colesevelam

General

Pronunciation:
koe-le-sev-e-lam

Trade Name(s)

• Lodalis 
• Welchol

Ther. Class.

lipid-lowering agents

Pharm. Class.

bile acid sequestrants

Indications

• Adjunctive therapy to diet and exercise for the reduction of LDL cholesterol (LDL-C) in patients with primary hypercholesterolemia; may be used alone or in combination with statins.
• Adjunctive therapy to diet and exercise for the reduction of LDL cholesterol in children 10–17 yr with heterozygous familial hypercholesterolemia if diet therapy fails (LDL-C remains ≥190 mg/dL or remains ≥160 mg/dL [with family history of premature cardiovascular disease or ≥2 risk factors for cardiovascular disease]); may be used alone or in combination with statin.
• Adjunctive therapy to diet and exercise to improve glycemic control in patients with type 2 diabetes.

Action

• Binds bile acids in the GI tract.
• Results in increased clearance of cholesterol.
• Mechanism for lowering blood glucose unknown.

Therapeutic Effect(s):

Decreased LDL-C and blood glucose.

Pharmacokinetics

Absorption: Not absorbed; action is primarily local in the GI tract.

Distribution: Unknown.

Metabolism and Excretion: Unknown.

Half-life: Unknown.

TIME/ACTION PROFILE (LDL-C lowering effect)

Contraindication/Precautions

Contraindicated in:

• Hypersensitivity;
• Bowel obstruction;
• Triglycerides >500 mg/dL;
• History of pancreatitis due to hypertriglyceridemia.

Use Cautiously in:

• Triglycerides >300 mg/dL;
• Dysphagia, swallowing disorders, severe GI motility disorders, or major GI tract surgery;
• Phenylketonuria (oral suspension packets contain phenylalanine);
• OB:   Use during pregnancy not expected to result in fetal exposure (not systemically absorbed);
• Lactation:  Not expected to be present in breast milk (not systemically absorbed);
• Pedi:   Safety and effectiveness not established in children <10 yr (hyperlipidemia) or <18 yr (type 2 diabetes).

Adverse Reactions/Side Effects

GI: constipation, dyspepsia

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

• May ↓ absorption and effectiveness of  glyburide,  glimepiride,  glipizide,  levothyroxine,  olmesartan,  phenytoin,  cyclosporine,  warfarin, and  estrogen-containing oral contraceptives ; give ≥4 hr before colesevelam.
• May ↑ levels and risk of toxicity of  metformin extended-release.

Route/Dosage

Hyperlipidemia

PO (Adults and Children  10–17 yr): 6 tablets once daily  or  3 tablets twice daily  or  one 3.75-g packet once daily.

Type 2 Diabetes

PO (Adults): 6 tablets once daily  or  3 tablets twice daily  or  one 3.75-g packet once daily.

Availability (generic available)

Granules for oral suspension: 3.75 g/packet (contains 27 mg phenylalanine)

Tablets: 625 mg

Assessment

• Hypercholesterolemia: Obtain a diet history, especially in regard to fat consumption.
• Type 2 Diabetes: Observe for signs and symptoms of hypoglycemic reactions (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety).
• Monitor for signs and symptoms of bowel obstruction (constipation, obstipation, abdominal distention, abdominal pain, nausea, vomiting, watery diarrhea); discontinue therapy if severe abdominal pain or severe constipation occurs.

Lab Test Considerations:

Monitor lipid panel before initiating, 4–6 wk after starting, and periodically during therapy. May cause hypertriglyceridemia.

• Monitor serum glucose and A1c periodically during therapy in patients with diabetes.

Implementation

• Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
• May be administered at the same time as an HMG-CoA reductase inhibitor.
• PO Administer once or twice daily with meals. Should be taken with a liquid. For oral suspension, empty the entire contents of one packet into a glass or cup. Add 1 cup (8 ounces) of water, fruit juice, or a diet soft drink; do not take in dry form to avoid esophageal distress.
  • Pedi:  Due to tablet size, oral suspension is recommended for use in children.

Patient/Family Teaching

• Explain the purpose and side effects to patient. Instruct patient to take medication as directed; do not skip doses or double up on missed doses. Advise patient to read  Patient Information  before starting and with each Rx refill in case of changes.
• Advise patients taking oral vitamin supplementation or oral contraceptives to take their vitamins ≥4 hr prior to colesevelam, especially those taking warfarin. Colesevelam may ↓ absorption of fat-soluble vitamins A, D, E, and K.
• Instruct patient to consume a diet that promotes bowel regularity. Patients should be instructed to promptly discontinue colesevelam and notify health care professional if severe abdominal pain or severe constipation or symptoms of acute pancreatitis (severe abdominal pain with or without nausea and vomiting) occur.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking other Rx, OTC, or herbal products.
• Hypercholesterolemia: Advise patient that this medication should be used in conjunction with diet restrictions (fat, cholesterol, carbohydrates, alcohol), exercise, and cessation of smoking.
• Diabetes:

  Explain to patient that this medication controls hyperglycemia but does not cure diabetes. Therapy is long term.

  • Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to drink a glass of orange juice or ingest 2–3 teaspoons of sugar, honey, or corn syrup dissolved in water or an appropriate number of glucose tablets and notify health care professional.
  • Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hypoglycemic or hyperglycemic episodes.
  • Instruct patient in proper testing of serum glucose and ketones. These tests should be closely monitored during periods of stress or illness and health care professional notified if significant changes occur.
  • Advise patient to carry a form of sugar (sugar packets, candy) and identification describing disease process and medication regimen at all times.
  Rep:  Insulin is the recommended method of controlling blood sugar during pregnancy. Advise women of reproductive potential that colesevelam may ↓ effectiveness of oral contraceptives; advise patients to take oral contraceptives ≥4 hr prior to taking colesevelam or use a form of contraception other than oral contraceptives and to notify health care professional promptly if pregnancy is planned or suspected.

Evaluation/Desired Outcomes

• Decrease in serum total cholesterol, LDL-C, apolipoprotein, and blood glucose levels.
• Control of blood glucose levels without the appearance of hypoglycemic or hyperglycemic episodes.