Schedule H

Oral, Intramuscular (IM), Intravenous (IV — slow injection only)

• Tablet: 0.125 mg (as maleate)

• Injection: 0.2 mg/mL in 1 mL ampoule (as maleate)

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Prevention and Treatment of Postpartum Haemorrhage (PPH) — Uterine Atony

A. Intramuscular Route (Preferred for PPH)

Step Dose Clinical Notes

Starting dose 0.2 mg IM immediately after delivery of anterior shoulder or placenta Onset of action: 2–5 minutes

Titration Not applicable Response-based repeat dosing

Usual maintenance dose 0.2 mg IM every 2–4 hours if continued atony Assess uterine tone before each dose

Maximum dose 1 mg (5 doses) in 24 hours Exceeding this increases ergotism risk

B. Intravenous Route (Emergency Use Only)

Step Dose Clinical Notes

Starting dose 0.2 mg IV slowly over ≥1 minute Reserve for severe PPH with IV access

Titration Not applicable Single emergency dose

Usual maintenance dose Switch to IM route after initial control IV bolus increases hypertensive crisis risk

Maximum dose 0.2 mg IV per dose; total 1 mg/24 hours (all routes combined) Never give rapid IV push

Key points:

• Administer only AFTER delivery of baby — never before delivery

• Rule out retained products of conception before use

• Second-line agent after oxytocin in normotensive women

• Absolutely contraindicated in hypertensive disorders

1. Uterine Subinvolution (Postpartum)

Oral Route

Step Dose Clinical Notes

Starting dose 0.125 mg three times daily Start after ruling out retained products

Titration May increase to 0.25 mg TID based on response Assess for improvement in involution

Usual maintenance dose 0.125–0.25 mg three times daily Continue for 5–7 days

Maximum dose 0.75 mg/day (0.25 mg TID) for up to 7 days Do not exceed 7 days — ergotism risk

Key points:

• Confirm complete placental expulsion before initiating

• Monitor blood pressure during treatment

• Limit duration to maximum 7 days

1. Prevention of Haemorrhage After Evacuation (Post-Abortion/Post-MTP)

Route Dose Clinical Notes

IM 0.2 mg IM immediately after evacuation Promotes uterine contraction

Oral (follow-up) 0.125 mg TID for 3–5 days If ongoing mild atony; ensure complete evacuation

Secondary Indications — Adults (Off-label)

Indication Dose Duration Notes

Menorrhagia (uterine atony-related) 0.125–0.25 mg orally 2–3 times daily during menses 3–5 days per cycle OFF-LABEL; Specialist only; Evidence: Indian gynaecology practice; lacks RCT evidence; use only after excluding organic pathology

PAEDIATRIC DOSING (Specialist Only)

Primary Indications

Not applicable. Methylergometrine is not indicated in paediatric patients. Use is restricted to postpartum/post-abortion women.

Secondary Indications — Paediatrics (Off-label)

Not applicable.

Mild-moderate impairment No specific adjustment; use with caution

Severe impairment (eGFR <30) Avoid use if possible; risk of accumulation and prolonged vasoconstriction

Dialysis No data available; avoid unless essential

Note: Limited pharmacokinetic data; use oxytocin as preferred alternative in significant renal impairment

• Hypertension (any degree — including gestational hypertension)

• Pre-eclampsia or eclampsia

• Peripheral vascular disease

• Coronary artery disease or ischaemic heart disease

• Cerebrovascular disease or history of stroke

• Sepsis or septicaemia

• Severe hepatic impairment

• Severe renal impairment

• Known hypersensitivity to methylergometrine or other ergot alkaloids

• Use BEFORE delivery of the infant (risk of uterine tetany, fetal hypoxia, uterine rupture)

• Concurrent use with potent CYP3A4 inhibitors (macrolides, azole antifungals, HIV protease inhibitors)

• Concurrent use with triptans or other ergot alkaloids

• Mild cardiac disease (non-ischaemic) — may worsen with vasoconstriction

• Raynaud's phenomenon

• History of migraine — may exacerbate

• Retained placenta — ensure complete expulsion before administration

• Multiple gestation — increased uterine sensitivity

• Grand multiparity

• Concurrent use of vasoconstrictors

• Prolonged use (>7 days) — risk of ergotism

• Rapid IV injection — acute severe hypertension (always inject over ≥1 minute)

• Elderly women — increased vascular sensitivity

Parameter Recommendation

Safety category Contraindicated during pregnancy; causes tetanic uterine contraction → fetal hypoxia, uterine rupture

Preferred alternatives Not applicable — methylergometrine is used postpartum only; oxytocin is first-line for AMTSL

When it may be used Third stage of labour (after delivery of baby) and postpartum period only for PPH management in normotensive women

Monitoring Maternal blood pressure; uterine tone; confirm complete placental delivery

Note: NEVER administer before delivery of the infant

Parameter Recommendation

Compatibility Compatible for short-term use (single dose or few days); avoid prolonged use

Drug levels in milk Low (with single/short-term doses)

Preferred alternatives Oxytocin for PPH (no effect on lactation); avoid methylergometrine for >7 days

Infant monitoring Monitor for feeding adequacy, irritability; ergot alkaloids may suppress prolactin with prolonged use → reduced milk production

Note: Limit duration to avoid interference with lactation establishment

• Recommended starting dose: Not routinely indicated in elderly

• Titration: If used (rare gynaecological indications), use lowest oral dose

• Additional risks:

