Prpmsrosuvastatin rosuvastatin calcium tablets 5 mg, 10 mg, 20 mg and 40 mg rosuvastatin as rosuvastatin calcium lipid metabolism regulator pharmascience inc. The active substance is a white powder which shows no polymorphism. Keywords rosuvastatin calcium, superdisintegrants, crospovidone, sodium starch glycolate, kyron t314, patient compliance. The british national formulary lists 5 statins available for use in the uk. Rosuvastatin is an inhibitor of 3hydroxy3methylglutarylcoenzyme a hmgcoa reductase. When diet and exercise alone arent enough to lower cholesterol, adding crestor can help. Princeton, new jersey, july 21, 2016 sandoz today announced the u. This study assessed the metabolism, excretion, and pharmacokinetics of a single oral dose of radiolabeled rosuvastatin 14 crosuvastatin in healthy volunteers. Active liver disease, including unexplained, persistent elevations of hepatic aminotransferases. Formulation and in vitro evaluation of rosuvastatin calcium niosomes article pdf available in international journal of pharmacy and pharmaceutical sciences 5suppl 4. Crestor rosuvastatin calcium dose, indications, adverse. Rosuvastatin was seen to lower ldlc by 50% and hscrp by 37%.
Rosuvastatin is a 3hydroxy3methylglutaryl coenzyme areductase inhibitor, or statin, that has been developed for the treatment of dyslipidemia. Accidental release measures contain spill and collect, as appropriate. There can be risks and side effects for taking rosuvastatin, so it is important to have all of the facts before taking. Rosuvastatin calcium usp is a white amorphous powder that is sparingly soluble in water and methanol, and slightly soluble in ethanol. Rosuvastatin is available as the brandname drug crestor.
The objective of this study is to confirm if two formulations of rosuvastatin calcium 20 mg tablets are bioequivalent. This binding is reversible and independent of plasma concentrations. Formulation and evaluation of rosuvastatin immediate. These interactions can cause your body to metabolize the medicines differently than intended, increase the risk of muscle problems, and cause significant reactions, among other things.
Antacidspabsorption administer 2 hr after rosuvastatin. Rosuvastatin selectively and competitively binds to and inhibits hepatic hydroxymethylglutaryl coenzyme a reductase, the enzyme which catalyzes the conversion of hmgcoa to mevalonate, a precursor of cholesterol. Rosuvastatin is a new generation hmgcoa reductase inhibitor which exhibits some unique pharmacologic and pharmacokinetic properties. Rosuvastatin information, calcium, side effects, dosage. It is a drug prescribed most commonly to fight high cholesterol, that is often advised to combine with a newimproved healthy diet and exercise program. Rosuvastatin calcium is antilipemic and is used to reduce plasma cholesterol levels and prevent cardiovascular disease. Transfer a number of tablets per table 1 into a suitable extraction flask. Rosuvastatin calcium is a white to offwhite powder that is soluble in dimethyl formamide, dimethyl sulpboxide, acetonitrile and acetone, slightly soluble in water and methanol.
Rosuvastatin is used along with a proper diet to help lower bad cholesterol and fats such as ldl, triglycerides and raise good cholesterol hdl in the blood. Industriel september 27, 2016 laval, quebec h7l 3w9 control no 198363. Rosuvastatin is 88% bound to plasma proteins, mostly albumin. Antilipemic pregnancy risk category x action selectively and competitively inhibits hmgcoa reductase, which catalyzes its conversion to the cholesterol precursor mevalonate and thus limits cholesterol synthesis. Crestor rosuvastatin calcium tablets prescribing information. Comparison of effects on lowdensity lipoprotein cholesterol and highdensity lipoprotein cholesterol with rosuvastatin versus atorvastatin in patients with type iia or iib hypercholesterolemia. It has a role as an antiinflammatory agent, a cetp inhibitor and a cardioprotective agent.
The usual initial dose of rosuvastatin is 5 or 10 mg once daily, depending on plasmacholesterol concentrations, cardiovascular risk factors, and risk factors for adverse. Rosuvastatin calcium rs and rosuvastatin diastereomers prepared by mixing system suitability stock solution and diluent 1. Rosuvastatin calcium which chemical name is bis e744fluorophenyl6isopropyl2methylmethylsulfonylaminopyrimidin5. The empirical formula for rosuvastatin calcium usp is c 22 h 27 fn 3 o 6 s 2 ca and the molecular weight is 1001. The empirical formula for rosuvastatin calcium is c22h27fn3o6s2ca. Dosage and administration, hefh in pediatric patients 10 to 17 years of age 2. Rosuvastatin selectively and competitively binds to and inhibits hepatic hydroxymethylglutaryl coenzyme a hmgcoa reductase, the enzyme which catalyzes the conversion of hmgcoa to mevalonate, a precursor of cholesterol. Muscle problems, including muscle breakdown, can be serious in some people and rarely cause kidney damage that can lead to death. Pr ipgrosuvastatin rosuvastatin calcium tablets 5mg, 10mg, 20mg and 40 mg rosuvastatin as rosuvastatin calcium lipid metabolism regulator marcan pharmaceuticals inc. A precise, accurate, specific, linear, rugged and robust analytical method was developed and validated for estimation of process and degradant impurities of rosuvastatin calcium rsc in rosuvastatin calcium tablets. Rosuvastatin calcium is an organic calcium salt that is the hemicalcium salt of rosuvastatin. Other drugs that have the same active ingredients e. Known hypersensitivity to rosuvastatin or any ingredient in the formulation.
