Rosuvastatin increases the number of liver LDL (low-density lipoprotein) cell surface receptors, promotes LDL absorption and breakdown metabolism, inhibits VLDL (very low-density lipoprotein) liver synthesis, reduces the total number of VLDL and LDL particles, and achieves the effect of lowering blood lipids.

1、 Drug name

1. Common name: Rosuvastatin Calcium

2. Product Name: CRESTOR ®

2、 Indications

1. Primary prevention of cardiovascular disease: Used for adults without coronary heart disease but with increased risk based on age, high-sensitivity C-reactive protein ≥ 2mg/L, and at least one cardiovascular risk factor, to reduce the risk of major cardiovascular adverse events (cardiovascular death, non fatal myocardial infarction, non fatal stroke, or arterial revascularization).

2. As a dietary adjuvant therapy:

Primary hyperlipidemia in adults: reducing low-density lipoprotein cholesterol.

Delay the progression of atherosclerosis in adults.

Heterozygous familial hypercholesterolemia patients aged 8 years and above: reduce LDL-C.

As an adjunct to other LDL-C lowering therapies, or used alone for homozygous familial hypercholesterolemia patients aged 7 years and older.

Primary abnormal beta lipoproteinemia in adults.

Adult hypertriglyceridemia.

3、 Specifications and characteristics

1. Specification: 10mg.

2. Appearance: Pink, round, biconvex, thin film coating.

4、 Main components

Active ingredient: Rosuvastatin calcium

5、 Usage and dosage

1. Conventional usage: once daily, oral, can be taken with food or on an empty stomach, whole tablet swallowed. It can be taken at any time of the day.

2. Recommended dose for adults: 5mg to 40mg, once daily.

Heterozygous familial hypercholesterolemia in children aged 8 to 10 years old: 5mg to 10mg, once daily.

Heterozygous familial hypercholesterolemia in children aged 10 and above: 5mg to 20mg, once daily.

Children with homozygous familial hypercholesterolemia (aged 7 years and above): 20mg, once daily.

Asian patients: starting dose of 5mg, once daily. If the dose control of 20mg is poor, the benefits and risks need to be evaluated.

3. Severe renal insufficiency patients (non dialysis): Initial dose of 5mg, once daily, maximum dose not exceeding 10mg.

6、 Dose adjustment

1. Adjustment due to combined medication:

Combined with cyclosporine: dose not exceeding 5mg, once daily.

Co administration with Teriflunomide, Ensidipine, and Carbatinib: dose not exceeding 10mg, once daily.

Co administration with fentanyl and febuxostat: dose not exceeding 20mg, once daily.

When used in combination with gemfibrozil: avoid use; If necessary, the initial dose should be 5mg and not exceed 10mg, once daily.

Used with Tafamotidine: avoid use; If necessary, the initial dose should be 5mg and not exceed 20mg, once daily.

Combination with multiple antiviral drugs: starting dose of 5mg but not exceeding 10mg, once daily.

Co administration with darotamine: dose not exceeding 5mg, once daily.

Combination with Regorafenib: dose not exceeding 10mg, once daily.

2. Adjustment due to adverse reactions: When muscle symptoms or significant elevation of creatine kinase occur, medication should be paused or stopped; Discontinue medication when severe liver damage occurs.

7、 Medication precautions

1. Before and after meals: can be taken with food or on an empty stomach, and the food does not affect the total absorption.

2. Omission treatment: If missed, there is no need to supplement, just take the next dose at the regular time. Do not take double the dosage.

3. Post vomiting treatment: If vomiting occurs after taking medication, there is no need to take additional medication, wait for the next regular medication time.

4. Co administration with antacids: If taking a compound antacid containing aluminum and magnesium, the antacid should be taken at least 2 hours before taking rosuvastatin.

5. Blood sample monitoring: LDL-C levels need to be evaluated 4 weeks after initiating treatment or after dose adjustment.

8、 Medication for special populations

1. Pregnant women: This product should be discontinued during pregnancy. Based on the mechanism of action, it may cause harm to the fetus. Animal studies have shown embryonic toxicity at high doses.

2. Breastfeeding women: This product can enter human milk, but breastfeeding is not recommended during treatment as it may cause serious adverse reactions to infants.

