Colesevelam

Hyperlipidemia, Type 2 Diabetes Mellitus

Oral Adult: Hypercholesterolaemia, Adjunct to Type 2 diabetes mellitus Tablet: 1.875 g (3 tablets) 12 hourly or 3.75 g (6 tablets) once daily Oral suspension: 1.875 g (½ packet) 12 hourly or 3.75 g (1 packet) once daily

Heterozygous Familial Hypercholesterolemia Indicated to reduce LDL-C levels in boys and postmenarchal girls (10-17 years) with heterozygous familial hypercholesterolemia (HeFH) who are unable to reach LDL-C target levels despite an adequate trial of dietary therapy and lifestyle modification <10 years: Safety and efficacy not established 10-17 years Oral suspension: 1.875 g (½ packet) 12 hourly or 3.75 g (1 packet) once daily

Oral Administration Tablet: Take with meals and plenty of liquid; use oral suspension if the patient has difficulty swallowing tablets (eg, pediatric patients) Oral suspension: Empty packet in 4-8 oz of water, fruit juice, or diet soft drink and stir; drink with meal(s); do not take oral suspension in dry form May be coadministered with statins or administered at separate times; monitor lipid levels within 4-6 weeks after initiation

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

Tablets can cause dysphagia or esophageal obstruction due to size; for patients with difficulty swallowing tablets use oral suspension May increase serum TG concentrations, hypertriglyceridemia can cause acute pancreatitis Secondary causes of hyperlipidemia must be ruled out before therapy is initiated Postmarketing cases of bowel obstruction have occurred; not recommended in gastroparesis (constipating effects); instruct patients to promptly discontinue therapy and seek medical attention if severe abdominal pain or severe constipation occurs May exacerbate preexisting constipation (initiate therapy at lower dosage in patients with history of constipation) Seek prompt medical attention if symptoms of acute pancreatitis occur (e.g., severe abdominal pain with or without nausea and vomiting) Phenylalanine can be harmful to patients with phenylketonuria (PKU); before prescribing oral suspension to a patient with PKU, consider combined daily amount of phenylalanine from all sources, including oral suspension Monitoring Parameters Monitor lipid parameters, including serum triglyceride and non-HDL cholesterol concentrations prior to therapy and periodically thereafter. Patients receiving ciclosporin should have their blood-ciclosporin concentration monitored before, during, and after treatment with colesevelam.

Not Classi 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

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.

>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%)

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.