Rosuvastatin

General dosing:

The 40 mg dose should be reserved for patients who have not achieved their LDL-C goal utilizing the 20 mg dose including patients switched from another HMG-CoA reductase inhibitor.

Adults:

– Homozygous familial hypercholesterolemia:

Usual dosage: 5 to 40 mg once daily.

Initial dosage: 20 mg once daily

– Hyperlipidemia, mixed dyslipidemia

Usual dosage: 5 to 40 mg once daily.

Initial dosage: 10 to 20 mg once daily; 20 mg once daily may be used in patients with severe hyperlipidemia (LDL >190 mg/dL) and aggressive lipid targets.

Dosage titration: After initiation or upon titration, analyze lipid levels within 2 to 4 weeks (peak, steady-state lowering effects usually seen between 4 to 6 weeks and adjust dose accordingly

– Prevention of cardiovascular disease:

Primary prevention:

LDL-C ≥190 mg/dL: High-intensity therapy: 20 to 40 mg once daily.

Type 1 or 2 diabetes and age 40 to 75 years: Moderate-intensity therapy: 5 to 10 mg once daily.

Type 1 or 2 diabetes, age 40 to 75 years, and an estimated 10-year ASCVD risk ≥7.5%: High intensity

therapy: 20 to 40 mg once daily.

Age 40 to 75 years and an estimated 10-year ASCVD risk ≥7.5%: Moderate to high intensity therapy:

5 to 40 mg once daily.

Secondary prevention:

Age ≤75 years: High-intensity therapy: 20 to 40 mg once daily.

Age >75 years or not a candidate for high-intensity therapy: Moderate-intensity therapy: 5 to 10 mg

once daily.

Dosage adjustment for toxicity:

Severe muscle symptoms or fatigue: Promptly discontinue use; evaluate CPK, creatinine, and

urinalysis for myoglobinuria.

Mild to moderate muscle symptoms: Discontinue use until symptoms can be evaluated; evaluate patient for conditions that may increase the risk for muscle symptoms. Upon resolution, resume the original or lower dose of rosuvastatin. After muscle symptom resolution, may then use a low dose of a different statin; gradually increase if tolerated.

Contraindications:

In patients with hypersensitivity to rosuvastatin or to any of the excipients, patients with active liver disease including unexplained, persistent elevations of serum transaminases and any serum transaminase elevation exceeding 3 x the upper limit of normal (ULN), patients with severe renal impairment (creatinine clearance <30 ml/min), patients with myopathy, patients receiving concomitant ciclosporin, during pregnancy and lactation and in women of childbearing potential not using appropriate contraceptive measures.

The 40 mg dose is contraindicated in patients with pre-disposing factors for myopathy/rhabdomyolysis. Such factors include:

moderate renal impairment (creatinine clearance < 60 ml/min), hypothyroidism, personal or family, history of hereditary muscular disorders, previous history of muscular toxicity with another HMG, CoA reductase inhibitor or fibrate, alcohol abuse, situations where an increase in plasma levels may occur, Asian patients, concomitant use of fibrates.

Interactions:

Transporter protein inhibitors, Ciclosporin, Protease inhibitors, Gemfibrozil and other lipid lowering products, Ezetimibe, Antacid, Erythromycin, Cytochrome P450 enzymes, Interactions, requiring rosuvastatin dose adjustments, Vitamin K antagonists, Oral contraceptive/hormone.

 Other medicinal products: Digoxin, Fusidic Acid, Pediatric population

Pregnancy and Lactation:

Women of child bearing potential should use appropriate contraceptive measures.

Since cholesterol and other products of cholesterol biosynthesis are essential for the development of the fetus, the potential risk from inhibition of HMG-CoA reductase outweighs the advantage of treatment during pregnancy. Rosuvastatin is excreted in the milk of rats. There are no data with respect to excretion in milk in humans

Warning and Precaution:

Renal Effects, Skeletal Muscle Effects, Liver Effects, Race, Protease inhibitors, Lactose intolerance, Interstitial lung disease, Diabetes Mellitus, Pediatric population

Adverse Reactions:

Endocrine disorders in Diabetes mellitus, Headache, Dizziness, Constipation, Nausea, Abdominal pain, Musculo-skeletal and connective tissue disorders, Myalgia, General disorders and administration site conditions, Asthenia.

Storage:

Store below 30 and protect from light and moisture.