3. Women with fertility should be informed of potential fetal risks.

4. Children:

Heterozygous familial hypercholesterolemia: Safety and efficacy established for ages 8 and above.

Homozygous familial hypercholesterolemia: Safety and efficacy established for ages 7 and above.

The safety and efficacy of other types of hyperlipidemia or younger children have not been established yet.

5. Elderly patients: Patients aged 65 and above do not need to adjust their dosage, but age ≥ 65 years is a risk factor for myopathy and requires strengthened monitoring.

6. Renal insufficiency:

Mild to moderate (creatinine clearance rate ≥ 30ml/min/1.73m ²): No adjustment required.

Severe (creatinine clearance rate<30ml/min/1.73m ²): starting at 5mg, not exceeding 10mg.

7. Liver dysfunction:

Acute liver failure or decompensated cirrhosis: contraindicated.

Chronic alcoholic liver disease: Mild increase in blood drug concentration, caution is required.

Asian patients: Due to blood drug concentration being about twice that of Caucasians, the initial dose is 5mg.

9、 Adverse reactions

1. Common adverse reactions (incidence rate ≥ 2%): headache, nausea, muscle pain, fatigue, constipation.

2. Common adverse reactions in METEOR study (40mg, 1.7 years) include muscle pain (12.7%), joint pain (10.1%), headache (6.4%), dizziness (4.0%), elevated CPK (2.6%), abdominal pain (2.4%), and elevated ALT>3 times the upper limit of normal (2.2%).

3. Common adverse reactions in JUPITER study (20mg, 2 years): myalgia (7.6%), arthralgia (3.8%), constipation (3.3%), diabetes (2.8%), nausea (2.4%).

4. Children with heterozygous familial hypercholesterolemia: The incidence of CPK elevation>10 times the normal upper limit is 3%, which is higher than the placebo group.

5. Post listing report:

Hematological system: thrombocytopenia.

Hepatobiliary system: hepatitis, jaundice, liver failure (lethal and non lethal).

Musculoskeletal: Joint pain, immune-mediated necrotizing myopathy.

Nervous system: peripheral neuropathy, cognitive impairment (memory loss, forgetfulness, blurred consciousness), newly developed or aggravated myasthenia gravis.

Mental system: depression, sleep disorders (insomnia, nightmares).

Reproductive system: Male breast development.

Respiratory system: interstitial lung disease.

Skin: DRESS syndrome, lichenoid drug eruption.

6. Laboratory abnormalities: proteinuria, microscopic hematuria, elevated CPK, elevated transaminase, elevated blood glucose, elevated gamma glutamyl transferase, elevated alkaline phosphatase, elevated bilirubin, thyroid dysfunction.

10、 Contraindications

1. Acute liver failure or decompensated cirrhosis.

2. Individuals who are allergic to rosuvastatin or any excipients of this product.

11、 Drug interactions

1. Medications that increase the risk of myopathy and rhabdomyolysis include cyclosporine, teriflunomide, amlodipine, cabozantinib, futatinib, febuxostat, gefitirozil (avoid co administration), tafamotidine (avoid co administration), various antiviral drugs (such as sofosbuvir/vapatavir/fusirevar, atazanavir/ritonavir, lopinavir/ritonavir, etc.), darotamine, regorafenib, beta, niacin (lipid-lowering dose ≥ 1g/day), colchicine, ticagrelor, etc.

2. Medications that reduce the efficacy of rosuvastatin: Compound antacids containing aluminum and magnesium (should be taken at least 2 hours in advance).

3. The effects of rosuvastatin on other medications:

Warfarin: can significantly increase the international normalized ratio, and frequent monitoring of INR is required when starting or adjusting the dose of rosuvastatin.

Oral contraceptives (ethinylestradiol/norgestrel): can increase the AUC of ethinylestradiol by about 1.3 times and the AUC of norgestrel by about 1.3 times.

12、 Storage method

1. Storage temperature: 20 ℃ to 25 ℃, allowed to fluctuate between 15 ℃ to 30 ℃.

2. Store away from light and moisture.

3. Keep out of reach of children.

13、 Manufacturer

Manufacturer: AstraZeneca Pharmaceuticals LP (AstraZeneca).

Rosuvastatininformation