Methylergonovine (Systemic)



Primary: GU600

Commonly used brand name(s): Methergine.

Another commonly used name is
methylergometrine {12} {15} .
Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).

Not commercially available in Canada.


Uterine stimulant—


Note: Bracketed information in the Indications section refers to uses that are not included in U.S. product labeling.


Hemorrhage, postpartum and postabortal (prophylaxis and treatment)—Methylergonovine is indicated in the prevention or treatment of postpartum or postabortal uterine bleeding due to uterine atony or subinvolution. Its use is not recommended prior to delivery of the placenta since placental entrapment may occur. {18} {25}

[Abortion, incomplete (treatment)]—In cases of incomplete abortion, methylergonovine may be used to hasten expulsion of uterine contents.

Methylergonovine is not as effective in treatment of migraine as other ergot alkaloids and use is not recommended. {15}

Methylergonovine is not indicated for induction or augmentation of labor, to induce abortion, or in cases of threatened spontaneous abortion because of its propensity to produce nonphysiologic, tetanic contractions and its long duration of action. {11} {12} {15} {18} {22} {25}


Physicochemical characteristics:

Chemical group—
    Amine ergot alkaloid. {12} {25}
Molecular weight—
    455.51 {33}

Mechanism of action/Effect:

Uterine stimulant:

Methylergonovine directly stimulates the uterine muscle to increase force and frequency of contractions {11} {12} {22} {23} {25}. When usual doses of methylergonovine are used, these contractions precede periods of relaxation; when larger doses are used, basal uterine tone is elevated and these relaxation periods will be decreased {11} {12} {25} {27}. Contraction of the uterine wall around bleeding vessels at the placental site produces hemostasis {14}. The sensitivity of the uterus to the oxytocic effect is much greater toward the end of pregnancy. {11} {12} {15} {22} The oxytocic actions of methylergonovine are greater than its vascular effects. {12} {17}


Methylergonovine, like other ergot alkaloids, produces arterial vasoconstriction by stimulation of alpha-adrenergic and serotonin receptors and inhibition of endothelial-derived relaxation factor release {12} {13} {22} {23} {25} {26}. It is a less potent vasoconstrictor than ergotamine. {12}

Other actions/effects:

Methylergonovine has minor actions on the central nervous system (CNS). {12} In the CNS, methylergonovine is a partial agonist and partial antagonist at some serotonin and dopamine receptors. {12} Methylergonovine also possesses weak dopaminergic antagonist actions in certain blood vessels {12} and partial agonist actions at serotonin receptors in umbilical and placental blood vessels {12}. It does not possess significant alpha-adrenergic blocking activity. {12}


Absorption is rapid after oral (60%) and intramuscular (78%) administration. {07} {12} {15} {22} {25}


Rapidly, primarily to plasma and extracellular fluid following intravenous administration; distribution to tissues also occurs rapidly {25}.

In a study in women who had received 125 mcg of methylergonovine orally 3 times a day for 5 days, concentrations in breast milk ranged from less than 0.5 (limit of detection) to 1.3 nanograms per mL at 1 hour after a 250 mcg oral dose and from 0 to 1.2 nanograms per mL at 8 hours {10} {15} {16}.


Likely hepatic, with extensive first-pass metabolism. {12} {22} {25}



2 to 3 minutes or less (alpha phase). {07} {25}

20 to 30 minutes or longer (beta phase). {07} {25}

Onset of action:

Contraction of uterus, postpartum:

Oral: 5 to 10 minutes. {07} {08} {18} {22} {25}

Intramuscular: 2 to 5 minutes. {07} {11} {22} {25}

Intravenous: Immediate. {07} {25}

Time to peak concentration:

In a study in postpartum patients, peak plasma concentrations occurred at 3 hours after a 250 mcg oral dose {25}. In a study in healthy fasting males, peak plasma concentrations occurred at 30 minutes {25}.

