Schedule H

Oral

• Capsules: 8 mcg

• Capsules: 24 mcg

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Chronic Idiopathic Constipation (CIC) in Adults

Parameter Details

Starting dose 24 mcg orally twice daily

Titration Not applicable — fixed dose regimen

Usual maintenance dose 24 mcg twice daily

Maximum dose 48 mcg/day

Clinical Notes:

• Must be taken with food and water to reduce nausea

• Swallow capsule whole; do not crush or chew

• Assess response after 2 weeks; consider discontinuation if no improvement by 4–8 weeks

• Effect usually seen within 1 week of initiation

1. Irritable Bowel Syndrome with Constipation (IBS-C) in Adult Women

Parameter Details

Starting dose 8 mcg orally twice daily

Titration Not applicable — fixed dose regimen

Usual maintenance dose 8 mcg twice daily

Maximum dose 16 mcg/day

Clinical Notes:

• Approved in India specifically for use in women

• Safety and efficacy in men with IBS-C not established in Indian context

• Take with food and water

• Reassess if no meaningful improvement within 4 weeks

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

Indication Dose Duration Notes

Opioid-induced constipation (non-cancer patients) 24 mcg orally twice daily As required during opioid therapy OFF-LABEL — Specialist only. Supported by international RCTs; used in select Indian tertiary gastroenterology centres. Efficacy may be reduced with diphenylheptane opioids (e.g., methadone).

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

NOT APPROVED for paediatric use in India.

Age Group Recommendation

Below 18 years Not recommended — No established safety or efficacy data

Minimum Age: 18 years (adults only)

Secondary Indications — Paediatric Doses (Off-label, if any)

NOT RECOMMENDED — No reliable paediatric dosing established.

Use below 18 years should only be considered in clinical trial settings or tertiary specialist centres with appropriate justification and monitoring.

• Known or suspected mechanical gastrointestinal obstruction

• History of hypersensitivity to lubiprostone or any excipient in the formulation

• Severe diarrhoea — may lead to dehydration and electrolyte disturbance; higher risk in elderly and renally impaired patients

• Dyspnoea — transient episodes reported (typically within 30–60 minutes of first dose); usually self-limiting and resolves within 3 hours

• Nausea — most common adverse effect; taking with food reduces incidence

• Hypotension — secondary to fluid loss from severe diarrhoea

• Pregnancy — avoid unless clearly indicated

• Patients with inflammatory bowel disease — limited data; use with caution

Parameter Details

Risk category Category C (based on animal studies; limited human data)

Safety statement Not recommended during pregnancy unless benefit clearly outweighs risk

Preferred alternatives Bulk-forming laxatives (ispaghula husk), osmotic agents (lactulose, PEG)

When may be used Only if no safer alternative available and after specialist consultation

Monitoring Maternal hydration status, fetal growth; discontinue if severe diarrhoea develops

Parameter Details

Compatibility Unknown — limited human data; likely minimal transfer to breast milk due to low systemic absorption

Expected levels in milk Likely low (minimal systemic bioavailability)

Preferred alternatives Lactulose, ispaghula husk

Infant monitoring Loose stools, feeding difficulties, hydration status

Recommendation Use with caution; consider alternatives where possible

Parameter Recommendation

Starting dose Same as adult doses; however, initiate cautiously

Titration Slower dose escalation may be prudent if tolerability concerns

Special risks Volume depletion, reduced renal reserve, orthostatic hypotension, falls

Monitoring Close monitoring of hydration status; assess renal function periodically

Precautions Ensure adequate oral fluid intake; avoid concurrent high-dose diuretics

Drug/Class Interaction Recommendation

No major drug interactions requiring avoidance have been reported Lubiprostone acts locally with minimal systemic absorption —

Concurrent laxatives or prokinetics Theoretical risk of additive diarrhoea and fluid loss Avoid combination unless clearly indicated; monitor closely

Drug/Class Interaction Recommendation

Methadone (diphenylheptane opioid) May reduce lubiprostone efficacy in opioid-induced constipation setting Monitor response; consider alternative agents

Antihypertensives Additive hypotensive effect if lubiprostone causes significant fluid loss Monitor blood pressure; ensure adequate hydration

Diuretics Increased risk of dehydration and electrolyte imbalance Monitor hydration and electrolytes

Note: No significant CYP450 interactions documented.

• Nausea (most common — up to 30%)

• Diarrhoea

• Abdominal pain or discomfort

• Abdominal distension

• Flatulence

• Headache

• Dyspnoea (transient, non-cardiac; typically within 1 hour of dose)

Adverse Effect Notes

Severe diarrhoea with dehydration May cause hypotension, electrolyte disturbance — requires drug discontinuation and supportive care

Syncope Rare; secondary to hypotension from fluid loss

Hypersensitivity/anaphylactoid reactions Very rare — discontinue immediately; provide supportive management

Ischaemic colitis Very rare case reports — discontinue if suspected

Timing Parameter

Baseline Exclude mechanical bowel obstruction; pregnancy status in women of childbearing age; baseline renal function in elderly

First 1–2 weeks Monitor for diarrhoea, dyspnoea, nausea, hypotension

Ongoing Bowel movement frequency and consistency; hydration status

Long-term Weight, hydration status; periodic renal function in elderly or those on diuretics

• Amitiza® (imported/licensed)

• Lubimust® (Alkem)

• Lubrexa® (Sun Pharma)

• Lubowel® (Torrent)

Note: Available as single-ingredient capsules only; no FDCs.

Note: Lubiprostone is NOT listed in NLEM; not under NPPA price control. Available in private market only.

• Always administer with food and water — significantly reduces nausea incidence

• Transient dyspnoea occurring within 1 hour of first dose is non-cardiac in nature and typically resolves spontaneously within 3 hours; reassure patients

• For IBS-C, approved only for women in India; safety data in men is limited

• Reassess after 4–6 weeks — if no meaningful benefit, discontinue and consider alternatives

• Lower risk of electrolyte disturbance compared to stimulant or osmotic laxatives with prolonged use

• Avoid combining with stimulant laxatives unless under specialist supervision

lubiprostone; chronic idiopathic constipation; CIC; IBS-C; irritable bowel syndrome; chloride channel activator; Schedule H; gastroenterology; pregnancy-caution; nausea-prone

RxIndia v1.0 — 13 May 2025

• CDSCO approved product labels

• National Formulary of India (NFI) 2021

• AIIMS Hospital Formulary

• API Textbook of Medicine

• Goodman & Gilman's The Pharmacological Basis of Therapeutics

• Indian gastroenterology specialist prescribing practices

• International RCTs (off-label opioid-induced constipation — marked appropriately)