DrugindexOnline^{2nd edition}

Pronouncation: (koe-leh-SEV-eh-lam HIGH-droe-KLOR-ide)
Class: Anti-hyperlipidemic agent, Bile acid sequestrant

Trade Names:
WelChol
- Tablets 625 mg

Mechanism of Action

Pharmacology

Increases removal of bile acids from the body by binding bile acids in the intestine, impeding their reabsorption. As the bile acid pool becomes depleted, the conversion of cholesterol to bile acids is increased, which decreases serum cholesterol.

Pharmacokinetics

Absorption

Not absorbed.

Onset

Maximum reduction in serum cholesterol is achieved within 2 wk.

Indications and Usage

Adjunctive therapy to diet and exercise given alone or with an HMG-CoA reductase inhibitor for the reduction of elevated LDL cholesterol in patients with primary hypercholesterolemia (Fredrickson type IIa).

Contraindications

Bowel obstruction; hypersensitivity to any component of the product.

Dosage and Administration

Adults Monotherapy

PO 1,875 mg (3 tablets) twice daily with meals or 3,750 mg (6 tablets) once daily with a meal. Depending upon the desired effect, the dose can be increased to 4,375 mg/day (7 tablets).

Combination therapy

PO 2,500 to 3,750 mg (4 to 6 tablets) daily.

General Advice

• Administer with liquid and a meal.
• Caution patient to swallow tablets whole and not to crush, chew, or break tablets.

Storage/Stability

Store at controlled room temperature (59° to 86°F). Protect from moisture.

Drug Interactions

Verapamil, sustained-release

AUC and C _max may be reduced; clinical significance unknown.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (6%), asthenia (4%).

GI

Flatulence (12%); constipation (11%); dyspepsia (8%); abdominal pain, diarrhea (5%); nausea (4%).

Musculoskeletal

Myalgia (2%).

Respiratory

Pharyngitis, rhinitis (3%); increased cough, sinusitis (2%).

Miscellaneous

Infection (10%); pain (5%); accidental injury (4%); back pain, flu syndrome (3%).

Precautions

Monitor Determine total cholesterol, LDL, and triglyceride levels before starting therapy and periodically thereafter based on National Cholesterol Education Program (NCEP) guidelines.

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

No special considerations.

Fat-soluble vitamins

Use with caution when treating patients with susceptibility to vitamin K or fat-soluble vitamin deficiencies (A, D, and E).

GI disorders

Use with caution in patients with dysphagia, swallowing disorders, severe GI motility disorders, or major GI tract surgery.

Hypertriglyceridemia

Use caution when treating patients with triglyceride levels higher than 300 mg/dL.

Secondary causes of hypercholesterolemia

Ensure that secondary causes of hyperlipidemia (eg, poorly controlled diabetes, hypothyroidism, nephritic syndrome, dysproteinemias, obstructive liver disease, other drug therapy, alcoholism) have been excluded before starting therapy.

Overdosage

Symptoms

Because colesevelam is not absorbed, the risk of toxicity is low.

Patient Information

• Advise patient to read patient information leaflet before using the first time and to reread and check for new information with each refill.
• Advise patient to drink plenty of fluids and maintain a high fiber intake to minimize risk of constipation.
• Advise patient to take each dose with liquid and a meal.
• Caution patient to swallow tablets whole and not to crush, chew, or break tablets.
• Inform patient that constipation, gas, nausea, and heartburn may occur but usually go away with continued therapy. Advise patient to notify health care provider if these effects become bothersome, or if bleeding or unusual bruising occurs.
• Inform patient that drug helps control, but not does cure, lipid abnormality and to continue taking drug as prescribed when lipid levels are lowered.
• Caution patient not to change the dose or stop taking unless advised by health care provider.
• Instruct patient to continue taking other cholesterol-lowering medications as prescribed by health care provider.
• Emphasize to patient importance of other modalities on cholesterol control such as dietary changes (reduced saturated fat intake, increase soluble fiber intake); weight control; regular exercise; smoking cessation.