Methylergometrine Maleate

(BANM, rINNM)
Methylergometrine Maleate Chemical formula
Synonyms: Maleato de metilergometrina; Methylergobasine Maleate; Méthylergométrine, hydrogénomaléate de; Méthylergométrine, Maléate de; Methylergometrini hydrogenomaleas; Methylergometrini Maleas; Methylergonovine Maleate; Metilergobazin Maleat; Metilergometrin Maleat. N-[(S)-1-(Hydroxymethyl)propyl]drogen maleate.
Cyrillic synonym: Метилэргометрина Малеат.

💊 Chemical information

Chemical formula: C20H25N3O2,C4H4O4 = 455.5.
CAS — 113-42-8 (methylergometrine); 57432-61-8 ATC — G02AB01.
ATC Vet — QG02AB01.

Pharmacopoeias.

In Eur., Jpn, and US.

Ph. Eur. 6.2

(Methylergometrine Maleate). A white or almost white, hygroscopic, crystalline powder. Soluble in water; slightly soluble in anhydrous alcohol. pH of a 0.5% solution is 4.4 to 5.2. Store in airtight containers. Protect from light.

USP 31

(Methylergonovine Maleate). A white to pinkish-tan, odourless, microcrystalline powder. Soluble 1 in 100 of water, 1 in 175 of alcohol, 1 in 1900 of chloroform, and 1 in 8400 of ether. pH of a 0.02% solution in water is between 4.4 and 5.2. Store in airtight containers at a temperature not exceeding 8°. Protect from light.

Stability.

For mention of slight variations in the methylergometrine content of the injection after transport to a tropical climate, see under Ergometrine Maleate.

💊 Adverse Effects, Treatment, and Precautions

As for Ergometrine Maleate.

Overdosage.

References.
1. Aeby A, et al. Methylergometrine poisoning in children: review of 34 cases. J Toxicol Clin Toxicol 2003; 41: 249–53
2. Bangh SA, et al. Neonatal ergot poisoning: a persistent iatrogenic illness. Am J Perinatol 2005; 22: 239–43.

💊 Pharmacokinetics

Methylergometrine maleate is reported to be rapidly absorbed when given orally or intramuscularly, with onset of uterine contractions in about 5 to 15 minutes and 2 to 5 minutes, respectively. Oral bioavailability may show considerable interindividual variation. It undergoes extensive first-pass hepatic metabolism and only small amounts of unchanged drug are excreted in the urine. The elimination half-life is reported to be about 2 to 3 hours. Small amounts of methylergometrine have been detected in breast milk.4,5
1. Mäntylä R, et al. Methylergometrine (methylergonovine) concentrations in the human plasma and urine. Int J Clin Pharmacol Biopharm 1978; 16: 254–7
2. de Groot ANJA, et al. Comparison of the bioavailability and pharmacokinetics of oral methylergometrine in men and women. Int J Clin Pharmacol Ther 1995; 33: 328–32
3. Allonen H, et al. Methylergometrine: comparison of plasma concentrations and clinical response of two brands. Int J Clin Pharmacol Biopharm 1978; 16: 340–2
4. Erkkola R, et al. Excretion of methylergometrine (methylergonovine) into the human breast milk. Int J Clin Pharmacol Biopharm 1978; 16: 579–80
5. Vogel D, et al. Misoprostol versus methylergometrine: pharmacokinetics in human milk. Am J Obstet Gynecol 2004; 191: 2168–73.

💊 Uses and Administration

Methylergometrine maleate has an action on the uterus similar to that of ergometrine maleate and is used similarly in the active management of the third stage of labour, and in the prevention and treatment of postpartum or postabortal haemorrhage. In the management of the third stage of labour, it may be given in a dose of 200 micrograms intramuscularly after delivery of the anterior shoulder or, at the latest, immediately after delivery of the infant. The same dose may be used for the prevention or treatment of postpartum or postabortal haemorrhage, and may be repeated every 2 to 4 hours as necessary up to a maximum of 5 doses. In emergencies it may be given in similar doses by slow intravenous injection over at least 1 minute to reduce the risk of adverse effects, particularly hypertension. During the puerperium, methylergometrine maleate has been given in oral doses of 200 micrograms 3 or 4 times daily for up to a week or 125 to 250 micrograms up to 3 times daily. Methylergometrine is a metabolite of methysergide.

Diagnosis and testing.

For reference to the use of methylergometrine maleate in the diagnosis of variant angina, see Ergometrine Maleate.

💊 Preparations

USP 31: Methylergonovine Maleate Injection; Methylergonovine Maleate Ta b l e t s .

Proprietary Preparations

Arg.: Basofortina; Austria: Methergin; Belg.: Methergin; Braz.: Ergometrin; Methergin; Chile: Methergin†; Denm.: Methergin; Fin.: Methergin; Fr.: Methergin; Ger.: Methergin; Methylergobrevin; Gr.: Demergin; Methergin; Hong Kong: Methergin†; India: Ergogin; Ingagen-M; Methergin; Utergin; Indon.: Bledstop; Glomethyl; Methergin; Metherinal; Methovin; Metilat; Metvell; Myomergin; Myotonic; Pospargin; Israel: Methergin; Ital.: Methergin; Malaysia: Methergin; Mex.: Methergin; Neth.: Methergin; Philipp.: Medisyl; Mergot; Mergotrex; Methergin; Myometril; Usamema; Port.: Methergin; Spain: Methergin; Swed.: Methergin; Switz.: Methergin; Thai.: Ergotyl; Expogin; Metrine; Nathergen†; Turk.: Methergin; Metiler; Uterjin; USA: Methergine; Venez.: Methergin. Multi-ingredient: Ger.: Syntometrin†.
Published November 03, 2018.