QuickView for Ergonovine (compound)

Summary
General Info

PubChem

PubChem Compound 4210613

Name:	Ergonovine
PubChem Compound ID:	4210613
Description:	An ergot alkaloid (ERGOT ALKALOIDS) with uterine and VASCULAR SMOOTH MUSCLE contractile properties.
Molecular formula:	C₁₉H₂₃N₃O
Molecular weight:	309.406 g/mol

DrugBank

Identification

Name:	Ergonovine
Name (isomeric):	DB01253
Drug Type:	small molecule
Description:	An ergot alkaloid (ERGOT ALKALOIDS) with uterine and VASCULAR SMOOTH MUSCLE contractile properties.
Synonyms:	Ergobasine; Ergotrate maleate; Ergometrine
Brand:	Ergotrate
Category:	Oxytocics
CAS number:	60-79-7

Pharmacology

Indication:	Used to treat postpartum haemorrhage and postabortion haemorrhage in patients with uterine atony.
Pharmacology:	Ergonovine belongs to the group of medicines known as ergot alkaloids. These medicines are usually given to stop excessive bleeding that sometimes occurs after abortion or a baby is delivered. They work by causing the muscle of the uterus to contract.
Mechanism of Action:	Ergonovine directly stimulates the uterine muscle to increase force and frequency of contractions. With usual doses, these contractions precede periods of relaxation; with larger doses, basal uterine tone is elevated and these relaxation periods will be decreased. Contraction of the uterine wall around bleeding vessels at the placental site produce... show more » Ergonovine directly stimulates the uterine muscle to increase force and frequency of contractions. With usual doses, these contractions precede periods of relaxation; with larger doses, basal uterine tone is elevated and these relaxation periods will be decreased. Contraction of the uterine wall around bleeding vessels at the placental site produces hemostasis. Ergonovine also induces cervical contractions. The sensitivity of the uterus to the oxytocic effect is much greater toward the end of pregnancy. The oxytocic actions of ergonovine are greater than its vascular effects. Ergonovine, like other ergot alkaloids, produces arterial vasoconstriction by stimulation of alpha-adrenergic and serotonin receptors and inhibition of endothelial-derived relaxation factor release. It is a less potent vasoconstrictor than ergotamine. As a diagnostic aid (coronary vasospasm), ergonovine causes vasoconstriction of coronary arteries. show less «
Absorption:	Absorption is rapid and complete after oral or intramuscular administration.
Biotransformation:	Hepatic.
Route of elimination:	Thought to be eliminated by non-renal mechanisms (i.e. hepatic metabolism, excretion in feces)
Half Life:	t_{1/2 α}=10 minutes; t_{1/2 β}=2 hours
Toxicity:	The principal symptoms of overdose are convulsions and gangrene. Other symptoms include bradycardia, confusion, diarrhoea, dizziness, dyspnoea, drowsiness, fast and/or weak pulse, miosis, hypercoagulability, loss of consciousness, nausea and vomiting, numbness and coldness of the extremities, pain in the chest, peripheral vasoconstriction, respiratory depression, rise or fall in blood pressure, severe cramping of the uterus, tachycardia, tingling, and unusual thirst.
Affected organisms:	Humans and other mammals

Interactions

Drug interaction:

Tramadol	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Delavirdine	The antiretroviral agent may increase the ergot derivative toxicity
Trimipramine	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Erythromycin	Possible ergotism and severe ischemia with this combination
Epinephrine	Possible marked increase of arterial pressure

Tramadol	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Delavirdine	The antiretroviral agent may increase the ergot derivative toxicity
Trimipramine	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Erythromycin	Possible ergotism and severe ischemia with this combination
Epinephrine	Possible marked increase of arterial pressure
Tranylcypromine	Increased risk of serotonin syndrome. Use caution during concomitant therapy and monitor for symptoms of serotonin syndrome.
Isosorbide Mononitrate	Possible antagonism of action
Labetalol	Ischemia with risk of gangrene
Bisoprolol	Ischemia with risk of gangrene
Phenylephrine	Possible marked increase of arterial pressure
Venlafaxine	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Nitroglycerin	Possible antagonism of action
Tipranavir	Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Ergonovine. Concomitant therapy is contraindicated.
Zolmitriptan	Concomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, ergonovine, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
Naratriptan	Possible severe and prolonged vasocontriction
Propranolol	Ischemia with risk of gangrene
Trazodone	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Esmolol	Ischemia with risk of gangrene
Metoprolol	Ischemia with risk of gangrene
Desvenlafaxine	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Oxprenolol	Ischemia with risk of gangrene
Telithromycin	Telithromycin may reduce clearance of Ergonovine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Ergonivine if Telithromycin is initiated, discontinued or dose changed.
Atenolol	Ischmeia with risk of gangrene
Pindolol	Ischemia with risk of gangrene
Eletriptan	Possible severe and prolonged vasoconstriction
Timolol	Ischemia with risk of gangrene
Voriconazole	Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of ergonovine by decreasing its metabolism. Concomitant therapy is contraindicated.
Efalizumab	The antiretroviral agent may increase the ergot derivative
Isosorbide Dinitrate	Possible antagonism of action
Pentaerythritol Tetranitrate	Possible antagonism of action
Frovatriptan	Possible severe and prolonged vasoconstriction
Carvedilol	Ischemia with risk of gangrene
Acebutolol	Ischemia with risk of gangrene
Nadolol	Ischemia with risk of gangrene
Almotriptan	Possible severe and prolonged vasoconstriction

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Targets

Alpha-1A adrenergic receptor

Enzymes

Cytochrome P450 3A4

Transporters

Multidrug resistance protein 1