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Methergine

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Methergine

Methylergometrine (other names include methylergonovine, methylergobasin, methergine, and D-lysergic acid 1-butanolamide) is a synthetic analogue of ergonovine, a psychedelic alkaloid found in ergot, and many species of morning glory. It is a member of the ergoline family and chemically similar to LSD, ergine, ergometrine, and lysergic acid. Due to its oxytocic properties, it has a medical use in obstetrics. According to Jonathan Ott, methylergonovine has LSD-like actions above 2 milligrams. Clinical dosages are ten times lower.

Methylergometrine maleate is marketed under the trade name Methergine.

Uses

Obstetric use

Methylergometrine is a smooth muscle constrictor that mostly acts on the uterus. It is most commonly used to prevent or control excessive bleeding following childbirth and spontaneous or elective abortion, and also to aid in expulsion of retained products of conception after a missed abortion (miscarriage in which all or part of the fetus remains in the uterus) and to help deliver the placenta after childbirth. It is available as tablets or injection (IM or IV) or in liquid form to be taken orally.[1][2][3]

Migraine

Methylergometrine is sometimes used for both prevention[4] and acute treatment[5] of migraine. It is an active metabolite of methysergide.

Contraindications

Methylergometrine is contraindicated in patients with hypertension and preeclampsia, and also during pregnancy and birth.[1]

Side effects

Adverse effects include:[1]

  • Cholinergic effects such as nausea, vomiting, and diarrhea
  • Dizziness
  • Pulmonary hypertension
  • Coronary artery vasoconstriction
  • Severe systemic hypertension (especially in patients with preeclampsia)
  • Convulsions

In excessive doses, methylergometrine can also lead to cramping, respiratory depression and coma.[1]

Interactions

Methylergometrine likely interacts with drugs that inhibit the liver enzyme CYP3A4, such as azole antifungals, macrolide antibiotics and many HIV drugs. It can also increase constriction of blood vessels caused by sympathomimetic drugs and other ergot alkaloids.[1]

Mechanism of action

Methylergometrine is a partial agonist/antagonist on serotonergic, dopaminergic and alpha-adrenergic receptors. Its specific binding and activation pattern on these receptors leads to a highly, if not completely, specific contraction of smooth uterus muscle via 5-HT2A serotonin receptors,[6] while blood vessels are affected to a lesser extent compared to other ergot alkaloids.[1]

References

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