Colesevelam Hydrochloride (2 brand names, 4 dosage forms, 1 route)
Available dosage forms: TABLET, FOR SUSPENSION, CAPSULE, BAR, CHEWABLE.
Routes of administration: ORAL.
Brand Names
- COLESEVELAM HYDROCHLORIDE
- WELCHOL
Contraindications
Colesevelam hydrochloride is contraindicated in patients with: Serum TG concentrations greater than 500 mg/dL [see Warnings and Precautions (5.1)] History of hypertriglyceridemia-induced pancreatitis [see Warnings and Precautions (5.1)] A history of bowel obstruction [see Warnings and Precautions (5.2)]
Adverse Reactions
The following important adverse reactions are described below and elsewhere in the labeling: Hypertriglyceridemia and Pancreatitis [see Warnings and Precautions (5.1)] Gastrointestinal Obstruction [see Warnings and Precautions (5.2)] Vitamin K or Fat-Soluble Vitamin Deficiencies [see Warnings and Precautions (5.3)]
Mechanism of Action
Primary Hyperlipidemia: Colesevelam hydrochloride, the active pharmaceutical ingredient in colesevelam hydrochloride, is a non-absorbed, lipid-lowering polymer that binds bile acids in the intestine, impeding their reabsorption. As the bile acid pool becomes depleted, the hepatic enzyme, cholesterol 7-α-hydroxylase, is upregulated, which increases the conversion of cholesterol to bile acids. This causes an increased demand for cholesterol in the liver cells, resulting in the dual effect of increasing transcription and activity of the cholesterol biosynthetic enzyme, HMG-CoA reductase, and increasing the number of hepatic LDL receptors. These compensatory effects result in increased clearance of LDL-C from the blood, resulting in decreased serum LDL-C levels. Serum TG levels may increase or remain unchanged.
Overdosage
Colesevelam hydrochloride is not absorbed and the risk of systemic toxicity is low. Excessive doses of colesevelam hydrochloride may cause more severe local gastrointestinal effects (e.g., constipation).