Version July 2025
Postpartum hemorrhage:
Oral: 0.2 mg 3 to 4 times daily in the puerperium for up to 7 days (maximum duration: 1 week).
IM, IV: 0.2 mg after delivery of anterior shoulder, after delivery of placenta, or during puerperium; may be repeated every 2 to 4 hours as needed. Note: IV administration should only be considered during life-threatening situations.
No dosage adjustment provided in manufacturer's labeling; use with caution.
No dosage adjustment provided in manufacturer's labeling; use with caution.
The following adverse drug reactions are derived from product labeling unless otherwise specified.
Frequency not defined:
Cardiovascular: Hypertension, hypotension, palpitations, tachycardia, thrombophlebitis, vasoconstriction, vasospasm
Dermatologic: Diaphoresis, skin rash
Endocrine & metabolic: Water intoxication
Gastrointestinal: Abdominal pain, diarrhea, nausea, unpleasant taste, vomiting
Genitourinary: Hematuria
Nervous system: Dizziness, hallucination, headache, seizure
Neuromuscular & skeletal: Lower limb cramp
Otic: Tinnitus
Respiratory: Dyspnea, nasal congestion
Postmarketing:
Cardiovascular: Acute myocardial infarction (Tsui 2001), angina pectoris, atrioventricular block, bradycardia (Ibrahim 2008), chest pain (Ibrahim 2008), coronary artery vasospasm (Jang 2023), ventricular fibrillation, ventricular tachycardia
Hypersensitivity: Anaphylaxis
Nervous system: Cerebrovascular accident, paresthesia
Hypersensitivity to methylergonovine or any component of the formulation; hypertension; preeclampsia; pregnancy
Concerns related to adverse effects:
• Coronary artery disease: Patients with coronary artery disease (CAD) or risk factors for CAD may be more likely to develop myocardial ischemia and infarction following methylergonovine-induced vasospasm.
Disease-related concerns:
• Labor: Use with caution in the second stage of labor.
• Sepsis: Use with caution in patients with sepsis.
• Vascular disease: Use with caution in patients with obliterative vascular disease.
Other warnings/precautions:
• IV administration: Not for routine IV administration due to risk of inducing sudden hypertensive and cerebrovascular accidents. IV administration should only be considered during life-threatening situations.
• Medication errors: Inadvertent administration to newborns has been reported.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Injection, as maleate:
Generic: 0.2 mg/mL (1 mL)
Solution, Injection, as maleate [preservative free]:
Generic: 0.2 mg/mL (1 mL)
Tablet, Oral, as maleate:
Methergine: 0.2 mg [contains methylparaben, propylparaben]
Generic: 0.2 mg
Yes
Solution (Methylergonovine Maleate Injection)
0.2 mg/mL (per mL): $18.00 - $37.54
Tablets (Methergine Oral)
0.2 mg (per each): $74.70
Tablets (Methylergonovine Maleate Oral)
0.2 mg (per each): $67.23 - $70.97
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
IV: Administer slowly over a period of no less than 60 seconds with careful monitoring of blood pressure. Do not routinely administer IV because of the possibility of inducing sudden hypertension and cerebrovascular accident; only consider IV administration during life-threatening situations.
IM: May be administered intramuscularly.
Oral: Available in tablets for oral administration.
Hazardous agent (NIOSH 2024 [table 2]).
Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2023; NIOSH 2024; USP-NF 2020).
Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.
Postpartum hemorrhage: Management of uterine atony, hemorrhage and subinvolution of the uterus following delivery of the placenta; control of uterine hemorrhage following delivery of the anterior shoulder in the second stage of labor.
Methergine may be confused with Brethine
Methylergonovine and terbutaline parenteral dosage forms look similar. Due to their contrasting indications, use care when administering these agents.
The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs (contraindicated in pregnancy) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Community/Ambulatory Care Settings).
Inadvertent administration of methylergonovine to newborns has been reported in place of routine medications (eg, vitamin K or hepatitis B vaccine); store methylergonovine injection separately from medications used for neonates.
