Methylergonovine, Ergonovine (Monograph)

Brand names: Ergotrate, Methergine
Drug class: Oxytocics
ATC class: G02AB03
VA class: GU600
CAS number: 57432-61-8

Introduction

Stimulates contractions of uterine smooth muscle; amine ergot alkaloids.

Uses for Methylergonovine, Ergonovine

Postpartum Hemorrhage

Prevention and treatment of postpartum hemorrhage in the presence of uterine atony.

Administration of parenteral ergot alkaloids in the third stage of labor decreases mean blood loss and incidence of postpartum blood loss of ≥500 mL.

Methylergonovine maleate: A first-line agent for the treatment of postpartum hemorrhage; usually given after oxytocin.

Should not be used for the induction or augmentation of labor. Should not be used in cases of threatened spontaneous abortion.

Test for Variant Angina

Ergonovine maleate: Has been useful in diagnosing variant angina^{† [off-label]}. Administered IV to induce coronary artery spasm in patients with suspected variant angina.

Methylergonovine, Ergonovine Dosage and Administration

Administration

Ergonovine maleate: Administer orally or by IM injection. When used for diagnosis of variant angina^{† [off-label]}, has been administered IV.

Methylergonovine maleate: Administer orally or by IM or slow IV injection. Parenteral preparation also has been administered directly into the uterine corpus^{† [off-label]}.

Do not administer by intra-arterial or periarterial injection.

IV Administration

Methylergonovine maleate: For drug compatibility information, see Compatibility under Stability.

Methylergonovine maleate: Reserve IV administration for severe uterine bleeding or other life-threatening emergency situations. (See IV Administration under Cautions.)

If given IV, monitor BP.

Dilution

Methylergonovine maleate: May be diluted to a volume of 5 mL with 0.9% sodium chloride injection.

Rate of Administration

Methylergonovine maleate: Administer over at least 1 minute.

Dosage

Available as ergonovine maleate; dosage expressed in terms of ergonovine maleate.

Available as methylergonovine maleate; dosage expressed in terms of methylergonovine maleate.

Adults

Postpartum Hemorrhage

Oral or Sublingual

Ergonovine maleate: To minimize late postpartum bleeding, 0.2–0.4 mg every 6–12 hours until uterine atony has passed (usually 48 hours). Lower dose may be used if severe cramping occurs.

Oral

Methylergonovine maleate: To control uterine bleeding during the puerperium, 0.2 mg 3 or 4 times daily for up to 1 week.

IM

Ergonovine maleate: 0.2 mg. Repeat as necessary; manufacturer states that IM dose rarely needed more frequently than once in 2–4 hours.

IV or IM

Methylergonovine maleate: 0.2 mg; repeat as necessary every 2–4 hours.

Test for Variant Angina† [off-label]

IV

Ergonovine maleate: 0.1–0.4 mg has been used.

Special Populations

Hepatic Impairment

No specific dosage recommendations for hepatic impairment.

Renal Impairment

No specific dosage recommendations for renal impairment.

Geriatric Patients

Methylergonovine maleate: Manufacturer recommends selecting dose with caution; start at the lower end of the dosing range due to the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy.

Cautions for Methylergonovine, Ergonovine

Contraindications

• Hypersensitivity to ergonovine, methylergonovine, or any ingredient in the formulation.

• Hypertension.

• Toxemia.

• Pregnancy.

Warnings/Precautions

Warnings

IV Administration

Methylergonovine maleate: Do not routinely administer IV. Possibility of sudden hypertension and cerebrovascular accident when administered IV.

Methylergonovine maleate: If IV administration is considered lifesaving, administer slowly; monitor BP. (See IV Administration under Dosage and Administration.)

General Precautions

Avoid prolonged use; discontinue if ergotism develops.

Concomitant Diseases

Caution in patients with sepsis, heart disease, venoatrial shunts, mitral valve stenosis, or obliterative vascular disease.

Specific Populations

Pregnancy

Methylergonovine maleate: Category C.

Methylergonovine and Ergonovine: contraindicated during pregnancy because of the drugs’ uterotonic effects. (See Contraindications.)

Lactation

Methylergonovine maleate: Distributed into human milk. Use with caution in nursing women.

Methylergonovine maleate: May be administered orally for a maximum of 1 week postpartum to control uterine bleeding. (See Postpartum Hemorrhage under Dosage and Administration.)

Pediatric Use

Safety and efficacy not established in children.

Geriatric Use

Methylergonovine maleate: Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.

Hepatic Impairment

Use with caution.

Renal Impairment

Use with caution.

Common Adverse Effects

Hypertension, seizures, headache, hypotension, nausea, vomiting.

Drug Interactions

Drugs Affecting Hepatic Microsomal Enzymes

Methylergonovine maleate: Interaction possible with drugs that are inhibitors of CYP3A4; potential for vasospasm, cerebral ischemia, and/or ischemia of the extremities.

Concomitant use of ergot alkaloids and HIV protease inhibitors, delavirdine, or efavirenz is contraindicated. Because postpartum hemorrhage due to uterine atony is often managed with methylergonovine, the Perinatal HIV Guidelines Working Group of the Public Health Service Task Force has issued recommendations concerning use of methylergonovine in women receiving certain antiretroviral agents. For recommendations concerning use of methylergonovine in patients receiving HIV protease inhibitors, delavirdine, or efavirenz, see Specific Drugs under Interactions.

Specific Drugs

Methylergonovine, Ergonovine Pharmacokinetics

Absorption

Bioavailability

Rapidly absorbed after oral or IM administration. Following oral administration of ergonovine, bioavailability reported as 34–117%. Following oral administration of methylergonovine, bioavailability is about 60%.

Onset

Oral administration: Uterine contractions occur within 5–15 minutes.

IM injection: Uterine contractions occur within 2–5 minutes.

IV administration: Uterine contractions occur immediately.

Duration

Oral administration or IM injection: Uterine contractions persist ≥3 hours.

IV injection: Uterine contractions persist for 45 minutes.

Distribution

Extent

Following IV administration of methylergonovine, rapidly distributed to tissues (i.e., in 2-3 minutes).

Methylergonovine is distributed into milk.

Elimination

Metabolism

Metabolized in the liver.

Elimination Route

Methylergonovine is excreted principally in feces and bile. Minimal urinary excretion.

Half-life

Following IV administration of ergonovine, initial phase (t_½α) half-life is about 10 minutes, and the terminal phase (t_½β) half-life is about 2 hours.

Following IV administration of methylergonovine, initial phase (t_½α) half-life is about 1–5 minutes, and the terminal phase (t_½β) half-life is about 0.5–2 hours.

Special Populations

Elimination may be prolonged in neonates.

Stability

Storage

Oral

Tablets

Ergonovine maleate: Tight, light-resistant container at 15–30°C.

Methylergonovine maleate: Tight, light-resistant container at <25°C.

Parenteral

Injection

Ergonovine maleate: <8°C. May be stored at room temperature for short periods of time (i.e., <60 days). Protect from light.

Methylergonovine maleate: 2–8°C. Protect from light.

Compatibility

Drug Compatibility

Actions

• Directly stimulates contractions of uterine and vascular smooth muscle.

• Increases the amplitude and frequency of uterine contractions and uterine tone which in turn impedes uterine blood flow.

• Induces a rapid and sustained tetanic uterotonic effect.

• Produces vasoconstriction.

Advice to Patients

• Importance of women informing clinicians if they plan to breast-feed.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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