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Methylergonovine (methylergometrine): Drug information

Methylergonovine (methylergometrine): Drug information
(For additional information see "Methylergonovine (methylergometrine): Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Methergine
Pharmacologic Category
  • Ergot Derivative
Dosing: Adult
Postpartum hemorrhage

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.

Dosing: Kidney Impairment: Adult

No dosage adjustment provided in manufacturer's labeling; use with caution.

Dosing: Hepatic Impairment: Adult

No dosage adjustment provided in manufacturer's labeling; use with caution.

Adverse Reactions

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

Contraindications

Hypersensitivity to methylergonovine or any component of the formulation; hypertension; preeclampsia; pregnancy

Warnings/Precautions

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.

Dosage Forms: US

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

Generic Equivalent Available: US

Yes

Pricing: US

Solution (Methylergonovine Maleate Injection)

0.2 mg/mL (per mL): $8.80 - $35.90

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.

Administration: Adult

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 Drugs Handling Considerations

Hazardous agent (NIOSH 2016 [group 3]).

Use appropriate precautions for receiving, handling, administration, and disposal. Gloves (single) should be worn during receiving, unpacking, and placing in storage. NIOSH recommends single gloving for administration of intact tablets or capsules. For injection preparation, NIOSH recommends double gloving, a protective gown, ventilated engineering controls (a class II biological safety cabinet or a compounding aseptic containment isolator), and closed system transfer devices (CSTDs). Double gloving, a gown, and (if dosage form allows) CSTDs are required during injection administration (NIOSH 2016).

Use: Labeled Indications

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.

Medication Safety Issues
Sound-alike/look-alike issues:

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.

High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs that have a heightened risk of causing significant patient harm when used in error.

Administration issues:

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.

Metabolism/Transport Effects

Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

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 Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Alpha-/Beta-Agonists: Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates) may enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Risk X: Avoid combination

Alpha1-Agonists: Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates) may enhance the vasoconstricting effect of Alpha1-Agonists. Risk X: Avoid combination

Aprepitant: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor therapy

Beta-Blockers: May enhance the vasoconstricting effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor therapy

Bromocriptine: Ergot Derivatives may enhance the adverse/toxic effect of Bromocriptine. Risk X: Avoid combination

Chloroprocaine (Systemic): May enhance the hypertensive effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor therapy

Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of Methylergonovine. Risk C: Monitor therapy

CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination

Delavirdine: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination

Dihydroergotamine: Ergot Derivatives may enhance the vasoconstricting effect of Dihydroergotamine. Risk X: Avoid combination

Erythromycin (Systemic): May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination

Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination

Fosamprenavir: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination

Lenacapavir: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination

Letermovir: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination

Lisuride: May enhance the adverse/toxic effect of Ergot Derivatives. Risk X: Avoid combination

Lorcaserin (Withdrawn From US Market): May enhance the adverse/toxic effect of Ergot Derivatives. Specifically, use of these drugs together may increase the risk of developing valvular heart disease. Lorcaserin (Withdrawn From US Market) may enhance the serotonergic effect of Ergot Derivatives. This could result in serotonin syndrome. Risk X: Avoid combination

Methysergide: Ergot Derivatives may enhance the vasoconstricting effect of Methysergide. Risk X: Avoid combination

Nefazodone: May enhance the serotonergic effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). This could result in serotonin syndrome. Nefazodone may increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination

Nitroglycerin: Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates) may diminish the vasodilatory effect of Nitroglycerin. Nitroglycerin may increase the 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 enhance the adverse/toxic effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor therapy

Reboxetine: May enhance the hypertensive effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor therapy

Roxithromycin: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination

Serotonergic Agents (High Risk): Ergot Derivatives may enhance the serotonergic effect 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 therapy

Serotonin 5-HT1D Receptor Agonists (Triptans): May enhance the vasoconstricting effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination

Tipranavir: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination

Pregnancy Considerations

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).

