Dosing and uses of WelChol (colesevelam)
Adult dosage forms and 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
Pediatric dosage forms and 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
WelChol (colesevelam) adverse (side) effects
>10%
Constipation (9-11%)
1-10%
Dyspepsia (4.8%)
Myalgia (2%)
Asthenia (1.7%)
Accidental injury (1%)
Nausea (1%)
Flu syndrome (1%)
Hypertension (1%)
Hypoglycemia (1%)
Pharyngitis (1%)
Rhinitis (1%)
Postmarketing Reports
Increased seizure activity or decreased phenytoin levels in patients receiving phenytoin; administer phenytoin 4 hours before colesevelam
Reduced international normalized ratio (INR) in patients receiving warfarin; monitor INr
Elevated thyroid-stimulating hormone (TSH) level in patients receiving thyroid hormone replacement therapy; administer thyroid hormones 4 hours before colesevelam
GI: Bowel obstruction, dysphagia, esophageal obstruction, fecal impaction, pancreatitis, increased transaminase levels
Warnings
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 and lactation
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.
Pharmacology of WelChol (colesevelam)
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
Absorbed only to insignificant extent
Onset: 2 wk (lipid-lowering effect)
Elimination
Excretion: Feces, urine (trace amounts [0.05%])
