Methylergometrine 0.125 mg Tablet Dosing
The recommended dose of oral methylergometrine 0.125 mg tablet is one tablet three times daily for a maximum of one week postpartum, though the standard FDA-approved formulation is 0.2 mg tablets given 3-4 times daily. 1
Standard Dosing Regimen
The FDA-approved oral dose is 0.2 mg (one tablet) taken 3 or 4 times daily during the puerperium for a maximum of 1 week. 1
The 0.125 mg formulation represents a lower-strength tablet that was historically used at a dosing frequency of three times daily (t.i.d.) in clinical studies. 2, 3
Peak serum concentrations occur approximately 3 hours after oral administration in postpartum women, indicating delayed gastrointestinal absorption compared to non-pregnant individuals. 2
Clinical Context and Limitations
Methylergometrine is contraindicated in cardiovascular disease management during pregnancy and postpartum due to significant risk (>10%) of vasoconstriction and hypertension. 4
The European Society of Cardiology explicitly states that methylergonovine should not be used for postpartum hemorrhage prevention in women with cardiovascular conditions, as prostaglandin F analogues are safer alternatives unless pulmonary artery pressure elevation is undesirable. 4
For routine third-stage management, a single intramuscular dose of oxytocin is preferred over ergometrine derivatives, with ergometrine being contraindicated during active labor management. 4
Evidence Quality Concerns
Oral methylergometrine has demonstrated unfavorable pharmacokinetic properties with unpredictable absorption and no proven clinical effect on reducing postpartum blood loss compared to placebo. 5
A prospective randomized double-blind study of 217 women found no significant difference in lochia amount, analgesic requirements, or hospital stay duration between methylergometrine 0.125 mg three times daily and placebo when given for 72 hours postpartum. 3
The medication is unstable even under refrigerated conditions, raising concerns about its reliability in clinical practice, particularly in resource-limited settings. 5
Role in Uterine Atony Management
Methylergonovine serves as a highly effective second-line agent for treating established uterine atony when oxytocin fails, despite its severe potential side effects including vasoconstriction and hypertension. 6
Oxytocin remains the first-line uterotonic agent, with methylergonovine reserved for refractory cases rather than routine prophylaxis. 6
Critical Safety Considerations
Avoid methylergometrine in women with hypertension, preeclampsia, cardiovascular disease, or any condition where vasoconstriction poses risk. 4
Side effects are generally mild when they occur, but the cardiovascular risks necessitate careful patient selection. 2
The maximum treatment duration should not exceed one week postpartum to minimize cumulative adverse effects. 1