Ropitor 10

Generic

Rosuvastatin

 

Indications

Rosuvastatin is indicated in-

• Heterozygous Hypercholesterolemia (Familial and Non familial)
• Homozygous Hypercholesterolemia (Familial)
• Mixed Dyslipidemia (Fredrickson Type IIa and IIb)
• Primary prevention of cardiovascular disease

 

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 amount of hepatic LDL receptors on the cell surface, which improves LDL absorption and degradation. Second, Rosuvastatin decreases the total quantity of VLDL and LDL particles by inhibiting VLDL formation in the liver.

 

Dosage & Administration

• 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 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.
• Rosuvastatin can be taken with or without food, at any time of day.

 

Interaction

• The significant drug interaction of rosuvastatin is
•  cyclosporine: the combination increases the exposure of rosuvastatin. The dose of rosuvastatin should be limited to 5 mg once a day.
•  Gemfibrosil: Joint use should be avoided. If used together, the dose of rosuvastatin should be limited to 10 mg once a day.
•  Lopinavir/Ritonavir or Atazanavir/Ritonavir: The combination increases the exposure of rosuvastatin. The dose of rosuvastatin should be 10 mg once a day.
•  Coumarin anticoagulant: the combination extends the international normalized ratio (INR). Before starting rosuvastatin, a stable INR should be achieved. The INR should be monitored frequently until it stabilizes after starting or changing rosuvastatin therapy.
•  Concomitant lipid lowering therapy: Use with fibrates and niacin products may increase the risk of effects on skeletal muscle.

 

Contraindications

• If you have a known hypersensitivity to any of the product's ingredients, you should avoid taking rosuvastatin.
• Unexplained chronic rises in hepatic transaminase values are a sign of liver illness.
• Women who are pregnant or may become pregnant
• Mothers who are breastfeeding

 

Side Effects

The majority of people tolerate rosuvastatin effectively. The most prevalent adverse effects associated with Rosuvastatin were headache, myalgia, constipation, asthenia, stomach pain, and nausea.

 

Pregnancy & Lactation

The safety in pregnant women has not been established. It is not known whether Rosuvastatin is excreted in human milk or not.

 

Precautions & Warnings

Effects on skeletal muscle (e.g., myopathy and rhabdomyolysis): Usage of the 40 mg dose, advanced age (>65 years), hypothyroidism, renal impairment, and use of cyclosporine, lopinavir/ritonavir, atazanavir/ritonavir, or certain other lipid-lowering medicines all enhance the risks. Patients should be encouraged to report any unexplained muscle discomfort, soreness, or weakness as soon as possible. If indications or symptoms arise, rosuvastatin can be stopped.

Abnormalities in liver enzymes and monitoring: Hepatic transaminases might be persistently elevated. Before and during treatment, liver enzymes should be checked.

 

Therapeutic Class

Other Anti-anginal & Anti-ischaemic drugs, Statins

 

Storage Conditions

Keep below 30oC temperature, protected from light & moisture. Keep out of the reach of children.

 

Pharmaceutical Name

Opsonin Pharma Ltd.