Medication Information: Crestor

Drug Classification

Crestor, known generically as rosuvastatin, is classified as a statin medication. Statins are lipid-lowering agents that inhibit the enzyme HMG-CoA reductase, which plays a critical role in the production of cholesterol in the liver.

Therapeutic Use

Crestor is primarily prescribed to patients for lowering total cholesterol, low-density lipoprotein (LDL) cholesterol, and triglyceride levels in the blood. It is also used to increase high-density lipoprotein (HDL) cholesterol.

Dosage Forms

Crestor is available in oral tablet form. Tablets are produced in various strengths, including 5 mg, 10 mg, 20 mg, and 40 mg doses. The appropriate dose varies based on the patient’s condition, severity of lipid levels, and presence of other risk factors.

Administration Guidelines

Crestor should be taken orally, typically once daily. The medication can be taken with or without food. Swallow the tablet whole with water, without crushing or chewing it.

Initial Dosage

The usual starting dose for adults is 10 mg to 20 mg once daily. Initial dosing may vary based on individual patient factors such as age, accompanying medical conditions, and concurrent medications.

Maintenance Dose

Maintenance doses can range from 5 mg to 40 mg daily, adjusted according to the patient’s response to the medication and lipid level goals. Regular monitoring of lipid levels and dose adjustments may be necessary to achieve optimal efficacy.

Mechanism of Action

Crestor works by inhibiting HMG-CoA reductase, an enzyme involved in the synthesis of cholesterol in the liver. This inhibition results in decreased cholesterol production and increased clearance of LDL cholesterol from the bloodstream.

Effect on Lipids

Crestor is effective at lowering LDL cholesterol by approximately 20%-55%. It also reduces triglycerides by 10%-35% and can increase HDL cholesterol by 7%-14%.

Drug Interactions

Significant drug interactions include those with cyclosporine, gemfibrozil, and certain protease inhibitors. Concurrent use with these medications can increase the risk of muscle-related side effects and necessitates careful monitoring or dosage adjustments.

Common Side Effects

Common side effects associated with Crestor use include headache, myalgia (muscle pain), abdominal pain, nausea, and constipation. These side effects are generally mild and transient.

Serious Side Effects

Serious side effects include rhabdomyolysis (muscle breakdown) and liver enzyme abnormalities. Immediate medical attention is needed if patients experience unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever.

Monitoring Requirements

Before initiating Crestor, baseline lipid levels, liver enzymes, and renal function should be assessed. During treatment, periodic monitoring of lipid levels and liver enzymes is recommended to evaluate therapeutic response and detect any potential adverse effects.

Renal Impairment Considerations

For patients with renal impairment, dosage adjustments may be necessary. Patients with severe renal impairment or those on hemodialysis should generally start with lower doses and be closely monitored to avoid toxicity.

Geriatric Use

In elderly patients, dosing should start at the lower end of the range due to a greater frequency of decreased renal function and concomitant diseases or therapies. Careful dose selection and monitoring are essential to ensure patient safety.

Pediatric Use

The safety and effectiveness of Crestor in pediatric patients have been established for ages 10 to 17 years for heterozygous familial hypercholesterolemia. The usual starting dose is generally 5 mg daily, which may be adjusted based on individual response and tolerance.

Hepatic Impairment

Patients with active liver disease or unexplained persistent elevations in liver transaminases should not be prescribed Crestor. Periodic monitoring of liver enzymes is advised for all patients during treatment.

Pregnancy Considerations

Crestor is contraindicated in pregnant women due to the potential risk to the fetus. It should also be avoided by breastfeeding mothers, as the risk to the neonate cannot be ruled out.

Overdose Management

In case of overdose, treatment is supportive and symptom-directed. There is no specific antidote for Crestor overdose. Immediate discontinuation of the drug and implementation of supportive measures such as activated charcoal may be necessary.

Storage and Handling

Crestor tablets should be stored at room temperature, protected from moisture and light. Keep the medication in its original container, tightly closed, and out of reach of children and pets. Do not store in the bathroom.