Methylergonovine 0.2mg Tablets
It is used to stop or treat bleeding that happens after a birth. If you have been given this drug for some other reason, talk with your doctor for more information.
Drug Class
Uterotonic
Pharmacologic Class
Ergot alkaloid
Pregnancy Category
Not applicable (used postpartum), but contraindicated during pregnancy
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Methylergonovine is a medication used after childbirth to help your uterus contract and stop heavy bleeding. It works by making the muscles in your uterus tighten up.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. Do not take this medication for more than 1 week unless your doctor specifically instructs you to do so.
Storing and Disposing of Your Medication
Keep your medication at room temperature in a dry location, away from the bathroom. Store all medications in a secure place, out of the reach of children and pets. Dispose of any unused or expired medication. Unless instructed to do so by your doctor or pharmacist, do not flush medication down the toilet or pour it down the drain. If you have questions about the proper disposal of your medication, consult with your pharmacist. You may also want to check if there are any drug take-back programs available in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it is close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed dose.
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. Do not take this medication for more than 1 week unless your doctor specifically instructs you to do so.
Storing and Disposing of Your Medication
Keep your medication at room temperature in a dry location, away from the bathroom. Store all medications in a secure place, out of the reach of children and pets. Dispose of any unused or expired medication. Unless instructed to do so by your doctor or pharmacist, do not flush medication down the toilet or pour it down the drain. If you have questions about the proper disposal of your medication, consult with your pharmacist. You may also want to check if there are any drug take-back programs available in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it is close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed dose.
Lifestyle & Tips
- Avoid grapefruit and grapefruit juice while taking this medication, as it can increase the drug's effects and side effects.
- Avoid smoking, as nicotine can worsen blood vessel constriction.
- Limit or avoid alcohol consumption, as it may exacerbate side effects.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
0.2 mg orally, three or four times daily
Dose Range:
0.2 - 0.8 mg
Condition-Specific Dosing:
postpartum_atony_hemorrhage:
0.2 mg orally, three or four times daily for a maximum of 1 week
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
Use with caution; no specific dose adjustment recommended, but monitor for toxicity.
Moderate:
Use with caution; no specific dose adjustment recommended, but monitor for toxicity.
Severe:
Use with caution; no specific dose adjustment recommended, but monitor for toxicity. Contraindicated in severe renal impairment if hypertension or toxemia is present.
Dialysis:
Not available; use with extreme caution due to potential for accumulation and increased sensitivity.
Hepatic Impairment:
Mild:
Use with caution; no specific dose adjustment recommended, but monitor for toxicity.
Moderate:
Use with caution; no specific dose adjustment recommended, but monitor for toxicity.
Severe:
Use with caution; no specific dose adjustment recommended, but monitor for toxicity. Contraindicated in severe hepatic impairment if hypertension or toxemia is present.
Pharmacology
Mechanism of Action
Methylergonovine is an ergot alkaloid that acts as a partial agonist and antagonist at alpha-adrenergic, dopaminergic, and serotonergic receptors. Its uterotonic effect is primarily due to direct stimulation of uterine and vascular smooth muscle, leading to rapid and sustained tonic contraction of the uterus, which decreases uterine bleeding and shortens the third stage of labor.
Pharmacokinetics
Absorption:
Bioavailability:
60% (oral)
Tmax:
0.5-1.5 hours
FoodEffect:
Not significantly affected by food, but absorption may be slightly delayed.
Distribution:
Vd:
57 L
ProteinBinding:
Approximately 80%
CnssPenetration:
Limited
Elimination:
HalfLife:
0.5-2 hours (variable)
Clearance:
Not precisely quantified, but rapid
ExcretionRoute:
Primarily renal (metabolites), some biliary
Unchanged:
<10%
Pharmacodynamics
OnsetOfAction:
5-10 minutes (oral)
PeakEffect:
Not precisely defined, but sustained contraction within 10-15 minutes
DurationOfAction:
3 hours or more
Safety & Warnings
BLACK BOX WARNING
Concomitant use of methylergonovine with potent CYP3A4 inhibitors (e.g., macrolide antibiotics, azole antifungals, protease inhibitors) is contraindicated due to the risk of acute ergot toxicity (ergotism) characterized by vasospasm, ischemia, and potentially gangrene of the extremities, as well as cerebral or myocardial ischemia.