This enzyme catalyzes the conversion of hmgcoa to mevalonate, an early and ratelimiting step in cholesterol biosynthesis. Rosuvastatin is a statin with antilipidemic and potential antineoplastic activities. This leads to a decrease in hepatic cholesterol levels and increase in uptake of ldl. Unlike a number of other statins, rosuvastatin calcium is not metabolized significantly by cytochrome p450 3a4, the major cytochrome p450 involved in drug metabolism, and. Rosuvastatin calcium definition of rosuvastatin calcium. Rosuvastatin, pitavastatin, and simvastatin are not affected by food, whereas. Rosuvastatin is given orally as the calcium salt, although doses are expressed in terms of the base. The following adverse reactions have been identified during postapproval use of rosuvastatin calcium. Advise patient that these symptoms may represent druginduced myopathy, and that myopathy can progress to severe muscle damage rhabdomyolysis. It comes in the form of a tablet you take by mouth. Test formulation is rosuvastatin calcium 20 mg tablets manufactured by laboratorios phoenix s.
Crestor filmcoated tablets contain 5 mg, 10 mg, 20 mg and 40 mg of rosuvastatin as calcium. There was significant benefit observed in the rosuvastatin group with regards the combined primary endpoint relative risk reduction 44% and its individual components. Their plasma concentrations are increased by inhibitors of cyp3a4 such as itraconazole. Rosuvastatin 5 and 10 mg were associated with improved achievement in atp ii 84% in both rosuvastatin groups vs 73% and atp iii 84% and 82% vs 72% ldl cholesterol goals, and rosuvastatin 10 mg. Rosuvastatin calcium is a competitive inhibitor of hydroxymethylglutarylcoe nzyme a hmgcoa reductase, the enzyme that catalyzes the conversion of hmgcoa to mevalonic acid, the ratelimiting step in cholesterol biosynthesis. Manufacture synthesis routes for the manufacturing of rosuvastatin calcium are presented. Rosuvastatin calcium is the calcium salt form of rosuvastatin, a statin with antilipidemic activity. Drug interactions with rosuvastatin gemfibrozil, ketoconazole, and birth control pills are among the medications that can cause rosuvastatin drug interactions. Pdf formulation and in vitro evaluation of rosuvastatin. The study is based on amlodipine besylate and rosuvastatin calcium the active ingredients of amlodipine besylate and rosuvastatin calcium, respectively, and amlodipine besylate and rosuvastatin calcium the brand names.
It has low extrahepatic tissue penetration, low potential for cyp3a4 interactions and substantial ldlc lowering capacity and therefore has distinct advantages. Side effects of crestor what are the possible side effects of crestor. Nominally 1 mgml of rosuvastatin prepared as follows. Rosuvastatin calcium is an amorphous solid, which is slightly soluble in water 7. Detailed information is present regarding nomenclature, structural and molecular formulas and molecular mass. Statins are rapidly absorbed following administration and excepting. Rosuvastatin is less likely to cause metabolic drug to drug interactions since it has limited metabolism by cyp isoenzymes. It is an organic calcium salt and a nacyl15methylhexadecasphinganine1phosphoethanolamine. Assess any joint pain or muscle pain, tenderness, or weakness, especially if accompanied by fever, malaise, and darkcolored urine.
Structural identification and estimation of rosuvastatin. If the suffix psy, narc or drug precursor, or motbiotox appears, export authorizations are mandatory in. All of them were previously treated with acei, arb or calcium channel blockers. Statins are moderately to well absorbed, with the time to reach peak plasma concentration averaging about 4 hours. In adults, crestor is prescribed along with diet to lower high cholesterol and to slow plaque buildup in arteries as part of a treatment plan to lower cholesterol to goal. Rosuvastatin appears to be metabolized to a limited extent to an ndesmethyl metabolite 7fold less potent than rosuvastatin and a 5slactone product. Methods and material for containment and cleaning up. Rosuvastatin calcium is also commonly known by its brand name, crestor. In patients with active liver disease or unexplained persistent elevations of serum transaminases exceeding 3 times the upper limit of normal see warnings and. As they were hypercholesterolemic, they were allocated to receive either dietary therapy or a dose of 10 mg. Introduction the need for new oral drug delivery system continues, due to poor patient acceptance for invasive methods, need for exploration of new market for drugs and coupled with high cost of disease.
The empirical formula for rosuvastatin calcium is c 22 h 27 fn 3 o 6 s 2 ca and the molecular weight is 1001. Rosuvastatin sandoz 40 mg tablets contain 40 mg rosuvastatin as calcium. Other hmgcoa reductase inhibitors such as atorvastatin and simvastatin are metabolised via cyp3a4. Prescribing information with patient information pdf 152k. Transfer to a chemical waste container for disposal in accordance with local regulations. Side effects of rosuvastatin calcium tablets rosuvastatin.
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