RiteMed Rosuvastatin

Rosuvastatin calcium.

A pink, round, film-coated tablet.
10 mg: Each film-coated tablet contains: Rosuvastatin (as calcium) 10.4 mg (as Rosuvastatin 10 mg).
20 mg: Each film-coated tablet contains: Rosuvastatin (as calcium) 20.8 mg (as Rosuvastatin 20 mg).

HMG-CoA Reductase Inhibitor.
Pharmacology: Pharmacodynamics: Pharmacodynamics Rosuvastatin 20mg Film-Coated Tablet is a selective and competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, a precursor of cholesterol. Studies in animals, and studies in cultured animal and human cells have known Rosuvastatin to have a high uptake into, and selectively for, action in the liver, the target organ for cholesterol lowering. In studies, Rosuvastatin produces its lipid-modifying effects in two ways. First, it increases the number of hepatic LDL (low-density lipoprotein) receptors on the cell-surface to enhance uptake and catabolism of LDL. Second, Rosuvastatin inhibits hepatic synthesis of VLDL (very low-density lipoprotein), which reduces the total number of VLDL and LDL particles.
Pharmacokinetics: Absorption: In clinical pharmacology studies in man, peak plasma concentrations of Rosuvastatin were reached 3 to 5 hours following oral dosing. The absolute bioavailability of Rosuvastatin is approximately 20%.
Distribution: Mean volume of distribution at steady-state of Rosuvastatin is approximately 134 liters.
Metabolism: Rosuvastatin is not extensively metabolized; approximately 10% of a radiolabeled dose is recovered as metabolite. The major metabolite is N-desmethyl rosuvastatin, which is formed principally by cytochrome P450/2C9.
Excretion: Following oral administration, Rosuvastatin and its metabolites are primarily excreted in the feces (90%). The elimination half-life (t1/2) of Rosuvastatin is approximately 19 hours. After an intravenous dose, approximately 28% of the total body clearance was via the renal route, and 72% by the hepatic route.
20 mg: Distribution: Rosuvastatin is 88% bound to plasma proteins, mostly albumin. This binding is reversible and independent of plasma concentrations.

Rosuvastatin 10 mg and 20 mg Film-Coated Tablet is indicated for: Adult patients with primary hyperlipidemia (including heterozygous familial hypercholesterolemia (Type IIa) or Mixed dyslipidemia (Type IIb) as an adjunct to diet and to reduce elevated total-C (cholesterol), LDL-C (Low-density lipoprotein - cholesterol), ApoB (Apolipoprotein B), non HDL-C (non high-density lipoprotein-cholesterol) and TG (Triglycerides) levels and to increase HDL-C (High-Density lipoprotein - cholesterol).
Homozygous familial hypercholesterolemia.
Reducing the risk of atherosclerosis by lowering total cholesterol levels and LDL (low-density lipoprotein) cholesterol levels.
Heterozygous familial hypercholesterolemia.
Primary dysbetalipoproteinemia (Type III).
Reducing the risk of cardiovascular diseases.

Primary hyperlipidemia including heterozygous familial hypercholesterolemia (Type IIa), Mixed dyslipidemia (Type IIb), Primary dysbetalipoproteinemia (Type III) and Homozygous familial hypercholesterolemia: Usual Starting Dose: 5 mg once daily.
Recommended Maintain Dose: 20 mg once daily.
Maximum Dose: 40 mg once daily.
Heterozygous familial hypercholesterolemia (10-17 years): Usual Dose: 5 mg once daily.
Maximum Dose: 20 mg once daily.
Over 70 years old: 10 mg once daily.
Under 10 years old: Do not take Rosuvastatin 10 mg or 20 mg Film-Coated Tablet. (It is not established the safety and effectiveness of use for children yet.)
Patient who has renal failure: A mild and moderate renal failure: 10 mg-20 mg once daily.
Severe renal failure: Do not take Rosuvastatin 10 mg or 20 mg Film-Coated Tablet.
Patient who has liver failure: Do not take Rosuvastatin 10 mg or 20 mg Film-Coated Tablet.
Asian: Recommended Starting Dose: 5 mg once daily.
Patient who has myopathy: Recommended Starting Dose: 5 mg once daily.
Do not take 40 mg of Rosuvastatin daily.
Administration: Swallow each tablet whole with a drink of water at any time of the day and regardless of food intake.
Missed Dose: Do not take a double dose to make up for the missed dose instead, take the next scheduled dose at the correct time.

There is no specific treatment in the event of overdose. In the event of overdose, the patient should be treated symptomatically and supportive measures instituted as required.
Hemodialysis does not significantly enhance clearance of Rosuvastatin.

Active liver disease including unexplained persistent elevations of hepatic transaminase levels, women who are pregnant or may become pregnant, nursing mothers.

