💊 Atorvastatin (Atorvastatin Calcium)

✅ What it is used for

• Reduce the risk of myocardial infarction (MI), stroke, revascularization procedures, and angina in adults with multiple risk factors for coronary heart disease (CHD) but without clinically evident CHD
• Reduce the risk of MI and stroke in adults with type 2 diabetes mellitus with multiple risk factors for CHD but without clinically evident CHD
• Reduce the risk of non-fatal MI, fatal and non-fatal stroke, revascularization procedures, hospitalization for congestive heart failure, and angina in adults with clinically evident CHD
• Adjunct to diet to reduce LDL-C in adults with primary hyperlipidemia
• Reduce LDL-C in adults and pediatric patients aged 10 years and older with heterozygous familial hypercholesterolemia (HeFH)
• Adjunct to other LDL-C-lowering therapies, or alone if unavailable, to reduce LDL-C in adults and pediatric patients aged 10 years and older with homozygous familial hypercholesterolemia (HoFH)
• Adjunct to diet for adults with primary dysbetalipoproteinemia and hypertriglyceridemia

🧪 Active ingredient

The active ingredient is atorvastatin calcium, a selective, competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis. By inhibiting this enzyme in the liver, it reduces cholesterol production and increases the number of hepatic LDL receptors, enhancing uptake and breakdown of LDL from the blood.

🌿 Benefits

• Lowers LDL cholesterol (LDL-C)
• Reduces the risk of heart attack and stroke in at-risk patients
• Reduces revascularization procedures and hospitalization for heart failure in patients with CHD
• Taken once daily with or without food

📝 How to use

• Take by mouth once daily at any time of day, with or without food
• The dose is set by your doctor or pharmacist based on your condition; do not change it on your own
• 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, do not take the missed dose; resume with your next scheduled dose

💊 Dosage forms

• Film-coated tablets 10 mg
• Film-coated tablets 20 mg
• Film-coated tablets 40 mg
• Film-coated tablets 80 mg

🔄 Drug interactions

• Cyclosporine and gemfibrozil: concomitant use not recommended (higher risk of myopathy)
• Certain anti-viral medicines (saquinavir plus ritonavir, darunavir plus ritonavir, fosamprenavir, elbasvir plus grazoprevir, letermovir): do not exceed 20 mg daily; nelfinavir: do not exceed 40 mg daily
• Clarithromycin or itraconazole: do not exceed 20 mg daily
• Grapefruit juice and certain other drugs may increase the risk of myopathy and rhabdomyolysis
• Rifampin: may reduce atorvastatin levels; administer simultaneously with atorvastatin
• Oral contraceptives: may increase levels of norethindrone and ethinyl estradiol
• Digoxin: levels may increase; patients should be monitored
• Tell your doctor or pharmacist about all medicines you take

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👨‍⚕️ For healthcare professionals

Mechanism of action

Selective, competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme converting HMG-CoA to mevalonate, a sterol precursor including cholesterol. It lowers plasma cholesterol and lipoproteins by inhibiting hepatic cholesterol synthesis and increasing hepatic LDL receptors, and also reduces LDL production and LDL particle number. Absolute bioavailability of the parent drug is ~14%; peak plasma concentrations occur within 1–2 hours.

Labeled dosing

Adults: recommended starting dosage 10–20 mg once daily; range 10–80 mg once daily; patients needing >45% LDL-C reduction may start at 40 mg once daily. Reassess LDL-C as early as 4 weeks. Pediatric ≥10 years with HeFH: start 10 mg, range 10–20 mg daily; with HoFH: start 10–20 mg, range 10–80 mg daily. The dose is determined by the doctor or pharmacist.

• Missed doses should not be made up
• Interaction dose caps: ≤20 mg with saquinavir/ritonavir, darunavir/ritonavir, fosamprenavir, elbasvir/grazoprevir, letermovir, clarithromycin, itraconazole; ≤40 mg with nelfinavir
• Avoid concomitant cyclosporine or gemfibrozil
• Discontinue if CK is markedly elevated, myopathy or IMNM is diagnosed or suspected
• Consider liver enzyme testing before initiation and as clinically indicated
• Most common adverse reactions (≥5%): nasopharyngitis, arthralgia, diarrhea, pain in extremity, urinary tract infection

🎓 Key points for students

• Class: HMG-CoA reductase inhibitor (statin)
• Mechanism: inhibits the rate-limiting enzyme of cholesterol synthesis and upregulates hepatic LDL receptors
• Substrate of CYP3A4 and transporters (OATP1B1/1B3, P-gp, BCRP), so inhibitors raise its levels
• Key serious adverse effects: myopathy/rhabdomyolysis and hepatic dysfunction
• Contraindications: acute liver failure or decompensated cirrhosis; hypersensitivity
• Pregnancy: may cause fetal harm; breastfeeding not recommended
• Dosing: once daily at any time with or without food; food reduces absorption (~25% Cmax) but LDL-C reduction is similar