methylergometrine

medtigo

methylergometrine

Brand Name :

Methergine

Synonyms :

methylergometrine

Class :

Ergot Derivatives

Action and Spectrum

Actions and Spectrum:

It works primarily by stimulating uterine smooth muscle contraction. It acts on the smooth muscle cells of the uterus, causing them to contract and constrict blood vessels. This contraction helps to control bleeding by reducing blood flow and promoting uterine involution (the return of the uterus to its pre-pregnancy state).

methylergometrine is specific to the uterus and has little or no effect on other smooth muscles. Its primary action is on the uterine muscle, making it an effective drug for preventing and treating postpartum hemorrhage and managing bleeding after a miscarriage or abortion.

Dosing & Uses

Drug Interaction

Adverse Reaction

Frequency not defined

Headache

Diaphoresis

Transient chest pain

Thrombophlebitis

Water intoxication

Hallucinations

Nasal congestion

Diarrhea

Dizziness

Tinnitus

Palpitation

Dyspnea

Hematuria

Leg cramps

Foul taste

Black Box Warning

Black box warning:

None

Contraindication / Caution

Contraindications/caution:

Contraindications:

Hypertension (high blood pressure): methylergometrine can cause vasoconstriction, which may increase blood pressure.
Preeclampsia or eclampsia: These are serious conditions that occur during pregnancy and are characterized by high blood pressure, organ damage, and in the case of eclampsia, seizures.
Hypersensitivity or allergy to ergot alkaloids: People with a known allergy or hypersensitivity to ergot alkaloids should not use methylergometrine, as it may trigger an allergic reaction.
Coronary artery disease or cardiovascular disorders: methylergometrine can cause vasoconstriction, which may exacerbate underlying heart conditions and pose a risk to individuals with coronary artery disease or other cardiovascular disorders.
Severe hepatic (liver) or renal (kidney) impairment: methylergometrine is metabolized in the liver and excreted through the kidneys. In individuals with severe liver or kidney impairment, the drug may not be adequately cleared from the body, leading to an increased risk of adverse effects.
Sepsis or severe infection: methylergometrine can potentially worsen blood flow in individuals with severe infections, so it is generally avoided in sepsis or severe infection cases.

Caution:

Captivation of the placenta: methylergometrine can cause strong uterine contractions, which may lead to the accidental retention of the placenta, also known as placental captivation.
Avoid accidental injection to newborn babies: methylergometrine should never be administered to babies, as it can have severe adverse effects.
Increased risk of myocardial ischemia and infarction: methylergometrine’s vasoconstrictive properties can pose a risk to individuals with coronary artery disease or those with risk factors for coronary artery disease. The medication may further compromise blood flow to the heart, increasing the risk of myocardial ischemia (reduced blood flow) and infarction (heart attack).
Sepsis, hepatic impairment, renal impairment, peripheral vascular disease: methylergometrine should be used with caution in individuals with sepsis (severe infection), hepatic impairment (liver dysfunction), renal impairment (kidney dysfunction), or peripheral vascular disease (circulation problems in the extremities). The drug’s effects on blood vessels and flow could exacerbate these conditions.
Prolonged use and fibrosis: Prolonged use of methylergometrine may lead to rare but serious complications, such as pleuropulmonary fibrosis (lung and chest fibrosis), cardiac fibrosis (fibrosis of the heart tissue), or retroperitoneal fibrosis (fibrosis behind the abdominal cavity).

Pregnancy / Lactation

Pregnancy consideration: It is mainly administered during the third stage of labor (after the baby is born) to prevent and treat postpartum hemorrhage, which is excessive bleeding that can occur after childbirth.

Pregnancy Category: C

Lactation: Excretion of the drug in human breast milk is known. Breastfeeding should be delayed for at least 12 hours following the previous dosage.

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:

methylergometrine acts as a potent uterotonic agent, stimulating strong and sustained contractions of the uterine muscle. This property prevents and treats postpartum hemorrhage by helping the uterus contract after childbirth.

Vasoconstriction: methylergometrine also has vasoconstrictive effects, causing the narrowing of blood vessels. This action reduces blood flow, primarily in the uterine area, which helps control bleeding after delivery.
Serotonergic and adrenergic activity: methylergometrine acts on certain receptors in the body, including serotonergic (5-HT) and adrenergic receptors. It has partial agonist activity at 5-HT2A and 5-HT2B receptors and acts as an alpha-adrenergic agonist, contributing to its uterotonic and vasoconstrictive effects.

Pharmacodynamics:

As a uterotonic agent, methylergometrine primarily acts on smooth muscle cells in the uterus and blood vessels, producing specific physiological responses.

Pharmacokinetics:

Absorption

It has a bioavailability of 60% when taken orally (PO) and 78% when administered intramuscularly (IM). The time to reach peak plasma concentration is 30 minutes, regardless of the route of administration (PO, IM, IV).The peak plasma concentration is 3 ng/mL.

Distribution

It has a Vd ranging from 39-73 L, indicating that it is distributed widely throughout the body.

Metabolism

It is primarily metabolized in the liver.

Elimination and Excretion

methylergometrine is excreted in both urine and feces. It has a short half-life of 1 to 5 minutes and a terminal phase of 0.5-2 hours. The drug is rapidly eliminated from the body.

Adminstartion

Administration:

Only administer intravenously in an emergency due to the risk of HTN and CVA.

Give more than a minute and monitor the blood pressure and uterine contractions.

Patient Information Leaflet

Patient information leaflet

Generic Name: methylergometrine

Why do we use methylergometrine?

methylergometrine is a medication with various medical uses, primarily related to its uterotonic and vasoconstrictive properties. Some of the primary uses of methylergometrine include:

methylergometrine

No data available for drug.

DRUG INTERACTION

methylergometrine

&

methylergometrine +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

methylergometrine

No data available for drug.

DRUG INTERACTION

methylergometrine

&

methylergometrine +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

medtigo

methylergometrine

Brand Name :

Synonyms :

Class :

Action and Spectrum

Dosing & Uses

Drug Interaction

Adverse Reaction

Black Box Warning

Contraindication / Caution

Pregnancy / Lactation

Pharmacology

Adminstartion

Patient Information Leaflet