Peak serum concentration:

In a study in postpartum patients, peak plasma concentrations were 3 nanograms per mL after a 250 mcg oral dose {25}. In a study in healthy fasting males, similar concentrations were achieved {25}. Women given 125 mcg by mouth 3 times a day for 5 days had plasma concentrations within the range of 0.6 to 4.4 nanograms per mL at 1 hour after a 250 mcg oral dose and from 0 to 0.6 nanograms per mL at 8 hours {15}.

Duration of action:

Contraction of uterus, postpartum:

Oral: Approximately 3 hours. {07} {25}

Intramuscular: Approximately 3 hours. {07} {25}

Intravenous: 45 minutes {25} (although rhythmic contractions may persist for up to 3 hours). {07}

    Primarily renal excretion of metabolites {22} {25}; some fecal {22} {25}. Renal elimination of unchanged drug is responsible for less than 5% of total elimination {22} {25}. Methylergonovine does not appear to accumulate after multiple doses {25}.

Precautions to Consider

Cross-sensitivity and/or related problems

Patients sensitive to other ergot derivatives may be sensitive to this medication also, although there is some degree of variation among ergot alkaloids in their ability to elicit oxytocic, CNS, or vasoconstrictive effects. {12}


Methylergonovine is contraindicated during pregnancy. {11} {16} {22} {23} {27} Tetanic contractions may result in decreased uterine blood flow and fetal distress. {11} {27}

Labor and delivery—

High doses of methylergonovine administered prior to delivery may cause uterine tetany and fetal distress {11} {35}. Methylergonovine should not be administered prior to delivery of the placenta {25}. Administration prior to delivery of the placenta may cause captivation of the placenta or missed diagnosis of twin gestation, due to excessive uterine contraction {14} {25}.


Problems in humans have not been documented. Ergot alkaloids are excreted in breast milk {25}. However, very little passes into breast milk in humans {10} {15} {16} {25}. In a study in women who had received 125 mcg of methylergonovine orally 3 times a day for 5 days, concentrations in breast milk ranged from less than 0.5 (limit of detection) to 1.3 nanograms per mL at 1 hour after a 250 mcg oral dose and from 0 to 1.2 nanograms per mL at 8 hours {10} {15} {16}.

Inhibition of lactation has not been reported for methylergonovine {32} . However, studies have shown that methylergonovine may interfere with the secretion of prolactin (to a lesser degree than bromocriptine) in the immediate postpartum period. {12} {16} {22} {25} This could result in delayed or diminished lactation with prolonged use. {12} {14} {16} {22} {25}

Ergot alkaloids have the potential to cause chronic ergot poisoning in the infant only if used in the mother in higher-than-recommended doses or if used for a longer period of time than is generally recommended. {12} {16}


In newborns, elimination of methylergonovine may be prolonged {25}. Neonates inadvertently administered ergonovine in overdose amounts have developed respiratory depression, myoclonic movements, purpuric symptoms, mild jaundice, and severe peripheral vasoconstriction. {15} {25} {28}


No information is available on the effects of methylergonovine in geriatric patients.

Drug interactions and/or related problems
The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

Note: Combinations containing any of the following medications, depending on the amount present, may also interact with this medication. {02}

Anesthetics, general, especially halothane{15}{17}{18}    (peripheral vasoconstriction may be potentiated by the concurrent use of general anesthetics with methylergonovine {17})

    (concurrent use of halothane in concentrations greater than 1% may interfere with the oxytocic actions of methylergonovine, resulting in severe uterine hemorrhage {15} {18})

Bromocriptine{13} or
Ergot alkaloids, other{13}{28}    (the incidence of rare cases of hypertension, strokes, seizures, and myocardial infarction associated with the postpartum use of bromocriptine or other ergot alkaloids may be increased with the use of ergot alkaloids {03} {04} {13})

Nicotine or
Smoking, tobacco    (nicotine absorption from heavy smoking may result in enhanced vasoconstriction)

Nitroglycerin{21}{29} or
Antianginal agents, other{29}    (ergot alkaloids may induce coronary vasospasm, lowering the efficacy of nitroglycerin or other antianginal agents {21} {29}; increased doses of nitroglycerin or antianginal agents and/or use of intracoronary nitroglycerin may be necessary {30})

