Not scheduled (OTC); high-dose formulations may require prescription

Oral

• Powder for oral suspension: 4 g per sachet

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Hypercholesterolaemia (Type IIa and IIb) — Adjunct to Diet Therapy

Parameter Details

Starting dose 4 g orally once or twice daily

Titration Increase by 4 g/day at 4-week intervals based on lipid response and GI tolerability

Usual maintenance dose 8–12 g/day in 1–2 divided doses

Maximum dose 24 g/day

Clinical Notes:

• May be used as monotherapy for LDL lowering in statin-intolerant patients

• Can be added to statin therapy for additional LDL reduction

• Take other oral medications ≥1 hour before OR ≥4–6 hours after cholestyramine

• Best taken before meals

1. Pruritus Due to Partial Biliary Obstruction

(Cholestatic liver diseases, primary biliary cholangitis)

Parameter Details

Starting dose 4 g orally once or twice daily

Titration Adjust based on symptom control and tolerability

Usual maintenance dose 8–12 g/day in 2–4 divided doses

Maximum dose 16 g/day

Clinical Notes:

• Symptom relief typically occurs within 1–3 days of initiation

• Monitor for fat-soluble vitamin deficiency with long-term use

• Not effective in complete biliary obstruction

Secondary Indications — Adults Only (Off-label)

Indication Dose Duration Remarks

Chronic diarrhoea due to bile acid malabsorption (post-cholecystectomy, Crohn's ileal resection) — OFF-LABEL 4–8 g once or twice daily Until symptom control; reassess periodically Specialist only (Gastroenterologist); supported by case series and international practice

Digitalis toxicity (adjunct therapy) — OFF-LABEL 4 g every 4–6 hours until levels decline Short-term under specialist supervision Specialist only; based on anion exchange binding of cardiac glycosides

PAEDIATRIC DOSING (Specialist Only)

Primary Indication: Familial Hypercholesterolaemia (Age ≥6 years)

6–10 years 4 g once daily Increase by 4 g/day every 4 weeks if tolerated 4–8 g/day in 1–2 divided doses 8 g/day

10 years 4 g once daily Increase by 4 g/day every 4 weeks based on LDL-C response 8–12 g/day in 1–2 divided doses 12 g/day

Monitoring:

• GI tolerance (constipation, bloating)

• Growth parameters

• Fat-soluble vitamin levels (A, D, E, K) with long-term use

Secondary Indications — Paediatric (Off-label)

Indication Dose Duration Remarks

Cholestatic pruritus (Alagille syndrome, PFIC) — OFF-LABEL 240 mg/kg/day in 2–4 divided doses; not exceeding 8 g/day Based on symptom control; long-term use Specialist only (Paediatric Hepatologist); Indian hepatology practice

⚠️ Not recommended below 6 years of age except under specialist supervision with documented justification.

No dose adjustment required — cholestyramine is not systemically absorbed.

Safe in all stages of CKD including dialysis.

• Complete biliary obstruction

• Known hypersensitivity to cholestyramine or any excipient

• Severe chronic constipation or intestinal obstruction

• Primary hypertriglyceridaemia (Type I, IV, V) — risk of significant triglyceride elevation

• May worsen pre-existing hypertriglyceridaemia

• Significantly reduces absorption of concurrently administered oral medications

• Risk of fat-soluble vitamin (A, D, E, K) deficiency with prolonged use

• Use with caution in patients with chronic constipation or GI motility disorders

• Phenylketonuria — some formulations may contain aspartame

Parameter Details

Safety Category Generally considered safe — not systemically absorbed

Preferred alternatives Statins are contraindicated in pregnancy; cholestyramine is preferred for lipid control if required

When to use Severe hypercholesterolaemia or intractable pruritus of cholestasis not responsive to other measures

Monitoring Maternal nutritional status; fat-soluble vitamin supplementation recommended

Parameter Details

Compatibility Compatible with breastfeeding

Drug levels in milk Not excreted into breastmilk (no systemic absorption)

Preferred alternatives Not applicable — cholestyramine is appropriate choice

Infant monitoring Monitor infant growth and vitamin status if maternal long-term use

