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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Methergine
Generic Name
Methylergonovine Maleate
Active Ingredient
MethylergonovineCategory
Other
Salt Form
Maleate
Variants
1
Different strengths and dosage forms
| Strength | Form | Route | NDC |
|---|---|---|---|
| .2 mg/1 | TABLET | ORAL | 27437-050 |
Detailed information about Methergine
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Methergine, you must consult a qualified healthcare professional.
Methylergonovine is a semi-synthetic ergot alkaloid used primarily in the management of the third stage of labor to prevent and control postpartum hemorrhage by increasing uterine tone and contraction frequency.
The dosage of methylergonovine is highly standardized but must be tailored to the clinical urgency of the patient's condition.
Methylergonovine is not indicated for use in pediatric patients. Its clinical application is restricted to the management of pregnancy-related conditions in adult or adolescent patients who have reached reproductive maturity. There is no established safety or efficacy data for the use of this medication in children.
Because a portion of methylergonovine and its metabolites are excreted via the kidneys, patients with impaired renal function (kidney disease) may require closer monitoring. While specific dose-reduction formulas are not standardized, healthcare providers will use caution to avoid drug accumulation and increased risk of side effects.
Since the liver (specifically the CYP3A4 enzyme) is the primary site of metabolism, patients with hepatic impairment (liver disease) are at a significantly higher risk for toxicity. Dosage should be approached with extreme caution, and in cases of severe liver failure, the drug may be avoided entirely.
Methylergonovine is generally not used in the geriatric population, as its indications are limited to obstetric and gynecological events occurring during the reproductive years.
If you are prescribed the tablet form of methylergonovine to take at home:
If you miss a dose of methylergonovine, take it as soon as you remember. However, if it is almost time for your next scheduled dose, skip the missed dose and return to your regular dosing schedule. Do not double the dose to catch up, as this increases the risk of severe hypertension and other side effects.
An overdose of methylergonovine is a medical emergency. Symptoms of acute overdose (ergotism) include:
In the event of a suspected overdose, contact emergency services or a poison control center immediately. Treatment usually involves supportive care, including medications to lower blood pressure and maintain respiratory function.
> Important: Follow your healthcare provider's dosing instructions. Do not adjust your dose without medical guidance.
Most patients receiving methylergonovine will experience some degree of side effects, as the drug's mechanism of action affects smooth muscle throughout the body, not just in the uterus.
> Warning: Stop taking Methylergonovine and call your doctor immediately if you experience any of these.
Methylergonovine is intended for short-term use (maximum 7 days). Long-term use of ergot alkaloids is associated with more severe risks, including:
While methylergonovine does not have a traditional 'Black Box Warning' in the same way some antidepressants do, it carries a Contraindication Warning regarding the use of strong CYP3A4 inhibitors.
Warning on Drug Interactions: Serious and life-threatening peripheral ischemia (reduced blood flow to limbs) and cerebral ischemia (reduced blood flow to the brain) have been reported when methylergonovine is co-administered with potent CYP3A4 inhibitors, such as certain protease inhibitors (for HIV) and macrolide antibiotics. This combination is strictly contraindicated.
Report any unusual symptoms to your healthcare provider.
Methylergonovine is a high-alert medication in the obstetric setting. It must be used with extreme caution in patients with a history of cardiovascular disease. Because it causes systemic vasoconstriction (narrowing of blood vessels throughout the body), it can exacerbate pre-existing conditions like hypertension or heart disease. Patients must be monitored closely for changes in blood pressure and heart rate during administration, especially when the drug is given by injection.
No FDA black box warnings for Methylergonovine are currently listed; however, as noted in the side effects section, there is a critical warning regarding its use with CYP3A4 inhibitors. This interaction is considered so dangerous that it is listed as a primary contraindication in the 'Warnings' section of the FDA label.
When you are receiving methylergonovine in a hospital setting, your healthcare team will perform the following:
Methylergonovine can cause dizziness, headaches, and occasionally blurred vision. You should not drive or operate heavy machinery until you know how the medication affects you. Most patients are still in the hospital or in early postpartum recovery while taking this drug and should avoid these activities regardless.
Alcohol should be strictly avoided while taking methylergonovine. Alcohol can increase the risk of dizziness and may interact unpredictably with the drug's effects on blood pressure. Furthermore, alcohol consumption is generally discouraged during the early postpartum period, especially if breastfeeding.
