Schedule H (when used as dyslipidaemia therapy)

Oral

• Immediate-release tablets: 50 mg, 100 mg, 250 mg, 500 mg

• Extended-release tablets: 500 mg, 750 mg, 1000 mg

• Nutritional supplement formulations: 50 mg, 100 mg (available as OTC)

Note: Laropiprant combinations are NOT AVAILABLE in India (withdrawn globally in 2013). Niacin-statin FDCs have limited availability.

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Dyslipidaemia (Type IIa, IIb, IV hyperlipoproteinaemias)

Immediate-Release Formulation:

Parameter Dosing

Starting dose 250 mg orally once or twice daily with meals

Titration Increase by 250 mg every 4–7 days as tolerated

Usual maintenance dose 1.5–3 g/day in 2–3 divided doses

Maximum dose 6 g/day

Extended-Release Formulation:

Parameter Dosing

Starting dose 500 mg once daily at bedtime with a low-fat snack

Titration Increase by 500 mg every 4 weeks

Usual maintenance dose 1–2 g once daily at bedtime

Maximum dose 2 g once daily

Clinical Notes:

• ER formulations preferred due to reduced flushing

• Use as adjunct therapy; not first-line monotherapy for primary hypercholesterolaemia

• Do not substitute IR for ER formulations at equivalent doses (hepatotoxicity risk differs)

• Monitor liver enzymes and glucose at each titration step

1. Pellagra (Niacin Deficiency)

Parameter Dosing

Starting dose 100 mg orally three times daily

Titration Not applicable

Usual maintenance dose 300–500 mg/day in divided doses

Maximum dose 500 mg/day

Duration Until symptomatic resolution (typically 2–4 weeks), followed by dietary correction

Clinical Notes:

• Associated with dermatitis, diarrhoea, and dementia (3 D's)

• Nicotinamide may be preferred as it lacks vasodilatory flushing

Secondary Indications – Adults Only (Off-label)

Indication Dose Duration Notes Evidence

Prevention of recurrent pancreatitis due to severe hypertriglyceridaemia ER 1–2 g daily at bedtime Long-term Specialist only – OFF-LABEL Indian lipid specialist practice; AIIMS protocols

Isolated low HDL-cholesterol (when other therapies inadequate) ER 1–2 g daily Long-term Specialist only – OFF-LABEL Indian Lipid Association expert opinion

PAEDIATRIC DOSING (Specialist Only)

Primary Indication: Pellagra (Nutritional Niacin Deficiency)

<6 months 5–10 mg/day Single or divided 10 mg/day

6 months–2 years 50–150 mg/day 2–3 divided doses 150 mg/day

2–12 years 100–300 mg/day 2–3 divided doses 300 mg/day

12 years 300–500 mg/day 2–3 divided doses 500 mg/day

Safety Monitoring:

• Assess for flushing, gastrointestinal upset

• Monitor liver enzymes if treatment exceeds 4 weeks

• Check blood glucose in children with diabetes risk

Minimum Age: No absolute minimum for pellagra treatment; use appropriate age-based dosing

Secondary Indications – Paediatrics (Off-label)

Indication Dose Notes Evidence

Familial dyslipidaemia Start 100–250 mg/day; titrate slowly to 500–1000 mg/day Specialist only – OFF-LABEL. Only under paediatric endocrinologist or lipidologist Limited paediatric data; extrapolated from adult guidelines

Clear Statement: Not recommended for dyslipidaemia in children below 10 years except under specialist supervision. For pellagra, use is acceptable at any age with appropriate dosing.

CrCl >60 mL/min No adjustment required

CrCl 30–60 mL/min Use with caution; standard dosing acceptable

CrCl <30 mL/min Reduce dose; avoid high doses; increased accumulation risk

Haemodialysis Avoid immediate-release forms; ER may be used with reduced dose and close monitoring

Peritoneal dialysis Limited data; use with caution

• Active hepatic disease or unexplained persistent elevation of serum transaminases

• Active peptic ulcer disease

• Arterial haemorrhage

• Severe hypotension

• Known hypersensitivity to niacin or any excipients

• Severe or unstable gout

• Diabetes mellitus (may worsen glycaemic control)

• History of peptic ulcer disease (risk of reactivation)

• Gout or hyperuricaemia

• Unstable angina or acute phase of myocardial infarction

• Concurrent alcohol use (additive hepatotoxicity)

• Renal impairment

• Hypotension or autonomic dysfunction

• Concurrent statin therapy (myopathy risk)

• Phosphorus deficiency (niacin may reduce phosphorus levels)

Parameter Details

Safety Statement Nutritional doses (≤20 mg/day) are safe. Pharmacologic doses (>500 mg/day) lack adequate safety data; use only if benefit outweighs risk

Risk Category Not formally classified; treat as potentially risky at high doses

Preferred alternatives Dyslipidaemia treatment generally deferred in pregnancy; dietary management preferred

When may be used Pellagra treatment at therapeutic doses when dietary correction insufficient

