Cholestagel

Action

Binds bile acids in GI tract and forms insoluble complex, impeding bile acid reabsorption and promoting its excretion. As a result, cholesterol and low-density lipoprotein (LDL) levels decrease.

Availability

Oral suspension: 3.75 g packet

Tablets: 625 mg

Indications and dosages

➣ Adjunct to diet and exercise to reduce LDL cholesterol in patients with primary hypercholesterolemia

Adults and children ages 10 to 17: Three tablets (1,875 mg) P.O. b.i.d., or six tablets (3,750 mg) once daily; or, one 3.75-g packet P.O. once daily.

➣ Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus

Adults: Three tablets (1,875 mg) P.O. b.i.d., or six tablets (3,750 mg) P.O. once daily; or, one 3.75-g packet P.O. once daily

Contraindications

• Hypersensitivity to drug

• Bowel obstruction

• Serum triglyceride level above 500 mg/dl or history of hypertriglyceridemia-induced pancreatitis

Precautions

Use cautiously in:

• susceptibility to vitamin K deficiency (such as patients on warfarin or those with malabsorption syndrome), concomitant use of fat-soluble vitamins

• patients with dysphagia or swallowing disorders, gastroparesis, other GI motility disorders; those who have had major GI tract surgery and who may be at risk for bowel obstruction

• children (safety and efficacy not established).

Administration

• Give with meals and fluids.

• Ensure that patient swallows tablets whole without crushing or chewing.

• Mix prescribed powder packet with 4 to 8 ounces of water, fruit juice, or diet soft drinks.

• Know that drug may be used alone or with HMG-CoA reductase inhibitor.

Adverse reactions

CNS: headache, anxiety, vertigo, dizziness, insomnia, fatigue, syncope

EENT: tinnitus

GI: nausea, vomiting, diarrhea, constipation, abdominal discomfort, flatulence, fecal impaction, loose stools, fatty stools, rectal or hemorrhoidal bleeding, other GI bleeding

GU: increased libido

Hematologic: anemia, bleeding tendency

Metabolic: malabsorption of vitamins A, D, E, and K

Musculoskeletal: back, muscle, or joint pain

Skin: bruising

Interactions

Drug-drug. Fat-soluble vitamins (A, D, E, and K): decreased vitamin absorption

Patient monitoring

• Monitor lipid levels before starting therapy and periodically thereafter.

Patient teaching

• Instruct patient to take drug with meals as directed.

• Instruct patient to mix powder packet for oral suspension with 4 to 8 ounces of water, fruit juice, or diet soft drinks; stir well, and drink. Tell patient not to take powder in its dry form.

• Instruct patient to take any vitamins at least 4 hours before taking this drug.

• Tell patient to report persistent GI upset, back or muscle pain or weakness, and respiratory problems.

• If drug causes constipation, instruct patient to increase exercise, drink plenty of fluids, consume more fruits and fiber, or take a stool softener.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs mentioned above.