Breastfeeding Considerations

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).

Monitoring Parameters

Blood pressure

Mechanism of Action

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.

Pharmacokinetics (Adult Data Unless Noted)

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

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Methergin;
  • (AR) Argentina: Basofortina;
  • (AT) Austria: Methergin;
  • (BD) Bangladesh: Methergin | Metherspan;
  • (BF) Burkina Faso: Lerin;
  • (BG) Bulgaria: Methergin | Methylergobrevin | Methylergometrin;
  • (BR) Brazil: Ergometrin | Methergin;
  • (CH) Switzerland: Methergin;
  • (CI) Côte d'Ivoire: Lerin;
  • (CL) Chile: Methergin;
  • (CO) Colombia: Methergin;
  • (DE) Germany: Methergin;
  • (DO) Dominican Republic: Methergin;
  • (EC) Ecuador: Methergina;
  • (EG) Egypt: Methergin;
  • (ES) Spain: Methergin;
  • (FI) Finland: Methergin | Myomergin;
  • (FR) France: Methergin;
  • (GR) Greece: Demergin | Ergovit | Methergine | Mitrotan;
  • (HK) Hong Kong: Methergin;
  • (ID) Indonesia: Methergin | Metherinal | Methovin | Methyl ergometrine | Methylergometrine | Metiagin | Metilat | Metvell | Myotonic | Pospargin;
  • (IL) Israel: Methergin;
  • (IN) India: Algometrine | Ergagin | Ergogin | Ergolin | Ergoriv | Gotrin | Hicon | Ingagen-m | Lerin | Limitex | Mem | Memcad | Memjet | Mergox | Merzen | Metergo | Metermin | Metharmed | Methastar | Methergin | Methygin | Methylergometrine | Utergin | Wergomet;
  • (IT) Italy: Methergin;
  • (JO) Jordan: Methergin;
  • (JP) Japan: Derganin | Derganin taiyo | Levospan | Metenarin | Methecrine | Methergin | Methylegyl kayaku | Partan m | Ryegonovin | Takimetrin m | Uruteon;
  • (KR) Korea, Republic of: Ergospar m | Methergin | Unidergin | Unidergine;
  • (KW) Kuwait: Methergin;
  • (LB) Lebanon: Methergine;
  • (LT) Lithuania: Methergin;
  • (LV) Latvia: Methergin | Methylergometrin;
  • (MA) Morocco: Methergin;
  • (MX) Mexico: Methergin;
  • (MY) Malaysia: Methergin;
  • (NO) Norway: Methergin;
  • (PE) Peru: Methergin | Neometrin;
  • (PH) Philippines: Ergojen | Ergon | Ergotec | Mergot | Methergin | Mexytrine | Usa-methylergometrine maleate | Usamema | Utergin;
  • (PK) Pakistan: Ergomin | Methergin;
  • (PR) Puerto Rico: Methergine | Methylergonovine maleate;
  • (PT) Portugal: Methergin | Metilergometrina;
  • (PY) Paraguay: Basofortina | Femitranol;
  • (QA) Qatar: Methergin;
  • (SA) Saudi Arabia: Methergin;
  • (SE) Sweden: Methergin;
  • (TH) Thailand: Ermetrin | Gynogin | Methergin | Methylergometrine;
  • (TN) Tunisia: Ergotyl;
  • (TR) Turkey: Methergin | Metiler | Uterjin;
  • (TW) Taiwan: Methergin | Methylergonovine;
  • (UA) Ukraine: Methylergometrin;
  • (UG) Uganda: Ergomin;
  • (UY) Uruguay: Methergin;
  • (VE) Venezuela, Bolivarian Republic of: Methergin;
  • (ZM) Zambia: Ergogin
  1. American College of Obstetricians and Gynecologists (ACOG) Committee on Practice Bulletins - Obstetrics. Practice bulletin no. 183: postpartum hemorrhage. Obstet Gynecol. 2017;130(4):e168-e186. [PubMed 28937571]
  2. Anderson PO, Sauberan JB. Modeling drug passage into human milk. Clin Pharmacol Ther. 2016;100(1):42-52. [PubMed 27060684]