Vasoconstrictors, other, including those present in local anesthetics or{12}{14}{15}{25}
Vasopressors{12}{15}{21}    (concurrent use may result in enhanced vasoconstriction; dosage adjustments may be necessary {12} {15})

    (the pressor effect of sympathomimetic pressor amines may be potentiated, resulting in potentially severe hypertension, headache, and rupture of cerebral blood vessels {15} {25}; gangrene developed in a patient receiving both dopamine and ergonovine infusions {15} {21})

Laboratory value alterations
The following have been selected on the basis of their potential clinical significance (possible effect in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

With physiology/laboratory test values
Blood pressure or{12}{13}{14}{22}{25}{29}
Central venous pressure{25}    (may be elevated due to peripheral vasoconstriction primarily of postcapillary vessels {12} {13} {25}; less likely with methylergonovine than ergonovine {18} {22} {25}; has sometimes been associated with preeclampsia, history of hypertension, intravenous administration of methylergonovine, or concurrent use of local anesthetics containing vasoconstrictors {13}; hypotension has also been reported {12} {13} {25})

Heart rate{12}{13}{15}{17}    (may be decreased due primarily to an increase in vagal tone, and possibly to decreased central sympathetic activity and direct depression of the myocardium {12} {13} {17})

Prolactin{22}{25}{27}    (serum concentrations may be decreased {22} {25} {27})

Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).

Except under special circumstances, this medication should not be used when the following medical problems exist:
» Angina pectoris, unstable or{15}{19}{25}{29}{34}
» Myocardial infarction, recent{15}{19} {25}{26}{29}{34}    (vasospasm caused by methylergonovine may precipitate angina or myocardial infarction {03} {07} {16} {29} {31} {34})

» Cardiovascular disease or{34}{35}{36}
» Coronary artery disease{12}{15}{23}{25}{26}{29}{31}{34}{35}{36}    (patients may be more susceptible to angina or myocardial infarction caused by methylergonovine-induced vasospasm {31} {34})

» Cerebrovascular accident, history of or{19}{26}{29}{34}
» Transient ischemic attack, history of{19}{26}{29}{34}    (patients may be susceptible to recurrence due to increases in blood pressure)

» Eclampsia or{15}{28}{29}{34}
» Preeclampsia{13}{14}{15}{25}{28}{29}{34}    (may be exacerbated {15} {25} {26} {28} {31} {34}; patients may be more likely to develop methylergonovine-induced hypertension {14} {18} {28} {34}; headaches, severe cardiac arrhythmias, seizures, and cerebrovascular accidents have occurred {18} {25} {28} {29} {34})

» Hypertension, severe, or history of{13}{14}{15}{18}{23}{25}{26}{28}{29}{34}    (may be exacerbated {15} {25} {26} {28} {31} {34})

» Occlusive peripheral vascular disease{12}{15}{18}{23}{25}{29}{34} or
» Raynaud's phenomenon, severe{12}{26}{29}{34}    (may be exacerbated {12} {26} {34}; a patient with Raynaud's phenomenon developed impalpable arterial pulses with use of ergonovine {12} {17} {18} {34})

Risk-benefit should be considered when the following medical problems exist
Allergy or sensitivity to methylergonovine or other ergot alkaloids{18}{25}{34}
» Hepatic function impairment{12}{15}{18}{22}{23}{25}{34}    (impaired metabolism of methylergonovine may result in ergot overdose {34})

Hypocalcemia{25}{34}    (oxytocic response to methylergonovine may be reduced {25} {34}; cautious use of intravenous calcium gluconate may restore oxytocic response to methylergonovine {25} {34})

» Mitral valve stenosis or{25}{29}{34}
» Venoatrial shunts{25}{29}{34}    (vasospasm caused by methylergonovine may precipitate angina or myocardial infarction {29} {31} {34})

» Renal function impairment{15}{18}{23}{25}{31}{34}
» Sepsis{12}{15}{23}{25}{34}    (possible increased sensitivity to effects of methylergonovine {12} {34})

Patient monitoring
The following may be especially important in patient monitoring (other tests may be warranted in some patients, depending on condition; » = major clinical significance):

Blood pressure determinations and{22}{23}{25}
Pulse rate determinations and{23}
Uterine response{25}    (recommended at frequent intervals after parenteral therapy to monitor for adverse reactions; especially important with intravenous administration or before repeating doses {35})

Side/Adverse Effects

Note: Because the duration of therapy with methylergonovine is generally short, many of the side effects seen with other ergot alkaloids do not occur {25}.

