ROSUCARD

Each film coated tablets contains:

(Rosuvastatin Calcium IP equivalent to Rosuvastatin 5 mg / 10 mg / 20 mg)

Tablet for Oral Use

Rosuvastatin is a statin medication and a competitive inhibitor of the enzyme HMG-CoA (3-hydroxy-3-methylglutaryl coenzyme A) reductase, which catalyzes the conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol biosynthesis. Hepatocytes respond to this decreased intracellular cholesterol concentration by increased synthesis of LDL receptors to enhance hepatic LDL reuptake from the circulation. The net result of this process is an increased fractional catabolism of LDL which reduces serum LDL-C concentration and total cholesterol. Rosuvastatin also inhibits hepatic synthesis of very low density lipoprotein (VLDL). The overall effect is a decrease in plasma LDL and VLDL.

Absorption: The absolute oral bioavailability of Rosuvastatin was found to be approximately 20% while absorption was estimated to be 50%, which is consistent with a substantial first-pass effect after oral dosing

Distribution: The mean volume of distribution at steady-state of Rosuvastatin is approximately 134 litres.

Plasma Binding: Rosuvastatin is 88% bound to plasma proteins, mostly albumin. This binding is reversible and independent of plasma concentration.

Metabolism: Rosuvastatin is not extensively metabolized; approximately 10% of a radiolabeled dose is recovered as metabolite. Following oral administration, Rosuvastatin and its metabolites are primarily excreted in the feces (90%). After an intravenous dose, approximately 28% of total body clearance was via the renal route, and 72% by the hepatic route.

Half Life: Rosuvastatin has a plasma half-life of 19 hours 

• Homozygous familial hypercholesterolemia
• Heterozygous familial hypercholesterolemia
• Hyperlipidemia, Mixed dyslipidemia , Primary dysbetalipoproteinemia, Hypertriglyceridemia
• Prevention of cardiovascular disease.

ADVERSE REACTION Creatinine kinase of greater than ten times the upper limit of normal, Severe myopathy, Rhabdomyolysis, AST or ALT elevations of greater than three times the upper limit of normal, Renal failure

• Rare adverse effects include diabetes mellitus, hematuria, proteinuria, and hypersensitivity.
• Other reported symptomatic adverse effects include headache, dizziness, nausea, constipation, interstitial cystitis, arthralgia, and weakness.

DOSAGE AND ADMINISTRATION:

For atherosclerosis: 5 to 40 milligrams (mg) once a day.

For heterozygous familial hypercholesterolemia:

• Adults—5 to 40 milligrams (mg) once a day.
• Children 10 to 17 years of age—5 to 20 mg per day.
• Children 8 to 9 years of age—5 to 10 mg per day.

For homozygous familial hypercholesterolemia:

• Adults- At first, 20 milligrams (mg) once a day.
• Children 7 to 17 years of age—20 mg once a day.
• Children younger than 7 years of age—Use and dose must be determined by your doctor.

CONTRAINDICATIONS: Hypersensitivity to Rosuvastatin, Pregnancy (pregnancy category X): There are reports of congenital abnormalities Breastfeeding, Active liver disease

Unexplained persistent elevations of serum transaminases

WARNINGS AND PRECAUTIONS: Rosuvastatin therapy should be discontinued if markedly elevated creatine kinase levels occur or myopathy is diagnosed or suspected.

It is recommended that liver enzyme tests be performed before the initiation of Rosuvastatin calcium tablets, and if signs or symptoms of liver injury occur.

Caution should be exercised when anticoagulants are given in conjunction with Rosuvastatin 

Pregnancy Category: X. There are reports of congenital anomalies

Drug Interaction: The following medications may enhance the myopathic effect of Rosuvastatin: acipimox, bezafibrate, ciprofibrate, colchicine, daptomycin, fenofibrate, fusidic acid, gemfibrozil, niacin, niacinamide, raltegravir, red yeast rice, rupatadine.The following medications may decrease the serum concentration of Rosuvastatin: antacids, apalutamide, elagolix, eslicarbazepine.The following medications may increase the serum concentrations of Rosuvastatin: asunaprevir, clopidogrel, cobicistat, cyclosporine, daclatasvir, dasabuvir, dronedarone, elbasvir, eltrombopag, eluxadoline, fostamatinib, glecaprevir, pibrentasvir, grazoprevir, itraconazole, ledipasvir, letermovir, ombitasvir, paritaprevir, ritonavir, osimertinib, protease inhibitors, simeprevir, teriflunomide, velpatasvir, voxilaprevir.