• Increased sensitivity to vasoconstrictive effects

• Higher risk of coronary and peripheral vasospasm

• Hypertensive responses more severe

• Risk of confusion, hallucinations (ergot effects)

• Recommendation: Avoid use; if essential, close cardiovascular monitoring required

Drug Interaction Management

Potent CYP3A4 inhibitors (erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir, HIV protease inhibitors) Markedly increased methylergometrine levels → severe vasospasm, peripheral ischaemia, gangrene CONTRAINDICATED — do not use together

Triptans (sumatriptan, rizatriptan, zolmitriptan) Additive vasospasm → coronary and cerebral ischaemia AVOID — do not use within 24 hours of each other

Other ergot alkaloids (ergometrine, ergotamine, dihydroergotamine) Cumulative ergot toxicity → severe vasospasm, gangrene AVOID concurrent use

Sympathomimetic agents (adrenaline, noradrenaline, dopamine) Additive vasoconstriction → severe hypertension, arrhythmia AVOID concurrent use; if essential, use lowest doses with continuous BP monitoring

Bromocriptine/Cabergoline Additive vasoconstrictive effects Avoid combination; if sequential use needed, allow washout period

Drug Interaction Management

Beta-blockers May enhance peripheral vasoconstriction Monitor for cold extremities, peripheral ischaemia

Antihypertensives Methylergometrine may counteract antihypertensive effect Monitor blood pressure; contraindicated in hypertensive patients anyway

Moderate CYP3A4 inhibitors (fluconazole, diltiazem, verapamil, grapefruit juice) Possible increased methylergometrine levels Use with caution; monitor for ergot toxicity

CYP3A4 inducers (rifampicin, phenytoin, carbamazepine) May reduce methylergometrine efficacy Monitor clinical response; may need dose adjustment

Nitrates (GTN, isosorbide) May partially antagonise ergot-induced vasoconstriction Note for treatment of inadvertent ergot toxicity

• Nausea and vomiting

• Abdominal cramping/pain

• Elevated blood pressure

• Headache

• Dizziness

• Diaphoresis (sweating)

• Palpitations

• Leg cramps

Reaction Action Required

Hypertensive crisis Stop administration immediately; IV labetalol or hydralazine; ICU care if severe

Myocardial infarction / Coronary vasospasm Discontinue immediately; standard MI management; cardiology input

Cerebrovascular accident (Stroke) Discontinue; emergency stroke management; neurology input

Peripheral vasospasm / Limb ischaemia / Gangrene Discontinue; limb warming; IV vasodilators (nitroprusside, GTN); vascular surgery consultation

Ergotism (chronic) — numbness, tingling, cold extremities, hallucinations Discontinue; supportive care; limit total duration of use

Seizures Discontinue; supportive care; benzodiazepines

Uterine tetany/Rupture (if given before delivery) Emergency surgical intervention

During IV administration Continuous BP monitoring during slow injection

First 2 hours post-administration Blood pressure every 15–30 minutes; uterine tone; vaginal bleeding assessment

Oral therapy (prolonged) BP at each visit; monitor for signs of ergotism (cold extremities, numbness, paresthesia); limit to ≤7 days

Single-ingredient products:

• Methergine (Novartis) — most widely available

• Myomet (Zydus)

• Methyler (Macleods)

• Utergin-M (Samarth)

Note: Methylergometrine (methyl ergonovine maleate) is DIFFERENT from ergometrine maleate — they are not interchangeable; methylergometrine is longer-acting

NLEM status: Methylergometrine maleate injection 0.2 mg/mL is included in NLEM 2022 — ceiling price applicable under NPPA

Government supply: Available through maternal health programmes at public facilities

• Hypertension is absolute contraindication: NEVER use methylergometrine in any hypertensive disorder (gestational hypertension, pre-eclampsia, chronic hypertension) — use oxytocin or carboprost instead

• Check BP before every dose: A single elevated BP reading contraindicates methylergometrine; always confirm normotension before administration

• Slow IV injection critical: Rapid IV push causes acute severe hypertension and coronary vasospasm — always inject over at least 1 minute; IM is safer

• Oxytocin is first-line: Methylergometrine is second-line for PPH after oxytocin; reserve for normotensive women when oxytocin insufficient

• Maximum 7 days oral use: Prolonged use beyond 7 days increases risk of ergotism (peripheral ischaemia, gangrene); counsel patients on duration limit

• Different from ergometrine: Methylergometrine is longer-acting than ergometrine; both are ergot alkaloids but not interchangeable — verify correct drug dispensed

methylergometrine; uterotonic; PPH prevention; PPH treatment; ergot alkaloid; hypertension contraindicated; vasospasm risk; postpartum; subinvolution; NLEM India

RxIndia v1.1 — 14 Jun 2025

• CDSCO Approved Product Information

• Indian Pharmacopoeia 2022

• National Formulary of India 2021

• NLEM 2022 (National List of Essential Medicines)

• MoHFW Guidelines — Prevention and Management of Postpartum Haemorrhage

• National Health Mission Protocols for Skilled Birth Attendants

• FOGSI Good Clinical Practice Recommendations

• AIIMS Obstetrics Protocols

• Goodman & Gilman's The Pharmacological Basis of Therapeutics (13th Edition)

• Harrison's Principles of Internal Medicine (21st Edition)