There is no requirement to taper methylergonovine, as it is used for a very short duration (usually 2 to 7 days). There is no known withdrawal syndrome associated with stopping the drug after a standard course. However, you should never stop taking the medication earlier than prescribed without consulting your doctor, as this could lead to a return of uterine bleeding.
> Important: Discuss all your medical conditions with your healthcare provider before starting Methylergonovine.
Certain drugs must NEVER be used with methylergonovine because they inhibit the enzyme (CYP3A4) responsible for breaking it down. This leads to toxic levels of methylergonovine in the blood, causing severe vasospasm (clamping of the blood vessels) and potential loss of limbs or stroke.
Methylergonovine is not known to significantly interfere with most common laboratory tests. However, it may cause a transient increase in serum prolactin levels, which could theoretically affect tests measuring this hormone.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking.
In certain scenarios, the risks of methylergonovine far outweigh any possible benefit. It must NEVER be used in the following cases:
Healthcare providers will perform a careful risk-benefit analysis in patients with:
Patients who have had allergic reactions to other ergot-derived medications (such as Ergomar, Cafergot, or Migranal) are highly likely to be allergic to methylergonovine. Always inform your doctor if you have had a reaction to any 'ergot' medication in the past.
> Important: Your healthcare provider will evaluate your complete medical history before prescribing Methylergonovine.
Methylergonovine is classified as FDA Pregnancy Category C (under the old system), but its contraindication during pregnancy is absolute. It is used exclusively after the baby has been delivered. If taken during pregnancy, it can cause the uterus to contract so violently that it cuts off blood flow to the fetus or causes the uterus to tear (rupture). It is not used in fertility treatments.
Methylergonovine does pass into breast milk. While short-term use is common, there are two main concerns:
As mentioned, methylergonovine is not used in children. In adolescent patients (teens) who have given birth, the dosing is generally the same as in adults, though extra care is taken regarding blood pressure monitoring.
There is no indication for methylergonovine in the elderly. Clinical trials did not include patients over 65, as the drug is used for obstetric purposes.
In patients with kidney disease, the drug's metabolites may accumulate. While no specific dose adjustment is mandated by the FDA, clinical practice dictates using the lowest effective dose and monitoring for signs of ergotism (numbness, coldness in limbs).
Patients with liver impairment require extreme caution. Because the CYP3A4 enzyme in the liver is the primary way the body gets rid of methylergonovine, liver failure can lead to dangerously high drug levels. Healthcare providers may choose alternative medications (like oxytocin or misoprostol) if liver function is severely compromised.
> Important: Special populations require individualized medical assessment.
Methylergonovine is a semi-synthetic analogue of the naturally occurring ergot alkaloid, ergonovine. It acts as a powerful stimulant of uterine smooth muscle. Its primary molecular mechanism involves acting as a partial agonist at alpha-adrenergic and serotonergic (5-HT2) receptors. By binding to these receptors on the myometrial cells, it triggers the G-protein coupled receptor signaling pathway, which ultimately increases intracellular calcium. This calcium surge facilitates the interaction between actin and myosin filaments, leading to a sustained, tetanic contraction of the uterus. It also possesses some minor dopaminergic activity, which contributes to its side effect profile (like nausea).
| Parameter | Value |
|---|---|
| Bioavailability | ~60% (Oral) |
| Protein Binding | ~35% |
| Half-life | 0.5 to 3.4 hours (Average 2h) |
| Tmax | 0.5 to 1.5 hours |
| Metabolism | Hepatic (Primarily CYP3A4) |
| Excretion | Biliary/Fecal (Main), Renal (Minor) |
Methylergonovine is classified as an Ergot Alkaloid and a Uterine Stimulant. It is related to other ergot derivatives like ergotamine (used for migraines) and bromocriptine (used for Parkinson's and prolactin disorders).
Common questions about Methergine
Methylergonovine is primarily used in the obstetric setting to prevent and treat postpartum hemorrhage, which is excessive bleeding after childbirth. It works by causing the muscles of the uterus to contract firmly, which helps to clamp down on blood vessels at the site where the placenta was attached. Healthcare providers may also use it following a miscarriage or an induced abortion to ensure the uterus returns to its normal size and stops bleeding. It is considered a second-line agent, often used when oxytocin alone is not sufficient to control bleeding. This medication is strictly for use after delivery and is never used to start or induce labor.
