Drug reference

Rosuvastatin + Aspirin

Statin · Lipid-lowering agent and Antiplatelet agent for Cardiovascular Prophylaxis

Also known as Rosuvas-A, Rozavel-A, Roseday-A, Novastat-A, Crestor-A, Statigyn-A

StatinLipid-lowering agent and Antiplatelet agent for Cardiovascular ProphylaxisATC C10BX05

CDSCO approvedSchedule HATC C10BX05

Pharmacokineticsplasma · t hours

ONSET: 3w · Rosuvastatin: Lipid-lowering effects begin within 1 week, maximal effect by 2-4 weeks. Aspirin: Antiplatelet effect within 60 minutes for immediate release.
PEAK: 4h · Rosuvastatin: Plasma concentration in 3-5 hours. Aspirin: Platelet inhibition within 1-2 hours.
t½: 2.5h · Rosuvastatin: Approximately 19 hours. Aspirin: Parent drug ~20 minutes; active metabolite (salicylic acid) ~2-3 hours (dose-dependent).
DURATION: 1.2w · Rosuvastatin: Sustained lipid-lowering effect with daily dosing. Aspirin: Antiplatelet effect lasts for the lifespan of the platelet (7-10 days).

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

AmiodaroneSevereTextbookG&G 14e · p736
Azole AntifungalsSevereTextbookG&G 14e · p736
CyclosporineSevereTextbookG&G 14e · p736
ErythromycinSevereTextbookKDT 7e · p637

Mechanism

Rosuvastatin, an HMG-CoA reductase inhibitor, reduces cholesterol synthesis in the liver by inhibiting the rate-limiting enzyme. This leads to an upregulation of LDL receptors and increased clearance of LDL-C from the blood. Aspirin irreversibly inhibits cyclooxygenase-1 (COX-1) in platelets, preventing the synthesis of thromboxane A2 (TXA2), a potent inducer of platelet aggregation and vasoconstriction. The combination synergistically lowers elevated lipid levels and provides antiplatelet effects, thereby reducing the risk of thrombotic cardiovascular events in high-risk patients. Combination rationale: This fixed-dose combination provides a dual therapeutic approach to cardiovascular risk reduction. Rosuvastatin effectively lowers LDL-C and provides pleiotropic effects like plaque stabilization, while aspirin inhibits platelet aggregation, preventing thrombotic events. Combining these agents in a single formulation improves patient adherence to chronic therapy, which is crucial for the long-term management and prevention of major adverse cardiovascular events in high-risk individuals.

Indications

Primary prevention of atherosclerotic cardiovascular disease (ASCVD) in patients with multiple risk factorsSecondary prevention of cardiovascular events (e.g., myocardial infarction, stroke) in patients with established ASCVDTreatment of dyslipidemia in patients requiring both lipid lowering and antiplatelet therapy

Dosing

Adult: Typical strengths include Rosuvastatin 5 mg/10 mg/20 mg combined with Aspirin 75 mg/150 mg, administered orally once daily, usually at bedtime. Dosing should be individualized based on lipid goals and antiplatelet needs.
Pediatric: This fixed-dose combination is generally not indicated for pediatric use.
Renal adjustment: For Rosuvastatin: In patients with CrCl <30 mL/min, initiate with 5 mg once daily and do not exceed 10 mg once daily. For Aspirin: Use with caution in severe renal impairment, as it may exacerbate renal dysfunction and increase risk of toxicity.
Hepatic adjustment: Contraindicated in active liver disease or severe hepatic impairment. Use with caution in patients with moderate hepatic impairment; monitor liver function tests regularly.
Geriatric: Use with caution due to increased risk of bleeding and myopathy. Lower starting doses of rosuvastatin may be considered. Closely monitor for adverse effects.
Max dose: Rosuvastatin component: 40 mg daily. Aspirin component (for antiplatelet prophylaxis): 150 mg daily in FDC formulations.

Pharmacokinetics

Onset

Rosuvastatin: Lipid-lowering effects begin within 1 week, maximal effect by 2-4 weeks. Aspirin: Antiplatelet effect within 60 minutes for immediate release.

Peak effect

Rosuvastatin: Plasma concentration in 3-5 hours. Aspirin: Platelet inhibition within 1-2 hours.

Duration

Rosuvastatin: Sustained lipid-lowering effect with daily dosing. Aspirin: Antiplatelet effect lasts for the lifespan of the platelet (7-10 days).

Half-life

Rosuvastatin: Approximately 19 hours. Aspirin: Parent drug ~20 minutes; active metabolite (salicylic acid) ~2-3 hours (dose-dependent).

Bioavailability

Rosuvastatin: Approximately 20%. Aspirin: Rapid and complete absorption, but undergoes extensive first-pass hydrolysis to salicylic acid.

Protein binding

Rosuvastatin: Approximately 90% (primarily to plasma proteins). Aspirin: Salicylic acid is highly protein-bound (70-90%).

Metabolism

Rosuvastatin: Limited metabolism, primarily by CYP2C9 and CYP2C19. Aspirin: Rapidly hydrolyzed to salicylic acid by esterases; salicylic acid then undergoes hepatic conjugation and hydroxylation.

Excretion

Rosuvastatin: Primarily via feces (90%), with minor renal excretion. Aspirin: Salicylic acid and its metabolites are primarily excreted renally.

Contraindications

Active bleeding or hemorrhagic diathesis (e.g., active peptic ulcer, intracranial hemorrhage)
Hypersensitivity to rosuvastatin, aspirin, salicylates, or any component of the formulation
Severe hepatic impairment or active liver disease (including unexplained persistent elevations of serum transaminases)
Severe renal impairment (CrCl <30 mL/min for rosuvastatin)
Asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs
Congestive heart failure (NYHA Class II-IV)
Pregnancy and lactation

Side effects

Common

MyalgiaHeadacheNauseaAbdominal painDyspepsiaConstipationDiarrheaIncreased liver transaminasesMinor bleeding (e.g., epistaxis, bruising)

Serious

Rhabdomyolysis
Hepatotoxicity (liver failure)
Pancreatitis
Severe bleeding (e.g., gastrointestinal hemorrhage, intracranial hemorrhage)
Angioedema
Renal impairment
Hemorrhagic stroke
Thrombotic thrombocytopenic purpura (TTP)
Stevens-Johnson Syndrome (SJS)

Pregnancy & lactation

Pregnancy

Lactation

Contraindicated. Both rosuvastatin and aspirin (salicylates) are excreted in breast milk and may cause serious adverse effects in the nursing infant.

Drug interactions

Amiodarone

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736

Azole Antifungals

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736

Cyclosporine

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy. For simvastatin, coadministration is contraindicated.

Source: G&G 14e · p736

Erythromycin

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: KDT 7e · p637

Gemfibrozil

Severe

Textbook

Increased plasma concentration of statin hydroxy acids, leading to an increased risk of myopathy (including rhabdomyolysis).

Avoid coadministration. The FDA withdrew approval for statin drug combinations containing fibrates in 2016.

Source: G&G 14e · p736

Hiv Protease Inhibitor

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: KDT 7e · p637

Hiv Protease Inhibitors

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Source: G&G 14e · p736

Ketoconazole

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: KDT 7e · p637

Macrolide Antibiotics

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Source: G&G 14e · p736

Nefazodone

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736

Niacin

Severe

Textbook

Increased risk of myopathy.

Avoid coadministration. The FDA withdrew approval for statin drug combinations containing niacin in 2016.

Source: G&G 14e · p736

Nicotinic Acid

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

A lower dose of statin is advisable when nicotinic acid is given concurrently. Close monitoring for muscle symptoms is essential.