Bile Acid Sequestrants
Severe
Database
Binds bile acid in gut
Separate by ≥4–6 h
Source: Kimi deep-research + Cla
Drug reference
Chenodeoxycholic Acid
Endogenous bile acid (oral) · Cholelitholytic Agent
Also known as Chenodiol, CDCA
START
CTX: 250 mg PO three times daily, titrate
TYPICAL MAX
~1500 mg/day (CTX); 16 mg/kg/day (gallstone)
STOP IF
Significant hepatotoxicity, severe diarrhoea, or gallstone calcification
WATCH
LFTs (baseline + periodic), urinary sterols (CTX), stool
CDSCO approvedSchedule HATC A05AA01
KDIGO 2024 + manufacturer label
- ONSET
- 30min · absorption
- PEAK
- 1.5h · Tmax
- t½
- 4h · t½ (apparent)
- DURATION
- 8h · TID dosing
EXCRETION
Mainly biliary/faecal; small renal
route + CYP
INTERACTIONS
6 major
SEVERE in our sources
PREGNANCY
Contraindicated (fetal harm).
FDA category + note
Top interactionssee all 10 →
- Bile Acid SequestrantsSevereDatabaseKimi deep-research + Cla
- LeflunomideSevereDatabaseDDInter
- LomitapideSevereDatabaseDDInter
- MipomersenSevereDatabaseDDInter
Mechanism
Replacement of an endogenous primary bile acid: suppresses hepatic cholesterol synthesis and reduces biliary cholesterol secretion (dissolving cholesterol gallstones); replaces deficient bile acids in cerebrotendinous xanthomatosis (CTX), normalising sterol metabolism.
Indications
Cerebrotendinous xanthomatosis (CTX)Dissolution of cholesterol gallstones (selected non-calcified, when surgery unsuitable)
Dosing
- Adult
- CTX: 250 mg PO 3 times daily (titrate). Gallstones: 13–16 mg/kg/day in divided doses for up to 24 months.
- Pediatric
- CTX: weight-based (specialist).
- Renal adjustment
- No specific adjustment.
- Hepatic adjustment
- Contraindicated in significant hepatic disease; monitor LFTs.
- Geriatric
- No specific adjustment.
- Max dose
- ~1500 mg/day (CTX) / 16 mg/kg/day (gallstone)
Pharmacokinetics
Onset
Biochemical correction over weeks (CTX); months (gallstone)
Peak effect
~1–2 h (Tmax serum)
Duration
Enterohepatic recirculation; dosing-dependent
Half-life
Short systemic; enterohepatic recycling
Bioavailability
Variable (~60% in healthy subjects)
Protein binding
High (~98% bile-acid binding proteins)
Metabolism
Hepatic; conjugation; bacterial 7-dehydroxylation in gut
Excretion
Mainly biliary/faecal; small renal
Contraindications
- Chronic active liver disease (hepatitis, cirrhosis)
- Bile-duct/gallbladder disease (non-functioning gallbladder, calcified stones)
- Pregnancy
- Hypersensitivity
Side effects
Common
Diarrhoea (dose-related)Transaminase elevationAbdominal discomfort
Serious
- Hepatotoxicity (significant ALT rise)
- Severe diarrhoea
- Gallstone calcification on therapy
Pregnancy & lactation
Pregnancy
Contraindicated (fetal harm).
Lactation
Avoid; limited data.
Drug interactions
Leflunomide
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Lomitapide
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Mipomersen
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Pexidartinib
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Teriflunomide
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Aluminium Containing Antacids
Moderate
Database
Adsorption of bile acid
Separate dosing
Source: Kimi deep-research + Cla
Clofibrate
Moderate
Database
Increase biliary cholesterol
Avoid concurrent for gallstone indication
Source: Kimi deep-research + Cla
Combined Hormonal Contraceptives
Moderate
Database
Increase biliary cholesterol
Reduce/discontinue if treating gallstones
Source: Kimi deep-research + Cla
Hepatotoxic Drugs
Moderate
Database
Additive hepatotoxicity
Monitor LFTs
Source: Kimi deep-research + Cla
2 additional low-confidence interactions hidden — those rows lack a documented mechanism or management plan in our sources.
Related guidelines
Ask House about Chenodeoxycholic Acid
Continue into a citation-backed clinical answer with the drug context already attached.
Sources: Katzung, BNF·Verified: 2026-05-20 · House clinical team·Cockpit curated: 2026-05-20