colesevelam hydrochloride

colesevelam hydrochloride

Cholestagel (UK), Welchol

Pharmacologic class: Bile acid sequestrant

Therapeutic class: Antihyperlipidemic

Pregnancy risk category B

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.

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References in periodicals archive ?
Low-dose combination therapy with colesevelam hydrochloride and lovastatin effectively decreases low-density lipoprotein cholesterol in patients with primary hypercholesterolemia.
Coadministration of colesevelam hydrochloride with atorvastatin lowers LDL cholesterol additively.
Colesevelam hydrochloride (HCI) is a bile acid sequestrant indicated alone or in combination with a statin, and as an adjunct to diet and exercise, for the reduction of elevated low-density lipoprotei n-cholesterol (LDL-C) in patients with primary hypercholesterolemia.
Results of the glucose-lowering effect of WelChol study (GLOWS): A randomized, double-blind, placebo-controlled pilot study evaluating the effect of colesevelam hydrochloride on glycemic control in subjects with type 2 diabetes.
Colesevelam hydrochloride therapy in patients with type 2 diabetes mellitus treated with metformin: Glucose and lipid effects.
A clinical trial by Knapp and colleagues demonstrated that adding colesevelam hydrochloride 3-8 g to simvastatin 20 mg resulted in a 42% mean reduction from baseline in LDL-C level, with excellent safety and tolerabiliry.
Hunninghake's clinic, the drug, colesevelam hydrochloride (Cholestagel), reduced LDL levels by an additional 15%-18% when combined with a statin.