Indications

As an adjunct to diet in adults with primary non-familial hyperlipidemia to reduce LDL-C.
Alone or with other LDL-C lowering therapies in patients with homozygous familial hypercholesterolemia (HoFH) to reduce LDL-C.

Pharmacology

Rosuvastatin: Inhibits HMG-CoA reductase, reduces cholesterol synthesis in the liver, increases hepatic LDL receptors, enhances LDL uptake and catabolism, lowers LDL particle production.
Ezetimibe: Inhibits intestinal absorption of cholesterol via sterol transporter, reducing blood cholesterol and phytosterol uptake.

Dosage & Administration

Range: 5/10 mg to 40/10 mg orally once daily.
Severe renal impairment (not on dialysis): Start at 5/10 mg once daily; max 10/10 mg daily.
Tablets must be swallowed whole; do not crush, dissolve, or chew.
Administer ≥2 hours before or ≥4 hours after bile acid sequestrants.
Administer ≥2 hours before aluminium/magnesium hydroxide antacids.
Pediatric use: Not established.
Geriatric use: No dosage adjustment required.

Interactions

Avoid concomitant use with Cyclosporine or Gemfibrozil.
Dosage modifications required with certain antivirals, Darolutamide, Regorafenib.
Niacin, fibrates, colchicine may increase risk of myopathy/rhabdomyolysis.

Contraindications

Active liver disease or decompensated cirrhosis.
Hypersensitivity to any component.

Side Effects Common: headache, nausea, myalgia, arthralgia, dizziness, asthenia, constipation, abdominal pain, respiratory tract infection, diarrhea, sinusitis, extremity pain, fatigue, influenza, back pain.

Pregnancy & Lactation

Contraindicated in pregnancy.
Breastfeeding not recommended.

Precautions & Warnings

Myopathy/rhabdomyolysis: Risk factors include age ≥65, hypothyroidism, renal impairment, drug interactions, high dose. Discontinue if CK markedly elevated or myopathy suspected.
Hepatic dysfunction: Monitor liver enzymes before initiation and as clinically indicated. Rare cases of hepatic failure reported.

Use in Special Populations

Hepatic impairment: Contraindicated in acute liver failure or decompensated cirrhosis. Discontinue if jaundice or hyperbilirubinemia occurs.
Renal impairment: Severe impairment (CrCl <30 mL/min/1.73 m², not on dialysis): start 5/10 mg daily, max 10/10 mg. No adjustment needed for mild/moderate impairment.