The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention
Incidence less frequent
Bradycardia {12}{14}{15}{28}(slow heartbeat)
coronary vasospasm {12}{13}{14}{15}{21}{23}{25}(chest pain)

Incidence rare
Allergic reaction, including shock{25}
cardiac arrest{13}{14}{19}{26}{28} or ventricular arrhythmias, including fibrillation and tachycardia (irregular heartbeat){14}{15}{19}{22}{25}{28}
dyspnea {15}{22}{25}(unexplained shortness of breath)
hypertension, sudden and severe {12}{13}{14}{15}{17}{18}{20}{22}{25}(sudden, severe headache; blurred vision; seizures)
myocardial infarction {13}{14}{15}{19}(crushing chest pain; unexplained shortness of breath)—has occurred with the use of ergot preparations in the postpartum period{13}{14}
peripheral vasospasm (itching of skin; pain in arms, legs, or lower back; pale or cold hands or feet; weakness in legs)—dose-related{22}{25}{37}

Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent
Nausea —especially after intravenous use{12}{15}{18}{19}{22}{25}
uterine cramping{11}{15}{19}{25}
vomiting —especially after intravenous use{12}{15}{18}{19}{22}{25}

Note: Uterine cramping will occur to some degree in all patients and is indicative of efficacy. However, dosage reduction may be required in occasional patients with severe or intolerable uterine cramps. {25}

Incidence less frequent
Abdominal or stomach pain{15}
tinnitus {15}{22}{25}(ringing in the ears)

For specific information on the agents used in the management of methylergonovine overdose, see:
   • Charcoal, Activated (Oral-Local) monograph;
   • Chlorpromazine in Phenothiazines (Systemic) monograph;
   • Diazepam in Benzodiazepines (Systemic) monograph;
   • Hydralazine (Systemic) monograph;
   • Laxatives (Local) monograph;
   • Nitroglycerin in Nitrates (Systemic) monograph;
   • Nitroprusside (Systemic) monograph;
   • Phentolamine (Systemic) monograph;
   • Phenytoin in Anticonvulsants, Hydantoin (Systemic) monograph; and/or
   • Tolazoline (Parenteral-Systemic) monograph.
For more information on the management of overdose or unintentional ingestion, contact a Poison Control Center (see Poison Control Center Listing ).

Clinical effects of overdose
The following effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:
Angina {12}{25}(chest pain)
bradycardia {12}( slow heartbeat)
confusion {12}
drowsiness {12}
fast, weak pulse {12} {25}
miosis {12}(small pupils)
peripheral vasoconstriction, severe (coolness, paleness, or numbness of arms or legs; muscle pain; weak or absent arterial pulse in arms or legs ; tingling, itching, and coolness of skin {12} {17} {25})
respiratory depression {15}{25}(decreased breathing rate or trouble in breathing ; bluish color of skin or inside of nose or mouth)
seizures {12} {15}
tachycardia {12}( fast heartbeat)
unconsciousness {12} {25}
unusual thirst {12}
uterine tetany {11}{12}(severe cramping of the uterus)

Formication {12}{17}{25}(false feeling of insects crawling on the skin )
gangrene {12}{15}{20}{25}(dry, shriveled appearance of skin on hands, lower legs, or feet)
hemiplegia {12}(paralysis of one side of the body)
thrombophlebitis {12}{20}{25}(pain and redness in an arm or leg)

Note: Chronic overdose symptoms are unlikely with proper use since treatment is of short duration. {12} {15} {14} {25}

Treatment of overdose
Immediate discontinuation of methylergonovine. {12} {14} Since there is no specific antidote for the management of methylergonovine overdose, treatment is primarily supportive and symptomatic and may include the following: {12} {15} {26} {38}

