Rosuvastatin Calcium (rosuvastatin calcium)

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Rosuvastatin calcium, a hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor (i.e., statin), is an antilipemic agent.

Rosuvastatin calcium is a synthetic heptenoic acid-derivative antilipemic agent. The drug is a selective, competitive inhibitor of 3-hydroxymethylglutaryl-CoA (HMG-CoA) reductase (i.e., statin), an enzyme that catalyzes the conversion of HMG-CoA to mevalonate (an early and rate-limiting step in cholesterol biosynthesis). Rosuvastatin reduces total and low-density lipoprotein (LDL)-cholesterol, apolipoprotein B (apo B), non-high-density lipoprotein (HDL)-cholesterol, and triglyceride concentrations, and increases HDL-cholesterol concentrations in patients with primary hyperlipidemia or mixed dyslipidemia.

Rosuvastatin also reduces triglyceride concentrations in patients with primary hypertriglyceridemia. Other favorable effects of statins (pleiotropic effects) include an antiproliferative influence on smooth muscle cells, reconstruction of endothelial activity, antioxidant, antithrombotic, anticancer, and anti-inflammatory effects.

Rosuvastatin is hydrophilic; peak plasma concentrations are reached in 3-5 hours, and both peak plasma concentration and AUC increase in an approximate dose-proportional manner. The absolute bioavailability of rosuvastatin is approximately 20%. Rosuvastatin AUC does not differ following evening or morning drug administration; AUC is also not affected by administration with food.

Therapeutic response is generally achieved within 4 weeks and maintained during continued therapy. Rosuvastatin is 88% bound to plasma proteins, mostly albumin; such binding is reversible and independent of plasma concentrations.

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 P-450 (CYP) isoenzyme 2C9. Clearance of rosuvastatin is not dependent on metabolism by CYP3A4 to a clinically important extent.

Based on in vitro studies, N-desmethyl rosuvastatin has approximately 17-50% of the HMG-CoA reductase inhibitory activity of the parent drug. The parent drug accounts for greater than 90% of the active plasma HMG-CoA reductase inhibitory activity. Rosuvastatin is a substrate for the organic anion transport protein (OATP) 1B1 and the breast cancer resistance protein (BCRP).

Pharmacogenomics of statin therapy include genetic polymorphism of the OATP1B1 gene, which may affect rosuvastatin exposure. Higher plasma rosuvastatin concentrations have been reported in a limited number of patients with 2 reduced-function variant OATP1B1 alleles. The frequency of this genotype (SLCO1B1 521 C/C) generally is less than 5% in most populations.

The effect of this genetic variation on efficacy and safety of rosuvastatin has not been established. Rosuvastatin and its metabolites are mainly eliminated in feces (90%) following oral administration. The elimination half-life of rosuvastatin is approximately 19 hours.

Following an IV dose, approximately 28% of total body clearance was via the renal route and 72% by the hepatic route. Pharmacokinetic differences were not observed among Caucasian, Hispanic, and Black or Afro-Caribbean groups; however a 2-fold elevation in median exposure (peak plasma concentrations and AUC) was observed in Asian subjects when compared with a Caucasian control group.

USES: 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. It belongs to a group of drugs known as "statins." It works by reducing the amount of cholesterol made by the liver. Lowering "bad" cholesterol and triglycerides and raising "good" cholesterol decreases the risk of heart disease and helps to prevent strokes and heart attacks.

In addition to eating a proper diet (such as a low cholesterol/low-fat diet), other lifestyle changes that may help this medication work better include exercising, losing weight if overweight, and stopping smoking. Talk with your doctor for more details.

