Methylergonovine
- Atc Codes:G02AB01
- CAS Codes:57432-61-8#7054-07-1#113-42-8
- PHARMGKB ID:57432-61-8#7054-07-1#113-42-8
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
Brand Names
Europe
Austria: Methergin; Belgium: Methergin; Bulgaria: Methergin; Czech Republic: Methylergometrine; Denmark: Methergin; Finland: Methergin; France: Methergin; Germany: Methergin, Methylergobrevin, Methylergometrin; Greece: Methergin; Italy: Methergin, Metilergom; Luxembourg: Methergin; Netherlands: Methergin; Portugal: Methergin; Slovakia: Methylergometrin; Spain: Methergín; Sweden: Methergin; UK: Methergin.
North America
USA: Methergine.
Latin America
Argentina: Basofortina; Brazil: Methergin; Mexico: Methergín.
Asia
Japan: Derganin, Metenarin, Methylergometrine, Partan.
Drug combinations
Chemistry
Methylergonovine Maleate: C~20~H~25~N~3~O~2~ C~4~H~4~O~4~. Mw: 455.50. (1) Ergoline-8-carboxamide, 9,10-didehydro-N-[1-(hydroxymethyl)propyl]-6-methyl-, [8β(S)]-, (Z)-2-butenedioate (1:1); (2) 9,10-Didehydro-N-[(S)-1-(hydroxymethyl)propyl]-6-methylergoline-8β-carboxamide maleate (1:1). CAS-57432-61-8; CAS-7054-07-1 (replaced); CAS-113-42-8 (methylergonovine).
Pharmacologic Category
Oxytocics; Ergot Derivative. (ATC-Code: G02AB01).
Mechanism of action
Affects primarily uterine smooth muscles producing sustained contractions and thereby shortens third stage of labor and reduces blood loss.
Therapeutic use
Prevention and treatment of postpartum and postabortion hemorrhage caused by uterine atony or subinvolution.
Pregnancy and lactiation implications
Use with caution in second stage of labor. Methylergonovine is intended for use after delivery of infant. At normal doses used to control postpartum uterine bleeding, small amounts excreted in breast milk (use caution).
Unlabeled use
Contraindications
Hypersensitivity to methylergonovine or any component of the formulation. Ergot alkaloids contraindicated with potent inhibitors of CYP3A4 (includes protease inhibitors, azole antifungals, and some macrolide antibiotics). Hypertension. Toxemia. Pregnancy.
Warnings and precautions
Ergot alkaloids associated with fibrotic valve thickening (e.g. aortic, mitral, tricuspid). Ergot alkaloid use may result in ergotism (intense vasoconstriction) resulting in peripheral vascular ischemia and possible gangrene. Use should be avoided in cardiovascular disease, including hypertension, coronary artery disease and peripheral vascular disease. Rare cases of pleural and/or retroperitoneal fibrosis reported with prolonged daily use of other ergot alkaloids. Use with caution in hepatic or renal impairment, in second stage of labor, in sepsis, and in obliterative vascular disease. Concomitant use with potent inhibitors of CYP3A4 and ergot alkaloids associated with acute ergot toxicity (ergotism). Use with extreme caution or avoid use in the elderly (vasoconstrictive properties and cardiovascular adverse effects). Use with extreme caution when administering intravenously (risk of inducing sudden hypertensive and cerebrovascular accidents).