💊 Simvastatin (Simvastatin)

🏷️ Brand names & manufacturers

Zocor🏭 Organon LLCDailyMed

Simvastatin🏭 NorthStar Rx LLCDailyMed

Simvastatin🏭 NCS HealthCare of KY, LLC dba Vangard LabsDailyMed

Simvastatin🏭 Quallent Pharmaceuticals Health LLCDailyMed

✅ What it is used for

• To reduce the risk of total mortality, coronary heart disease death, non-fatal myocardial infarction, stroke, and the need for coronary and non-coronary revascularization in adults with established coronary heart disease, cerebrovascular disease, peripheral vascular disease, and/or diabetes who are at high risk of coronary heart disease events
• As an adjunct to diet to reduce LDL-C in adults with primary hyperlipidemia
• As an adjunct to diet to reduce LDL-C in adults and pediatric patients aged 10 years and older with heterozygous familial hypercholesterolemia (HeFH)
• As an adjunct to other LDL-C-lowering therapies to reduce LDL-C in adults with homozygous familial hypercholesterolemia (HoFH)
• As an adjunct to diet for adults with primary dysbetalipoproteinemia or hypertriglyceridemia

🧪 Active ingredient

Simvastatin: a prodrug converted in the body to its active acid form, which inhibits HMG-CoA reductase, the enzyme that drives cholesterol synthesis in the liver, lowering LDL-C and total cholesterol.

🌿 Benefits

• Lowers LDL cholesterol and total cholesterol
• Reduces the risk of heart attack, stroke and coronary heart disease death in high-risk patients
• Reduces the need for coronary and non-coronary revascularization procedures

📝 How to use

• Take by mouth once daily in the evening
• The dose is set by your doctor or pharmacist; do not change it yourself
• Your doctor may check your LDL-C as early as 4 weeks after starting and adjust the dose if needed
• If you miss a dose, take it as soon as possible; do not double the next dose

💊 Dosage forms

• Film-coated tablets: 5 mg, 10 mg, 20 mg, 40 mg, 80 mg

🔄 Drug interactions

• Strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, posaconazole, voriconazole, erythromycin, clarithromycin, nelfinavir, ritonavir, boceprevir, telaprevir, cobicistat-containing products, nefazodone): contraindicated; if unavoidable, suspend simvastatin during treatment
• Cyclosporine, danazol, gemfibrozil: contraindicated
• Lomitapide: reduce simvastatin dose by 50%; do not exceed 20 mg daily
• Verapamil, diltiazem, dronedarone: do not exceed simvastatin 10 mg daily
• Amiodarone, amlodipine, ranolazine: do not exceed simvastatin 20 mg daily
• Coumarin anticoagulants: obtain INR before starting and monitor during initiation or dose adjustment
• Digoxin: monitor digoxin levels when starting simvastatin
• Grapefruit juice may increase the risk of myopathy and rhabdomyolysis

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👨‍⚕️ For healthcare professionals

Mechanism of action

Simvastatin is a prodrug hydrolyzed to its active β-hydroxyacid, which with its metabolites inhibits HMG-CoA reductase, the rate-limiting enzyme converting HMG-CoA to mevalonate (a cholesterol precursor). This upregulates LDL receptor expression and hepatic LDL-C uptake, lowering plasma LDL-C and total cholesterol, and also decreases VLDL. Maximum LDL-C reduction is usually reached by 4 weeks and maintained. Systemic availability is low (<5%) due to extensive hepatic first-pass extraction; total radioactivity peaks at about 4 hours; a low-fat meal does not affect the total inhibitor profile.

Labeled dosing

Adults: 20 mg to 40 mg once daily in the evening. Pediatric patients 10 years and older with HeFH: 10 mg to 40 mg once daily. Maximum recommended dosage 40 mg once daily; 80 mg is restricted to patients on it chronically (e.g., 12 months or more) without muscle toxicity. Severe renal impairment (CLcr 15 to 29 mL/min): starting dose 5 mg once daily; no adjustment for mild or moderate impairment. Assess LDL-C as early as 4 weeks and adjust as needed. The actual dose is determined by the doctor or pharmacist.

• Interaction-based dose limits: lomitapide (reduce 50%, max 20 mg, or 40 mg if previously on 80 mg chronically); verapamil/diltiazem/dronedarone (max 10 mg); amiodarone/amlodipine/ranolazine (max 20 mg)
• For patients needing a high-intensity statin or not reaching LDL-C goal on 40 mg, prescribe alternative LDL-C-lowering treatment
• Myopathy incidence (CK >10xULN) in clinical studies with median follow-up of at least 4 years: approximately 0.03%, 0.08% and 0.61% with 20 mg, 40 mg and 80 mg daily
• Consider liver enzyme testing before initiation and as clinically indicated; discontinue for serious hepatic injury with symptoms, hyperbilirubinemia or jaundice
• Report suspected adverse reactions to FDA at 1-800-FDA-1088

🎓 Key points for students

• Simvastatin is a prodrug converted to an active β-hydroxyacid that inhibits HMG-CoA reductase
• It is a substrate of CYP3A4 and the transporter OATP1B1, so inhibitors of these raise exposure and myopathy risk
• As a statin it lowers LDL-C and VLDL by increasing LDL receptor expression
• Key adverse effects: myopathy and rhabdomyolysis, immune-mediated necrotizing myopathy, hepatic dysfunction
• Contraindications: strong CYP3A4 inhibitors, cyclosporine, danazol, gemfibrozil, acute liver failure, decompensated cirrhosis
• Avoid in pregnancy and breastfeeding; taken once daily in the evening