colesevelam (Rx)

Brand and Other Names:WelChol
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 625mg

powder for oral suspension

  • 3.75g/packet

chewable bar

  • 3.75g

Hyperlipidemia

Indicated as adjunctive therapy to diet and exercise to reduce elevated low-density lipoprotein cholesterol (LDL-C) in adults with primary hyperlipidemia

Tablet: 1.875 g (3 tablets) PO q12hr or 3.75 g (6 tablets) PO qDay

Oral suspension: 1.875 g (½ packet) PO q12hr or 3.75 g (1 packet) PO qDay

Chewable bar: 3.75 g (1 bar) PO qDay

Type 2 Diabetes Mellitus

Indicated as adjunctive therapy to improve of glycemic control in adults

Tablet: 1.875 g (3 tablets) PO q12hr or 3.75 g (6 tablets) PO qDay

Oral suspension: 1.875 g (½ packet) PO q12hr or 3.75 g (1 packet) PO qDay

Chewable bar: 3.75 g (1 bar) PO qDay

Dosing Considerations

Obtain lipid panel, including triglycerides (TG) levels and non-HDL-C, before starting treatment; contraindicated in patients with TG levels >500 mg/dL

Limitations of use

  • Should not be used for treatment of type 1 diabetes or diabetic ketoacidosis
  • Effect of colesevelam on cardiovascular morbidity and mortality not determined
  • Not studied
    • Type 2 diabetes in combination with a dipeptidyl peptidase 4 inhibitor
    • Fredrickson Type I, III, IV, and V dyslipidemia

Dosage Forms & Strengths

tablet

  • 625mg

powder for oral suspension

  • 3.75g/packet

chewable bar

  • 3.75g

Heterozygous Familial Hypercholesterolemia

Indicated to reduce LDL-C levels in boys and postmenarchal girls (10-17 years) with heterozygous familial hypercholesterolemia (HeFH) who are unable to reach LDL-C target levels despite an adequate trial of dietary therapy and lifestyle modification

<10 years: Safety and efficacy not established

10-17 years

  • Tablet: 1.875 g (3 tablets) PO q12hr or 3.75 g (6 tablets) PO qDay
  • Oral suspension: 1.875 g (½ packet) PO q12hr or 3.75 g (1 packet) PO qDay
  • Chewable bar: 3.75 g (1 bar) PO qDay
  • Due to tablet size, oral suspension is recommended for use in the pediatric population

Dosing Considerations

Obtain lipid panel, including triglycerides (TG) levels and non-HDL-C, before starting treatment; contraindicated in patients with TG levels >500 mg/dL

Limitations of use

  • Should not be used for treatment of type 1 diabetes or diabetic ketoacidosis
  • Effect of colesevelam on cardiovascular morbidity and mortality not determined
  • Not studied
    • Type 2 diabetes in combination with a dipeptidyl peptidase 4 inhibitor
    • Fredrickson Type I, III, IV, and V dyslipidemia
    • Children <10 years or in premenarchal girls
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Interactions

Interaction Checker

and colesevelam

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    Interactions Found

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            Adverse Effects

            >10%

            Constipation (6.5-11%)

            1-10%

            Dyspepsia (2.8-8.3%)

            Headache (3.9-7.6%)

            Nasopharyngitis (5.4-6.2%)

            Upper respiratory tract infection (4.9%)

            Nausea (4.2%)

            Influenza (3.8%)

            Nausea (2.6-3.8%)

            Accidental injury (3.7%)

            Asthenia (3.6%)

            Hypoglycemia (3.4%)

            Pharyngitis (3.2%)

            Flu syndrome (3.2%)

            Rhinitis (3.2%)

            Fatigue (3.9%)

            Hypertension (2.6%)

            Creatine phosphokinase increase (2.3%)

            Rhinitis (2.3%)

            Vomiting (2.3%)

            Back pain (2.3%)

            Myalgia (2.1%)

            Postmarketing Reports

            Gastrointestinal: Bowel obstruction (in patients with a history of bowel obstruction or resection), dysphagia or esophageal obstruction (occasionally requiring medical intervention), fecal impaction, pancreatitis, abdominal distension, exacerbation of hemorrhoids, and increased transaminases

            Laboratory abnormalities: Hypertriglyceridemia

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            Warnings

            Contraindications

            Serum TG concentrations >500 mg/dL

            History of hypertriglyceridemia-induced pancreatitis

            History of bowel obstruction

            Cautions

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

            May increase serum TG concentrations, hypertriglyceridemia can cause acute pancreatitis

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

            Postmarketing cases of bowel obstruction have occurred; not recommended in gastroparesis (constipating effects)

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

            Oral suspension contains phenylalanine

            Drug interactions overview

            • May reduce absorption of some drugs and nutrients; administer drugs with known interactions or narrow therapeutic index 4 hr before colesevelam
            • Bile acid sequestrants may decrease absorption of fat-soluble vitamins; administer vitamin at least 4 hr prior to colesevelam
            • In vivo drug interactions studies showed a decrease in exposure of ethinyl estradiol, norethindrone, olmesartan, and sulfonylureas when coadministered with colesevelam; also showed increase in metformin ER when coadministered colesevelam
            • Adverse reactions resulting from coadministration with colesevelam
              • Increased seizure activity or decreased phenytoin levels in patients receiving phenytoin
              • Reduced INR in patients receiving warfarin therapy; monitor INR
              • Elevated thyroid-stimulating hormone (TSH) in patients receiving thyroid hormone replacement therapy; administer thyroid hormone replacement therapy 4 hr prior to colesevelam
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            Pregnancy & Lactation

            Pregnancy

            There are no adequate and well-controlled studies of colesevelam hydrochloride use in pregnant women

            In the postmarketing setting, there have been reports of pregnancy and a causal association with congenital anomalies has not been established

            Contraception

            • Coadministration with colesevelam and oral contraceptives may reduce efficacy of oral contraceptives; advise patients to take oral contraceptives at least 4 hr prior to taking therapy

            Lactation

            Not absorbed systemically by mother following oral administration, and breastfeeding is not expected to result in exposure of child to drug

            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.

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            Pharmacology

            Mechanism of Action

            Forms complex with bile acids that is not absorbed through intestine; inhibits enterohepatic reuptake of intestinal bile salts, and this, in turn, increases fecal loss of bile salt-bound LDL and consequently reduces serum cholesterol in patients with primary hypercholesterolemia

            Absorption

            Colesevelam HCl is a hydrophilic, water-insoluble polymer not hydrolyzed by digestive enzymes and is not absorbed

            Distribution

            Distribution is limited to the gastrointestinal tract

            Metabolism

            Not metabolized systemically and does not interfere with systemic drug-metabolizing enzymes (eg, CYP450)

            Elimination

            Excretion: Urine (0.05%)

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            Administration

            Oral Administration

            Tablet: Take with meals and plenty of liquid; use oral suspension if patient has difficulty swallowing tablets (eg, pediatric patients)

            Oral suspension: Empty packet in 4-8 oz of water, fruit juice, or diet soft drink and stir; drink with meal(s); do not take oral suspension in dry form

            Chewable bar: Take with meals; each chewable bar contains ~80 calories

            May be coadministered with statins or administered at separate times; monitor lipid levels within 4-6 weeks after initiation

            Storage

            Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F)

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            Formulary

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
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            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.