Rosuvastatin
Rosuvastatin is in a group of drugs called HMG CoA reductase inhibitors. Rosuvastatin is used in adults and children who are at least 8 years old, to lower cholesterol and triglycerides (types of fat) in the blood and to slow the build-up of plaque (fatty deposits) in blood vessels.
Rosuvastatin is also used to lower the risk of stroke, heart attack, and other heart complications in certain people with diabetes, coronary heart disease, or other risk factors.
Rosuvastatin is also used to treat hereditary forms of high cholesterol, including the heterozygous type (inherited from one parent) and the homozygous type (inherited from both parents). For the heterozygous type, rosuvastatin can be used in children who are at least 8 years old. For the homozygous type, rosuvastatin can be used in children as young as 7 years old.
Mechanism of effect
Rosuvastatin is a selective and competitive inhibitor of HMG - CoA reductase
Pharmacodynamic
Rosuvastatin calcium is a synthetic lipid-lowering agent for oral administration.
Pharmacokinetics
peak plasma concentrations of rosuvastatin were reached 3 to 5 hours following oral dosing.
The absolute bioavailability of rosuvastatin is approximately 20%.
Rosuvastatin is 88% bound to plasma proteins, mostly albumin Rosuvastatin is not extensively metabolized; approximately 10% of a radiolabeled dose is recovered as metaboliteprimarily excreted in the feces (90%).
The elimination half-life (t1/2) of rosuvastatin is approximately 19 hours.
Drug indications
Hyperlipidemia , Heterozygous Familial Hypercholesterolemia , Homozygous Familial Hypercholesterolemia , Hypertriglyceridemia , AtherosclerosisDosage
Usual Adult Dose for Hyperlipidemia
Initial dose: 10 mg to 20 mg orally once a day
Maintenance dose: 5 mg to 40 mg orally once a day
Usual Pediatric Dose for Homozygous Familial Hypercholesterolemia
7 to 17 years: 20 mg orally once a day
Usual Pediatric Dose for Heterozygous Familial Hypercholesterolemia
8 to less than 10 years: 5 mg to 10 mg orally once a day; safety and efficacy of doses greater than 10 mg/day have not been studied
10 to 17 years: 5 mg to 20 mg orally once a day; safety and efficacy of doses greater than 20 mg/day have not been studied
Drug contraindications
Pregnancy , Lactation , hypersensitivity to drug or its components. , Active liver diseaseSide effects
nausea , Headache , constipation , abdominal pain , asthenia , myalgia , Increased ALT , Increased AST , diabetes mellitusInteractions
Digoxin , MG , Aluminium MG+simeticone , Aluminium MGS , Aluminium gel , Bosentan , Gemfibrozil , nelfinavir , Daptomycin , Magnesium hydroxide , Eltrombopag , Sofosbuvir and velpatasvir , Contraceptive HD , Contraceptive LD , ledipasvir and sofosbuvir , Darunavir , Ethinyl Estradiol , ritonavir , Diltiazem , Cyclosporine , Warfarin , Verapamil , Contraceptive , Contraceptive DE , triparanol , Metaxalone , Darolutamide , ELBASVIR/GRAZOPREVIR , Nilutamide , MethyclothiazideAlerts
1-For patients with severe renal impairment (CLcr less than 30 mL/min/1.73 m2) not on hemodialysis, dosing of rosuvastatin calcium tablets should be started at 5 mg once daily and not exceed 10 mg once daily
2-Rosuvastatin should be prescribed with caution in patients with predisposing factors for myopathy (e.g., age greater than or equal to 65 years, inadequately treated hypothyroidism, renal impairment).
Points of recommendation
1-All patients should be advised to promptly report to their physician unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever or if muscle signs and symptoms persist after discontinuing rosuvastatin
2-It is recommended that liver enzyme tests be performed before the initiation of rosuvastatin, and if signs or symptoms of liver injury occur.
3-May be taken orally once a day at any time; swallow whole with or without food
4-If antacids are needed, take antacids at least 2 hours after taking this drug.
5-This drug should be used in addition to a diet restricted in saturated fat and cholesterol when response to diet and nonpharmacologic interventions alone has been inadequate.
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