rosuvastatin calcium

ro·su·va·stat·in calcium (r-sv-sttn)

n.

A statin drug used to treat hyperlipidemia.

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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 heterozygous hypercholesterolemia; mixed dyslipidemia (Fredrickson types IIa and IIb)

Adults: Initially, 10 mg/day P.O. Patients who need less aggressive cholesterol reduction or have predisposing factors for myopathy may start at 5 mg/day. Patients with marked hypercholesterolemia (LDL above 190 mg/dl) and more aggressive LDL goals may start at 20 mg/day. For maintenance, 5 to 40 mg/day P.O.

➣ Homozygous familial hypercholesterolemia

Adults: 20 mg/day P.O. Maximum recommended dosage is 40 mg/day.

➣ Hypertriglyceridemia (Fredrickson type IV)

Adults: Initially, 10 mg/day P.O. For maintenance, 5 to 40 mg/day P.O.

Contraindications

• Hypersensitivity to drug or its components
• Active hepatic disease or persistent, unexplained hepatic enzyme elevations
• Pregnancy or breastfeeding

Precautions

Use cautiously in:
• predisposing factors for myopathy (such as renal impairment, advanced age, hypothyroidism)
• heavy alcohol use
• history of hepatic disease or hypersensitivity to other HMG-CoA reductase inhibitors (such as fluvastatin, simvastatin)
• patients of Japanese or Chinese descent
• women of childbearing age (except those who are highly unlikely to conceive and have been informed of potential hazards)
• children (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.

Route	Onset	Peak	Duration
P.O.	Unknown	3-5 hr	Unknown

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

GU: urinary tract infection, acute renal failure

Hematologic: anemia

Metabolic: hypokalemia, hyperglycemia, hypoglycemia

Musculoskeletal: myalgia; myopathy; arthritis; pathologic fractures; back, pelvic, neck, or joint pain; rhabdomyolysis

Respiratory: respiratory tract infection, bronchitis, increased cough, dyspnea, pneumonia, asthma

Skin: rash, pruritus, bruising

Other: periodontal abscess, flulike symptoms, infection

Interactions

Drug-drug. Antacids: decreased rosuvastatin blood level

Cyclosporine, gemfibrozil: increased rosuvastatin bioavailability

Hormonal contraceptives: increased contraceptive blood level

Warfarin: increased International Normalized Ratio

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

Potassium: decreased level

Thyroid function tests: altered results

Urine protein: present beyond trace

Drug-food. Caffeine-containing foods and beverages: increased stimulant effect

Oat bran, pectin: impaired drug absorption

Urine-acidifying foods: increased drug blood level

Drug-herbs. Caffeine-containing herbs (such as cola nut, yerba maté), ephedra (ma huang): increased stimulant effect

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.