Colesevelam

Indications

Colesevelam is used for: Hyperlipidemia, Type 2 Diabetes Mellitus

Adult Dose

Oral Hypercholesterolaemia, Adjunct to Type 2 diabetes mellitus Adult: 3.75 g daily in 1-2 divided doses. Max: 4.375 g daily. In combination w/ a statin w/ or w/o ezetimibe: 2.5-3.75 g daily.

Child Dose

Renal Dose

Administration

Should be taken with food.

Contra Indications

History of bowel obstruction, serum triglyceride concentrations >500 mg/dL, history of hypertriglyceridemia-induced pancreatitis.

Precautions

Patient w/ triglyceride concentration >300 mg/dL, dysphagia or swallowing disorders, gastroparesis or other GI motility disorders. Patient susceptible to vit K deficiency (e.g. malabsorption syndromes) or other fat-soluble vit. Patient who underwent major GI tract surgery and who may be at risk for bowel obstruction. Pregnancy and lactation. Monitoring Parameters Monitor lipid parameter, including serum triglyceride and non-HDL cholesterol concentrations prior to therapy and periodically thereafter.

Pregnancy-Lactation

Pregnancy There are no adequate and well-controlled studies of colesevelam hydrochloride use in pregnant women In the postmarketing setting, there have been reports of pregnancy and a causal association with congenital anomalies has not been established Contraception Coadministration with colesevelam and oral contraceptives may reduce efficacy of oral contraceptives; advise patients to take oral contraceptives at least 4 hr prior to taking therapy Lactation Not absorbed systemically by mother following oral administration, and breastfeeding is not expected to result in exposure of child to drug

Interactions

May decrease absorption of fat-soluble vit A, D, E and K. May interfere w/ anticoagulant effect of warfarin. May reduce serum concentration of ciclosporin, phenytoin, glibenclamide, ethinyl estradiol, norethindrone.

Adverse Effects

Side effects of Colesevelam : >10% Constipation (6.5-11%) 1-10% Dyspepsia (2.8-8.3%) Headache (3.9-7.6%) Nasopharyngitis (5.4-6.2%) Upper respiratory tract infection (4.9%) Nausea (4.2%) Influenza (3.8%) Nausea (2.6-3.8%) Accidental injury (3.7%) Asthenia (3.6%) Hypoglycemia (3.4%) Pharyngitis (3.2%) Flu syndrome (3.2%) Rhinitis (3.2%) Fatigue (3.9%) Hypertension (2.6%) Creatine phosphokinase increase (2.3%) Rhinitis (2.3%) Vomiting (2.3%) Back pain (2.3%) Myalgia (2.1%)

Mechanism of Action

Colesevelam, a nonabsorbable hydrogel, binds w/ bile acids in the intestine to form a nonabsorbable complex that is excreted in the faeces. This results in increased conversion of cholesterol to bile acids in the liver causing a compensatory increase in hepatic uptake of circulating LDL cholesterol.