To decrease absorption:
Gastrointestinal decontamination for oral overdose, preferably with multiple doses of activated charcoal and an appropriate cathartic. {03} {23} {25} Gastric lavage may also be considered. {03} {15} {23} {25}

Specific treatment:
Use of nitroglycerin for treatment of myocardial ischemia {03} {12} {15} {19}. Intracoronary nitroglycerin may be necessary. {15} {19}

Use of diazepam or phenytoin for treatment of seizures. {03} {15} {23} {25}

Use of sodium nitroprusside, tolazoline, or phentolamine for treatment of peripheral ischemia. {03} {12} {15} {23} {25}

Use of sodium nitroprusside, chlorpromazine 15 mg, or hydralazine for treatment of severe hypertension. {07} {12} {15} {23} {25}

Frequent monitoring of vital signs, arterial blood gases, and electrolytes. {03} {23} Electrocardiogram monitoring to assess cardiac function and perfusion. {03} Monitoring of serum methylergonovine levels is not predictive of the outcome of overdose. {03}

Supportive care:
May include maintaining an open airway and breathing, maintaining proper fluid and electrolyte balance, correcting hypertension, and controlling seizures. Patients in whom intentional overdose is known or suspected should be referred for psychiatric consultation.

Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Ergonovine/Methylergonovine (Systemic).

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Allergies or sensitivity to methylergonovine or other ergot alkaloids

Pregnancy—Should not be used prior to delivery or delivery of the placenta

Breast-feeding—Ergot alkaloids are excreted in breast milk
Other medical problems, especially cardiac or vascular disease, hepatic function impairment, severe hypertension or history of hypertension, renal function impairment, and sepsis

Proper use of this medication
» Importance of not using more medication or using for longer than prescribed; risk of ergotism and gangrene with prolonged use

» Proper dosing
Missed dose: Not taking missed dose; not doubling doses

» Proper storage

Precautions while using this medication
Notifying physician if infection develops, since infection may cause increased sensitivity to medication

Side/adverse effects
Signs of potential side effects, especially allergic reaction, coronary vasospasm or other cardiovascular complications, dyspnea, severe hypertension, or peripheral vasospasm

General Dosing Information
Antiemetic medications such as prochlorperazine may be administered prior to use of methylergonovine. {12} {15} {25}

For parenteral dosage forms only
Because the risk of severe adverse effects is increased with intravenous use of methylergonovine, such use is recommended only for emergencies such as excessive uterine bleeding. {14} {15} {18} {19} {22} {24} {25} {28}

If intravenous use is warranted, administration must be done slowly, over a period of at least 1 minute {15} {22} {24} {25}; some clinicians recommend dilution of the solution with normal saline before administration. {14} {24} {25}

In some patients who do not respond to methylergonovine because of hypocalcemia, cautious intravenous administration of calcium gluconate (provided the patient is not receiving digitalis) may restore the oxytocic action. {25}

Oral Dosage Forms


Usual adult and adolescent dose
Uterine stimulant
Oral, 200 to 400 mcg (0.2 to 0.4 mg) two to four times a day (every six to twelve hours) until the danger of uterine atony and hemorrhage has passed. {15} {18} {19} {22} {25}

Note: Generally, a treatment course of 48 hours is sufficient {18} {25}. However, in some patients, treatment for up to 7 days may be necessary, especially when used for treatment of incomplete abortion {15} {25}. Oral administration usually follows an initial parenteral dose. {25}

Strength(s) usually available

200 mcg (0.2 mg) (Rx) [Methergine]

Not commercially available.

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight container. Protect from light.

Parenteral Dosage Forms


Usual adult and adolescent dose
Uterine stimulant
Intramuscular or intravenous, 200 mcg (0.2 mg), repeated in two to four hours if necessary, up to five doses. {15} {18} {19} {24} {25}

Strength(s) usually available

200 mcg (0.2 mg) per mL (Rx) [Methergine]

Not commercially available.

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from light. Protect from freezing.

Discolored solutions or solutions containing visible particles should not be used. {24}

Revised: 06/07/1993

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