Colesevelam

WELCHOL

What it isBile acid sequestrant; hyperlipidemia and type 2 diabetes.

Why this oneBetter tolerated and less drug-binding than cholestyramine, and it lowers A1c as well as LDL.

What limits itIt still binds levothyroxine and glyburide. Constipation; it raises triglycerides.

FDA-approved for

FDA dosing	Population	Start	Target	Max
Primary hyperlipidemia	Adults	3.75 g/day (6 tab QD or 3 tab BID)	3.75 g/day	3.75 g/day
Primary hyperlipidemia (HeFH)	Boys & postmenarchal girls 10–17 y	3.75 g/day	3.75 g/day	3.75 g/day
Type 2 diabetes mellitus	Adults	3.75 g/day	3.75 g/day	3.75 g/day

Renal Undefined

Hepatic Undefined

Take with a meal and liquid
Obtain lipid/TG levels before starting
For difficulty swallowing tablets, use oral suspension (also preferred in pediatrics due to tablet size)
Give other drugs at least 4 hours before colesevelam; oral vitamins at least 4 hours before

Can increase triglycerides; hypertriglyceridemia may cause acute pancreatitis
Bowel obstruction; not recommended in gastroparesis, GI motility disorders, or after major GI surgery
May decrease absorption of fat-soluble vitamins (vitamin K risk in warfarin/malabsorption patients)
May decrease absorption of concomitant oral drugs

Pregnancy Not absorbed systemically; fetal exposure not expected; data insufficient

Lactation Undefined

NO BOXED WARNINGS

Principal riskBinds levothyroxine and glyburide; raises triglycerides

Cost, est. cash$5–$150/month

Generic entry2018

Therapeutic safety burden0 / 4

Overdose danger0 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk0 / 4

Legacy pregnancy categoryC

Defining liabilityLocal irritation, sensitization or administration-site injury; negligible systemic toxicity at usual use.