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Methylergometrine information from DrugsUpdate  

See Available Brands of Methylergometrine in India

P - Contraindicated in pregnancy
L - Caution when used during lactation
FI - Food *

Methylergometrine (other names include methylergonovine, methylergobasin, 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.

Pharmacodynamics

Pharmacokinetics

Methylergometrine is an ergot alkaloid, which directly stimulates contractions of uterine and vascular smooth muscle.

Onset

5-15 minutes (oral); 2-5 minutes (IM); immediate (IV).

Duration
≥3 hours (oral/IM); 45 minutes (IV).

Absorption
Rapidly absorbed (oral; IM).

Distribution
Mainly distributed into plasma and extracellular fluid; rapidly distributed into tissues. Enters the breast milk.

Metabolism
Hepatic: Undergoes first-pass metabolism.

Excretion
Mainly via faeces; via urine (small amounts as unchanged drug); 2-3 hours (elimination half-life).

Methylergometrine Indications / Methylergometrine Uses

Information Not Available

Methylergometrine Adverse Reactions / Methylergometrine Side Effects

Headache, dizziness, hallucinations; tinnitus; nausea, vomiting, foul taste, diarrhoea; hypertension, temporary chest pain, palpitations, bradycardia; nasal congestion, dyspnoea; diaphoresis; thrombophlebitis; haematuria; water intoxication; leg cramps; allergic reactions.

Potentially Fatal: Shock.

Precautions

Information Not Available

Special Precautions

Captivation of the placenta may occur if given during the 2nd or 3rd stage of labour prior to delivery of the placenta; use in this situation should only be done by a qualified personnel. Avoid prolonged use. Caution in patients with sepsis, hepatic or renal impairment. Lactation.

Other Drug Interactions

Possible increase in serum levels and risk of severe vasoconstrictive effects with potent CYP3A4 inhibitors (e.g. erythromycin, troleandomycin, clarithromycin, ritonavir, indinavir, nelfinavir, delavirdine, ketoconazole, itraconazole, voriconazole) and less potent CYP3A4 inhibitors (e.g. saquinavir, nefazodone, fluconazole, fluoxetine, fluvoxamine, zileuton, clotrimazole).

Other Interactions

Food Interaction
Possible increase in serum levels and risk of severe vasoconstrictive effects with grapefruit juice.

Dosage

Oral
Prophylaxis of postpartum haemorrhage
Adult: 200 mcg 3-4 times daily in the puerperium for 2-7 days.

Intravenous
Treatment and prophylaxis of postpartum and postabortal haemorrhage
Adult: As an emergency measure: 200 mcg by slow inj over at least 1 minute, may repeat every 2-4 hours, up to a max of 5 doses.

Intramuscular
Treatment and prophylaxis of postpartum and postabortal haemorrhage
Adult: 200 mcg. May repeat every 2-4 hours. Max: 5 doses.

Food(before/after)

Information Not Available

List of Contraindications

Methylergometrine and Pregnancy

Contraindicated in pregnancy

Methylergometrine and Lactation

Caution when used during lactation

Methylergometrine and Children

Information Not Available

Methylergometrine and Geriatic

Information Not Available

Methylergometrine and Other Contraindications

Hypertension, eclamptic or previously hypertensive patients, heart disease, venoatrial shunts, mitral valve stenosis, obliterative vascular disease. Do not use in cases of threatened spontaneous abortion. Pregnancy.

Storage

Intramuscular
Store under refrigeration at 2-8°C (36-46°F). Protect from light.


Intravenous
Store under refrigeration at 2-8°C (36-46°F). Protect from light.

Oral

Store below 25°C (77°F).

Lab interference

Intramuscular
Store under refrigeration at 2-8°C (36-46°F). Protect from light.


Intravenous
Store under refrigeration at 2-8°C (36-46°F). Protect from light.

Oral

Store below 25°C (77°F).

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