COLESTID
Clinical safety rating: caution
Comprehensive clinical and safety monograph for COLESTID (COLESTID).
Binds bile acids in the intestine, forming an insoluble complex that is excreted in the feces, thereby increasing fecal loss of bile acids and reducing enterohepatic circulation of bile salts. This leads to increased hepatic conversion of cholesterol to bile acids, reduction in hepatic cholesterol stores, and decreased plasma LDL cholesterol levels.
| Metabolism | Not absorbed systemically; not metabolized; excreted unchanged in feces. |
| Excretion | Primarily fecal (≥95%) as unchanged drug; minimal renal excretion (<5%) |
| Half-life | Not applicable due to non-systemic action; local gastrointestinal half-life not clinically defined |
| Protein binding | Not significantly absorbed; binding not applicable |
| Volume of Distribution | Not applicable (non-absorbed; confined to gastrointestinal lumen) |
| Bioavailability | Oral: <0.05% (negligible systemic absorption) |
| Onset of Action | Oral: 24-48 hours for reduction in serum cholesterol; maximal effect may take weeks |
| Duration of Action | Duration correlates with dosing interval; continuous therapy required for sustained effect |
5-10 g orally once or twice daily, maximum 30 g/day.
| Dosage form | GRANULE |
| Renal impairment | No specific dosage adjustment required for renal impairment; use with caution in patients with renal dysfunction due to potential for hyperchloremic metabolic acidosis. |
| Liver impairment | No specific dosage adjustment required for hepatic impairment; use with caution in patients with pre-existing gastrointestinal disorders. |
| Pediatric use | Safety and efficacy not established; limited data suggest 5-10 g daily in divided doses for children aged 12-18 years. |
| Geriatric use | No specific dosage adjustment; monitor for constipation and gastrointestinal adverse effects; initiate at low end of dosing range. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for COLESTID (COLESTID).
| Breastfeeding | Colestipol is not absorbed systemically, thus is not expected to be excreted into breast milk. M/P ratio is not applicable. Considered compatible with breastfeeding, but monitor infant for potential gastrointestinal effects secondary to maternal use. |
| Teratogenic Risk | FDA Pregnancy Category C. Animal studies have shown no evidence of teratogenicity at doses up to 10 times the human dose. However, colestipol is not absorbed systemically; therefore, fetal risk is considered minimal. Trimester-specific risks: First trimester: No known risk due to lack of absorption. Second and third trimesters: Potential for decreased absorption of fat-soluble vitamins and folate, which may affect fetal development. Vitamin K deficiency may increase neonatal bleeding risk. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Complete biliary obstruction","Hypersensitivity to colestipol or any component of the formulation"]
| Precautions | ["May cause fecal impaction, especially in patients with hemorrhoids or constipation.","May interfere with absorption of fat-soluble vitamins (A, D, E, K).","May reduce absorption of other drugs; take other medications at least 1 hour before or 4-6 hours after colestipol.","Use with caution in patients with bleeding tendencies or with impaired hepatic function.","Hypertriglyceridemia may occur."] |
| Food/Dietary | Colestipol may bind to fat-soluble vitamins (A, D, E, K) and decrease their absorption. Take vitamin supplements at least 1 hour before or 4 hours after colestipol. High-fat meals may reduce binding efficacy; take with meals containing moderate fat. |
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| Fetal Monitoring | Monitor maternal lipid profile. Assess prothrombin time and international normalized ratio (PT/INR) if warfarin coadministered. Monitor for signs of vitamin deficiencies: Vitamin A, D, E, K. Consider periodic monitoring of serum folate. In neonates, observe for signs of bleeding due to potential vitamin K deficiency (prolonged PT). |
| Fertility Effects | No known effects on fertility. Colestipol is not absorbed and does not interact with hormonal pathways. Animal studies have not shown impairment of fertility. |
| Clinical Pearls | Colestipol is a bile acid sequestrant; administer with meals to bind bile acids. Monitor for constipation and increase fluid/fiber intake. Reduce doses of other medications by at least 1 hour before or 4 hours after colestipol. May increase triglyceride levels; monitor lipids. Use with caution in patients with renal impairment. |
| Patient Advice | Take exactly as prescribed, usually once or twice daily with food and a full glass of water. · Do not take other medications within 1 hour before or 4 hours after colestipol. · Drink plenty of fluids and eat high-fiber foods to prevent constipation. · Inform your doctor if you have a history of hemorrhoids or digestive problems. · Keep out of reach of children; store at room temperature. |