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Methylergonovine

Pronunciation

(meth il er goe NOE veen)

Index Terms

  • Methylergometrine Maleate
  • Methylergonovine Maleate

Dosage Forms

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

Brand Names: U.S.

  • Methergine

Pharmacologic Category

  • Ergot Derivative

Pharmacology

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.

Absorption

Rapid

Distribution

Vd: 39-73 L

Metabolism

Hepatic

Excretion

Urine and feces

Onset of Action

Oxytocic: Oral: 5-10 minutes; IM: 2-5 minutes; IV: Immediately

Time to Peak

Serum: Oral: 0.3-2 hours; IM: 0.2-0.6 hours

Duration of Action

Oral: ~3 hours; IM: ~3 hours; IV: 45 minutes

Half-Life Elimination

~3 hours (range: 1.5-12.7 hours)

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

Contraindications

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

Dosing: Adult

Prevention of hemorrhage:

Oral: 0.2 mg 3-4 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 2-4 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.

Administration

IV: Administer over ≥60 seconds. 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 agent; use appropriate precautions for handling and disposal (NIOSH 2014 [group 3]).

Compatibility

Stable in NS.

Storage

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).

Drug 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. Avoid combination

Alpha1-Agonists: Ergot Derivatives may enhance the hypertensive effect of Alpha1-Agonists. Ergot Derivatives may enhance the vasoconstricting effect of Alpha1-Agonists. Avoid combination

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

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

Antihepaciviral Combination Products: May increase the serum concentration of Ergot Derivatives. 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 or rasagiline is combined with a serotonin modulator. Use of transdermal selegiline with serotonin modulators is contraindicated. 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. Monitor therapy

Aprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Beta-Blockers: May enhance the vasoconstricting effect of Ergot Derivatives. Consider therapy modification

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

Cobicistat: May increase the serum concentration of Methylergonovine. Avoid combination

Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Monitor therapy

CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates. Consider therapy modification

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

Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Itraconazole: May increase the serum concentration of Methylergonovine. Avoid combination

Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Ketoconazole (Systemic): May increase the serum concentration of Methylergonovine. 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. 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. Avoid combination

Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

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. Consider therapy modification

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

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

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. Monitor therapy

MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates. 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. Consider therapy modification

Netupitant: May increase the serum concentration of CYP3A4 Substrates. 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. Avoid combination

Palbociclib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Posaconazole: May increase the serum concentration of Methylergonovine. Avoid combination

Protease Inhibitors: May increase the serum concentration of Ergot Derivatives. Avoid combination

Reboxetine: May enhance the hypertensive effect of Ergot Derivatives. Monitor therapy

Roxithromycin: May increase the serum concentration of Ergot Derivatives. Avoid combination

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

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

Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Stiripentol: May increase the serum concentration of CYP3A4 Substrates. 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. Consider therapy modification

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

Telaprevir: May increase the serum concentration of Methylergonovine. 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. Monitor therapy

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

Adverse Reactions

Frequency not defined.

Cardiovascular: Angina pectoris, arterial spasm, atrioventricular block, bradycardia, cerebrovascular accident, chest pain, 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

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.

Special handling:

• Hazardous agent: Use appropriate precautions for handling and disposal (NIOSH 2014 [group 3]).

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.

Monitoring Parameters

Blood pressure

Pregnancy Risk Factor

C

Pregnancy Considerations

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

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience abdominal pain, nausea, vomiting, or diarrhea. Have patient report immediately to prescriber signs of severe cerebrovascular disease (change in strength on one side is greater than the other, trouble speaking or thinking, change in balance, or change in eyesight), angina, arrhythmia, severe dizziness, passing out, shortness of breath, severe headache, vision changes, hematuria, seizures, hallucinations, leg cramps, tinnitus, or sweating a lot (HCAHPS).

• Educate patient about signs of a significant reaction (eg, 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. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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