Description
Indications
The use of rosuvastatin is advised in the following situations:
- Hypercholesterolemia Heterozygous (Familial and Nonfamilial)
- Hypercholesterolemia Homozygous (Familial)
- Dyslipidemia (Mixed) (Fredrickson Type IIa and IIb)
- Primary cardiovascular disease prevention
Pharmacology
HMG-CoA reductase is the rate-limiting enzyme that transforms 3-hydroxy-3-methyl glutaryl coenzyme A to mevalonate, a precursor of cholesterol. Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase. Rosuvastatin has two mechanisms for altering lipid levels. To begin, it boosts the number of hepatic LDL receptors on the cell surface, which improves LDL absorption and degradation. Second, Rosuvastatin lowers the overall amount of VLDL and LDL particles by inhibiting VLDL production in the liver.
Dosage
Dose range: 5-40 mg once daily. Use 40 mg dose only for patients not reaching LDL-C goal with 20 mg
HoFH: Starting dose 20 mg/day.
Pediatric patients with HeFH: 5-10 mg/day for patients 8 to less than 10 years old, and 5-20 mg/day for patients 10 to 17 years of age.
Pediatric patients with HoFH: 20 mg/day for patients 7 to 17 years of age.
Administration
Interaction
The following are notable Rosuvastatin medication interactions:
- A combination of cyclosporine with rosuvastatin enhances Rosuvastatin exposure. The daily dose of rosuvastatin should be kept at 5 mg.
- The combination should be avoided with gemfibrozil. If used concurrently, the dose of rosuvastatin should be kept at 10 mg once a day.
- The combination of lopinavir/ritonavir or atazanavir/ritonavir enhances Rosuvastatin exposure. The dose of rosuvastatin should be reduced to 10 mg once a day.
- A combination of coumarin anticoagulants increases the international normalized ratio (INR). Prior to commencing Rosuvastatin, make sure your INR is stable. When starting or stopping Rosuvastatin treatment, the INR should be checked often until it is stable.
- Concurrent lipid-lowering therapies: Using fibrates and niacin products at the same time may raise the risk of skeletal muscle side effects.
Contraindications
If you’re using rosuvastatin, you should avoid it if you have any of the following conditions:
- Hypersensitivity to product components is known.
- Liver disease, which might include unexplained chronic increases in liver enzymes, is one example.
- levels of hepatic transaminase
- Women who are pregnant or may become pregnant
- Mothers who are breastfeeding
Side Effects
Rosuvastatin is well tolerated by most people. Headache, myalgia, constipation, asthenia, stomach discomfort, and nausea were the most common side effects linked to Rosuvastatin.
Pregnancy & Lactation
The safety of the drug in pregnant women has yet to be determined. Rosuvastatin is not known whether it is excreted in human milk.
Precautions & Warnings
A combination of coumarin anticoagulants increases the international normalized ratio (INR). Prior to commencing Rosuvastatin, make sure your INR is stable. When starting or stopping Rosuvastatin treatment, the INR should be checked often until it is stable.
Concurrent lipid-lowering therapies: Using fibrates and niacin products at the same time may raise the risk of skeletal muscle side effects.
Therapeutic Class
Storage Conditions
Keep the temperature below 30°C and keep it away from light and moisture. Keep out of children’s reach.