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Cholestyramine

Bile acid sequestrant (anion-exchange resin) · Antilipidemic

Also known as Cholestyramine resin, Questran, Prevalite, LoCHOLEST, Cholesguard, Cholesta

START
4 g PO once–twice daily, mixed in fluid
TYPICAL MAX
24 g/day
STOP IF
Severe constipation/obstruction or bleeding (vit K)
WATCH
Bowel habit, fat-soluble vitamins, INR if on warfarin
CDSCO approvedSchedule HATC C10AC01
Dose laddermg/d
4kstart12kusual24kmax/day
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo dose adjustment (not absorbed)90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
1wONSET3wPEAK36s1dDURATION
ONSET
1w · LDL effect
PEAK
3w · max effect ~3 wk
36s · not absorbed
DURATION
1d · dosing-bound
EXCRETION
Faecal — resin–bile-acid complex
route + CYP
INTERACTIONS
9 major
SEVERE in our sources
PREGNANCY
Not systemically absorbed — acceptable; monitor fat-soluble vitamins.
FDA category + note
Top interactionssee all 12
  • LevothyroxineSevereDatabaseKimi deep-research + Cla
  • MycophenolateSevereDatabase
  • Mycophenolate MofetilSevereDatabaseDDInter
  • Mycophenolate SodiumSevereDatabase
Available in India

3 branded formulations. Look up specific brands in the Drugs workspace.

Mechanism

Non-absorbed resin that binds bile acids in the gut, interrupting enterohepatic recirculation; upregulates hepatic LDL receptors (lowering LDL-C) and increases faecal bile-acid excretion.

Indications

Primary hypercholesterolaemiaPruritus from partial biliary obstruction/cholestasisBile acid diarrhoeaAdjunct in some toxin/drug elimination (e.g., leflunomide washout)

Dosing

Adult
4 g PO once–twice daily initially; usual 12–24 g/day in 1–4 divided doses (mixed in fluid).
Pediatric
240 mg/kg/day in 2–3 divided doses (max ~8 g/day).
Renal adjustment
No adjustment (not absorbed).
Hepatic adjustment
No adjustment; ineffective in complete biliary obstruction.
Geriatric
Constipation risk; start low.
Max dose
24 g/day

Pharmacokinetics

Onset
LDL reduction within ~1–2 weeks; pruritus relief days
Peak effect
Maximal lipid effect ~2–4 weeks
Duration
Duration of dosing (not absorbed)
Half-life
Not applicable (non-absorbed resin)
Bioavailability
Negligible (acts in gut lumen)
Protein binding
Not applicable
Metabolism
Not metabolised
Excretion
Faecal (resin–bile-acid complex)

Contraindications

  • Complete biliary obstruction
  • Hypersensitivity
  • Caution in constipation/phenylketonuria (aspartame forms)

Side effects

Common
ConstipationBloating/flatulenceNauseaAbdominal discomfort
Serious
  • Fat-soluble vitamin (A,D,E,K) deficiency
  • Hyperchloraemic acidosis (children, high dose)
  • GI obstruction (rare)
  • Bleeding (vitamin K depletion)

Pregnancy & lactation

Pregnancy

Not systemically absorbed — acceptable; monitor fat-soluble vitamins.

Lactation

Not absorbed; compatible (monitor maternal vitamin status).

Drug interactions

Levothyroxine
Severe
Database

Resin binds thyroxine in gut

Separate by ≥4 h; monitor TSH

Source: Kimi deep-research + Cla

Mycophenolate
Severe
Database

40% reduction in MPA levels, rejection risk

Avoid combination.

Mycophenolate Mofetil
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Mycophenolate Sodium
Severe
Database

Significantly reduced MPA exposure (AUC), potentially leading to a substantial decrease in immunosuppressive efficacy and increased risk of rejection.

Avoid concomitant use if possible. If co-administration is unavoidable, separate administration by several hours (e.g., mycophenolate 2 hours before or 4-6 hours after cholestyramine) and closely monitor mycophenolate levels and clinical response. Significant dose increase of mycophenolate may be necessary.

Mycophenolic Acid
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Raloxifene
Severe
Database

Markedly reduced raloxifene absorption (interrupts enterohepatic recycling)

Do not co-administer; separate timing

Source: Kimi deep-research + Cla

Teriflunomide
Severe
Database

Drug interaction classified as: absorption, metabolism

Source: DDInter

Thyroxine
Severe
Database

Significantly decreased thyroxine efficacy, leading to severe hypothyroidism symptoms or increased TSH levels

Administer thyroxine at least 4-5 hours before or after cholestyramine. Monitor TSH levels closely and adjust thyroxine dose as needed.

Warfarin
Severe
Database

Reduced warfarin + vitamin K absorption

Separate dosing; monitor INR

Source: Kimi deep-research + Cla

Alirocumab
Moderate
Textbook

Reduced efficacy of statins.

Patients should take other medications 1 h before or 3 to 4 h after a dose of cholestyramine.

Source: G&G 14e · p738

Atorvastatin + Aspirin
Moderate
Textbook

Reduced efficacy of statins.

Patients should take other medications 1 h before or 3 to 4 h after a dose of cholestyramine.

Source: G&G 14e · p738

Evolocumab
Moderate
Textbook

Reduced efficacy of statins.

Patients should take other medications 1 h before or 3 to 4 h after a dose of cholestyramine.

Source: G&G 14e · p738

Related guidelines

Ask House about Cholestyramine

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-20 · House clinical team·Cockpit curated: 2026-05-20