Generic name: rosuvastatin calcium
Pronunciation: (roe-SUE-vuh-stah-tin)

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

The following indications are listed for Rosuvastatin Calcium:

  • Atherosclerotic Cardiovascular Disease
  • Heterozygous Familial Hypercholesterolemia
  • Homozygous Familial Hypercholesterolemia
  • Hypercholesterolemia
  • Hyperlipidemia
  • Hypertriglyceridemia
  • Mixed Hyperlipidemia
  • Myocardial Infarction Prevention
  • Prevention Of Cerebrovascular Accident
  • Prevention Of Transient Ischemic Attack
  • Primary Dysbetalipoproteinemia
  • Primary Prevention Of Coronary Heart Disease

Also known as: Abnormally Increased Triglycerides In The Blood, Acute Mi Prophylaxis, Acute Myocardial Infarction Prophylaxis, Ami Prophylaxis, Atherosclerosis, Atherosclerotic Vascular Disease, Cardiac Infarct Prophylaxis, Cardiac Infarction Prophylaxis, Cardiovascular Disease Related To Atherosclerosis, Combined Hypercholesterolemia And Hypertriglyceridemia, Coronary Heart Disease Primary Prophylaxis, Cva Prophylaxis, Elevated Blood Cholesterol Level, Elevated Triglyceride Level, Familial Heterozygous Hypercholesterolemia, Familial Homozygous Hypercholesterolemia, Familial Type 3 Hyperlipoproteinemia, Fredrickson Type Iii Hyperlipoproteinemia, Heterozygous Familial Elevated Blood Cholesterol, Hyperlipoidemia, Increased Triglyceride Levels, Lipemia, Lipidemia, Lipoidemia, Mi Prophylaxis, Mixed Dyslipidemia, Myocardial Infarct Prophylaxis, Myocardial Infarction Prophylaxis, Primary Prevention Of Cardiac Ischemia, Primary Prevention Of Ischemic Heart Disease, Primary Prevention Of Myocardial Infarct, Stroke Prophylaxis, Tia Prophylaxis, Tias Prophylaxis, Transient Ischemic Attack Prophylaxis, Type Iii Hyperlipoproteinemia.

Dosing

Dosage of rosuvastatin calcium is expressed in terms of rosuvastatin.

The dosage range of rosuvastatin in adults is 5-40 mg once daily.

Table. Dosage Modification for Concomitant Therapy

Concomitant Drug Rosuvastatin Dosage Modifications Antiviral Medications: Simeprevir Initiate at 5 mg once daily; do not Elbasvir/Grazoprevir exceed 10 mg once daily Sofosbuvir/Velpatasvir Glecaprevir/Pibrentasvir Atazanavir/Ritonavir Lopinavir/Ritonavir Capmatinib Do not exceed 10 mg once daily Cyclosporine Do not exceed 5 mg once daily Darolutamide Do not exceed 5 mg once daily Enasidenib Do not exceed 10 mg once daily Febuxostat Do not exceed 20 mg once daily Fostamatinib Do not exceed 20 mg once daily Gemfibrozil Avoid concomitant use. If used concomitantly, initiate at 5 mg once daily and do not exceed 10 mg once daily Regorafenib Do not exceed 10 mg once daily Tafamadis Avoid concomitant use. If used concomitantly, initiate at 5 mg once daily and do not exceed 20 mg once daily Teriflunomide Do not exceed 10 mg once daily

Drug interactions

Rosuvastatin is minimally (approximately 10%) metabolized by cytochrome P-450 (CYP) isoenzyme 2C9. Clearance of rosuvastatin is not dependent on metabolism by CYP3A4 to a clinically important extent. Rosuvastatin is also a substrate for the organic anion transport protein (OATP) 1B1 and the breast cancer resistance protein (BCRP).

Contraindications

*Acute liver failure or decompensated cirrhosis.

*Known hypersensitivity to rosuvastatin or any component of the formulation. Hypersensitivity reactions including rash, pruritus, urticaria, and angioedema have been reported.

Adverse reactions

Adverse effects reported in at least 2% of patients receiving rosuvastatin include headache, nausea, myalgia, asthenia, and constipation.

Precautions

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ICD codes

No ICD codes are available for this drug.

Formulary status

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Last reviewed · Source: First Databank (FDB) drug data