Home Drug Guide Ezetimibe; Rosuvastatin Calcium

Drug Guide

Generic Name

Ezetimibe; Rosuvastatin Calcium

Brand Names Roszet

Classification

Therapeutic: Lipid-lowering agent

Pharmacological: Cholesterol absorption inhibitor combined with HMG-CoA reductase inhibitor

FDA Approved Indications

Homozygous familial hypercholesterolemia
Heterozygous familial hypercholesterolemia
Non-familial hypercholesterolemia to reduce LDL-C

Mechanism of Action

Ezetimibe inhibits intestinal absorption of cholesterol, while rosuvastatin inhibits HMG-CoA reductase, decreasing cholesterol synthesis in the liver.

Dosage and Administration

Adult: Typically, 10/5 mg once daily, titrated based on response.

Pediatric: Not approved for use in children.

Geriatric: Adjust dose based on tolerability and response.

Renal Impairment: Use with caution; dosage adjustments may be necessary.

Hepatic Impairment: Contraindicated in active liver disease; caution in elevated liver enzymes.

Pharmacokinetics

Absorption: Ezetimibe and rosuvastatin are well absorbed orally.

Distribution: Ezetimibe extensively metabolized; rosuvastatin highly protein-bound.

Metabolism: Ezetimibe undergoes glucuronidation; rosuvastatin metabolized minimally by CYP2C9.

Excretion: Ezetimibe primarily excreted in feces; rosuvastatin excreted mainly via biliary/fecal route.

Half Life: Ezetimibe: ~22 hours; Rosuvastatin: ~19 hours.

Contraindications

Active liver disease
Unexplained persistent elevations of serum transaminases

Precautions

Pregnancy and lactation; hepatic impairment; concurrent use with other hepatotoxic drugs.

Adverse Reactions - Common

Myalgia (Common)
Diarrhea (Common)
Elevations in liver enzymes (Common)

Adverse Reactions - Serious

Rhabdomyolysis (Rare)
Hepatotoxicity (Rare)

Drug-Drug Interactions

Gemfibrozil and other fibrates may increase risk of myopathy.
Cyclosporine may increase rosuvastatin levels.

Drug-Food Interactions

N/A

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Monitor lipid profile, liver enzymes, and CK levels.

Diagnoses:

Risk for impaired liver function
Risk for muscle injury

Implementation: Administer with or without food; advise patients to report muscle pain, weakness, or signs of liver dysfunction.

Evaluation: Assess lipid levels periodically; monitor for adverse effects.

Patient/Family Teaching

Take medication as prescribed.
Report unexplained muscle pain, weakness, or signs of liver problems.
Maintain a healthy diet and lifestyle for cholesterol management.

Special Considerations

Black Box Warnings:

Potential for myopathy/rhabdomyolysis, especially when combined with certain other lipid-lowering medications.

Genetic Factors: Genetic variations may affect drug metabolism and response.

Lab Test Interference: May elevate liver enzymes, which should be monitored.

Overdose Management

Signs/Symptoms: Muscle pain, weakness, elevated liver enzymes.

Treatment: Supportive care; no specific antidote. Discontinue medication; symptomatic treatment.

Storage and Handling

Storage: Store at room temperature, away from moisture and heat.

Stability: Stable under normal storage conditions.