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

For abbreviations and symbols that may be used in Lexicomp (show table)
Brand Names: US
  • Methergine
Brand Names: Canada
  • Methergine®
Pharmacologic Category
  • Ergot Derivative
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.

Dosing: Renal Impairment

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

Dosing: Hepatic Impairment

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

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

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 [DSC]

Generic Equivalent Available (US)

Yes

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.

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

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.

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.

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

Contraindications

Hypersensitivity to methylergonovine or any component of the formulation; hypertension; toxemia; 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.

Metabolism/Transport Effects

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

Drug Interactions

(For additional information: Launch drug interactions program)

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

Antiemetics (5HT3 Antagonists): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Risk C: Monitor therapy

Antihepaciviral Combination Products: May increase the serum concentration of Ergot Derivatives. Risk X: Avoid combination

Anti-Parkinson Agents (Monoamine Oxidase Inhibitor): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity if selegiline, rasagiline, or safinamide is combined with a serotonin modulator. Use of transdermal selegiline with serotonin modulators is contraindicated. Risk D: Consider therapy modification

Antipsychotic Agents: Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Risk C: Monitor therapy

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

Boceprevir: May increase the serum concentration of Methylergonovine. Risk X: Avoid combination

Ceritinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of ceritinib with a narrow therapeutic index CYP3A substrate (eg, alfentanil, cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, tacrolimus) should be avoided when possible. Risk C: Monitor therapy

Chloroprocaine: May enhance the hypertensive effect of Ergot Derivatives. 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

Dapoxetine: May enhance the adverse/toxic effect of Serotonin Modulators. Risk X: Avoid combination

Dasatinib: 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

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

Letermovir: May increase the serum concentration of Ergot Derivatives. Risk X: Avoid combination

Linezolid: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Management: Due to a risk of serotonin syndrome/serotonin toxicity, discontinue serotonin modulators 2 weeks prior to the administration of linezolid. If urgent initiation of linezolid is needed, discontinue serotonin modulators immediately and monitor closely. Risk D: Consider therapy modification

Lorcaserin: 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 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 D: Consider therapy modification

Metaxalone: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Risk C: Monitor therapy

Methylene Blue: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Risk X: Avoid combination

Methylphenidate: May enhance the adverse/toxic effect of Serotonin Modulators. Specifically, the risk of serotonin syndrome or serotonin toxicity may be increased. Risk C: Monitor therapy

Metoclopramide: Serotonin Modulators may enhance the adverse/toxic effect of Metoclopramide. This may be manifest as symptoms consistent with serotonin syndrome or neuroleptic malignant syndrome. Risk C: Monitor therapy

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

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

Opioid Analgesics: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Risk C: Monitor therapy

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

Serotonin 5-HT1D Receptor Agonists: Ergot Derivatives may enhance the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists. Serotonin 5-HT1D Receptor Agonists may enhance the vasoconstricting effect of Ergot Derivatives. Risk X: Avoid combination

Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Exceptions: Nicergoline; Tedizolid. Risk C: Monitor therapy

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

Tedizolid: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Risk C: Monitor therapy

Telaprevir: May increase the serum concentration of Methylergonovine. Risk X: Avoid combination

TraMADol: Serotonin Modulators may enhance the adverse/toxic effect of TraMADol. The risk of seizures may be increased. TraMADol may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Risk C: Monitor therapy

Voriconazole: May increase the serum concentration of Methylergonovine. Risk X: Avoid combination

Pregnancy Risk Factor

C (show table)

Pregnancy Implications

Animal reproduction studies have not been conducted. Methylergonovine is intended for use after delivery of the infant; use is contraindicated during pregnancy.

Breast-Feeding Considerations

At normal doses used to control postpartum uterine bleeding, small amounts are excreted in breast milk. In one study, ten women were given a single dose of methylergonovine 0.5 mg once lactation was established. Simultaneous maternal milk and plasma samples were taken 1 and 2 hours later. Maximum milk concentrations were 410-830 pg/mL, 2-3 hours after the dose and declined to 0.2 pg/mL (median) at 5 hours. The mean M/P ratios were 0.18 (at 1 hour) and 0.17 (at 2 hours) (Vogel, 2004). Methylergonovine may decrease breast milk production. Some manufacturers do not recommend breast-feeding during therapy or for 12 hours after the last dose due to adverse reactions reported in breast-feeding infants.

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.

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

Pricing: US

Solution (Methylergonovine Maleate Injection)

0.2 mg/mL (1 mL): $6.00

Tablets (Methergine Oral)

0.2 mg (12): $896.40

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.

Brand Names: International
  • Basofortina (AR, PY);
  • Bledstop (ID);
  • Demergin (GR);
  • Ergojen (PH);
  • Ergomet (PH);
  • 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, EG, ES, ET, FI, FR, GB, GH, GM, GN, HK, HN, ID, IE, IL, 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, LB, SA, TR);
  • Metiagin (ID);
  • Metvell (ID);
  • Mitrotan (BG);
  • Myotonic (ID);
  • Neo-Ergo (TW);
  • Pospargin (ID, VN);
  • Utergin (ID);
  • Uterine (PH)
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REFERENCES

  1. 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]
  2. 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]
  3. Methergine (methylergonovine maleate) [prescribing information]. Baltimore, MD: Lupin Pharma; January 2016.
  4. 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.
  5. 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]
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