Substrate of CYP3A4 (Major with inhibitors), CYP3A4 (Minor with inducers); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential;
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Alpha-/Beta-Agonists: Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates) may increase vasoconstricting effects of Alpha-/Beta-Agonists. Risk X: Avoid
Alpha1-Agonists: Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates) may increase vasoconstricting effects of Alpha1-Agonists. Risk X: Avoid
Aprepitant: May increase serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor
Beta-Blockers: May increase vasoconstricting effects of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor
Bromocriptine: Ergot Derivatives may increase adverse/toxic effects of Bromocriptine. Risk X: Avoid
Chloroprocaine (Systemic): May increase hypertensive effects of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor
Clofazimine: May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor
CYP3A4 Inducers (Strong): May decrease serum concentration of Methylergonovine. Risk C: Monitor
CYP3A4 Inhibitors (Moderate): May increase serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor
CYP3A4 Inhibitors (Strong): May increase serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid
Dihydroergotamine: Ergot Derivatives may increase vasoconstricting effects of Dihydroergotamine. Risk X: Avoid
Erythromycin (Systemic): May increase serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid
Fosamprenavir: May increase serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid
Fusidic Acid (Systemic): May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Consider avoiding this combination if possible. If required, monitor patients closely for increased adverse effects of the CYP3A4 substrate. Risk D: Consider Therapy Modification
Grapefruit Juice: May increase serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor
Itraconazole: May increase serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid
Lenacapavir: May increase serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid
Letermovir: May increase serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid
Lisuride: May increase adverse/toxic effects of Ergot Derivatives. Risk X: Avoid
Metergoline: Ergot Derivatives may increase adverse/toxic effects of Metergoline. Management: Combined use of metergoline with other ergot alkaloids after birth and during the postpartum period is specifically not recommended. Risk D: Consider Therapy Modification
Methysergide: Ergot Derivatives may increase vasoconstricting effects of Methysergide. Risk X: Avoid
Nefazodone: May increase serotonergic effects of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). This could result in serotonin syndrome. Nefazodone may increase serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid
Nicotine: May increase vasoconstricting effects of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor
Nitroglycerin: Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates) may decrease vasodilatory effects of Nitroglycerin. Nitroglycerin may increase serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Management: Avoid the use of ergot derivatives in patients receiving nitroglycerin for angina (or in any angina patient) if possible. If combined, monitor for decreased effects of nitroglycerin and increased adverse effects of the ergot derivative (eg, ergotism). Risk D: Consider Therapy Modification
Pergolide: May increase adverse/toxic effects of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor
Reboxetine: May increase hypertensive effects of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor
Roxithromycin: May increase serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid
Serotonergic Agents (High Risk): Ergot Derivatives may increase serotonergic effects of Serotonergic Agents (High Risk). This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity (eg, hyperreflexia, clonus, hyperthermia, diaphoresis, tremor, autonomic instability, mental status changes) when these agents are combined. Risk C: Monitor
Serotonin 5-HT1D Receptor Agonists (Triptans): May increase vasoconstricting effects of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid
Sulprostone: May increase vasoconstricting effects of Ergot Derivatives. Risk C: Monitor
Tipranavir: May increase serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid
Methylergonovine is intended for use after delivery of the anterior shoulder, after delivery of the placenta, or during the puerperium; use is contraindicated during pregnancy.
Methylergonovine is used for the treatment of postpartum hemorrhage due to uterine atony. Methylergonovine is recommended when a supplemental uterotonic agent is needed; due to maternal side effects it is not preferred for initial use (ACOG 183 2017).
Methylergonovine is present in breast milk.
Data related to the presence of methylergonovine in breast milk are available from multiple studies (Erkkola 1978; Iwamura 1981; Nakamichi 2012; Vogel 2004).
• Methylergonovine 0.125 mg was administered orally 3 times daily for 5 days to 8 women treated for incomplete postpartum involution. Milk concentrations were evaluated 1 and 8 hours after the morning dose on day 5. The highest milk concentrations were observed 1 hour after the dose and ranged from <0.5 ng/mL (lower limit of detection) to 1.3 ng/mL (Erkkola 1978). Using data from this study and a milk concentration of 1.3 ng/mL, the estimated daily infant dose via breast milk is 195 ng/kg/day and the relative infant dose (RID) of methylergonovine is 3.9% compared to the weight-adjusted maternal. Higher doses are recommended in current product labeling.
• In general, breastfeeding is considered acceptable when the RID of a medication is <10% (Anderson 2016; Ito 2000).
Adverse events may be observed in breastfed infants and may include agitation, diarrhea, increased blood pressure, bradycardia, seizures, tachycardia, or vomiting (Methylergometrine 2014). Prolactin concentrations (and possibly milk supply) may be changed following methylergonovine administration; this may be dependent upon dose and route of administration (Del Pozo 1975; Weiss 1975).
Some manufacturers do not recommend breastfeeding during therapy or for 12 hours after the last dose due to adverse reactions reported in breastfeeding infants. However, other sources note use may be acceptable if breastfeeding (Ito 2000).
Blood pressure
Increases the tone, rate and amplitude of contractions on the smooth muscles of the uterus, producing sustained contractions which shortens the third stage of labor and reduces blood loss.
Onset of action: Oxytocic: Oral: 5-10 minutes; IM: 2-5 minutes; IV: Immediately
Duration: Oral: ~3 hours; IM: ~3 hours; IV: 45 minutes
Absorption: Rapid
Distribution: Vd: 39-73 L
Metabolism: Hepatic
Bioavailability: Oral: 60%; IM: 78%
Half-life elimination: ~3 hours (range: 1.5-12.7 hours)
Time to peak, serum: Oral: 0.3-2 hours; IM: 0.2-0.6 hours
Excretion: Urine and feces
