ZYROVA 10

Indications

• Primary hyperlipidemia
• Mixed dyslipidemia
• Familial hypercholesterolemia
• Prevention of cardiovascular disease

Dosage

Children: Refer to the BNF for Children for appropriate dosing guidelines in paediatric patients.

Adults: Dosage varies based on the indication and individual patient factors. Refer to the BNF for specific dosing recommendations.

Mechanism of action

Rosuvastatin works by competitively inhibiting HMG-CoA reductase, the rate-limiting enzyme in the cholesterol synthesis pathway. This inhibition leads to a decrease in cholesterol production in the liver, resulting in upregulation of LDL receptors, increased clearance of LDL from the bloodstream, and ultimately a reduction in total cholesterol and LDL levels.

Pharmacodynamics

The pharmacodynamic profile of rosuvastatin includes its ability to lower plasma concentrations of LDL cholesterol significantly. It also improves the lipid profile by increasing HDL cholesterol and decreasing triglycerides. The effects on LDL cholesterol can be observed within one week of administration, with maximum effect typically reached within 4 weeks. Rosuvastatin also has anti-inflammatory properties that may contribute to its cardiovascular protective effects.

Pharmacokinetics

Rosuvastatin is rapidly absorbed after oral administration, with peak plasma concentrations occurring approximately 5 hours post-dose. It has a bioavailability of approximately 20%, and its absorption is not significantly affected by food. The drug is highly bound to plasma proteins (approximately 88%), and it undergoes extensive hepatic metabolism primarily via CYP2C9. Rosuvastatin has a long half-life of approximately 19 hours, allowing for once-daily dosing. It is excreted primarily in the feces, with less than 10% eliminated via the kidneys.

Contra-indications

• Active liver disease
• Hypersensitivity to rosuvastatin or any component of the formulation
• Pregnancy
• Breastfeeding

Adverse effects

• Myopathy
• Rhabdomyolysis
• Hepatotoxicity
• Gastrointestinal disturbances (e.g., nausea, abdominal pain)
• Headache
• Dizziness
• Fatigue
• Skin reactions (e.g., rash, pruritus)

Interactions

• Gemfibrozil (increased risk of myopathy)
• Other statins (potentiation of statin effects)
• Warfarin (increased anticoagulant effect)
• Cyclosporine (increased rosuvastatin levels)
• Antacids (may reduce absorption of rosuvastatin)

Precautions

• Monitor liver function tests before and during treatment
• Consider risk factors for myopathy and rhabdomyolysis
• Use caution in patients with a history of alcohol abuse
• Assess renal function, particularly in high-dose therapy

Pregnancy

Rosuvastatin is contraindicated in pregnancy due to potential harm to the fetus.

Breast-feeding

It is not recommended to use rosuvastatin while breastfeeding due to the potential for adverse effects on the infant.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Tablets (5 mg, 10 mg, 20 mg, 40 mg)