DIPILOR 5MG TABLETS

Indications

• Primary hyperlipidemia (heterozygous familial and non-familial)
• Mixed dyslipidemia
• Hypertriglyceridemia
• Prevention of cardiovascular events in patients with a high risk of atherosclerotic cardiovascular disease
• Familial homozygous hypercholesterolemia

Dosage

Children: Refer to the BNF for Children for specific dosing guidelines.

Adults: Refer to the BNF for specific dosing guidelines.

Mechanism of action

Rosuvastatin inhibits HMG-CoA reductase, the rate-limiting enzyme in the cholesterol biosynthetic pathway. This inhibition leads to a decrease in cholesterol synthesis in the liver, resulting in a compensatory increase in the expression of LDL receptors on hepatocyte membranes. Increased LDL receptor expression enhances the uptake of circulating LDL cholesterol, thereby lowering plasma LDL levels.

Pharmacodynamics

The primary pharmacodynamic effect of rosuvastatin is the reduction in serum cholesterol levels, particularly LDL cholesterol. It also has favorable effects on triglyceride levels and increases HDL cholesterol. Additionally, rosuvastatin may have pleiotropic effects, such as improving endothelial function, reducing inflammation, and stabilizing atherosclerotic plaques.

Pharmacokinetics

Rosuvastatin is well-absorbed after oral administration, with peak plasma concentrations occurring approximately 3 to 5 hours post-dose. It has a bioavailability of about 20%, and its absorption is not significantly affected by food. The drug is extensively metabolized in the liver, mainly via the CYP2C9 enzyme pathway, and is excreted mainly in the bile. The elimination half-life is approximately 19 hours, allowing for once-daily dosing.

Contra-indications

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

Adverse effects

• Myopathy
• Rhabdomyolysis
• Elevated liver enzymes
• Gastrointestinal disturbances (e.g., nausea, constipation)
• Headache
• Dizziness
• Allergic reactions (e.g., rash, pruritus)

Interactions

• CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may increase rosuvastatin levels
• Antacids may reduce absorption if taken concurrently
• Gemfibrozil significantly increases rosuvastatin plasma concentrations
• Warfarin may have altered effects when taken with rosuvastatin

Precautions

• Monitor liver function tests before and during treatment
• Consider risk of myopathy, especially in patients with renal impairment
• Use with caution in patients with a history of muscle disorders
• Exercise caution in elderly patients over the age of 70

Pregnancy

Rosuvastatin is contraindicated during pregnancy due to potential risk to the fetus.

Breast-feeding

Rosuvastatin is contraindicated during breastfeeding as it may be excreted in breast milk.

Storage

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

Formulations

• Oral tablets (5 mg, 10 mg, 20 mg, 40 mg)