Starez

Starez

rosuvastatin

Manufacturer:

Stadpharm

Distributor:

Stadpharm
Full Prescribing Info
Contents
Rosuvastatin calcium.
Description
One Starez 10 tablet contains 10 mg of rosuvastatin (as rosuvastatin calcium 10.4 mg).
Action
Pharmacology: Pharmacodynamics: Rosuvastatin 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. In vivo studies in animals, and in vitro studies in cultured animal and human cells have shown rosuvastatin to have a high uptake into, and selectivity for, action in the liver, the target organ for cholesterol lowering. In in vivo and in vitro studies, rosuvastatin produces its lipid-modifying effects in two ways. First, it increases the number of hepatic LDL receptors on the cell-surface to enhance uptake and catabolism of LDL. Second, rosuvastatin inhibits hepatic synthesis of VLDL, which reduces the total number of VLDL and LDL particles.
Pharmacokinetics: Rosuvastatin is incompletely absorbed from the gastro-intestinal tract, with a bioavailability of about 20%. Peak plasma concentrations are achieved about 5 hours after an oral dose. It is taken up extensively by the liver, its primary site of action, and undergoes limited metabolism, mainly by the cytochrom P450 isoenzym CYP2C9. It is about 90% bound to plasma proteins. The plasma elimination half-life of rosuvastatin is about 19 hours. About 90% of an oral dose of rosuvastatin is excreted in the faeces, including absorbed and nonabsorbed drug, and the remainder is excreted in the urine; about 5% of a dose is excreted unchanged in the urine.
Indications/Uses
Rosuvastatin is used to reduce LDL cholesterol, apolipoprotein B, and to increase HDL cholesterol in the management of hyperlipidaemias, including primary hypercholesterolaemia (type IIa), mixed dyslipidaemia (type IIb).
Dosage/Direction for Use
Administration: The patient should be placed on a standard cholesterol-lowering diet before receiving rosuvastatin and should continue on this diet during treatment.
Rosuvastatin is administered orally as a single dose at any time of day, with or without food.
Dosage: Primary Hypercholesterolemia and Mixed Dyslipidemia: The usual initial dosage of rosuvastatin in adults is 10 mg once daily given without regard to meals.
Initiation of therapy with 5 mg once daily may be considered for patients requiring less aggressive LDL-cholesterol reductions, patients who have predisposing factors for myopathy, or patients who are at risk of increased exposure to rosuvastatin.
For patients with marked hypercholesterolemia and aggressive lipid targets, an initial rosuvastatin dosage of 20 mg once daily may be considered.
Dosage may be increased as necessary to a maximum recommended dosage of 40 mg daily. The 40-mg daily dosage of rosuvastatin should be reserved for those patients who have not achieved their LDL-cholesterol goal with the 20-mg daily dosage.
Asian Patients: The manufacturer recommends an initial rosuvastatin dosage of 5 mg once daily in Asian patients.
Renal Impairment: The usual dose range applies in patients with mild to moderate renal impairment. The use of rosuvastatin in patients with severe renal impairment is contraindicated.
Patients with pre-disposing factors to myopathy: The recommended start dose is 5 mg in patients with pre-disposing factors to myopathy.
Concomitant therapy: Rosuvastatin is a substrate of various transporter proteins (e.g. OATP1B1 and BCRP). The risk of myopathy (including rhabdomyolysis) is increased when rosuvastatin is administered concomitantly with certain medicinal products that may increase the plasma concentration of rosuvastatin due to interactions with these transporter proteins (e.g. certain protease inhibitors including combinations of ritonavir with atazanavir, lopinavir, and/or tipanavir). Whenever possible, alternative medications should be considered, and if necessary, consider temporarily discontinuing Starez 10 mg therapy. In situations where co-administration of these medicinal products with rosuvastatin is unavoidable, the benefit and the risk of concurent treatment and rosuvastatin dosing adjustments should be carefully considered.
Overdosage
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.
Contraindications
Known hypersensitivity to rosuvastatin or any ingredient in the formulation.
Active liver disease or unexplained, persistent increases in serum aminotransferase concentrations.
All statins are contraindicated in pregnant or nursing women.
Starez 10 is contraindicated in patients receiving concomitant cyclosporine.
Special Precautions
Fetal/Neonatal Morbidity and Mortality: If the patient becomes pregnant while taking the drug, discontinue therapy and apprise the patient of the potential hazard to the fetus.
Hepatic Effects: Therapy with rosuvastatin and other statins has been associated with increases in serum aminotransferase (transaminase) concentrations (i.e., AST [SGOT], ALT [SGPT]). Liver function tests be performed before and at 12 weeks after initiation of rosuvastatin therapy or any increase in dosage and periodically (e.g., semiannually) thereafter.
