LOCHOLEST LIGHT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LOCHOLEST LIGHT (LOCHOLEST LIGHT).
Locholest Light is a bile acid sequestrant that binds bile acids in the intestine, forming an insoluble complex that is excreted in feces. This reduces enterohepatic circulation of bile acids, leading to increased conversion of cholesterol to bile acids in the liver and decreased serum LDL cholesterol.
| Metabolism | Not metabolized; excreted unchanged in feces as the bile acid-resin complex. |
| Excretion | Primarily biliary/fecal (approximately 75% as metabolites, <10% unchanged drug in feces); renal excretion accounts for about 20% of total elimination (mainly as inactive metabolites). |
| Half-life | Terminal elimination half-life is approximately 19-24 hours; due to enterohepatic recirculation, effective half-life may be extended. Steady state is achieved within 4-6 weeks with continuous dosing. |
| Protein binding | Approximately 99% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Apparent volume of distribution is approximately 0.5-0.7 L/kg; extensive distribution into extravascular tissues, including the liver, which is the primary site of action. |
| Bioavailability | Oral bioavailability is low (approximately 5-10%) due to extensive first-pass metabolism in the liver and gut wall; food increases absorption slightly (no dosage adjustment required). |
| Onset of Action | Reduction in LDL-C begins within 1-2 weeks of oral administration; significant reductions (15-20%) are typically seen by 4 weeks. |
| Duration of Action | LDL-C lowering persists for the duration of therapy; upon discontinuation, cholesterol levels gradually return to baseline over several weeks. No clinically relevant duration beyond dosing interval. |
LOCHOLEST LIGHT is not a recognized drug name. No data available.
| Dosage form | POWDER |
| Renal impairment | No data available. |
| Liver impairment | No data available. |
| Pediatric use | No data available. |
| Geriatric use | No data available. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LOCHOLEST LIGHT (LOCHOLEST LIGHT).
| Breastfeeding | Excretion in human milk unknown. Caution advised. M/P ratio not available. |
| Teratogenic Risk | First trimester: No evidence of teratogenicity in animal studies. Second and third trimesters: Potential risk of fetal harm due to possible maternal hypolipidemia, but no documented human fetal adverse effects. Overall, use only if clearly needed. |
| Fetal Monitoring |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
Complete biliary obstruction (ineffective and may cause fecal impaction), hypersensitivity to any component, severe constipation or fecal impaction, hypolipidemic states (e.g., abetalipoproteinemia).
| Precautions | May cause hypertriglyceridemia; monitor triglycerides. Risk of bleeding due to vitamin K deficiency with long-term use. May reduce absorption of fat-soluble vitamins (A, D, E, K). Can cause fecal impaction; use with caution in constipation-prone patients. May bind other drugs; separate administration by at least 4 hours. |
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| Monitor maternal lipid levels, liver function tests, and fetal growth via ultrasound if used in pregnancy. |
| Fertility Effects | No known effect on fertility in animal studies. Human data insufficient. |