) P2Y12 receptor on platelets for their lifespan, thereby inhibiting their activation and decreasing subsequent platelet aggregation.

Primary Characteristics

Molecular Weight: 409.9 · pKa: 5.1 · Solubility in Water: soluble at pH 2. · Solubility in Alcohol: freely in methanol and is slightly soluble in 1- and 2-propanol and acetone · Non-proprietary name: Prasugrel HCl.

Molecular structure of Prasugrel HCl

Pharmacokinetics

Distribution: Prasugrel HCl has a volume of distribution is for active metabolite is 40.3-66.4 L.. plasma protein binding is for active metabolite R-138727 is 98%..

Elimination: it is metabolised via by Cytochrome P450 enzyme., plasma half-life is 7.4 Hrs (2-15 Hr) for active metabolites, renal excretion is 68% and 27% in faeces over 10 days.

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Indications

Contraindications

Prasugrel HCl is contraindicated in conditions like Bleeding, Transient ischaemic attacks.

Dosage

Prasugrel HCl's dosage details are as follows:

DoseSingle DoseFrequencyRouteInstructions
Adult Dosage
5 mg5 mgEvery 24hPOInitiate with single loading dose of 60mg oral. Consider lowering the maintenance dose to 5 mg in patients < 60 kg. It may be taken with or without food.
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

1 interaction

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Prasugrel HCl produces potentially life-threatening effects which include Thrombocytopenia , Bleeding , Hypersensitivity , Jaundice , Atrial fibrillation, blood in urine, blood in stool, Thrombotic thrombocytopenic purpura, Peripheral edema. Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Prasugrel HCl are Vomiting, Lacrimation, hepatocellular atrophy, Decreased locomotor activity, Blurred vision, Mydriasis, Shortness of breadth.

Prasugrel HCl is known to cause more or less tolerable side effects which are usually transient. These include Abnormal hepatic function, Back pain, Cough , Diarrhea, Dizziness, Dyspnea, Hypotension , Mild headache, Minor chest pain, Nausea, Pain in upper & lower extremities, Tiredness .

Warnings / Precautions

It can cause significant, sometimes fatal, bleeding. Do not use in patients with active pathological bleeding or a history of transient ischemic attack or stroke. In patients greater then or equal to 75 years of age, it is generally not recommended because of the increased risk of fatal and intracranial bleeding and uncertain benefit, except in high-risk patients (diabetes or prior MI), where its effect appears to be greater and its use may be considered. Do not start Prasugrel in patients likely to undergo urgent coronary artery bypass graft surgery (CABG). When possible, discontinue it at least 7 days prior to any surgery. Additional risk factors for bleeding include: Body weight < 60 kg Propensity to bleed Concomitant use of medications that increase the risk of bleeding. Suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, Percutaneous coronary intervention (PCI), CABG, or other surgical procedures in the setting of Prasugrel. If possible, manage bleeding without discontinuing it. Stopping Prasugrel, particularly in the first few weeks after acute coronary syndrome, increases the risk of subsequent cardiovascular events .

Available Brands

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Single Ingredient

Multi-Ingredient Combinations

Storage Conditions

Prasugrel HCl should be stored tab.

Drug Classification

  1. 1.10.2Anticoagulants/Platelet deaggregators

Manufacturers