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Methylergometrine

Ergot alkaloid uterotonic agent · Obstetric agent, Postpartum hemorrhage management

Also known as Methylergonovine, Methergine

START
Ensure delivery is complete (retained placenta is contraindication). Check BP (contraindicated if hypertensive/preeclamptic). IV oxytocin is first-line for PPH; reserve methylergometrine for oxytocin failure or as second-line.
TYPICAL MAX
5 x 0.2mg IM doses (1mg total). Do not exceed—risk of severe hypertension and vasoconstriction.
STOP IF
Severe hypertension (SBP >160 or DBP >110), chest pain, severe headache, signs of peripheral vasospasm (cold, pale extremities), uterine tetany.
WATCH
BP monitoring every 15 minutes after IM injection. NEVER give IV (risk of severe hypertension, stroke, death)—IM or PO only. Contraindicated in preeclampsia/eclampsia due to hypertensive effect. Oxytocin is preferred first-line uterotonic; methylergometrine is second-line.
CDSCO approvedSchedule HJan AushadhiATC G02AB03
Dose laddermg/d
0.2start0.6max1ceiling
Renal dose adjustmenteGFR mL/min/1.73m²
CAUTIONUse with caution30AVOIDAvoid (reduced clearance)90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
5minONSET30minPEAK3.4h3hDURATION
ONSET
5min · IM onset 2-5 minutes
PEAK
30min · IM peak 30 minutes
3.4h · t½ ~3.4 hours
DURATION
3h · 2-4 hours (IM)
EXCRETION
Fecal/biliary as metabolites (~90%)
route + CYP
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
Contraindicated during pregnancy before delivery—causes uterine contractions and fetal distress. Safe for postpartum use.
FDA category + note
Top interactionssee all 12
  • RitonavirContraindicatedDatabaseDDInter
  • AlmotriptanSevereDatabaseDDInter
  • AmprenavirSevereDatabaseDDInter
  • AtazanavirSevereDatabaseDDInter
Available in India

78 branded formulations. Look up specific brands in the Drugs workspace.

Jan Aushadhi — generic available at GoI pharmacies

Mechanism

Direct agonist at 5-HT2A serotonin and alpha-adrenergic receptors on uterine smooth muscle, causing sustained tetanic uterine contractions. Also has partial agonist/antagonist activity at dopamine D2 receptors. Contracts uterine fundus and mid-zone more than lower segment.

Indications

Prevention and treatment of postpartum hemorrhage (PPH) due to uterine atonyIncomplete abortion (after uterine evacuation)Subinvolution of the uterusUterine atony following cesarean section

Dosing

Adult
PPH prevention/treatment: 0.2mg IM q2-4h after delivery (max 5 doses). OR 0.2mg PO TID-QID x 2-7 days. Uterine subinvolution: 0.2mg PO TID x up to 7 days.
Pediatric
Not used in children.
Renal adjustment
Avoid in severe renal impairment (reduced clearance, increased toxicity).
Hepatic adjustment
Avoid in hepatic impairment (extensively hepatically metabolized).
Geriatric
Not applicable (postpartum use only).
Max dose
1mg/day (5 x 0.2mg IM); 0.8mg/day PO

Pharmacokinetics

Onset
IM: uterine contraction within 2-5 minutes; PO: 5-10 minutes
Peak effect
IM: peak in 30 minutes; PO: Tmax 30-120 minutes
Duration
IM: 2-4 hours; PO: 3-4 hours
Half-life
~3.4 hours (plasma); biological effects persist longer
Bioavailability
~60% (oral)
Protein binding
~50%
Metabolism
Extensive hepatic via CYP3A4 (major) and CYP2D6 to inactive metabolites
Excretion
~90% biliary/fecal (metabolites); ~5% renal (unchanged)

Contraindications

  • Pregnancy (before delivery—causes uterine contractions and fetal distress)
  • Hypersensitivity to ergot alkaloids
  • Hypertension or preeclampsia/eclampsia
  • Peripheral vascular disease
  • Coronary artery disease
  • Hepatic or renal impairment
  • Sepsis
  • Concomitant CYP3A4 inhibitors (ergotism risk)

Side effects

Common
Nausea and vomitingAbdominal crampingHypertension / vasoconstrictionHeadacheDizzinessDiaphoresis
Serious
  • Severe hypertension (cerebrovascular accident risk)
  • Ergotism (peripheral vasospasm, gangrene—rare with therapeutic doses)
  • Myocardial ischemia / infarction
  • Seizures
  • Thrombosis
  • Uterine tetany / rupture (rare)

Pregnancy & lactation

Pregnancy

Contraindicated during pregnancy before delivery—causes uterine contractions and fetal distress. Safe for postpartum use.

Lactation

Excreted in breast milk; may cause GI upset, weakness, and poor feeding in infants. Use lowest effective dose for shortest duration; monitor infant.

Drug interactions

Ritonavir
Contraindicated
Database

Ergotism: vasospasm, gangrene

Absolute contraindication in HIV patients on PIs.

Source: DDInter

Almotriptan
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amprenavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Atazanavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Boceprevir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Bromocriptine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Ceritinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Clarithromycin
Severe
Database

Ergotism

Avoid. Use alternative uterotonic.

Source: DDInter

Cobicistat
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Conivaptan
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Darunavir
Severe
Database

Clinical effect not specified

Source: DDInter

Delavirdine
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

Ask House about Methylergometrine

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: Katzung·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19