Embedded Files
Pharmacologic Category
Dosing: Adult
Prevention of 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.
* See Dosage and Administration in AHFS Essentials for additional information.
Dosing: Renal 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.
Use: Labeled Indications
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
* See Uses in AHFS Essentials for additional information.
Administration: IM
May be administered intramuscularly.
Administration: IV
Administer slowly over a period of no less than 60 seconds with careful monitoring of blood pressure. Should not be routinely administered IV because of possibility of inducing sudden hypertension and cerebrovascular accident. IV administration should only be considered during life-threatening situations.
Administration: Injectable Detail
pH: 2.7-3.5
Administration: 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).
Storage/Stability
Injection: Store under refrigeration at 2°C to 8°C (36°F to 46°F). Protect from light. The following stability information has also been reported: May be stored at room temperature for up to 14 days (Cohen, 2007).
Tablet: Store below 25°C (77°F).
Compatibility
See Trissel’s IV Compatibility Database
Open Trissel's IV Compatibility
Medication Patient Education with HCAHPS Considerations
What is this drug used for?
• It is used to stop or treat bleeding that happens after a birth.
• It may be given to you for other reasons. Talk with the doctor.
Frequently reported side effects of this drug
• Abdominal pain
• Nausea
• Vomiting
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
• Severe cerebrovascular disease like change in strength on one side is greater than the other, trouble speaking or thinking, change in balance, or change in eyesight.
• Severe dizziness
• Passing out
• Severe headache
• Vision changes
• Seizures
• Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.
Medication Safety Issues
Sound-alike/look-alike issues:
Administration issues:
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.
• Ergotism: Ergot alkaloid use may result in ergotism (intense vasoconstriction) resulting in peripheral vascular ischemia and possible gangrene. Ergotism is usually associated with overdosage or prolonged chronic use; do not exceed dosing guidelines and avoid prolonged administration.
• Pleural/retroperitoneal fibrosis: Rare cases of pleural and/or retroperitoneal fibrosis have been reported with prolonged daily use of other ergot alkaloids.
Disease-related concerns:
• Hepatic impairment: Use with caution in patients with hepatic impairment.
• Labor: Use with caution in the second stage of labor.
• Renal impairment: Use with caution in patients with renal impairment.
• Sepsis: Use with caution in patients with sepsis.
• Vascular disease: Use with caution in patients with obliterative vascular disease.
Concurrent drug therapy issues:
• CYP3A4 inhibitors: Concomitant use with potent inhibitors of CYP3A4 (includes protease inhibitors, azole antifungals, and some macrolide antibiotics) and ergot alkaloids has been associated with acute ergot toxicity (ergotism); concurrent use of certain ergot alkaloids (eg, ergotamine and dihydroergotamine) are not recommended by the manufacturer.
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.
* See Cautions in AHFS Essentials for additional information.
Pregnancy Risk Factor
C
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 recommended when a supplemental uterotonic agent is needed; due to maternal side effects it is not preferred for initial use (ACOG 183 2017).
Breast-Feeding Considerations
Methylergonovine is present in breast milk.
The relative infant dose (RID) of methylergonovine is 3.9% when calculated using the highest breast milk concentration located and compared to a weight-adjusted maternal dose of 0.375 mg/day.
In general, breastfeeding is considered acceptable when the RID of a medication is <10% (Anderson 2016; Ito 2000).
The RID of methylergonovine was calculated using a milk concentration of 1.3 ng/mL, providing an estimated daily infant dose via breast milk of 195 ng/kg/day. This milk concentration was obtained following maternal administration methylergonovine 0.125 mg three times daily for 5 days to eight 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). Higher doses are recommended in current product labeling.
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).
Briggs' Drugs in Pregnancy & Lactation
Adverse Reactions
Frequency not defined.
Cardiovascular: Angina pectoris, atrioventricular block, bradycardia, cerebrovascular accident, chest pain, coronary artery vasospasm, hypertension, hypotension, local thrombophlebitis, myocardial infarction, palpitations, paresthesia, tachycardia, vasospasm, ventricular fibrillation
Central nervous system: Dizziness, hallucination, headache, seizure
Dermatologic: Diaphoresis, skin rash
Endocrine & metabolic: Water intoxication
Gastrointestinal: Abdominal pain, diarrhea, nausea, unpleasant taste, vomiting
Genitourinary: Hematuria
Hypersensitivity: Anaphylaxis
Neuromuscular & skeletal: Leg cramps
Otic: Tinnitus
Respiratory: Dyspnea, nasal congestion
* See Cautions in AHFS Essentials for additional information.
