Methylergonovine (Methylergometrine) is available as oral, IM, and IV formulation. It causes the contraction of uterine smooth muscles and is used during the third stage of labor to control uterine bleeding.

Methylergonovine Uses:

• After the placenta has been delivered, it is utilized to treat uterine atony, hemorrhage, and subinvolution of the uterus.
• After the anterior shoulder has been delivered during the second stage of labor, it may be utilized to reduce uterine haemorrhage.

Methylergonovine Dose in Adults

Methylergonovine (Methylergometrine) Dose in the Prevention of hemorrhage:

• Oral:
  • 0.2 mg three times per day or four times per day for up to seven days in the puerperium.
  • The length of therapy should not go beyond one week.
• IM, IV:
  • 0.2 milligrams after placenta delivery, throughout puerperium, or after anterior shoulder birth.
  • If necessary, the dosage may be given twice daily or four times daily.
• Note: Consider the intravenous administration only during life-threatening situations.

Use in Children:

Not indicated.

Pregnancy Risk Factor X

• It is not recommended for use in the third stage (after delivery of the anterior shoulder, placenta, or postpartum period). It is not recommended for use during pregnancy.
• It is not recommended for use due to its maternal side effects. It is used only as a supplementary uterotonic agent.

Methylergonovine use during breastfeeding:

• Breast milk contains methylergonovine.
• An infant might experience adverse reactions like agitation, increased blood pressure, seizures, tachycardia (sometimes bradycardia), vomiting, or diarrhea.
• It can also impact maternal milk supply and production and could affect maternal prolactin levels.
• Experts recommend that you avoid breastfeeding for at least 12 hours following the last maternal dose. However, some experts suggest that breastfeeding is possible.

Dose in Kidney Disease:

Although the manufacturer's labeling does not specify a dose modification, individuals with renal impairment should use this medication with caution.

Dose in Liver disease:

No dosage adjustment is provided in the manufacturer's labeling, however, it should be used with caution.

Side effects of Methylergonovine (Methylergometrine):

• Cardiovascular:

  • Cerebrovascular Accident
  • Chest Pain
  • Hypotension
  • Local Thrombophlebitis
  • Coronary Artery Vasospasm
  • Paresthesia
  • Tachycardia
  • Hypertension
  • Angina Pectoris
  • Atrioventricular Block
  • Bradycardia
  • Ventricular Fibrillation
  • Myocardial Infarction
  • Palpitations
  • Vasospasm

• Central Nervous System:

  • Headache
  • Dizziness
  • Hallucination
  • Seizure

• Endocrine & Metabolic:

  • Water Intoxication

• Dermatologic:

  • Diaphoresis
  • Skin Rash

• Gastrointestinal:

  • Abdominal Pain
  • Diarrhea
  • Nausea
  • Unpleasant Taste
  • Vomiting

• Genitourinary:

  • Hematuria

• Neuromuscular & Skeletal:

  • Leg Cramps

• Otic:

  • Tinnitus

• Hypersensitivity:

  • Anaphylaxis
•  

• Respiratory:

  • Dyspnea
  • Nasal Congestion

Contraindication to Methylergonovine Include:

• Allergic responses to methylergonovine and any other formulation ingredients
• Pregnancy
• Preeclampsia
• Hypertension

Warnings and precautions

• Coronary artery disease

  • Patients suffering from coronary artery disease or other conditions should not take the drug.
  • Patients are more likely to experience myocardial ischemia, myocardial disease, or coronary heart disease if they have an underlying coronary disease.

• Ergotism:

  • Ergotism occurs when patients use excessive amounts of ergot alkaloids and for a longer time. 
  • It causes intense vasoconstriction that results in ischemia, gangrene and tissue damage.
  • This affects primarily the distal parts of the body such as the fingers and toes.
  • Avoid prolonged use and follow all dosing recommendations and guidelines.

• Retroperitoneal and pleural fibrosis

  • Rarely, ergot alkaloids have been linked to retroperitoneal and pleural fibrosis. Avoid prolonged use.

• Hepatic impairment

  • Patients suffering from liver impairment should be cautious when using the drug.

• Labor

  • Take care in the second stage of labor.

• Renal impairment

  • It should be used with caution by patients who have renal disease because of a higher risk of hypertension and other side effects.

• Sepsis:

  • Avoid patients suffering from sepsis.

• Vascular disease

  • Patients suffering from peripheral vascular disease must be cautious when using it as it can cause vasospasm, which could lead to gangrene.

Methylergonovine (methylergometrine): Drug Interaction

Monitoring parameters:

• Blood Presssure
• ECG

How to administer Methylergonovine (Methylergometrine)?

IV:

• Routine intravenous administrations should be avoided as it may cause a sudden rise in blood pressure and causes cerebrovascular events. Intravenous use should be administered only during life-threatening states.
• It is administered slowly while monitoring the blood pressure. It should not be administered as a rapid push and no less than a minute.

IM:

• Intramuscular administration is an option.

Oral:

• For oral administration, it is supplied as tablets.

Mechanism of action of Methylergonovine (Methylergometrine):

• It reduces labor's third stage by reducing blood flow and causing sustained uterine contractions. 
• It acts on the smooth muscles in the uterus to increase the frequency, tone, and magnitude of uterine contractions.

Duration:

• Oral: About 3 hours;
• IM: About 3 hours;
• IV: 45 minutes

Bioavailability:

• Oral: 60%;
• IM: 78%

Time to peak serum concentration:

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

Absorption:

• Rapid

The Oxytocic effect (the onset of action):

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

Metabolism:

• It is metabolized in the liver.

Half-life elimination:

• About 3 hours (range: 1.5-12.7 hours)

Excretion:

• Urine and feces

International Brand Names of Methylergonovine:

• Methergine
• Basofortina
• Bledstop
• Demergin
• Ergogin
• Ergojen
• Ergomet
• Ergomin
• ERruvin
• Expogin
• Femitranol
• Ingagen-M
• Mem
• Mergot
• Mergotrex
• Methergin
• Methergine
• Metiagin
• Metvell
• Mitrotan
• Morgin
• Myotonic
• Neo-Ergo
• Pospargin
• Uterine

Methylergonovine Brand Names in Pakistan:

• Methergine