colesevelam

REMS

Adjunctive therapy to diet and exercise for the reduction of LDL cholesterol 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 cholesterol 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 effects:

Decreased cholesterol and blood glucose.

Pharmacokinetics ⬆ ⬇

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

Distribution: Unknown.

Metabolism/Excretion: Unknown.

Half-Life: Unknown.

Time/Action Profile ⬆ ⬇

(cholesterol-lowering effect)

ROUTE	ONSET	PEAK	DURATION
PO	24–48 hr	2 wk	unknown

Contraind./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).

Adv. Reactions/Side Effects ⬆ ⬇

GI: constipation, dyspepsia

Interactions ⬆ ⬇

Drug-drug:

May ↓ absorption of glyburide, glimepiride, glipizide, levothyroxine, olmesartan, phenytoin, cyclosporine, warfarin, and estrogen-containing oral contraceptives (give ≥4 hr before colesevelam).
May ↑ levels 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 patient for signs and symptoms of hypoglycemic reactions (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety).

Lab Test Considerations:

Monitor serum total cholesterol, LDL, and triglyceride levels before initiating, 4–6 wk after starting, and periodically during therapy. May cause hypertriglyceridemia.
- Monitor serum glucose and glycosylated hemoglobin 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.
PO: Administer once or twice daily with meals. Colesevelam 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 oz) of water, fruit juice, or a diet soft drink; do not take in dry form to avoid esophageal distress.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed; do not skip doses or double up on missed doses.
Advise patients taking oral vitamin supplementation or oral contraceptives to take their vitamins at least 4 hr prior to colesevelam, especially those taking warfarin. Colesevelam may decrease 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.
Rep: Insulin is the recommended method of controlling blood sugar during pregnancy. Counsel females of reproductive potential that colesevelam may reduce efficacy of oral contraceptives; advise patients to take oral contraceptives at least 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.
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 tsp 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.

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