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high or low blood pressure, including:
+ Severe headache
+ Dizziness
+ Passing out
+ Changes in eyesight
Neurological symptoms, such as:
+ Weakness on one side of the body
+ Trouble speaking or thinking
+ Changes in balance
+ Drooping on one side of the face
+ Blurred eyesight
Seizures
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Headache
Stomach pain
* Upset stomach or vomiting
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. Your doctor can provide medical advice on managing side effects.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high or low blood pressure, including:
+ Severe headache
+ Dizziness
+ Passing out
+ Changes in eyesight
Neurological symptoms, such as:
+ Weakness on one side of the body
+ Trouble speaking or thinking
+ Changes in balance
+ Drooping on one side of the face
+ Blurred eyesight
Seizures
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Headache
Stomach pain
* Upset stomach or vomiting
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. Your doctor can provide medical advice on managing side effects.
Seek Immediate Medical Attention If You Experience:
- Severe headache
- Numbness, tingling, or coldness in fingers or toes
- Chest pain or tightness
- Nausea or vomiting that is severe or persistent
- Dizziness or lightheadedness
- Blurred vision
- Weakness in your legs
- Swelling, pain, or discoloration of an arm or leg
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
If you have high blood pressure or have experienced high blood pressure during pregnancy (preeclampsia).
If you are taking any medications, including prescription and over-the-counter (OTC) drugs, natural products, or vitamins, that may interact with this medication. Certain medications used to treat HIV, infections, depression, and other conditions should not be taken with this drug. Your doctor or pharmacist can advise you on potential interactions.
If you are pregnant or think you may be pregnant. Do not take this medication if you are pregnant.
* If you are breast-feeding. You should not breast-feed for at least 12 hours after receiving this medication.
This list is not exhaustive, and it is crucial to discuss all your medications and health conditions with your doctor and pharmacist to ensure safe treatment. You must verify that it is safe to take this medication with all your other medications and health conditions. Never start, stop, or change the dose of any medication without consulting your doctor.
It is essential to inform your doctor about the following conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
If you have high blood pressure or have experienced high blood pressure during pregnancy (preeclampsia).
If you are taking any medications, including prescription and over-the-counter (OTC) drugs, natural products, or vitamins, that may interact with this medication. Certain medications used to treat HIV, infections, depression, and other conditions should not be taken with this drug. Your doctor or pharmacist can advise you on potential interactions.
If you are pregnant or think you may be pregnant. Do not take this medication if you are pregnant.
* If you are breast-feeding. You should not breast-feed for at least 12 hours after receiving this medication.
This list is not exhaustive, and it is crucial to discuss all your medications and health conditions with your doctor and pharmacist to ensure safe treatment. You must verify that it is safe to take this medication with all your other medications and health conditions. Never start, stop, or change the dose of any medication without consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. If you have risk factors for heart disease, such as high blood pressure, high cholesterol, being overweight, having high blood sugar or diabetes, smoking cigarettes, being a male over 40 years old, having a family history of early heart disease, or being a female who has gone through menopause, exercise caution and discuss your individual situation with your doctor.
As this medication can cause high blood pressure, it is crucial to have your blood pressure monitored as directed by your doctor. Additionally, if you regularly consume grapefruit juice or eat grapefruit, you should consult with your doctor to discuss any potential interactions.
As this medication can cause high blood pressure, it is crucial to have your blood pressure monitored as directed by your doctor. Additionally, if you regularly consume grapefruit juice or eat grapefruit, you should consult with your doctor to discuss any potential interactions.
Overdose Information
Overdose Symptoms:
- Nausea
- Vomiting
- Abdominal pain
- Numbness, tingling, pain, and coldness of the extremities
- Peripheral ischemia
- Hypertension (sometimes hypotension)
- Tachycardia
- Bradycardia
- Confusion
- Convulsions
- Coma
What to Do:
Seek immediate medical attention or call a poison control center (e.g., 1-800-222-1222). Treatment is symptomatic and supportive, including vasodilation (e.g., nitroprusside, nitroglycerin) for severe vasospasm.
