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 ?
NYSE: VRX and TSX: VRX) announced that its wholly owned subsidiary, Valeant International (Barbados) SRL, has received notice that the New Drug Submission for colesevelam hydrochloride (colesevelam), an oral bile acid sequestrant for hypercholesterolemia, has been approved by the Canadian regulatory authority Health Canada.
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.
Colesevelam hydrochloride therapy in patients with type 2 diabetes mellitus treated with metformin: Glucose and lipid effects.
Three BAS are currently used for treating hypercholesterolemia in the United States: the conventional sequestrants, cholestyramine and colestipol, and the specifically engineered BAS, colesevelam hydrochloride (HCl).
The available BAS include the conventional sequestrants, cholestyramine and colestipol, and the specifically engineered BAS, colesevelam hydrochloride (HCl) (Table 1).
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.
Poster #498 - "Lipid-Lowering Effects of Colesevelam Hydrochloride (HCl) in Patients with Type 2 Diabetes": Examines WelChol's effect on lipid parameters, including LDL-C, total-C, non-HDL-C, apolipoprotein B, LDL particle concentration, and triglycerides in patients with type 2 diabetes.
Effects of Colesevelam Hydrochloride on Low-Density Lipoprotein Cholesterol and High-Sensitivity C-Reactive Protein When Added to Statins in Patients With Hypercholesterolemia" showed a substantial reduction in median hs-CRP.
Colesevelam hydrochloride has been marketed in the United States under the brand-name WelChol(R) for three years by Genzyme's U.
Colesevelam hydrochloride is a non-absorbed, lipid-lowering agent specifically engineered to efficiently bind bile acids in the intestine, impeding their reabsorption.
Colesevelam Hydrochloride (Cholestagel): A New Potent Bile Acid Sequestrant Associated with a Low Incidence of Gastrointestinal Side Effects.
With the acquisition, Genzyme General will have access to two patent- protected, marketed products -- Renagel(R) brand sevelamer hydrochloride and WelChol(TM) brand colesevelam hydrochloride -- along with a significant pipeline of promising products and a proven and productive polymer technology development team.