Drug/Small Molecule:
methylergonovine

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB contains no drug labels with pharmacogenomic information for this drug/small molecule. To report a drug label with PGx, click here.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Methylergobasin
  • Methylergobasine
  • Methylergobrevin
  • Methylergometrin
  • Methylergometrine
  • Methylergonovin
  • methylergonovine maleate
Trade Names
  • Basofortina
  • Metenarin
  • Methergen
  • Methergin
  • Methergine
  • Norforms
  • Partergin
  • Ryegonovin
  • Spametrin-M
Brand Mixture Names

PharmGKB Accession Id:
PA450461

Description

A homolog of ergonovine containing one more CH2 group. (Merck Index, 11th ed)

Source: Drug Bank

Indication

For the prevention and control of excessive bleeding following vaginal childbirth

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Methylergonovine acts directly on the smooth muscle of the uterus and increases the tone, rate, and amplitude of rhythmic contractions through binding and the resultant antagonism of the dopamine D1 receptor. Thus, it induces a rapid and sustained tetanic uterotonic effect which shortens the third stage of labor and reduces blood loss.

Source: Drug Bank

Pharmacology

Methylergonovine is a semisynthetic ergot alkaloid and a derivative of ergonovine and is used for the prevention and control of postpartum and post-abortion hemorrhage. In general, the effects of all the ergot alkaloids appear to results from their actions as partial agonists or antagonists at adrenergic, dopaminergic, and tryptaminergic receptors. The spectrum of effects depends on the agent, dosage, species, tissue, and experimental or physiological conditions. All of the alkaloids of ergot significantly increase the motor activity of the uterus. After small doses contractions are increased in force or frequency, or both, but are followed by a normal degree of relaxation. As the dose is increased, contractions become more forceful and prolonged, resting tonus is markedly increased, and sustained contracture can result.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic, with extensive first-pass metabolism.

Source: Drug Bank

Absorption

Absorption is rapid after oral (60% bioavailability) and intramuscular (78% bioavailability) administration.

Source: Drug Bank

Half-Life

3.39 hours

Source: Drug Bank

Toxicity

Signs and symptoms of overexposure: hypertension, seizures, headache, hypotension, nausea, and vomiting.

Source: Drug Bank

Route of Elimination

Ergot alkaloids are mostly eliminated by hepatic metabolism and excretion, and the decrease in bioavailability following oral administration is probably a result of first-pass metabolism in the liver.

Source: Drug Bank

Volume of Distribution

  • 56.1 ± 0 L

Source: Drug Bank

Chemical Properties

Chemical Formula

C20H25N3O2

Source: Drug Bank

Isomeric SMILES

CC[C@@H](CO)NC(=O)[C@H]1CN([C@@H]2CC3=CNC4=CC=CC(=C34)C2=C1)C

Source: Drug Bank

[H][C@@]12CC3=CNC4=C3C(=CC=C4)C1=C[C@H](CN2C)C(=O)N[C@@H](CC)CO

Source: Drug Bank

Canonical SMILES

CC[C@@H](CO)NC(=O)[C@H]

Source: Drug Bank

Average Molecular Weight

339.4314

Source: Drug Bank

Monoisotopic Molecular Weight

339.194677059

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Drug Targets

Gene Description
DRD1 (source: Drug Bank)

Drug Interactions

Drug Description
methylergonovine Possible severe and prolonged vasoconstriction (source: Drug Bank)
methylergonovine Possible severe and prolonged vasoconstriction (source: Drug Bank)
methylergonovine Increases the effect and toxicity of ergot derivative (source: Drug Bank)
methylergonovine Increases the effect and toxicity of ergot derivative (source: Drug Bank)
methylergonovine The antiretroviral agent may increase the ergot derivative toxicity (source: Drug Bank)
methylergonovine The antiretroviral agent may increase the ergot derivative toxicity (source: Drug Bank)
methylergonovine The antiretroviral agent may increase the ergot derivative toxicity (source: Drug Bank)
methylergonovine The antiretroviral agent may increase the ergot derivative toxicity (source: Drug Bank)
methylergonovine Possible severe and prolonged vasoconstriction (source: Drug Bank)
methylergonovine Possible severe and prolonged vasoconstriction (source: Drug Bank)
methylergonovine Possible marked increase of arterial pressure (source: Drug Bank)
methylergonovine Possible marked increase of arterial pressure (source: Drug Bank)
methylergonovine Possible ergotism and severe ischemia with this combination (source: Drug Bank)
methylergonovine Possible ergotism and severe ischemia with this combination (source: Drug Bank)
methylergonovine Possible severe and prolonged vasoconstriction (source: Drug Bank)
methylergonovine Possible antagonism of action (source: Drug Bank)
methylergonovine Possible antagonism of action (source: Drug Bank)
methylergonovine Possible antagonism of action (source: Drug Bank)
methylergonovine Possible antagonism of action (source: Drug Bank)
methylergonovine Possible severe and prolonged vasocontriction (source: Drug Bank)
methylergonovine Possible severe and prolonged vasocontriction (source: Drug Bank)
methylergonovine Possible antagonism of action (source: Drug Bank)
methylergonovine Possible antagonism of action (source: Drug Bank)
methylergonovine Possible marked increase of arterial pressure (source: Drug Bank)
methylergonovine Possible marked increase of arterial pressure (source: Drug Bank)
methylergonovine Telithromycin may reduce clearance of Methylergonovine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Methylergonovine if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank)
methylergonovine Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Methylergonovine. Concomitant therapy is contraindicated. (source: Drug Bank)
methylergonovine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
methylergonovine Increased risk of serotonin syndrome. Use caution during concomitant therapy and monitor for symptoms of serotonin syndrome. (source: Drug Bank)
methylergonovine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
methylergonovine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
methylergonovine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
methylergonovine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
methylergonovine Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of methylergonovine by decreasing its metabolism. Concomitant therapy is contraindicated. (source: Drug Bank)
methylergonovine Concomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, methylergonovine, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated. (source: Drug Bank)

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
May Prevent
Contraindicated With

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
12634-179-96
DrugBank:
DB00353
KEGG Drug:
D00680
PubChem Compound:
8226
PubChem Substance:
151359
46507746
IUPHAR Ligand:
150
ChemSpider:
7933
Therapeutic Targets Database:
DAP000978
FDA Drug Label at DailyMed:
b91d1729-2e8e-4398-9a0d-02763bcfe284

Clinical Trials

These are trials that mention methylergonovine and are related to either pharmacogenetics or pharmacogenomics.

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.