The most frequently reported side effects of methylergonovine include high blood pressure (hypertension), nausea, vomiting, and abdominal pain or cramping. Because the drug causes the uterus to contract, 'afterpains' are a very common sign that the medication is working. Some patients also experience headaches, dizziness, or a ringing in the ears (tinnitus). While these are common, they are usually temporary. However, if you notice severe symptoms like a sudden, intense headache or numbness in your fingers, you should notify your medical team immediately, as these could indicate more serious cardiovascular issues.
No, you should avoid drinking alcohol while taking methylergonovine. Alcohol can interact with the medication to increase the risk of side effects like dizziness, drowsiness, and lightheadedness. Additionally, alcohol can affect your blood pressure, which may complicate the monitoring your doctor needs to perform while you are on this drug. Since methylergonovine is used in the immediate postpartum period, alcohol is also generally discouraged to ensure proper recovery and to avoid passing alcohol to the infant through breast milk if you are nursing.
Methylergonovine is absolutely not safe to use during pregnancy or before the baby is delivered. Its primary function is to cause intense, sustained uterine contractions, which can be dangerous for a developing fetus by restricting blood flow or causing the uterus to rupture. It is specifically indicated for use only during the 'third stage of labor' (after the baby is born) or in the postpartum period. If you are pregnant, your doctor will use other medications if labor needs to be induced. Always inform your healthcare provider if there is any chance you could still be pregnant before receiving this drug.
The onset of action for methylergonovine depends on how it is administered. When given as an intramuscular (IM) injection, it typically begins to work within 2 to 5 minutes. If it is given intravenously (IV) in an emergency, the effect is almost immediate, occurring within 60 seconds. For the oral tablet form, it takes slightly longer, usually between 5 and 10 minutes to begin causing uterine contractions. The duration of these effects lasts for several hours, which helps maintain uterine firmness and prevent delayed bleeding.
Yes, you can typically stop taking methylergonovine suddenly once you have completed the course prescribed by your doctor. Because it is only used for a short period (usually no more than 7 days), the body does not develop a dependence on it, and there are no known withdrawal symptoms. However, it is vital that you do not stop taking it earlier than instructed. Stopping the medication too soon could result in the uterus relaxing prematurely, which might lead to a recurrence of heavy bleeding. Always follow the full course of treatment as directed by your healthcare provider.
If you miss a dose of methylergonovine tablets, take the missed dose as soon as you remember. If it is almost time for your next scheduled dose, skip the missed dose and continue with your regular schedule. Do not take two doses at once to make up for a missed one, as this can significantly increase your risk of dangerously high blood pressure. If you are concerned about missing a dose, especially if you notice an increase in vaginal bleeding, contact your healthcare provider or midwife immediately for further instructions.
There is no evidence to suggest that methylergonovine causes weight gain. The medication is used for a very short duration, typically between two and seven days, which is not long enough to cause changes in body fat or significant fluid retention. Any weight changes experienced during the time you are taking methylergonovine are more likely related to the natural physiological changes that occur after childbirth, such as the loss of pregnancy-related fluid and the return of the uterus to its pre-pregnancy size. If you experience sudden swelling or rapid weight gain, contact your doctor, as this could be a sign of a different postpartum complication.
Methylergonovine has several serious drug interactions that must be managed by a doctor. It should never be taken with strong CYP3A4 inhibitors, such as certain antibiotics (erythromycin), antifungals (ketoconazole), or HIV medications (ritonavir), as this can cause dangerous ergot toxicity. It also interacts with migraine medications called triptans and other ergot drugs, which can lead to severe heart or blood pressure problems. Always provide your healthcare provider with a complete list of all medications, over-the-counter drugs, and herbal supplements you are taking to ensure your safety.
Yes, methylergonovine maleate is available as a generic medication in both tablet and injectable forms. The brand name version most commonly known in the United States is Methergine. Generic versions are required by the FDA to have the same active ingredient, strength, dosage form, and route of administration as the brand-name drug, making them an equally effective and often more cost-effective option for patients. Your hospital or pharmacy will likely provide the generic version unless your doctor specifically requests the brand name.
Other drugs with the same active ingredient (Methylergonovine)