Musculoskeletal Effects: Myopathy (manifested as muscle pain, tenderness, or weakness and increases in serum creatinine kinase [CK] concentration exceeding 10 times the upper limit of normal) has been reported occasionally (up to 0.1 %) with rosuvastatin therapy.
Gemfibrozil increases the risk of myopathy when given concomitantly with some HMG-CoA reductase inhibitors. Therefore, the combination of rosuvastatin and gemfibrozil is not recommended. The benefit of further alteration in lipid levels by the combined use of rosuvastatin with fibrates or niacin should be carefully weighed against the potential risks of such combinations.
General Precautions: Prior to institution of antilipemic therapy, vigorously attempt to control serum cholesterol by appropriate dietary regimens, weight reduction, exercise, and treatment of any underlying disorder that might be the cause of lipid abnormality.
Asian Populations: Pharmacokinetic studies, including a large study conducted in the US, show an approximate twofold elevation in median exposure to rosuvastatin (peak plasma concentration and AUC) in Asian patients.
Immune-mediated necrotizing myopathy (IMNM): There have been very rare reports of an IMNM during or after treatment with some statins. IMNM is clinically characterized by: Persistent proximal muscle weakness and elevated serum creatinine kinase, which persist despite discontinuation of statin treatment;
Muscle biopsy showing necrotizing myopathy without significant inflammation;
Improvement with immunosuppressive agents.
Use In Pregnancy & Lactation
Pregnancy: Rosuvastatin is contraindicated in women who are or may become pregnant.
Rosuvastatin may cause fetal harm when administered to a pregnant woman. If the patient becomes pregnant while taking Rosuvastatin, the patient should be apprised of the potential risks to the fetus and the lack of known clinical benefit with continued use during pregnancy.
Lactation: Distributed into milk in animals; not known whether rosuvastatin is distributed into milk in humans.
Discontinue nursing or drug, taking into account the importance of the drug to the woman.
Adverse Reactions
The most frequent adverse effects thought to be related to rosuvastatin include myalgia, constipation, asthenia, abdominal pain, and nausea. Adverse effects reported without attribution of causality in at least 2% of patients receiving rosuvastatin include pharyngitis, headache, diarrhea, dyspepsia, nausea, myalgia, asthenia, back pain, flu syndrome, urinary tract infection, rhinitis, and sinusitis.
There have been rare post-marketing reports of cognitive impairment (e.g. memory loss, forgetfulness, amnesia, memory impairment, confusion) associated with statin use. These cognitive issues have been reported for all statins. The reports are generally non-serious and reversible upon statin discontinuation, with variable times to symptom onset (1 day to years) and symptom resolution (median 3 weeks).
Increases in HbA1c and fasting blood glucose have been reported with statins. The risk of hyperglycemia, however, is outweighed by the reduction in vascular risk with statins.
Musculoskeletal disorders: Frequency not known: Immune-mediated necrotizing myopathy.
Drug Interactions
Concurrent use of fibrates may cause severe myositis and myoglobinuria.
Gemfibrozil, fibrate and niacin: Gemfibrozil increases the risk of myopathy when given concomitantly with some HMG-CoA reductase inhibitors. Therefore, the combination of rosuvastatin and gemfibrozil is not recommended. The benefit of further alteration in lipid levels by the combined use of rosuvastatin with fibrates or niacin should be carefully weighed against the potential risks of such combinations.
Certain protease inhibitors: Rosuvastatin is a substrate of various transporter proteins (e.g. OATP1B1 and BCRP). The risk of myopathy (including rhabdomyolysis) is increased when rosuvastatin is administered concomitantly with certain medicinal products that may increase the plasma concentration of rosuvastatin due to interactions with these transporter proteins (e.g. certain protease inhibitors including combinations of ritonavir with atazanavir, lopinavir, and/or tipanavir). Whenever possible, alternative medications should be considered, and if necessary, consider temporarily discontinuing Starez 10 therapy. In situations where co-administration of these medicinal products with rosuvastatin is unavoidable, the benefit and the risk of concurent treatment and rosuvastatin dosing adjustments should be carefully considered.
Coumarin Anticoagulants: In patients taking coumarin anticoagulants with Rosuvastatin concomitantly, INR should be determined before starting Rosuvastatin and frequently enough during early therapy to ensure that no significant alteration of INR occurs.
Niacin: The risk of skeletal muscle effects may be enhanced when Rosuvastatin is used in combination with niacin, a reduction in Rosuvastatin dosage should be considered in this setting.
Storage
Do not store above 30°C.
ATC Classification
C10AA07 - rosuvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.
Presentation/Packing
FC tab 10 mg (light red, round-shaped, biconvex, breakable line on one side and plain on the other side) x 30's.
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