  3. Cohen V, Jellinek SP, Teperikidis L, et al, “Room-Temperature Storage of Medications Labeled for Refrigeration,” Am J Health-Syst Pharm, 2007, 64(16):1711-15. [PubMed 17687059]
  4. de Groot AN, van Dongen PW, Vree TB, et al, “Ergot Alkaloids. Current Status and Review of Clinical Pharmacology and Therapeutic Use Compared With Other Oxytocics in Obstetrics and Gynaecology,” Drugs, 1998, 56(4):523-35. [PubMed 9806101]
  5. Del Pozo E, Brun Del Re R, Hinselmann M. Lack of effect of methyl-ergonovine on postpartum lactation. Am J Obstet Gynecol. 1975;123(8):845-846. [PubMed 1200082]
  6. Erkkola R, Kanto J, Allonen H, Kleimola T, Mäntylä R. Excretion of methylergometrine (methylergonovine) into the human breast milk. Int J Clin Pharmacol Biopharm. 1978;16(12):579-580. [PubMed 730424]
  7. Ibrahim SM, Mustafa E, Louon A. Postpartum severe sinus bradycardia following methylergonovine administration. J Int Med Res. 2008;36(5):1129-1133. doi:10.1177/147323000803600534 [PubMed 18831911]
  8. Ito S. Drug therapy for breast-feeding women. N Engl J Med. 2000;343(2):118-126. [PubMed 10891521]
  9. Iwamura S, Kambegawa A. Determination of methylergometrine and dihydroergotoxine in biological fluids. J Pharmacobiodyn. 1981;4(4):275-281. doi:10.1248/bpb1978.4.275 [PubMed 7264872]
  10. Jang SK, Berlacher K, Hauspurg A. Post-partum myocardial ischemia due to intramuscular methylergonovine-induced coronary vasospasm: case report. BMC Cardiovasc Disord. 2023;23(1):199. doi:10.1186/s12872-023-03216-9 [PubMed 37069508]
  11. Methergine (methylergonovine maleate) [prescribing information]. Baltimore, MD: Lupin Pharma; January 2016.
  12. Methylergometrine: adverse effects in breastfed infants. Prescrire Int. 2014;23(148):102. [PubMed 24860899]
  13. Methylergonovine maleate [prescribing information]. Berlin, CT: Breckenridge Pharmaceutical, Inc; October 2019.
  14. Nakamichi T, Yawata A, Hojo H, Kagaya H, Kobayashi S, Chikuma T. Monitoring of methylergometrine in human breast milk by solid-phase extraction and high-performance liquid chromatography with fluorimetric detection. Pharmazie. 2012;67(6):482-484.
  15. Tsui BC, Stewart B, Fitzmaurice A, Williams R. Cardiac arrest and myocardial infarction induced by postpartum intravenous ergonovine administration. Anesthesiology. 2001;94(2):363-364. doi:10.1097/00000542-200102000-00033 [PubMed 11176106]
  16. US Department of Health and Human Services; Centers for Disease Control and Prevention; National Institute for Occupational Safety and Health. NIOSH list of antineoplastic and other hazardous drugs in healthcare settings 2016. https://www.cdc.gov/niosh/docs/2016-161/default.html. Updated September 2016. Accessed October 5, 2016.
  17. Vogel D, Burkhardt T, Rentsch K, et al, "Misoprostol versus Methylergometrine: Pharmacokinetics in Human Milk," Am J Obstet Gynecol, 2004, 191(6):2168-73. [PubMed 15592308]
  18. Weiss G, Klein S, Shenkman L, Kataoka K, Hollander CS. Effect of methylergonovine on puerperal prolactin secretion. Obstet Gynecol. 1975;46(2):209-210. [PubMed 1080266]
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