Allergy and Idiosyncratic Reactions
Metabolism/Transport Effects
Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Drug Interactions Open Interactions
Alpha-/Beta-Agonists: Ergot Derivatives may enhance the hypertensive effect of Alpha-/Beta-Agonists. Ergot Derivatives may enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Risk X: Avoid combination
Alpha1-Agonists: Ergot Derivatives may enhance the hypertensive effect of Alpha1-Agonists. Ergot Derivatives may enhance the vasoconstricting effect of Alpha1-Agonists. Risk X: Avoid combination
Antihepaciviral Combination Products: May increase the serum concentration of Ergot Derivatives. Risk X: Avoid combination
Aprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Beta-Blockers: May enhance the vasoconstricting effect of Ergot Derivatives. Risk D: Consider therapy modification
Chloroprocaine: May enhance the hypertensive effect of Ergot Derivatives. Risk C: Monitor therapy
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Cobicistat: May increase the serum concentration of Methylergonovine. Risk X: Avoid combination
Conivaptan: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Risk D: Consider therapy modification
Duvelisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Erdafitinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Fosnetupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Idelalisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Itraconazole: May increase the serum concentration of Methylergonovine. Risk X: Avoid combination
Ketoconazole (Systemic): May increase the serum concentration of Methylergonovine. Risk X: Avoid combination
Larotrectinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Letermovir: May increase the serum concentration 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
Macrolide Antibiotics: May increase the serum concentration of Ergot Derivatives. Cabergoline and Clarithromycin may interact, see specific monograph for full details. Exceptions: Azithromycin (Systemic); Fidaxomicin; Spiramycin. Risk X: Avoid combination
MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Risk D: Consider therapy modification
Nefazodone: Ergot Derivatives may enhance the serotonergic effect of Nefazodone. This could result in serotonin syndrome. Nefazodone may increase the serum concentration of Ergot Derivatives. Risk X: Avoid combination
Netupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Nitroglycerin: Ergot Derivatives may diminish the vasodilatory effect of Nitroglycerin. This is of particular concern in patients being treated for angina. Nitroglycerin may increase the serum concentration of Ergot Derivatives. Risk X: Avoid combination
Palbociclib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Posaconazole: May increase the serum concentration of Methylergonovine. Risk X: Avoid combination
Protease Inhibitors: May increase the serum concentration of Ergot Derivatives. Risk X: Avoid combination
Reboxetine: May enhance the hypertensive effect of Ergot Derivatives. Risk C: Monitor therapy
Roxithromycin: May increase the serum concentration of Ergot Derivatives. 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. Exceptions: Nefazodone. Risk C: Monitor therapy
Serotonin 5-HT1D Receptor Agonists (Triptans): May enhance the vasoconstricting effect of Ergot Derivatives. Ergot Derivatives may enhance the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists (Triptans). Risk X: Avoid combination
Simeprevir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Stiripentol: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Risk D: Consider therapy modification
Voriconazole: May increase the serum concentration of Methylergonovine. Risk X: Avoid combination
Genes of Interest
Monitoring Parameters
Blood pressure
Advanced Practitioners Physical Assessment/Monitoring
Blood pressure, CNS status, and vaginal bleeding should be monitored on a regular basis.
Nursing Physical Assessment/Monitoring
Monitor blood pressure, CNS status, and vaginal bleeding on a regular basis. May cause nausea. Patient may require antiemetic.
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
Anatomic Therapeutic Chemical (ATC) Classification
- G02AB01
Generic Available (US)
Yes
Pricing: US
Solution (Methylergonovine Maleate Injection)
0.2 mg/mL (per mL): $8.80 - $32.54
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.
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.
Pharmacodynamics/Kinetics
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
Local Anesthetic/Vasoconstrictor Precautions
Use vasoconstrictor with caution in patients taking methylergonovine; this ergot alkaloid derivative causes constriction of peripheral blood vessels
Effects on Dental Treatment
No significant effects or complications reported
Effects on Bleeding
Thrombosis has been reported; however, there are no special precautions associated with bleeding related to dental procedures.
Related Information
Index Terms
Methylergometrine Maleate; Methylergonovine Maleate
References
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]
Anderson PO, Sauberan JB. Modeling drug passage into human milk. Clin Pharmacol Ther. 2016;100(1):42-52.[PubMed 27060684]
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]
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]
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]
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]
Ito S. Drug therapy for breast-feeding women. N Engl J Med. 2000;343(2):118-126.[PubMed 10891521]
Methergine (methylergonovine maleate) [prescribing information]. Baltimore, MD: Lupin Pharma; January 2016.
Methylergometrine: adverse effects in breastfed infants. Prescrire Int. 2014;23(148):102.[PubMed 24860899]
Methylergonovine maleate [prescribing information]. Colombus, OH: American Health Packaging; September 2018.[PubMed 24860899]
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. http://www.cdc.gov/niosh/topics/antineoplastic/pdf/hazardous-drugs-list_2016-161.pdf. Updated September 2016. Accessed October 5, 2016.
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]
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]
Brand Names: International
Basofortina (AR, PY); Bledstop (ID); Demergin (GR); Ergogin (IN); Ergojen (PH); Ergomet (PH); Ergomin (IN); ERruvin (KR); Expogin (TH); Femitranol (PY); Ingagen-M (IN); Mem (PH); Mergot (PH); Mergotrex (PH); Methergin (AE, AT, BD, BE, BF, BG, BH, BJ, BR, CH, CI, CL, CO, CZ, DE, DK, EE, ES, ET, FI, FR, GB, GH, GM, GN, HK, HN, ID, IE, IS, IT, JO, JP, KE, KR, KW, LR, MA, ML, MR, MT, MU, MW, MX, MY, NE, NG, NL, PE, PH, PK, PT, QA, RU, SC, SD, SE, SG, SI, SK, SL, SN, TN, TW, TZ, UG, UY, VE, VN, ZA, ZM, ZW); Methergine (CY, SA, TR); Metiagin (ID); Metvell (ID); Mitrotan (BG); Morgin (ID); Myotonic (ID); Neo-Ergo (TW); Pospargin (VN); Uterine (PH)
Last Updated 3/28/20
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