Cholestagel

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.

Cholestagel®

Internal medicine A nonabsorbed cholesterol reducer, that ↓ LDL-C in hypercholesterolemia. See Cholestatin.
References in periodicals archive ?
Q I suffer from bile acid malabsorption and take cholestagel tablets for it, but have terrible flatulence.
by Daiichi Sankyo under the brand name WelChol and elsewhere by Genzyme under the tradename Cholestagel.
Genzyme markets Cholestagel in Europe for the treatment of patients with the genetic disease familial hypercholesterolemia (FH), and for statin-intolerant patients.
Cholestagel is a new, non-absorbed, cholesterol-lowering agent aimed at treating patients with primary hypercholesterolemia who cannot meet their targeted cholesterol levels with standard therapies alone.
The positive CPMP opinion is the final step before formal approval to market Cholestagel in the 15 countries of the European Union.
the expected timing of regulatory submissions and decisions concerning Cholestagel, Aldurazyme and AVONEX; expectations concerning the commercialization of Cholestagel and AVONEX; and clinical trial plans for a potential therapy for Pompe disease and other products, including the anticipated timing thereof.
The 1999 financial results primarily reflect clinical trial and process development costs associated with Cholestagel, costs associated with continued regulatory support, clinical trials and manufacturing support of Renagel (sevelamer hydrochloride), costs associated with the Company's other research programs, and a non-recurring charge for in-process research and development related to the acquisition of SunPharm Corporation.
I think that Cholestagel will address a commercial opportunity probably in the $200-300 million range after a couple of years on the market.
We are very excited to begin working with Sankyo and Sankyo Parke Davis on the planning for commercialization of Cholestagel," commented Mark Skaletsky, President and CEO of GelTex.
With Renagel on the market, and Cholestagel currently under FDA review, as well as ongoing earlier stage research and development programs, we look to Dr.
Sankyo will provide to GelTex upfront licensing and option fees of $13 million, a $20 million milestone payment upon marketing approval of Cholestagel by the U.
Cholestagel was developed by the Boston-based biotechnology firm GelTex Pharmaceuticals, Inc.