Should not be treated the following patients: Patients who have hypersensitivity to Rosuvastatin calcium or the ingredients contained in Rosuvastatin 10 mg or 20 mg Film-Coated Tablet; Pregnant or breast-feeding; Patients who have liver disease; Patients who have severe kidney problems; Patients who have repeated or unexplained muscle aches or pains; The highest dose 40 mg for a drug called Cyclosporine.
Should not take Rosuvastatin 40 mg (the highest dose): Patient who have moderate kidney problems; Patient who have problems in thyroid gland; Patient who have repeated or unexplained muscle aches or pains, a personal or family history of muscle problems, or a previous history of muscle problems when taking other cholesterol-lowering medicines; Patient who drink large amount of alcohol; Asian origin (Korea, Chinese, Japan, Filipino, Vietnamese, Indian); Patients who take other medicines called fibrates to lower cholesterol.
Should take Rosuvastatin 10 mg or 20 mg Film-Coated Tablet carefully: Patients who have problem in kidneys; Patients who have problems in liver; Patients who have repeated or unexplained muscle aches or pains should talk to the doctor or pharmacist before taking Rosuvastatin 10 mg or 20 mg Film-Coated Tablet. A personal or family history of muscle problems, or a previous history of muscle problems when taking other cholesterol-lowering medicines. Tell the doctor immediately if the patient has unexpected muscle aches or pains especially if the patient feels unwell or have a fever. Also tell the doctor or pharmacist if the patient has a muscle weakness that is constant; Patients who drink large amount of alcohol; Patients who have problems in thyroid gland; Patients who take other medicines called fibrates to lower cholesterol; Patients who take medicines used to treat HIV infection.

Pregnancy Category (US FDA)-X.
Do not take Rosuvastatin 10 mg or 20 mg Film-Coated Tablet if the patient is pregnant or breast-feeding. If the patient become pregnant while taking Rosuvastatin 10 mg or 20 mg Film-Coated Tablet, stop taking it immediately and tell the doctor.

Allergic reactions: Difficulty in breathing, with or without swelling of the face, lips, tongue and/or throat; Swelling of the face, lips, tongue and/or throat, which may cause difficulty in swallowing; Severe itching of the skin (with raised lumps).
Any unusual aches or pains in the muscles which go on for longer than might expected: Stop taking Rosuvastatin 10 mg or 20 mg Film-Coated Tablet and talk to the doctor immediately. It may be more common in children and adolescents than in adults.
Common possible side effects (these may affect between 1 in 10 and 1 in 100 patients): Headache; Stomach pain; Constipation; Feeling sick; Muscle pain; Feeling weak; Dizziness; An increase in the amount of protein in the urine (This usually returns to normal on its own without having to stop taking Rosuvastatin 10 mg or 20 mg Film-Coated Tablet); Diabetes (This is more likely if the patient has high levels of sugars and fats in the blood, are overweight and have high blood pressure. The doctor will monitor while the patient is taking this medicine).
Uncommon possible side effects (these may affect between 1 in 100 and 1 in 1,000 patients): Rash, itching or other skin reactions; An increase in the amount of protein in the urine. (This usually returns to normal on its own without having to stop taking Rosuvastatin 10 mg or 20 mg Film-Coated Tablet).
Rare possible side effects (These may affect between 1 in 1,000 and 1 in 10,000 patients): Severe allergic reaction (signs include swelling of the face, lips, tongue and/or throat, difficulty in swallowing and breathing, a severe itching of the skin (with raised lumps). If the patient thinks of having an allergic reaction, then stop taking Rosuvastatin 10 mg or 20 mg Film-Coated Tablet and seek medical help immediately); Muscle damage in adults (as a precaution, stop taking Rosuvastatin 10 mg or 20 mg Film-Coated Tablet and talk to the doctor immediately if the patient is having any unusual aches or pains in the muscles which go on for longer than expected); A severe stomach pain (inflamed pancreas); Increase in liver enzymes in blood.
Very rare possible side effects (these may affect less than 1 in 10,000 patients): Jaundice (yellowing of the skin and eyes); Hepatitis (an inflamed liver); Traces of blood in the urine; Damage to the nerves of legs and arms (such as numbness); Joint pain; Memory loss; Breast enlargement in men (gynecomastia).
Side effects of unknown frequency may include: Diarrhea (loose stools); Stevens-Johnson syndrome (serious blistering condition of the skin, mouth, eyes and genitals); Cough; Shortness of breath; Edema (swelling); Sleep disturbances, including insomnia and nightmares; Sexual difficulties; Depression; Breathing problems, including persistent cough and/or shortness of breath or fever; Tendon injury; Muscle weakness that is constant.

Increased risk of myopathy with some other lipid-lowering therapies (fibrates or niacin), gemfibrozil, cyclosporine, lopinavir/ritonavir, atazanavir/ritonavir, organic anion transporting polyprotein 1B1 inhibitors, or breast cancer resistance protein inhibitors. Avoid with gemfibrozil. Caution with coumarin anticoagulants; determine INR before initiation and frequently during early therapy. May enhance the risk of skeletal muscle effects with ≥1 g/day of niacin. Caution with drugs that may decrease levels or activity of endogenous steroid hormones (ex, ketoconazole, spironolactone, cimetidine), fenofibrates, or protease inhibitors in combination with ritonavir. Cyclosporine may increase levels. Caution with colchicine; cases of myopathy, including rhabdomyolysis, reported.

Store at temperatures not exceeding 30°C.

Dyslipidaemic Agents

C10AA07 - rosuvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.

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