ERGOSTAT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ERGOSTAT (ERGOSTAT).
Ergostat (ergotamine) is a serotonin (5-HT) receptor agonist, specifically at 5-HT1B and 5-HT1D receptors, leading to cranial vasoconstriction and inhibition of neurogenic inflammation. It also has partial agonist/antagonist activity at alpha-adrenergic receptors.
| Metabolism | Primarily hepatic via CYP3A4. Undergoes extensive first-pass metabolism. |
| Excretion | Primarily hepatic (biliary-fecal) elimination: ~90% of a dose is excreted in feces as metabolites; renal excretion accounts for <5% unchanged drug. |
| Half-life | Terminal half-life is 2–3 hours (intravenous) and 2–4 hours (oral). Short half-life necessitates frequent dosing; duration of action limited to 2–4 hours. |
| Protein binding | ~65% bound to plasma albumin. Metabolites are less extensively bound. |
| Volume of Distribution | Approximately 0.2–0.3 L/kg, indicating primarily extracellular and peripheral tissue distribution with limited CNS penetration. |
| Bioavailability | Oral: ~10–20% (extensive first-pass metabolism); Sublingual: ~50–60% (avoids portal circulation); Rectal: ~30–40% (variable). |
| Onset of Action | Oral: 10–20 minutes; Sublingual: 5–10 minutes; Rectal: 10–15 minutes; Intravenous: immediate (within 1 minute). |
| Duration of Action | Oral/sublingual/rectal: 2–4 hours (clinical effect wanes after 3 hours). Intravenous: 0.5–2 hours (short-lived, used for acute emergencies). |
| Molecular Weight | 581.67 Da |
0.2 mg intramuscularly or intravenously every 2-4 hours for maximum 5 doses; not to exceed 1 mg total dose.
| Dosage form | TABLET |
| Renal impairment | No specific adjustment; use with caution in severe renal impairment (GFR <30 mL/min) due to potential accumulation. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: avoid use. |
| Pediatric use | Intravenous: 0.1 mg/m² body surface area every 2-4 hours, maximum 0.5 mg total; intramuscular: 0.2 mg every 2-4 hours, maximum 1 mg. |
| Geriatric use | Start at 0.1 mg intramuscularly or intravenously; monitor for hypertension with higher doses. |
| 1st trimester | Contraindicated: ergotamine induces uterine contractions and may cause fetal hypoxia; associated with spontaneous abortion and congenital malformations. |
| 2nd trimester | Contraindicated: risk of uteroplacental insufficiency and fetal distress; avoid use. |
| 3rd trimester | Contraindicated: strong oxytocic effect can precipitate preterm labor; risk of neonatal ergotism. |
Clinical note
Comprehensive clinical and safety monograph for ERGOSTAT (ERGOSTAT).
| Placental transfer | Ergotamine crosses the placenta; detectable in fetal tissues. High degree of transfer. |
| Breastfeeding | Ergotamine is excreted into breast milk; may cause ergotism in infants (vomiting, diarrhea, seizures). Contraindicated during breastfeeding. |
| Lactation Rating |
■ FDA Black Box Warning
Concomitant use with strong CYP3A4 inhibitors (e.g., protease inhibitors, macrolide antibiotics, azole antifungals) can lead to serious and/or life-threatening peripheral ischemia and vasospasm. Avoid coadministration.
| Serious Effects |
PregnancyBreastfeedingPeripheral vascular diseaseCoronary artery diseaseHypertensionSepsisHepatic impairmentRenal impairment
| Precautions | Risk of ischemia (peripheral, cerebral, coronary) especially with prolonged use or overdose, Fibrotic complications (cardiac valvulopathy, pulmonary, retroperitoneal fibrosis) with chronic use, Medication overuse headache (MOH) with frequent use, Avoid in patients with uncontrolled hypertension, coronary artery disease, or peripheral vascular disease, Do not exceed recommended dosage; may cause ergotism |
| Food/Dietary | Avoid grapefruit juice as it may increase ergonovine levels. No other significant food interactions. |
Loading safety data…
| L5 - Contraindicated |
| Teratogenic Risk | Ergostat (ergonovine) is contraindicated in pregnancy due to its potent uterotonic effects, which can cause uterine tetany, fetal hypoxia, and placental abruption. It is classified as FDA Pregnancy Category X. Use in the first trimester may increase the risk of spontaneous abortion; in the second and third trimesters, it can precipitate preterm labor and fetal distress. There is no evidence of structural teratogenicity from direct drug effects, but the potential for ischemic injury to the fetus due to uterine hyperstimulation exists. |
| Fetal Monitoring | Maternal monitoring: Continuous blood pressure monitoring (risk of hypertension), heart rate, and uterine activity (tone and contraction frequency). Monitor for signs of ergotism (nausea, vomiting, paresthesias, chest pain). Fetal monitoring: Continuous fetal heart rate monitoring to detect signs of distress (late decelerations, bradycardia) due to reduced uteroplacental blood flow. Assess for vaginal bleeding indicating placental abruption. |
| Fertility Effects | Ergonovine may impair fertility due to its effects on uterine and ovarian blood flow. It can inhibit implantation if used around the time of conception. In men, no direct effects on sperm parameters have been reported, but ergot alkaloids can cause hyperprolactinemia and potentially suppress gonadotropins, though this is more associated with dopamine agonists than ergonovine. Overall, fertility effects are not well studied. |
| Clinical Pearls | ERGOSTAT (ergonovine) is an ergot alkaloid used for postpartum hemorrhage. It causes sustained uterine contraction. Contraindicated in hypertension, preeclampsia, and vascular disease. Administer IM or IV slowly over 1 minute to avoid severe vasoconstriction. Monitor blood pressure and uterine tone closely. Do not use in patients with hypersensitivity to ergot alkaloids. |
| Patient Advice | This medication is given to control bleeding after childbirth. · It may cause nausea, vomiting, or dizziness. · Report severe headache, chest pain, or vision changes immediately. · Avoid smoking or using nicotine products while on this drug. · Do not breastfeed within 12 hours after the last dose; discuss with your doctor. |