EZECHOL 10/MG TAB 30/TAB

Indications

Approved Uses

Adjunct to diet for: (1) primary (heterozygous familial and non-familial) hypercholesterolemia as monotherapy or with a statin; (2) homozygous familial hypercholesterolemia in combination with a statin; (3) homozygous sitosterolemia (phytosterolemia) as monotherapy.

Dosage & Administration

Dosing by Condition

Primary hypercholesterolemia (monotherapy or with statin): 10 mg once daily. Homozygous familial hypercholesterolemia (with statin): 10 mg once daily. Homozygous sitosterolemia: 10 mg once daily

Initial Dose

10mg orally once daily.

Maintenance Dose

10mg orally once daily.

Maximum Dose

10mg orally once daily.

Children's Dosage

For Homozygous Familial Hypercholesterolemia or Sitosterolemia in children 10 years and older: 10mg orally once daily. Safety and efficacy not established in children under 10 years of age.

Dose Adjustment Notes

No dosage adjustment is required in renal impairment or mild hepatic impairment; ezetimibe is not recommended in moderate-to-severe hepatic impairment. No titration is needed (standard dose 10 mg once daily).

How to Take

Swallow 1 tablet (ezetimibe 10 mg) once daily with water; may be taken at any time of day, with or without food. If co-administered with a bile acid sequestrant (e.g., cholestyramine/colestipol/colesevelam), take ezetimibe at least 2 hours before or at least 4 hours after the sequestrant.

Side Effects

Common Side Effects

Common adverse effects include diarrhea, abdominal pain, flatulence, fatigue, headache, and upper respiratory tract infection/nasopharyngitis; arthralgia and myalgia can occur (more often when combined with a statin).

Safety & Warnings

Contraindications

Hypersensitivity to ezetimibe or excipients; if co-administered with a statin, the statin’s contraindications apply (e.g., active liver disease or unexplained persistent transaminase elevations, pregnancy, breastfeeding).

Warnings & Precautions

Not a substitute for diet/lifestyle; if used with a statin monitor LFTs and for muscle symptoms (CK if symptomatic) and discontinue if myopathy/rhabdomyolysis suspected; avoid/not recommended in moderate-severe hepatic impairment; use caution/monitor with cyclosporine and with fibrates (gallstones).

Age Restriction

Not recommended/insufficient data in children <10 years; approved for ≥10 years (familial hypercholesterolemia).

Drug Interactions

Drug Interactions

Key interactions: cyclosporine (↑ ezetimibe exposure; monitor cyclosporine levels), bile-acid sequestrants e.g., cholestyramine/colesevelam (↓ ezetimibe absorption-give ezetimibe ≥2 h before or ≥4 h after), fibrates (caution-↑ gallstone risk; avoid with gemfibrozil; monitor with fenofibrate), warfarin/coumarins (monitor INR when starting/stopping), statins (additive LDL lowering; monitor for myopathy and LFT elevations).

Interaction Severity

MAJOR: Cyclosporine (increases ezetimibe exposure; monitor levels/clinical response and consider closer monitoring of cyclosporine). MODERATE: Fibrates (especially gemfibrozil) due to increased risk of cholelithiasis and possible increased ezetimibe exposure; Statins (additive myopathy risk-monitor for muscle symptoms; check LFTs per statin guidance). MINOR: Bile acid sequestrants (decrease ezetimibe absorption-separate dosing by ≥2 h before or ≥4 h after); Warfarin/other coumarins (possible INR changes-monitor INR when starting/stopping); Antacids (small reduction in rate of absorption-generally not clinically significant).

Food Interaction

No clinically meaningful food interaction; may be taken with or without food.

Special Populations

Children

For Homozygous Familial Hypercholesterolemia or Sitosterolemia in children 10 years and older: 10mg orally once daily. Safety and efficacy not established in children under 10 years of age.

Elderly

Standard adult dosing; no dose adjustment required based on age alone

Kidney Impairment

No adjustment needed.

Liver Impairment

Mild hepatic impairment (Child-Pugh A 5-6): no adjustment; moderate (Child-Pugh B 7-9) or severe (Child-Pugh C ≥10): not recommended.

Storage & Patient Advice

Patient Counseling

Take 1 tablet (10 mg) once daily at the same time each day, with or without food, and continue a cholesterol-lowering diet and lifestyle measures. If taking a bile acid sequestrant, separate dosing (ezetimibe ≥2 h before or ≥4 h after). Report unexplained muscle pain/weakness (especially if on a statin) and attend follow-up lipid tests; do not double doses if one is missed.

Pharmacology

Mechanism of Action

Selectively inhibits the NPC1L1 transporter at the intestinal brush border, reducing absorption of dietary and biliary cholesterol and decreasing hepatic cholesterol delivery, which increases LDL receptor-mediated clearance and lowers LDL-C.

Onset of Action

Cholesterol absorption inhibition begins within hours after the first dose; clinically meaningful LDL-C reduction is typically seen within ~2 weeks (with maximal/near-maximal effect by ~2 weeks) with continued daily therapy.

Bioavailability

Oral absorption is variable; ezetimibe undergoes extensive first-pass glucuronidation to an active metabolite (ezetimibe-glucuronide) with enterohepatic recirculation; absolute bioavailability has not been determined.

Metabolism

Primarily intestinal and hepatic glucuronidation to active ezetimibe‑glucuronide; minimal CYP450/oxidative metabolism.

Excretion

Excreted primarily in feces (~78%) and to a lesser extent in urine (~11%), mainly as ezetimibe and ezetimibe-glucuronide.

Protein Binding

>90%.

Product Information

Available Dosage Forms

Tablet.

Composition per Dose

Each tablet: 10 mg ezetimibe

Generic Availability

Yes

OTC Alternatives

No OTC alternative

Lipid Target

LDL

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