Description
Generic
Indications
Rosuvastatin is prescribed in-
- Hypercholesterolemia Heterozygous (Familial and Non familial)
- Hypercholesterolemia in a homozygous state (Familial)
- Dyslipidemia with a mix of lipids (Fredrickson Type IIa and IIb)
- Primary cardiovascular disease prevention
Pharmacology
Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, the enzyme responsible for converting 3-hydroxy-3-methyl glutaryl coenzyme A to mevalonate, a precursor of cholesterol. Rosuvastatin exerts its lipid-modifying properties in two ways. First, it increases the number of hepatic LDL receptors on the cell surface, which improves LDL absorption and catabolism. Second, rosuvastatin suppresses hepatic VLDL production, lowering the overall amount of VLDL and LDL particles.
Dosage
HoFH: Starting dose 20 mg/day.
Pediatric patients with HeFH: 5-10 mg/day for patients 8 to less than 10 years age, 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
Rosuvastatin has a number of notable medication interactions-
- The combination of cyclosporine with rosuvastatin enhances the exposure to rosuvastatin. The dose of rosuvastatin should be limited to 5 mg once day.
- Combination with gemfibrosil should be avoided. Rosuvastatin dosage should be reduced to 10 mg once daily if administered concurrently.
- The combination of lopinavir/ritonavir or atazanavir/ritonavir enhances Rosuvastatin exposure. Rosuvastatin should be taken at a dosage of 10 mg once day.
- Coumarin anticoagulants: The combination increases the international normalized ratio (INR). Prior to beginning Rosuvastatin, the INR should be stable. When starting or changing Rosuvastatin treatment, the INR should be evaluated on a regular basis until it reaches a stable level.
- Concurrent lipid-lowering therapies: When combined with fibrates and niacin products, the risk of skeletal muscle effects increases.
Contraindications
Rosuvastatin should be avoided if you have any of the following conditions:
- Hypersensitivity to product components is known.
- Liver illness, characterized by unexplained chronic increases in hepatic transaminase levels
- Women who are pregnant or may become pregnant
- Mothers who are breastfeeding
Side Effects
Rosuvastatin is well tolerated in most people. The most common side effects associated with Rosuvastatin were headache, myalgia, constipation, asthenia, stomach discomfort, and nausea.
Pregnancy & Lactation
Pregnant women’s safety has not been demonstrated. It is unknown whether or not Rosuvastatin is excreted in human milk.
Precautions & Warnings
Effects on skeletal muscles (e.g., myopathy and rhabdomyolysis): The risks rise with the usage of a 40 mg dosage, advanced age (>65 years), hypothyroidism, renal impairment, and use in conjunction with cyclosporine, lopinavir/ritonavir, atazanavir/ritonavir, or some other lipid-lowering medications. Patients should be urged to report any unexplained muscular discomfort, soreness, or weakness as soon as possible. If indications or symptoms occur, rosuvastatin can be stopped.
Abnormalities in liver enzymes and monitoring: Persistent increases in hepatic transaminases might develop.
Before and throughout therapy, liver enzymes should be measured.
Therapeutic Class
Storage Conditions
Maintain a temperature of less than 30 degrees Celsius and keep it away from light and moisture. Keep out of children’s reach.