methylergonovine

Action and Spectrum

Actions and spectrum: 

• Uterine Contraction: methylergonovine stimulates the smooth muscles of the uterus, leading to strong and sustained contractions. This property is utilized to prevent or treat postpartum hemorrhage (excessive bleeding after childbirth). 
• Vasoconstriction: methylergonovine also has vasoconstrictive effects, meaning it causes the narrowing of blood vessels. This action can help control bleeding and reduce blood flow to certain areas, making it effective in managing postpartum bleeding. 

Spectrum: methylergonovine is used in obstetrics and gynecology to prevent or treat excessive bleeding after childbirth. It is commonly administered to women shortly after delivery to ensure the contraction of the uterus and to prevent complications related to postpartum hemorrhage. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Dizziness 

Tinnitus 

Palpitation 

Dyspnea 

Hematuria 

Hallucinations 

Nasal congestion 

Foul taste 

Hypertension 

Nausea/vomiting 

Headache 

Diaphoresis 

Transient chest pain 

Thrombophlebitis
Water intoxication 

Leg cramps 

Diarrhea 

Allergic phenomena with shock  

Post marketing reports 

Cardiovascular:  ventricular tachycardia, atrioventricular block, Ventricular fibrillation, angina pectoris 

Nervous system: paraesthesia, Cerebrovascular accident 

Black Box Warning

Black Box Warning: 

Methylergonovine does not have a black box warning. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: It should not be used in individuals who have a known hypersensitivity or allergy to methylergonovine or any of its components. 
• Coronary artery disease: methylergonovine should not be used in individuals with known or suspected coronary artery disease. 
• Peripheral vascular disease: It is contraindicated in peripheral vascular disease. 
• Hepatic impairment: methylergonovine should not be used in patients with severe liver impairment.

Caution: 

• Hypertension: methylergonovine can cause an increase in blood pressure. It should be used with caution in individuals with controlled hypertension or a history of hypertension. 
• Cardiovascular disorders: Patients with a history of cardiovascular disorders, such as heart disease, angina (chest pain), arrhythmias (irregular heart rhythms), or valvular heart disease, should be closely monitored while taking methylergonovine. 
• Pregnancy and lactation: methylergonovine is contraindicated during pregnancy and lactation. It should only be used if the potential benefits outweigh the risks, and under the supervision of a healthcare professional. 
• Drug interactions: methylergonovine may interact with other medications, including certain antihypertensive drugs, ergot alkaloids, and protease inhibitors. Close monitoring and dose adjustments may be necessary when using methylergonovine in combination with other medications.

Comorbidities: 

• Cardiovascular disorders: methylergonovine may have vasoconstrictive effects on blood vessels, which can potentially exacerbate cardiovascular conditions. It should be used with caution in individuals with a history of heart disease, angina (chest pain), arrhythmias (irregular heart rhythms), or valvular heart disease. 
• Hepatic impairment: methylergonovine is metabolized in the liver, so individuals with hepatic impairment may have altered drug metabolism. Dose adjustments or careful monitoring may be necessary in patients with liver dysfunction. 
• Renal impairment: methylergonovine is primarily excreted in the urine, so individuals with impaired kidney function may experience altered drug elimination. Dose adjustments or close monitoring may be needed in patients with renal impairment. 
• History of drug abuse: methylergonovine is an ergot alkaloid and has the potential for abuse. It should be used with caution in individuals with a history of substance abuse or addiction. 

Pregnancy / Lactation

Pregnancy consideration: US FDA pregnancy category: C 

Lactation: Excreted into human milk: Yes  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

• Uterine contraction: methylergonovine stimulates the smooth muscles of the uterus, leading to strong and sustained contractions. It is used to prevent or treat postpartum hemorrhage by promoting uterine involution and reducing bleeding. 
• Vasoconstriction: methylergonovine causes vasoconstriction of blood vessels by acting on alpha-adrenergic receptors. This can help reduce excessive bleeding by constricting the blood vessels in the uterus and surrounding tissues. 
• Serotonin receptor modulation: methylergonovine acts as a partial agonist at serotonin (5-HT2) receptors, leading to vasoconstriction and smooth muscle contraction.

Pharmacodynamics: 

• Alpha-adrenergic receptor agonism: methylergonovine acts as an agonist at alpha-adrenergic receptors, leading to vasoconstriction of smooth muscles in blood vessels. This vasoconstrictive effect helps to reduce excessive bleeding. 
• Serotonin receptor modulation: methylergonovine is a partial agonist at serotonin (5-HT2) receptors. By interacting with these receptors, it causes contraction of smooth muscles, including those in the uterus. This uterine contraction helps to promote uterine involution and reduce bleeding. 
• Dopamine receptor agonism: methylergonovine also acts as an agonist at dopamine receptors, although the clinical significance of this action is not fully understood. 

Pharmacokinetics: 

Absorption 

methylergonovine is administered orally or intravenously. After oral administration, it is absorbed from gastrointestinal tract, reaching peak plasma concentrations within 30 to 60 minutes. 

Distribution 

methylergonovine is extensively distributed throughout the body. It has a high affinity for plasma proteins and readily crosses the blood-brain barrier. 

Metabolism 

methylergonovine undergoes extensive hepatic metabolism via enzymatic processes. It is primarily metabolized by cytochrome P450 enzymes, particularly CYP3A4. The main metabolite formed is 12-hydroxymethylergonovine. 

Elimination and excretion 

methylergonovine and its metabolites are excreted primarily in the bile. A small portion is also eliminated in the urine. The elimination half-life of methylergonovine is 3 to 4 hours. 

Adminstartion

Administration: 

Oral Administration: methylergonovine tablets are usually taken by mouth. The recommended dose and frequency will depend on the condition being treated. It is typically administered in divided doses over a specified period, such as several days or weeks. It is important to follow the prescribed dosage and schedule provided by your healthcare provider. methylergonovine can also be admi

Intravenous Administration: Administered intravenously, usually in a healthcare setting such as a hospital or clinic. The intravenous form is typically used for more severe cases or when immediate effects are desired. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: methylergonovine 

Pronounced: (meth-uh-ler-goh-NOH-veen)  

Why do we use methylergonovine? 

methylergonovine is primarily used for the prevention and treatment of postpartum hemorrhage following childbirth. It helps to control uterine bleeding by causing uterine contractions and promoting the contraction of blood vessels in the uterus. methylergonovine may also be used in the management of uterine atony and in the control of postpartum bleeding after surgical procedures.