PRASUGREL HYDROCHLORIDE

Clinical safety rating: safe

Other drugs that affect hemostasis increase bleeding risk Contraindicated in patients with history of stroke or TIA.

How it works

Prasugrel is an irreversible antagonist of the P2Y12 receptor on platelets, inhibiting ADP-mediated platelet aggregation.

What the body does with it

Metabolism	Prasugrel is a prodrug that undergoes rapid hydrolysis to a thiolactone intermediate (via carboxylesterases) and subsequent conversion to its active metabolite by CYP3A4 and CYP2B6, with minor contributions from CYP2C9 and CYP2C19.
Excretion	Approximately 68% of the administered dose is eliminated in urine (as inactive metabolites) and 27% in feces. Less than 1% is excreted as unchanged parent drug.
Half-life	The terminal elimination half-life of the active metabolite is approximately 7 hours (range 2–15 hours). Clinical context: Once-daily dosing achieves sufficient antiplatelet effect due to irreversible P2Y12 receptor binding; recovery of platelet function occurs over 5–7 days.
Protein binding	Active metabolite: approximately 98% bound to human serum albumin.
Volume of Distribution	Apparent volume of distribution of the active metabolite is approximately 44–68 L (0.6–1.0 L/kg), indicating extensive tissue distribution.
Bioavailability	Oral bioavailability is at least 79% (based on urinary recovery of metabolites) and is not significantly affected by food.
Onset of Action	Oral: Inhibition of platelet aggregation is evident within 30 minutes, with peak effect achieved at 2–4 hours.
Duration of Action	Duration of antiplatelet effect is for the lifespan of the platelet (approximately 7–10 days), consistent with irreversible binding to the P2Y12 receptor. Clinical note: Platelet function gradually returns after discontinuation; surgery should be delayed at least 7 days if possible.

Classification & Brands

Dosing & administration

Loading dose: 60 mg orally once. Maintenance: 10 mg orally once daily. Administered with aspirin 75-100 mg daily.

Dosage form	TABLET
Renal impairment	No dose adjustment required in patients with chronic kidney disease (including end-stage renal disease on hemodialysis); no data in acute kidney injury.
Liver impairment	Contraindicated in patients with severe hepatic impairment (Child-Pugh class C). Mild to moderate hepatic impairment (Child-Pugh class A or B): No dose adjustment required.
Pediatric use	Not approved for use in pediatric patients (<18 years). Safety and efficacy not established.
Geriatric use	No dose adjustment required based on age alone. Increased risk of bleeding; use lowest effective dose (10 mg daily). Caution in patients ≥75 years with low body weight (<60 kg) as no net benefit observed; consider alternative therapy.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Other drugs that affect hemostasis increase bleeding risk Contraindicated in patients with history of stroke or TIA.

FDA category	Animal
Breastfeeding	Unknown if prasugrel is excreted in human breast milk. M/P ratio: not established. Caution should be exercised when administered to a nursing woman due to potential for serious adverse reactions in nursing infants. Consider discontinuing nursing or drug.
Teratogenic Risk	Prasugrel is Pregnancy Category B. Animal studies have not shown teratogenic effects. There are no adequate and well-controlled studies in pregnant women. Use only if clearly needed. Risk during first trimester: unknown but likely low based on animal data. Second and third trimesters: potential risk of maternal hemorrhage and fetal bleeding due to antiplatelet effect.

Warnings & precautions

■ FDA Black Box Warning

Bleeding risk: Prasugrel causes significant, sometimes fatal, bleeding. Do not use in patients with active pathological bleeding or history of transient ischemic attack or stroke.

Side Effect Profile

Common Effects	Bleeding
Serious Effects

Absolute Contraindications

["Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage)","History of transient ischemic attack (TIA) or stroke","Severe hepatic impairment"]

Clinical Precautions

Precautions

["Increased bleeding risk","Do not use in patients with prior TIA or stroke","Avoid use in patients ≥75 years unless high risk","Use with caution in patients with renal or hepatic impairment","Risk of thrombotic thrombocytopenic purpura (TTP)"]

Clinical Tips & Counseling

Drug interactions

Loading safety data…

PRASUGREL HYDROCHLORIDE

Clinical safety rating: safe

Other drugs that affect hemostasis increase bleeding risk Contraindicated in patients with history of stroke or TIA.

