CHOLESTYRAMINE LIGHT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CHOLESTYRAMINE LIGHT (CHOLESTYRAMINE LIGHT).
Binds bile acids in the intestine, forming an insoluble complex that is excreted in feces, thereby preventing enterohepatic recirculation of bile acids and promoting hepatic conversion of cholesterol to bile acids, reducing serum LDL-cholesterol.
| Metabolism | Not metabolized; acts locally in the gastrointestinal tract and is excreted unchanged in feces. |
| Excretion | Primarily fecal as bile acid complex; <0.05% renal excretion of unchanged drug; negligible systemic absorption. |
| Half-life | Not applicable; cholestyramine is not absorbed systemically and has no plasma half-life; clinical effect duration reflects gastrointestinal transit time. |
| Protein binding | Not applicable (non-absorbed); no plasma protein binding. |
| Volume of Distribution | Not applicable (non-absorbed); confined to gastrointestinal lumen. |
| Bioavailability | Oral: <0.04% (minimal systemic absorption due to large molecular weight and quaternary ammonium structure). |
| Onset of Action | Oral: Reduction in pruritus occurs within 1-3 weeks; lipid-lowering effect begins within 24-48 hours with maximal effect in 1-2 weeks. |
| Duration of Action | Lipid-lowering effect persists as long as drug is taken; pruritus relief lasts for duration of therapy; rebound may occur upon discontinuation. |
4 g orally once or twice daily, increased gradually to 4 g 1-6 times daily; maintenance 4-24 g/day in divided doses.
| Dosage form | POWDER |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No specific dosage adjustment recommended; caution in patients with severe hepatic impairment. |
| Pediatric use | 240 mg/kg/day orally in 2-3 divided doses, not to exceed 8 g/day; adjust based on clinical response. |
| Geriatric use | Start at low end of dosing range (4 g/day) and titrate slowly; monitor for constipation and drug interactions. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CHOLESTYRAMINE LIGHT (CHOLESTYRAMINE LIGHT).
| Breastfeeding | Breastfeeding safety: Compatible due to negligible systemic absorption. M/P ratio: Not applicable (not absorbed). No adverse effects reported in breastfed infants. |
| Teratogenic Risk | Cholestyramine is a non-absorbed resin; systemic absorption is negligible. No teratogenic effects reported in animal studies or human case reports. Risk to fetus is minimal across all trimesters. |
| Fetal Monitoring |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
["Complete biliary obstruction (ineffective and may cause harm)","Hypersensitivity to cholestyramine or any component of the formulation"]
| Precautions | ["May reduce absorption of fat-soluble vitamins (A, D, E, K), requiring supplementation","May cause hyperchloremic metabolic acidosis, especially in children with large doses","May cause constipation, which can aggravate hemorrhoids; discontinue if impaction occurs","May interfere with absorption of other drugs; administer other medications at least 1 hour before or 4-6 hours after cholestyramine","Use with caution in patients with phenylketonuria (products may contain aspartame)"] |
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| Monitor maternal lipid levels and fat-soluble vitamin status (A, D, E, K) during prolonged use in pregnancy. Fetal monitoring: standard antenatal care. |
| Fertility Effects | No known adverse effects on fertility. Cholestyramine may interfere with absorption of folic acid, but no direct impairment of reproductive function reported. |