Monitoring Liver function tests, blood glucose, fetal growth monitoring

Parameter Details

Compatibility Compatible with breastfeeding at physiological/nutritional doses

Pharmacologic doses Avoid doses >1 g/day; insufficient safety data

Drug levels in milk Low at nutritional doses; unknown at pharmacologic doses

Preferred alternatives Nicotinamide for pellagra (less flushing)

Infant monitoring Flushing, rash, irritability, poor feeding (rare)

Parameter Recommendation

Starting dose IR: 250 mg once daily; ER: 500 mg at bedtime

Titration Slower than standard — increase every 2–4 weeks

Special risks Orthostatic hypotension, hepatic dysfunction, glucose intolerance, myopathy (especially with statins)

Monitoring Blood pressure, liver enzymes, fasting glucose, uric acid more frequently

Interacting Drug Effect Management

Statins (simvastatin, lovastatin, atorvastatin) Increased risk of myopathy and rhabdomyolysis Use lowest effective doses of both; avoid simvastatin >20 mg/day with niacin; monitor CK

Alcohol Additive hepatotoxicity; increased flushing Avoid or minimise alcohol consumption

Gemfibrozil Increased myopathy risk Avoid combination if possible

Vasodilators / Antihypertensives Additive hypotension Monitor blood pressure; caution in elderly

Interacting Drug Effect Management

Warfarin May enhance anticoagulant effect Monitor INR more frequently

Bile acid sequestrants (cholestyramine, colestipol) Reduced niacin absorption Administer niacin ≥4 hours before or 1 hour after

Antidiabetic agents Niacin may impair glycaemic control Monitor blood glucose; adjust antidiabetic dose as needed

Isoniazid Additive hepatotoxicity; may interfere with niacin metabolism Regular LFT monitoring

Valproate Additive hepatotoxicity risk Monitor liver function closely

Aspirin Reduces flushing (beneficial interaction) Low-dose aspirin 30 min before niacin can minimise flushing

• Flushing and warmth (very common, especially with IR forms)

• Pruritus

• Headache

• Gastrointestinal upset (nausea, vomiting, diarrhoea)

• Elevated blood glucose

• Elevated uric acid

• Tingling sensation

Adverse Effect Notes

Hepatotoxicity More common with sustained-release formulations; may present as elevated transaminases, jaundice, or fulminant hepatic failure; discontinue if ALT >3× ULN

Myopathy / Rhabdomyolysis Especially with concurrent statin use; monitor for muscle pain, weakness, dark urine

Macular oedema Rare; may cause blurred vision; reversible on discontinuation

Severe hypotension Particularly with concurrent antihypertensives

Peptic ulcer exacerbation Monitor for GI bleeding

Atrial fibrillation Rare; reported at high doses

Long-term LFTs every 3–6 months; lipid profile every 3–6 months; fasting glucose and HbA1c every 6 months; uric acid annually

Clinical Symptoms of myopathy, flushing tolerance, blood pressure

• Nialip (USV)

• Nicotinic Acid IP (various manufacturers)

• Niacin-SR (extended-release, various)

• Vitamin B3 supplements (OTC) — multiple brands

Note: Therapeutic high-dose niacin products for dyslipidaemia have limited market availability in India. Laropiprant-niacin combinations are NOT AVAILABLE (withdrawn globally 2013).

• NLEM status: Listed for nutritional deficiency indications

• High-dose lipid-lowering formulations not under NPPA price control

• Flushing management: Administer with meals; pre-treatment with aspirin 325 mg 30 minutes prior reduces flushing; tolerance develops over 1–2 weeks

• Do not interchange IR and ER forms at equivalent doses — ER forms have different hepatotoxicity profiles

• Avoid abrupt discontinuation and re-initiation at high doses — always re-titrate from low dose

• Less preferred agent for dyslipidaemia in current practice due to adverse effect profile and lack of cardiovascular outcome benefit in statin-treated patients (AIM-HIGH, HPS2-THRIVE trials)

• Pellagra remains the clearest indication — nicotinamide is often preferred as it lacks flushing

• Baseline and periodic LFT monitoring is mandatory — hepatotoxicity can occur suddenly, especially with sustained-release preparations

niacin; nicotinic acid; dyslipidaemia; hypertriglyceridaemia; pellagra; HDL-raising; flushing; hepatotoxicity; vitamin B3; NLEM India

RxIndia v1.0 — 10 Jun 2025

• CDSCO product information

• Indian Pharmacopoeia (IP)

• NLEM 2022

• API Textbook of Medicine, 11th Edition

• AIIMS Hospital Formulary

• Indian Lipid Association Guidelines

• Goodman & Gilman's The Pharmacological Basis of Therapeutics

• WHO Guidelines on Micronutrient Deficiencies

• HPS2-THRIVE Collaborative Group (N Engl J Med 2014) — for evidence on cardiovascular outcomes

• AIM-HIGH Investigators (N Engl J Med 2011) — for evidence on niacin efficacy