How it works

Prasugrel is an irreversible antagonist of the P2Y12 receptor on platelets, inhibiting ADP-mediated platelet aggregation.

What the body does with it

Metabolism	Prasugrel is a prodrug that undergoes rapid hydrolysis to a thiolactone intermediate (via carboxylesterases) and subsequent conversion to its active metabolite by CYP3A4 and CYP2B6, with minor contributions from CYP2C9 and CYP2C19.
Excretion	Approximately 68% of the administered dose is eliminated in urine (as inactive metabolites) and 27% in feces. Less than 1% is excreted as unchanged parent drug.
Half-life	The terminal elimination half-life of the active metabolite is approximately 7 hours (range 2–15 hours). Clinical context: Once-daily dosing achieves sufficient antiplatelet effect due to irreversible P2Y12 receptor binding; recovery of platelet function occurs over 5–7 days.
Protein binding	Active metabolite: approximately 98% bound to human serum albumin.
Volume of Distribution	Apparent volume of distribution of the active metabolite is approximately 44–68 L (0.6–1.0 L/kg), indicating extensive tissue distribution.
Bioavailability	Oral bioavailability is at least 79% (based on urinary recovery of metabolites) and is not significantly affected by food.
Onset of Action	Oral: Inhibition of platelet aggregation is evident within 30 minutes, with peak effect achieved at 2–4 hours.
Duration of Action	Duration of antiplatelet effect is for the lifespan of the platelet (approximately 7–10 days), consistent with irreversible binding to the P2Y12 receptor. Clinical note: Platelet function gradually returns after discontinuation; surgery should be delayed at least 7 days if possible.

Classification & Brands

Dosing & administration

Loading dose: 60 mg orally once. Maintenance: 10 mg orally once daily. Administered with aspirin 75-100 mg daily.

Dosage form	TABLET
Renal impairment	No dose adjustment required in patients with chronic kidney disease (including end-stage renal disease on hemodialysis); no data in acute kidney injury.
Liver impairment	Contraindicated in patients with severe hepatic impairment (Child-Pugh class C). Mild to moderate hepatic impairment (Child-Pugh class A or B): No dose adjustment required.
Pediatric use	Not approved for use in pediatric patients (<18 years). Safety and efficacy not established.
Geriatric use	No dose adjustment required based on age alone. Increased risk of bleeding; use lowest effective dose (10 mg daily). Caution in patients ≥75 years with low body weight (<60 kg) as no net benefit observed; consider alternative therapy.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Other drugs that affect hemostasis increase bleeding risk Contraindicated in patients with history of stroke or TIA.

FDA category	Animal
Breastfeeding	Unknown if prasugrel is excreted in human breast milk. M/P ratio: not established. Caution should be exercised when administered to a nursing woman due to potential for serious adverse reactions in nursing infants. Consider discontinuing nursing or drug.
Teratogenic Risk	Prasugrel is Pregnancy Category B. Animal studies have not shown teratogenic effects. There are no adequate and well-controlled studies in pregnant women. Use only if clearly needed. Risk during first trimester: unknown but likely low based on animal data. Second and third trimesters: potential risk of maternal hemorrhage and fetal bleeding due to antiplatelet effect.

Warnings & precautions

■ FDA Black Box Warning

Bleeding risk: Prasugrel causes significant, sometimes fatal, bleeding. Do not use in patients with active pathological bleeding or history of transient ischemic attack or stroke.

Side Effect Profile

Common Effects	Bleeding
Serious Effects

Absolute Contraindications

["Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage)","History of transient ischemic attack (TIA) or stroke","Severe hepatic impairment"]