colesevelam, Lodalis, Welchol

 Indications

Adjunctive therapy to diet and exercise for the reduction

of LDL cholesterol in patients with primary hypercholesterolemia;

may be used alone or in combination

with statins. Adjunctive therapy to diet and exercise for

the reduction of LDL cholesterol in children 10–17 yr

with heterozygous familial hypercholesterolemia if diet

therapy fails (LDL cholesterol remains 190 mg/dL or

remains 160 mg/dL [with family history of premature

cardiovascular disease or 2 risk factors for cardiovascular

disease]); may be used alone or in combination

with statin. Adjunctive therapy to diet and exercise to

improve glycemic control in patients with type 2 diabetes.

Action

Binds bile acids in the GI tract. Result in increased

clearance of cholesterol. Mechanism for lowering

blood glucose unknown. Therapeutic Effects: Decreased

cholesterol and blood glucose.

Pharmacokinetics

Absorption: Not absorbed; action is primarily local

in the GI tract.

Distribution: Unknown.

Metabolism and Excretion: Unknown.

Half-life: Unknown.

TIME/ACTION PROFILE (cholesterol-lowering

effect)

ROUTE ONSET PEAK DURATION

PO 24–48 hr 2 wk unknown

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Bowel obstruction;

Triglycerides 500 mg/dL; History of pancreatitis

due to hypertriglyceridemia.

Use Cautiously in: Triglycerides 300 mg/dL; Dysphagia,

swallowing disorders, severe GI motility disorders,

or major GI tract surgery; OB, Lactation, Pedi:

Pregnancy, lactation, or children 10 yr (safety not established).

Adverse Reactions/Side Effects

GI: constipation, dyspepsia.

Interactions

Drug-Drug: Maypabsorption of glyburide, glimepiride,

glipizide, levothyroxine, olmesartan, phenytoin,

cyclosporine, warfarin, and estrogen-containing

oral contraceptives (give 4 hr before

colesevelam). Mayqlevels of metformin extendedrelease.

Route/Dosage

Hyperlipidemia

PO (Adults): 3 tablets twice daily or 6 tablets once

daily.

PO (Adults and Children 10–17 yr): Suspension—

one 3.75-g packet once daily or one 1.875-g

packet twice daily.

Type 2 Diabetes

PO (Adults): 3 tablets twice daily or 6 tablets once

daily; Suspension—one 3.75-g packet once daily or

one 1.875-g packet twice daily.

Availability

Tablets: 625 mg. Granules for oral suspension:

1.875 g/packet (contains 13.5 mg phenylalanine), 3.75

g/packet (contains 27 mg phenylalanine).