ATOZET 10/40/MG FC TAB 30/FC TAB

Dosage & Administration

Dosing by Condition

Adults: 1 tablet orally once daily (with or without food); choose strength based on baseline LDL‑C and required reduction, and titrate at intervals of about 2-4 weeks; HoFH: 1 tablet once daily as adjunct to other lipid‑lowering therapies (strength individualized rather than fixed to 10/40).

Initial Dose

One tablet (ezetimibe 10 mg / atorvastatin 40 mg) once daily for patients requiring greater than 55% reduction in LDL-C

Maintenance Dose

One tablet once daily (strength selected based on LDL-C goal and tolerability)

Maximum Dose

Ezetimibe 10 mg / atorvastatin 80 mg once daily (10/80 mg).

Dose Adjustment Notes

Renal impairment: no dose adjustment generally required; hepatic impairment/active liver disease: contraindicated in active liver disease and avoid/use caution in hepatic impairment; assess lipids about 2-4 weeks after initiation or titration and adjust accordingly; with strong CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, certain HIV/HCV protease inhibitors) use the lowest necessary atorvastatin dose and apply product-specific maximums (often not exceeding the equivalent of atorvastatin 20 mg/day, and avoid with some protease inhibitor regimens).

Side Effects

Common Side Effects

Common: myalgia, arthralgia, pain in extremity, diarrhea, nausea, headache; may also include nasopharyngitis and fatigue, and laboratory increases in transaminases can occur.

Side Effect Frequency

Common (≥1% to <10%) adverse effects reported with ezetimibe/atorvastatin include: nasopharyngitis, headache, diarrhea, nausea, myalgia/muscle pain, arthralgia, pain in extremity, fatigue, and increases in ALT/AST; rare but clinically important events include myopathy/rhabdomyolysis and serious hypersensitivity/skin reactions.

Safety & Warnings

Contraindications

Hypersensitivity to atorvastatin, ezetimibe, or excipients; active liver disease or unexplained persistent elevations of serum transaminases; pregnancy; breastfeeding; concomitant use with systemic fusidic acid (temporarily stop statin during fusidic acid therapy).

Warnings & Precautions

Baseline LFTs before initiation and repeat as clinically indicated; discontinue/hold if persistent transaminases >3× ULN or if symptoms of hepatotoxicity occur; counsel to report unexplained muscle pain/weakness and check CK when indicated, stopping therapy if myopathy/rhabdomyolysis is suspected; myopathy risk increases with higher atorvastatin exposure (CYP3A4 inhibitors, cyclosporine), fibrates/niacin/colchicine, renal impairment, hypothyroidism, and older age; consider diabetes risk monitoring in at-risk patients.

Age Restriction

Not recommended in children and adolescents (<18 years); use is generally for adults unless a specialist determines benefit outweighs risk.

Driving Warning

Safe

Drug Interactions

Drug Interactions

Major/clinically important: strong CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, HIV/HCV protease inhibitors) and cyclosporine (↑ atorvastatin exposure/myopathy risk); gemfibrozil and other fibrates, niacin (lipid-lowering doses), colchicine (↑ myopathy risk); systemic fusidic acid (avoid/contraindicated-rhabdomyolysis risk); grapefruit juice in large quantities (↑ atorvastatin levels). Ezetimibe-specific: bile acid sequestrants reduce absorption (give ezetimibe ≥2 h before or ≥4 h after); warfarin-monitor INR when starting/stopping; antacids may slightly reduce ezetimibe absorption (separate if needed).

Food Interaction

May be taken with or without food; avoid large quantities of grapefruit juice (clinically relevant interaction risk increases with high intake, e.g., >1 quart/≈1 liter daily).

Special Populations

Pregnancy

Contraindicated

Breastfeeding

Contraindicated

Elderly

Standard adult dosing; use with caution in elderly patients (≥65 years) as they may be at higher risk for myopathy. Monitor for adverse effects.

Storage & Patient Advice

Stopping the Medicine

Do not stop without consulting the prescriber; stopping will allow LDL-C to rise and may increase cardiovascular risk.

Pharmacology

Mechanism of Action

Atorvastatin inhibits HMG‑CoA reductase to reduce hepatic cholesterol synthesis and upregulate LDL receptors; ezetimibe inhibits intestinal cholesterol absorption via NPC1L1, lowering delivery of cholesterol to the liver.

Onset of Action

Per dose: lipid-lowering activity begins within hours, with maximal LDL‑C reduction achieved within ~2-4 weeks of continuous once‑daily therapy.

Duration of Effect

Per dose: approximately 24 hours (supports once‑daily dosing); clinical LDL‑C lowering is maintained with continued daily therapy.

Half-Life

Atorvastatin: ~14 hours (HMG‑CoA reductase inhibitory activity persists ~20-30 hours due to active metabolites); Ezetimibe (total ezetimibe = parent + glucuronide): ~22 hours.

Bioavailability

Atorvastatin: ~14% systemic availability (extensive first-pass); Ezetimibe: ~35-65% (as total ezetimibe including glucuronide).

Metabolism

Atorvastatin: extensive hepatic metabolism mainly via CYP3A4 to active ortho‑ and parahydroxylated metabolites; Ezetimibe: rapidly conjugated (intestinal wall and liver) via glucuronidation to active ezetimibe‑glucuronide with enterohepatic recirculation.

Excretion

Atorvastatin: primarily biliary/fecal elimination with minimal renal excretion (<~2%); Ezetimibe: predominantly fecal (~78%) with some renal (~11%) excretion.

Product Information

Available Dosage Forms

Film-coated tablet

Composition per Dose

Each film-coated tablet: Atorvastatin 40 mg (as atorvastatin calcium) + Ezetimibe 10 mg

OTC Alternatives

No OTC alternative

Lipid Target

Both

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