Schedule H

Oral

• Tablets: 50 mg, 100 mg

• Sustained-release Tablets: 150 mg (limited availability)

• Oral Suspension: NOT AVAILABLE in India

• Injection: NOT AVAILABLE in India

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Functional Dyspepsia (Postprandial Distress Syndrome)

Parameter Recommendation

Starting dose 50 mg orally three times daily, 15–30 minutes before meals

Titration Not usually required

Usual maintenance dose 150 mg/day (50 mg TID)

Maximum dose 300 mg/day (100 mg TID)

Duration: 4–8 weeks; reassess need after 8 weeks

Clinical notes:

• Most effective for symptoms of early satiety, postprandial fullness, and bloating

• Less effective for epigastric pain syndrome; consider PPI if pain predominant

• Administer before meals for optimal gastric prokinetic effect

1. Gastroparesis (Diabetic and Idiopathic)

Parameter Recommendation

Starting dose 50 mg orally three times daily before meals

Titration May increase to 100 mg TID if inadequate response after 2–4 weeks

Usual maintenance dose 150–300 mg/day in three divided doses

Maximum dose 300 mg/day

Duration: Up to 12 weeks in documented gastroparesis; reassess periodically

Clinical notes:

• Confirm diagnosis with gastric emptying study if available

• Optimise glycaemic control in diabetic gastroparesis

• May be used as adjunct to dietary modifications (small, frequent, low-fat meals)

1. Non-erosive GERD with Functional Dysmotility Component

Parameter Recommendation

Starting dose 50 mg orally three times daily before meals

Titration Not applicable

Usual maintenance dose 150 mg/day (50 mg TID)

Maximum dose 300 mg/day

Duration: 4–8 weeks as adjunctive therapy

Clinical notes:

• Adjunctive therapy only; not a substitute for acid suppression

• Must be combined with PPI for GERD symptoms

• Not indicated for erosive oesophagitis — use PPI alone

• Reassess at 4 weeks for continued need

Secondary Indications — Adults Only (Off-label, if any)

Indication Dose Duration Notes Evidence Basis

Chronic intestinal pseudo-obstruction 50 mg TID before meals Variable; specialist discretion OFF-LABEL; Specialist only (gastroenterologist) Limited international case series; no Indian data

Post-surgical gastroparesis 50 mg TID 2–4 weeks postoperatively OFF-LABEL; Short-term use only Indian surgical gastroenterology practice

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

NOT APPROVED for routine paediatric use in India. No paediatric-specific formulations available.

Secondary Indications — Paediatrics (Off-label, if any)

Indication Age Group Dose Duration Notes Evidence Basis

Functional dyspepsia ≥12 years 1 mg/kg/day in 3 divided doses (max 150 mg/day) 4–8 weeks OFF-LABEL; Specialist only (paediatric gastroenterologist) Limited data from Japanese studies

Gastroparesis ≥12 years 50 mg TID 4–8 weeks OFF-LABEL; Specialist only Extrapolated from adult data

⚠️ Age Restriction Statement:

• Not recommended in children <12 years of age due to inadequate safety data

• Risk of extrapyramidal symptoms in younger children — avoid use

• Use only under paediatric gastroenterology specialist supervision

• Monitor for CNS adverse effects, growth, and development

• Known hypersensitivity to itopride or any excipient

• Gastrointestinal haemorrhage (active)

• Mechanical gastrointestinal obstruction

• Gastrointestinal perforation

• Prolactin-secreting pituitary tumour (prolactinoma)

• Concurrent use with levodopa in Parkinson's disease (dopamine antagonism reduces levodopa efficacy)

• Phaeochromocytoma (may enhance catecholamine release)

• Elderly patients: Increased sensitivity to CNS and extrapyramidal effects

• History of movement disorders: May unmask or exacerbate extrapyramidal symptoms

• Renal impairment: Accumulation possible; dose reduction may be needed

• Concurrent use with other dopamine antagonists: Additive risk of extrapyramidal symptoms and hyperprolactinaemia

• Breast cancer history: Potential concern due to prolactin elevation (theoretical)

• Prolonged use beyond 8 weeks: Reassess indication; data on long-term safety limited

• Concurrent anticholinergic drugs: May oppose prokinetic effect; avoid if possible

Aspect Recommendation

Overall safety Insufficient human data; animal studies inconclusive

Risk category Not formally classified; avoid routine use

Preferred alternatives Metoclopramide (short-term, first trimester avoided); dietary modifications first line

When to use Only if benefit clearly outweighs risk; avoid in first trimester

Monitoring Fetal growth and development if used beyond 2 weeks

Aspect Recommendation

Compatible with breastfeeding Not recommended — excretion in human milk unknown

Preferred alternatives Domperidone (minimal CNS penetration, established use in lactation); dietary measures

Drug levels in milk Unknown

Infant monitoring If use unavoidable: feeding pattern, sedation, irritability, weight gain