Drug Interactions
Contraindicated Interactions
- Potent CYP3A4 inhibitors (e.g., ritonavir, nelfinavir, indinavir, saquinavir, ketoconazole, itraconazole, voriconazole, posaconazole, clarithromycin, telithromycin, erythromycin)
- Triptans (e.g., sumatriptan, zolmitriptan) - concurrent use or within 24 hours
- Other ergot alkaloids (e.g., ergotamine, dihydroergotamine)
Major Interactions
- Moderate CYP3A4 inhibitors (e.g., fluconazole, grapefruit juice, cimetidine, fluvoxamine)
- Vasoconstrictors (e.g., dopamine, dobutamine, other sympathomimetics)
- Beta-blockers (increased risk of vasoconstriction)
- Bromocriptine (additive effects)
Moderate Interactions
- Weak CYP3A4 inhibitors
- SSRIs (potential for serotonin syndrome, though less common with methylergonovine)
- Nitrates (may reduce efficacy of nitrates)
Monitoring
Baseline Monitoring
Blood Pressure
Rationale: To establish baseline and identify pre-existing hypertension, which is a contraindication or requires caution.
Timing: Prior to initiation
Uterine Tone/Bleeding
Rationale: To assess the severity of postpartum hemorrhage and establish baseline uterine atony.
Timing: Prior to initiation
Routine Monitoring
Blood Pressure
Frequency: Frequently during initial treatment, then as clinically indicated (e.g., every 4-6 hours)
Target: Individualized, but avoid significant increases
Action Threshold: Systolic BP >140 mmHg or Diastolic BP >90 mmHg, or significant increase from baseline; consider dose reduction or discontinuation.
Uterine Tone and Vaginal Bleeding
Frequency: Regularly (e.g., every 15-30 minutes initially, then every few hours)
Target: Firm uterine fundus, minimal vaginal bleeding
Action Threshold: Boggy uterus, excessive bleeding; consider additional uterotonics or other interventions.
Signs of Ergotism (e.g., cold/numb extremities, chest pain, headache)
Frequency: Daily
Target: Absence of symptoms
Action Threshold: Presence of symptoms; discontinue drug immediately and seek medical attention.
Symptom Monitoring
- Headache (severe or persistent)
- Nausea
- Vomiting
- Abdominal pain or cramps (excessive)
- Dizziness
- Tinnitus
- Cold or numb fingers/toes
- Chest pain
- Shortness of breath
- Weakness in legs
- Blurred vision
- Seizures
Special Patient Groups
Pregnancy
Methylergonovine is contraindicated during pregnancy. It is used postpartum to prevent or treat uterine hemorrhage. Its potent uterotonic effects can cause uterine contractions and fetal distress/death if used during pregnancy.
Trimester-Specific Risks:
First Trimester:
Contraindicated due to potent uterotonic effects and potential for fetal harm/abortion.
Second Trimester:
Contraindicated due to potent uterotonic effects and potential for fetal harm/preterm labor.
Third Trimester:
Contraindicated during labor and before delivery due to potent uterotonic effects and risk of uterine rupture, fetal distress, and placental abruption.
Lactation
Not recommended during breastfeeding. Methylergonovine is excreted in breast milk and may cause adverse effects in the nursing infant, including ergotism (e.g., vomiting, diarrhea, weak pulse, unstable blood pressure, convulsions). If essential, consider temporary cessation of breastfeeding for at least 12 hours after the last dose.
Infant Risk:
Moderate risk (L3) due to potential for ergotism and other adverse effects in the infant.
Pediatric Use
Safety and efficacy have not been established in pediatric patients. Not indicated for use in this population.
Geriatric Use
Use with caution in elderly patients due to increased susceptibility to adverse effects, particularly cardiovascular effects (e.g., hypertension, vasospasm). Start with lower doses and monitor closely.
Clinical Information
Clinical Pearls
- Methylergonovine is primarily used for postpartum hemorrhage due to uterine atony, not for induction or augmentation of labor.
- Always check blood pressure before administering, as it is contraindicated in patients with hypertension or preeclampsia/eclampsia.
- Oral administration is for continued management after initial parenteral control of bleeding.
- Counsel patients to avoid grapefruit juice and certain medications (e.g., macrolide antibiotics, HIV protease inhibitors) due to severe interaction risk (ergotism).
- Monitor for signs of ergotism (e.g., cold/numb extremities, chest pain) and instruct patients to report these immediately.
Alternative Therapies
- Oxytocin (IV or IM)
- Carboprost tromethamine (Hemabate) (IM)
- Misoprostol (oral, sublingual, rectal)
- Tranexamic acid (IV)
Cost & Coverage
Average Cost:
Varies widely, typically $20-$100 per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.