rosuvastatin calcium


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rosuvastatin calcium

Crestor

Pharmacologic class: HMG-CoA reductase inhibitor

Therapeutic class: Antilipemic

Pregnancy risk category X

Action

Selectively and competitively inhibits HMG-CoA reductase, which catalyzes its conversion to the cholesterol precursor mevalonate and thus limits cholesterol synthesis. This action increases high-density lipoprotein level and decreases low-density lipoprotein (LDL) level.

Availability

Tablets: 5 mg, 10 mg, 20 mg, 40 mg

Indications and dosages

Primary prevention of cardiovascular disease; adjunct to diet for hyperlipidemia, mixed dyslipidemia, hypertriglyceridemia, primary dysbetalipoproteinemia (type III hyperlipoproteinemia); slowing of progression of atherosclerosis

Adults: 5 to 40 mg P.O. daily. Use 40-mg dose only for patients not reaching LDL-C goal with 20 mg.

Homozygous familial hypercholesterolemia

Adults: 20 mg/day P.O. daily. (Response to therapy should be estimated from preapheresis LDL-C levels.).

Heterozygous familial hypercholesterolemia after failure of an adequate trial of diet therapy

Children ages 10 to 17: 5 to 20 mg P.O. daily. Maximum recommended dosage is 20 mg/day. Individualize dosages according to recommended goal of therapy. Make adjustments at intervals of 4 weeks or more.

Dosage adjustment

• Patients with severe renal impairment (creatinine clearance less than 30 ml/minute/1.73 m2) not on hemodialysis

• Unexplained persistent proteinuria or hematuria

• Concurrent use of cyclosporine, niacin, fenofibrate, gemfibrozil, or combination of lopinavir and ritonavir or atazanavir and ritonavir

• Asian patients

Contraindications

• Hypersensitivity to drug or its components

• Active hepatic disease or persistent, unexplained hepatic enzyme elevations

• Women who are pregnant or may become pregnant

• Breastfeeding patients

Precautions

Use cautiously in:

• predisposing factors for myopathy (such as renal impairment, advanced age, hypothyroidism)

• heavy alcohol use or history of chronic liver disease

• hypersensitivity to other HMG-CoA reductase inhibitors (such as fluvastatin, simvastatin)

• proteinuria and hematuria

• concurrent use of drugs that may decrease levels or activity of endogenous steroid hormones (such as ketoconazole, spironolactone, and cimetidine)

• concurrent use of fenofibrate, lipid-modifying doses (1 g/day or more) of niacin, coumarin anticoagulants, protease inhibitors given in combination with ritonavir

• concurrent use of gemfibrozil (avoid use or, if used, don't exceed 10 mg daily)

• elderly patients

• children younger than age 10 (safety and efficacy not established).

Administration

Check liver function tests before therapy starts.

• Give with or without food.

• Measure lipid levels within 2 to 4 weeks after therapy starts and after titration.

• Know that drug should be used as adjunct to other lipid-lowering treatments, such as diet.

Adverse reactions

CNS: headache, dizziness, anxiety, depression, insomnia, hypertonia, paresthesia, asthenia, tremor, vertigo, neuralgia

CV: palpitations, tachycardia, chest pain, angina pectoris, hypertension, vasodilation, peripheral edema

EENT: rhinitis, sinusitis, pharyngitis

GI: nausea, vomiting, diarrhea, constipation, abdominal pain, dyspepsia, flatulence, gastritis, gastroenteritis, pancreatitis

GU: urinary tract infection, myoglobinuria, acute renal failure

Hepatic: fatal and nonfatal hepatic failure (rare)

Hematologic: anemia

Metabolic: hyperglycemia, diabetes mellitus

Musculoskeletal: myalgia, myopathy, joint pain, rhabdomyolysis

Skin: rash, pruritus, urticaria

Other: hypersensitivity reactions (including angioedema)

Interactions

Drug-drug. Antacids: decreased rosuvastatin blood level

Cyclosporine, gemfibrozil protease inhibitor combinations lopinavir/ritonavir and atazanavir/ritonavir: increased rosuvastatin bioavailability

Hormonal contraceptives: increased contraceptive blood level

Niacin in lipid-modifying doses (1 g/day or more): increased risk of enhanced musculoskeletal effects

Warfarin: increased International Normalized Ratio

Drug-diagnostic tests. Alanine aminotransferase (ALT), alkaline phosphatase, aspartate aminotransferase (AST), bilirubin, creatine kinase (CK), glucose: increased levels

Thyroid function tests: altered results

Urine protein: present beyond trace

Patient monitoring

Monitor CK, creatinine, and urine protein levels closely. Also watch for signs and symptoms of rhabdomyolysis with acute renal failure: CK level above 10 times normal limits, muscle ache or weakness, creatinine elevation, and urine protein level beyond trace, accompanied by hematuria. If these findings occur, withhold drug and notify prescriber immediately.

Monitor liver function tests 12 weeks after therapy begins, after dosage increases, and at least semiannually thereafter. Reduce dosage or withdraw drug if ALT or AST persists at three times normal levels.

Temporarily withhold drug in patients with acute, serious conditions predisposing to renal failure caused by rhabdomyolysis (such as sepsis, hypotension, major surgery, trauma, uncontrolled seizures, or severe metabolic, endocrine, and electrolyte disorders).

• Monitor blood glucose, electrolyte levels, and lipid panel.

• Assess vital signs and cardiovascular status, especially for tachycardia and palpitations.

• Monitor for signs and symptoms of respiratory tract infection.

• Stay alert for tremor and asthenia.

Patient teaching

• Tell patient he may take with or without food. If he's using antacids, instruct him to take these 2 hours after rosuvastatin.

• Instruct patient to maintain a standard cholesterol-lowering diet.

Tell patient to immediately report unexplained muscle pain, tenderness, or weakness (particularly if accompanied by malaise or fever).

Caution female patient of childbearing age not to take drug if she is pregnant, plans to become pregnant, or is breastfeeding.

• Teach patient how to check blood or urine glucose level and recognize signs and symptoms of hypoglycemia and hyperglycemia.

• Tell patient that foods, beverages, and preparations containing caffeine or ephedra may increase drug's stimulant effect. Encourage him to limit caffeine intake and avoid ephedra.

• Advise patient against heavy alcohol use, which increases risk of liver disease.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and herbs mentioned above.

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References in periodicals archive ?
The analytical reference standard (rosuvastatin calcium 98.2% purity, CAS no.
The United States Food and Drug Administration has approved United States-based Citron Pharma and its licensing partner's Abbreviated New Drug Application for Rosuvastatin Calcium 5, 10, 20 and 40 mg tablets, the generic version of AstraZeneca's CRESTOR (rosuvastatin calcium) tablets, it was reported on Friday.
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Since 2007, nine generic drug makers have filed abbreviated new drug applications (ANDAs) for copy-cat versions of Crestor, claiming non-infringement, invalidity or unenforceability of the RE37,314, or the 314 patent, protecting the active ingredient rosuvastatin calcium.
Manufactured by London-based AstraZeneca, Crestor (rosuvastatin calcium) is still on the market and has been used by more than 4.3 million patients in more than 70 countries.
Tenders are invited for Purchase of pharmaceutical substance Rosuvastatin calcium
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Tenders are invited for Substance Rosuvastatin calcium (Mandatory requirements: manufacturer Teva Assia Chemical Industries Ltd, Israel - ND RB 1335C-2014; Residual shelf life of the goods on the date of delivery should be at least 80% of the total shelf life)