Aspect Recommendation

Starting dose 50 mg twice daily (lower than standard adult dose)

Titration Increase cautiously to TID if tolerated and needed

Special considerations

• Increased sensitivity to extrapyramidal symptoms

• Monitor for confusion, restlessness, dizziness

• Assess renal function before initiation

• Fall risk may be increased

• Use lowest effective dose for shortest duration

Interacting Drug Effect Mechanism Recommendation

Levodopa Reduced antiparkinson efficacy Dopamine D2 receptor antagonism opposes levodopa action AVOID — contraindicated in Parkinson's disease

Anticholinergic agents (hyoscine, dicyclomine, tricyclic antidepressants with anticholinergic activity) Reduced prokinetic efficacy Pharmacological antagonism at gut level AVOID concurrent use if possible

Other dopamine antagonists (metoclopramide, domperidone, antipsychotics) Increased risk of extrapyramidal symptoms and hyperprolactinaemia Additive dopamine blockade AVOID concurrent use; choose one prokinetic only

Interacting Drug Effect Recommendation

Proton pump inhibitors No significant interaction Safe to co-prescribe; often used together in GERD/dyspepsia

H2 receptor blockers (famotidine) No direct interaction May be used together

CNS depressants (benzodiazepines, opioids) Possible additive sedation Monitor for excessive sedation

Antipsychotics (if combination unavoidable) Additive extrapyramidal and prolactin effects Monitor closely; prefer atypical antipsychotics with lower D2 affinity

Warfarin No significant interaction documented Routine monitoring sufficient

Note: Itopride has minimal effect on cardiac QT interval compared to other prokinetics (domperidone, metoclopramide). However, exercise caution when combining with known QT-prolonging drugs in high-risk patients.

• Diarrhoea

• Abdominal cramps/discomfort

• Headache

• Dizziness

• Nausea

• Increased salivation

• Constipation (paradoxical, rare)

• Insomnia or restlessness

Adverse Effect Clinical Notes

Extrapyramidal symptoms (dystonia, akathisia, parkinsonism) Rare with itopride (lower CNS penetration than metoclopramide); discontinue immediately if occurs

Hyperprolactinaemia May cause galactorrhoea, gynaecomastia, menstrual irregularities; reversible on discontinuation

Allergic reactions (rash, urticaria, angioedema) Discontinue if hypersensitivity suspected

Tardive dyskinesia Very rare; risk increases with prolonged use

Action: Discontinue immediately if extrapyramidal symptoms, severe allergic reaction, or tardive dyskinesia occurs.

Phase Parameters

Baseline Clinical assessment of symptoms; renal function (especially in elderly); exclude mechanical obstruction

After initiation (2–4 weeks) Symptom response; adverse effect assessment (CNS, GI); reassess diagnosis if no improvement

Long-term (if used >8 weeks) Periodic reassessment of need; monitor for hyperprolactinaemia symptoms (menstrual changes, galactorrhoea, gynaecomastia); renal function in elderly

Fixed-Dose Combinations (FDCs) available:

Note: FDCs should be used only when both components are indicated; avoid long-term FDC use without reassessment.

NLEM Status: Itopride is NOT included in NLEM 2022; not under NPPA price control.

Note: Prices vary across brands; generic options may be more affordable.

1. Preferred prokinetic in functional dyspepsia: Itopride is effective for postprandial symptoms (bloating, early satiety, fullness) but less useful for epigastric pain — add PPI if pain is prominent.

1. Safety advantage over alternatives: Unlike metoclopramide, itopride has minimal blood-brain barrier penetration, resulting in lower risk of extrapyramidal symptoms and tardive dyskinesia — preferred for longer-term use when prokinetic needed.

1. No significant QT prolongation: Unlike domperidone, itopride has minimal effect on cardiac QT interval — consider in patients with cardiac risk factors or on other medications.

1. Avoid in Parkinson's disease: Dopamine antagonism counteracts levodopa effect — contraindicated in patients on antiparkinsonian therapy.

1. Time-limited therapy: Use for defined courses (4–8 weeks); reassess at each visit; avoid indefinite prescribing.

1. Combination with PPI is common: In GERD with dysmotility features, itopride addresses motility while PPI addresses acid — rational combination when both components are needed.

Itopride; prokinetic; gastroparesis; functional dyspepsia; dopamine antagonist; acetylcholinesterase inhibitor; gastroenterology; GERD adjunct; low-EPS-risk; avoid-in-Parkinson

RxIndia v1.0 — 19 May 2025

• CDSCO approved prescribing information

• Indian Pharmacopoeia / National Formulary of India

• API Textbook of Medicine, 11th Edition

• Goodman & Gilman's The Pharmacological Basis of Therapeutics

• AIIMS Drug Formulary

• Indian Association of Gastroenterology clinical practice protocols

• NLEM 2022 (noted as not listed)