Colesevelam

Colesevelam comes as a tablet to take by mouth. It is usually taken once or twice a day with meals and a beverage. Your doctor will tell you how many tablets to take at each dose. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take colesevelam exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Continue to take colesevelam even if you feel well. Do not stop taking colesevelam without talking to your doctor.

Before taking colesevelam,

• tell your doctor and pharmacist if you are allergic to colesevelam or any other medications.
• tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: anticoagulants such as warfarin, insulin, and and verapamil (Calan SR).
• if you are taking phenytoin (Dilantin), glyburide, levothyroxine, oral contraceptives (birth control pills), or vitamins, take them at least 4 hours before colesevelam.
• tell your doctor if you have or have ever had blocked intestines,gastrointestinal surgery, triglyceride (fatty substance) levels greater than 500 mg/dL, or swelling of the pancreas caused by high levels of triglycerides in the blood. Your doctor will probably tell you not to take colesevelam.
• tell your doctor if you have or have ever had gastrointestinal problems, difficulty swallowing foods, triglyceride levels greater than 300 mg/dl, bleeding problems, and low amounts of fat-soluble vitamins (vitamins A, D, E, and K) in your body.
• tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking colesevelam, call your doctor.

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed dose.

Keep all appointments with your doctor and the laboratory. Your doctor will order certain lab tests to check your response to colesevelam.

Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.

Dosage Forms & Strengths

tablet

• 625mg

powder for oral suspension

• 3.75g

Hyperlipidemia

Reduction of elevated low-density lipoprotein (LDL) cholesterol (LDL-C) in adults with primary (Fredrickson type IIa) hyperlipidemia as adjunct to diet and exercise, either alone or in combination with a statin

Tablet: 1.875 g (3 tablets) PO q12hr with meals or 3.75 g (6 tablets) PO once daily with a meal

Oral suspension: 1.875 g (½ packet) PO q12hr or 3.75 g (1 packet) PO once daily, mixed with liquid

Overdose: Symptoms include gastrointestinal (GI) obstruction; treatment is supportive

Type 2 Diabetes Mellitus

Improvement of glycemic control in adults; taken in combination with insulin or oral antidiabetic agents

Tablet: 1.875 g (3 tablets) PO q12hr with meals or 3.75 g (6 tablets) PO once daily with a meal

Oral suspension: 1.875 g (½ packet) PO q12hr or 3.75 g (1 packet) PO once daily, mixed with liquid

Overdose: Symptoms include GI obstruction; treatment is supportive

Administration

Tablet: Take with meals and plenty of liquid

Oral suspension: Empty packet in 4-8 oz of water, fruit juice, or diet soft drink and stir; drink with meal(s)

May be coadministered with statins or administered at separate times

Dosage Forms & Strengths

tablet

• 625mg

powder for oral suspension

• 3.75g

Heterozygous Familial Hypercholesterolemia

Indication

• Reduction of LDL-C levels in boys and postmenarchal girls aged 10-17 years as adjunct to diet and exercise, either alone or in combination with statin after failure of adequate trial of diet therapy
• Diet therapy failure defined as either (a) LDL-C ≥190 mg/dL or (b) LDL-C ≥160 mg/dL with positive family history of premature cardiovascular disease (CVD) or ≥2 other CVD risk factors present

<10 years: Safety and efficacy not established

>10 years: 3.75 g/day PO once daily or divided q12hr

Contraindications

Current bowel obstruction or risk of bowel obstruction

Serum triglyceride (Tg) >500 mg/dL (5.65 mmol/L)

History of hypertriglyceridemia-induced pancreatitis

Cautions

Dysphagia (use oral suspension; large tablets can obstruct esophagus)

Not recommended in gastroparesis (constipating effects)

Not for glycemic control in type I diabetes mellitus or diabetic ketoacidosis

May reduce absorption of some drugs and nutrients; administer drugs with known interactions or narrow therapeutic index 4 hours before colesevelam

Not studied in Fredrickson I, III, IV, or V hyperlipidemia

May exacerbate preexisting constipation (initiate therapy at lower dosage in patients with history of constipation)

Oral suspension contains phenylalanine

Secondary causes of hyperlipidemia must be ruled out before therapy is initiated

Can increase Tg level, particularly when used with insulin or sulfonylureas; marked hypertriglyceridemia can cause acute pancreatitis

Bile acid sequestrants may decrease absorption of fat-soluble vitamins

Pregnancy category: B

Lactation: Drug not expected to be excreted in breast milk

Pregnancy Categories

A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA:Information not available.

Tablet: 625 mg, white.

Colesevelam should be stored at room temperature, away from heat and light, and out of the reach of children.

Colesevelam is a prescription medication used to treat elevated cholesterol alone or in combination with other drugs. Colesevelam may also be used to treat type II diabetes. Colesevelam belongs to group of drugs called bile acid sequetrants which reduce cholesterol levels by binding bile acids that are then removed from your body.

The medication comes in both a tablet and packets for oral suspension that are taken by mouth either once or twice a day based on your doctor’s instructions with a meal and a liquid.

Common side effects of colesevalam are gas, constipation, nausea, diarrhea and abdominal pain.

Colesevelam is part of the drug class:

• Bile acid sequestrants

Lipid lowering: Therapeutic: ~2 weeks

Reduction of hemoglobin A1C (Type II diabetes): 4-6 weeks initial onset; 12-18 weeks maximal effect

No dosage adjustments necessary; not absorbed from the gastrointestinal tract.

Granules for oral suspension: Empty 1 packet into a glass; add 1/2-1 cup (4-8 ounces) of water, fruit juice, or a diet soft drink and mix well.

Educate the patient on dietary guidelines.

Granules for oral suspension: Administer with meal(s). Powder is not to be taken in dry form (to avoid GI distress).

Tablets: Administer with meal(s) and a liquid. Due to tablet size, it is recommended that any patient who has trouble swallowing tablets should use the oral suspension form.

Animal studies have failed to reveal evidence of fetal harm. There are no controlled data in human pregnancy. Requirements for vitamins and other nutrients are increased during pregnancy, however, the effect of this drug on the absorption of fat-soluble vitamins has not been studied in pregnant women. US FDA pregnancy category B: Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women.

This drug should be used during pregnancy only if clearly needed. US FDA pregnancy category: B