Parameter Recommendation

Starting dose 4 g once daily

Titration Slower titration advised (every 6–8 weeks)

Special considerations Increased risk of constipation and intestinal obstruction; ensure adequate hydration; polypharmacy increases drug interaction risk

Additional risks Impaired GI motility; risk of faecal impaction

Drug Mechanism Clinical Effect Recommendation

Levothyroxine Binding in GI tract Markedly reduced thyroid hormone absorption Administer levothyroxine ≥4 hours before or after cholestyramine

Warfarin Binding + decreased vitamin K absorption Variable anticoagulant effect — may increase or decrease INR Monitor INR closely; separate dosing by ≥4–6 hours

Digoxin Binding in GI tract Reduced digoxin absorption and efficacy Administer digoxin ≥2 hours before or ≥6 hours after cholestyramine

Oral contraceptives Binding in GI tract Reduced contraceptive efficacy with chronic use Consider alternative contraception or separate dosing

Drug Interaction Recommendation

Thiazide diuretics, furosemide May reduce absorption Separate administration by ≥4 hours

Statins Reduced statin absorption Administer statin ≥1 hour before or ≥4 hours after cholestyramine

Iron supplements Reduced iron absorption Stagger dosing; monitor for iron deficiency

Fat-soluble vitamins (A, D, E, K) Reduced absorption Supplement if long-term therapy; give vitamins at separate time

Methotrexate May reduce absorption Monitor methotrexate efficacy; separate dosing

• Constipation (most frequent; dose-related)

• Bloating and flatulence

• Nausea

• Abdominal discomfort and cramping

• Unpleasant taste and gritty texture (affects adherence)

• Heartburn

• Intestinal obstruction — discontinue immediately if suspected; more common in elderly or those with pre-existing constipation

• Steatorrhoea — with prolonged high-dose use

• Fat-soluble vitamin deficiency (A, D, E, K) — bleeding diathesis (vitamin K), osteomalacia (vitamin D), night blindness (vitamin A)

• Hyperchloraemic metabolic acidosis — rare; reported primarily in paediatric patients with renal dysfunction

Phase Parameters

Baseline Lipid profile (total cholesterol, LDL-C, triglycerides, HDL-C), liver function tests, serum vitamin levels (if long-term anticipated), bowel habit history

During titration Lipid profile every 4–6 weeks; GI symptoms; INR if on anticoagulants

Long-term use Lipid profile every 3–6 months; fat-soluble vitamin levels annually; LFTs periodically

• Questran®

• Questran Lite®

• Choltran®

• Cholestyr®

Note: Limited brand availability in India compared to other markets.

Note: Not included in NLEM 2022; not NPPA price-controlled; prices vary by brand.

• Administration: Always mix powder thoroughly with water, juice, or pulpy fruit before consumption — never take dry powder; chilling the mixture may improve palatability

• Drug interaction timing: Universal rule — take all other oral medications ≥1 hour BEFORE or ≥4–6 hours AFTER cholestyramine

• Triglyceride caution: Avoid as monotherapy in patients with triglycerides >300 mg/dL — may cause significant TG elevation

• Vitamin supplementation: Prescribe prophylactic fat-soluble vitamin supplements (A, D, E, K) for patients on long-term therapy (>3 months)

• Constipation management: Increase dietary fibre and fluid intake; consider stool softeners if constipation develops

• Pregnancy advantage: One of the few lipid-lowering agents safe in pregnancy when lipid control is essential

hyperlipidaemia; bile acid sequestrant; cholestatic pruritus; LDL lowering; statin-intolerant; pregnancy-safe; renal-safe; drug interactions; vitamin deficiency; paediatric familial hypercholesterolaemia

RxIndia v1.0 — 10 Jun 2025

• CDSCO approved product labels

• Indian Pharmacopoeia

• API Textbook of Medicine — Lipid Disorders, Hepatobiliary Disease

• AIIMS Treatment Protocols — Gastroenterology, Cardiology

• ICMR Guidelines on Dyslipidaemia Management

• Goodman & Gilman's The Pharmacological Basis of Therapeutics

• Harrison's Principles of Internal Medicine

• WHO Model Formulary (supportive)