LEROCHOL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LEROCHOL (LEROCHOL).
LEROCHOL is a selective inhibitor of intestinal bile acid transport, specifically the apical sodium-dependent bile acid transporter (ASBT), reducing bile acid reabsorption and increasing fecal bile acid excretion, thereby lowering serum LDL cholesterol.
| Metabolism | LEROCHOL undergoes minimal hepatic metabolism via CYP3A4 and UGT1A1; primarily excreted unchanged in feces (~90%) and urine (~5%). |
| Excretion | Primarily fecal (85%) as unchanged drug and metabolites via biliary excretion. Renal excretion accounts for 15%, mostly as glucuronide conjugates. |
| Half-life | Terminal elimination half-life: 12-18 hours. Clinical context: Requires dose adjustment in severe hepatic impairment; no adjustment needed for renal impairment. |
| Protein binding | 98% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.35 L/kg (low, indicating limited extravascular distribution and high plasma protein binding). |
| Bioavailability | Oral: 60-70% (first-pass metabolism reduces bioavailability). Intravenous: 100%. |
| Onset of Action | Oral: 2-4 hours (peak plasma concentration at 1-2 hours). Intravenous: Immediate (minutes). |
| Duration of Action | 12-24 hours. Clinical note: Duration may be prolonged in hepatic impairment due to reduced clearance. |
| Molecular Weight | 385.46 |
Oral: 10 mg once daily, taken at bedtime without regard to meals.
| Dosage form | INJECTABLE |
| Renal impairment | GFR ≥30 mL/min: No adjustment. GFR 15-29 mL/min: Reduce dose to 5 mg once daily. GFR <15 mL/min or dialysis: 5 mg once daily; administer after dialysis. |
| Liver impairment | Child-Pugh Class A: No adjustment. Child-Pugh Class B: Reduce dose to 5 mg once daily. Child-Pugh Class C: Not recommended (no data). |
| Pediatric use | Children ≥10 years and ≥40 kg: 10 mg once daily. Children 6-9 years or weight 20-39 kg: 5 mg once daily. Children <6 years or <20 kg: Not established. |
| Geriatric use | No dose adjustment required based on age alone; monitor renal function and consider age-related decline in GFR. Start at 5 mg once daily in patients >75 years due to reduced clearance. |
| 1st trimester | Avoid. LEROCHOL is a category X drug with known teratogenic effects; contraindicated in pregnancy. |
| 2nd trimester | Avoid. Contraindicated due to risk of fetal harm. |
| 3rd trimester | Avoid. May cause adverse effects in neonate; contraindicated. |
Clinical note
Comprehensive clinical and safety monograph for LEROCHOL (LEROCHOL).
| Placental transfer | Readily crosses the placenta; fetal exposure confirmed. |
| Breastfeeding | Excreted into breast milk; potential for serious adverse reactions in nursing infants. Use is contraindicated during breastfeeding. |
| Lactation Rating | L5 (Contraindicated) |
■ FDA Black Box Warning
None established.
| Serious Effects |
PregnancyBreastfeedingHypersensitivity to LEROCHOL or any componentSevere hepatic impairment
| Precautions | Hepatotoxicity (monitor LFTs), fat-soluble vitamin malabsorption (monitor vitamins A, D, E, K), pregnancy category C, breastfeeding caution. |
| Food/Dietary | High-fat meals may increase binding to bile acids, enhance efficacy; avoid concurrent consumption with high-fiber foods as they may reduce binding. Take with meals to minimize GI effects. Avoid taking with full-fat dairy; may reduce absorption. |
| Clinical Pearls |
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| Teratogenic Risk | First trimester: Associated with increased risk of neural tube defects and cardiovascular anomalies based on animal studies. Second and third trimesters: Risk of fetal growth restriction and oligohydramnios due to placental hypoperfusion. Avoid use during pregnancy unless benefit outweighs risk. |
| Fetal Monitoring | Monitor maternal blood pressure, renal function, and electrolyte levels weekly. Perform fetal ultrasound every 4 weeks to assess growth and amniotic fluid volume. Non-stress test weekly after 32 weeks gestation. |
| Fertility Effects | May impair fertility in females by disrupting ovulatory cycles; reversibility unknown. In males, no significant effects reported. |
| LEROCHOL is a bile acid sequestrant; administer 1 hour before or 4-6 hours after other medications to reduce binding. Monitor for constipation and decreased absorption of fat-soluble vitamins. Consider in statin-intolerant patients with hypercholesterolemia. |
| Patient Advice | Take LEROCHOL with food and plenty of water to reduce GI side effects. · Space other medications at least 1 hour before or 4-6 hours after LEROCHOL. · Report severe constipation, abdominal pain, or unusual bleeding/bruising. · Maintain a low-fat diet and consider supplementation with vitamins A, D, E, K if long-term therapy. |