CHOLYBAR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CHOLYBAR (CHOLYBAR).
Binds bile acids in the intestine, forming an insoluble complex that is excreted in feces, preventing their reabsorption and promoting cholesterol catabolism.
| Metabolism | Not metabolized; excreted unchanged in feces as the bile acid complex. |
| Excretion | Primarily hepatic; Cholybar is not absorbed systemically, acting locally in the gut. Excretion is fecal (>99%) as the resin and bound bile acids. Renal excretion is negligible (<1%). |
| Half-life | Not applicable systemically because Cholybar is not absorbed. The local gastrointestinal transit half-life is approximately 2-4 hours, but clinical effects persist based on bile acid depletion. |
| Protein binding | Not applicable (non-absorbed resin; no systemic protein binding). |
| Volume of Distribution | Not applicable (minimal systemic absorption; Vd is clinically irrelevant for non-absorbed drug). |
| Bioavailability | Oral: <0.05% (essentially zero) due to lack of gastrointestinal absorption; acts locally. |
| Onset of Action | Oral: Onset of reduction in LDL cholesterol occurs within 1-2 weeks; maximal effect may take 4-8 weeks. For pruritus relief, onset may be 1-2 weeks. |
| Duration of Action | Duration of effect: After discontinuation, bile acid levels return to baseline within 1-2 weeks. Cholesterol-lowering effect persists as long as therapy continues; effect on pruritus diminishes over days to weeks after stopping. |
10 g (one packet) orally three times daily, mixed with 4-6 ounces of water or other liquid.
| Dosage form | BAR, CHEWABLE |
| Renal impairment | No dose adjustment required for renal impairment; however, monitor serum electrolytes (particularly chloride and bicarbonate) in patients with severe renal dysfunction (GFR <30 mL/min/1.73 m²) due to potential electrolyte imbalances. |
| Liver impairment | No specific dose adjustment for hepatic impairment; use with caution in patients with severe hepatic disease (Child-Pugh class C) due to possible worsening of metabolic alkalosis. |
| Pediatric use | Children 3-12 years: 5 g (half packet) orally three times daily; children 12-18 years: same as adult dose (10 g three times daily). |
| Geriatric use | No specific dose adjustment; monitor fluid and electrolyte status closely, as elderly patients may have decreased renal function and are more susceptible to volume overload and electrolyte disturbances. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CHOLYBAR (CHOLYBAR).
| Breastfeeding | Not excreted in breast milk due to lack of systemic absorption. M/P ratio is negligible. Considered compatible with breastfeeding; monitor infant for gastrointestinal effects. |
| Teratogenic Risk | CHOLYBAR is a bile acid sequestrant. Based on mechanism and limited data, no major teratogenic risk is expected. However, due to potential for decreased absorption of fat-soluble vitamins (A, D, E, K), there is a theoretical risk of fetal vitamin deficiency. No specific human studies exist; use only if clearly needed. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Complete biliary obstruction","Hypersensitivity to cholestyramine or any component"]
| Precautions | ["May cause fecal impaction, particularly in patients with constipation or reduced gut motility","May impair absorption of fat-soluble vitamins (A, D, E, K)","May bind concomitantly administered drugs, reducing their absorption"] |
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| Fetal Monitoring |
| Monitor maternal prothrombin time and fat-soluble vitamin levels (A, D, E, K) due to possible malabsorption. In pregnancy, consider fetal ultrasound for growth if prolonged use. |
| Fertility Effects | No known adverse effects on fertility. It may reduce absorption of oral contraceptives; advise additional non-hormonal contraception. |