Generic
Simvastatin
9 brands available in the market
At a glance
Simvastatin is a statin used to lower high cholesterol and reduce the risk of heart disease. It inhibits HMG-CoA reductase, lowering LDL cholesterol and triglycerides while increasing HDL cholesterol.
Description
Simvastatin is a competitive inhibitor of HMG-CoA reductase, the enzyme that catalyzes the early and rate-limiting step in cholesterol biosynthesis. By inhibiting HMG-CoA reductase in the liver, it increases LDL receptor density on liver cells, enhancing removal of LDL cholesterol from plasma and reducing VLDL cholesterol.
Indications
- Primary hypercholesterolemia (type IIa and IIb)
- Coronary heart disease and elevated plasma cholesterol
- High cholesterol
- Prevention of heart attack and stroke
Therapeutic class
Statins
Pharmacological class
HMG-CoA Reductase Inhibitor
Pharmacology
Simvastatin inhibits HMG-CoA reductase in the liver, reducing cholesterol synthesis. This increases LDL receptor numbers on liver cells, enhancing LDL cholesterol removal from plasma. It also reduces VLDL cholesterol and increases HDL cholesterol.
Mechanism of action
Inhibits HMG-CoA reductase to reduce cholesterol synthesis and lower LDL cholesterol.
Dosage
Adult Dose (Oral):
- Hypercholesterolemia: Start 5-10 mg/day (evening); max 40 mg/day
- High CV risk: Start 40 mg/day; adjust at 4-week intervals; max 80 mg/day
- Homozygous FH: 40 mg/day (evening) or 80 mg/day in 3 divided doses
- With dronedarone/verapamil/diltiazem: Do not exceed 10 mg/day
- With amiodarone/amlodipine/ranolazine: Do not exceed 20 mg/day
Pediatric Dose (Heterozygous FH, 10-17 years):
- Start 10 mg/day; increase at 4-week intervals; max 40 mg/day
Administration
- Take in the evening after dinner and before sleeping
- Swallow tablet whole; do not chew, crush, or break
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as possible; if almost time for the next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Headache, fatigue, insomnia
- Nausea, constipation/diarrhea, flatulence
- Abdominal cramps, dyspepsia
- Myalgia, myositis, myopathy
- Rhabdomyolysis (rare)
- Hepatitis, pancreatitis (rare)
Precautions & warnings
- Do not use in active liver disease or unexplained persistent transaminase elevations
- Do not use in pregnancy or lactation
- Chinese patients: Do not use 80 mg/day with niacin
- Do not use with strong CYP3A4 inhibitors
- Monitor for myopathy symptoms (muscle pain, weakness)
Contraindications
- Active liver disease or persistent transaminase elevations
- Pregnancy and lactation
- Strong CYP3A4 inhibitors (itraconazole, ketoconazole, clarithromycin, erythromycin, HIV protease inhibitors)
- Gemfibrozil, cyclosporine, danazol
- Grapefruit juice
- Hypersensitivity to simvastatin
Drug interactions
- Anticoagulants: Increased bleeding risk
- Bosentan, efavirenz, rifampicin: Decreased serum levels
- Colchicine, amiodarone, verapamil, diltiazem: Increased myopathy/rhabdomyolysis risk
- Amlodipine: Increased myopathy risk
- Ezetimibe: Increased hepatotoxicity
Food interactions
Alcohol is unsafe with Simvastatin (increased liver damage risk).
Use in pregnancy
Use in Pregnancy: Highly unsafe (Category X); significant fetal harm; do not use during pregnancy or if planning pregnancy; consult your doctor.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unsafe during breastfeeding; may cause toxicity to the baby; do not use; consult your doctor.
Pediatric use
Indicated for children 10-17 years with heterozygous FH; safety not established in children <10 years
Geriatric use
Caution required in elderly patients
Renal / hepatic impairment
Renal Impairment: Mild-moderate: no dose adjustment; severe: start 5 mg/day; consult your doctor.
Hepatic Impairment: Do not use in active or severe liver disease; consult your doctor.
Overdose effects
No overdose data available; no specific antidote; provide general measures and monitor liver function.
Storage conditions
Store in a cool and dry place, protected from light; keep out of reach of children.
Chemical structure
Simvastatin