View source for Ergotamine tartrate (sublingual tablet)

{{DrugProjectFormSinglePage
|authorTag={{AP}}
|genericName=Ergotamine tartrate
|aOrAn=an
|drugClass=alpha adrenergic blocking agent
|indicationType=prophylaxis
|indication=[[vascular migraine]]
|hasBlackBoxWarning=Yes
|adverseReactions=[[pruritus]], [[nausea and vomiting]], [[muscle weakness]], [[paresthesia]] and [[visual disturbance]]
|blackBoxWarningTitle=<span style="color:#FF0000;">WARNING</span>
|blackBoxWarningBody=<i><span style="color:#FF0000;"></span></i> Serious and/or life-threatening peripheral ischemia has been associated with the coadministration of ergotamine tartrate with potent CYP 3A4 inhibitors including protease inhibitors and macrolide antibiotics. Because CYP 3A4 inhibition elevates the serum levels of ergotamine tartrate, the risk for vasospasm leading to cerebral ischemia and/or ischemia of the extremities is increased. Hence, concomitant use of these medications is contraindicated.
|fdaLIADAdult======Abortion or prevention of vascular headache, e.g., migraine, migraine variants or a so-called "histaminic cephalalgia"=====
*For best results, dosage should start at the first sign of an attack. Early administration gives maximum effectiveness. At the first sign of an attack or to relieve symptoms after onset of an attack, one 2 mg tablet is placed under the tongue. Another tablet should be taken at half-hour intervals thereafter, if necessary, but dosage must not exceed three tablets in any 24hour period. Total weekly dosage should not exceed five tablets (10 mg) in any one week. Sublingual Tablets should not be used for chronic daily administration.
|offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Ergotamine in adult patients.
|offLabelAdultNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of Ergotamine in adult patients.
|offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Ergotamine in pediatric patients.
|offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of Ergotamine in pediatric patients.
|contraindications=*Coadministration of ergotamine with potent [[CYP 3A4]] inhibitors ([[ritonavir]], [[nelfinavir]], [[indinavir]], [[erythromycin]], [[clarithromycin]] and [[troleandomycin]]) has been associated with acute ergot toxicity ([[ergotism]]) characterized by [[vasospasm]] and [[ischemia]] of the extremities, with some cases resulting in amputation. There have been rare reports of [[cerebral ischemia]] in patients on protease inhibitor therapy when ergotamine was coadministered, at least one resulting in death. Because of the increased risk for [[ergotism]] and other serious vasospastic adverse events, ergotamine use is contraindicated with these drugs and other potent inhibitors of [[CYP3A4]] (e.g., [[ketoconazole]], [[itraconazole]]). 
*[[Ergomar]] Sublingual Tablets may cause fetal harm when administered to pregnant women. [[Ergomar]] Sublingual Tablets are contraindicated in women who are or may become pregnant. If this drug is used during pregnancy or if the patient becomes pregnant while taking this product, the patient should be apprised of the potential hazard to the fetus. [[Peripheral vascular disease]], [[coronary heart]] disease, [[hypertension]], impaired [[hepatic function]] or [[renal function]] and [[sepsis]][[Hypersensitivity]] to any of the components.
|warnings======CYP 3A4 Inhibitors (e.g. Macrolide Antibiotics and Protease Inhibitors)=====
*Coadministration of ergotamine with potent [[CYP3A4]] inhibitors such as [[protease inhibitors]] or [[macrolide antibiotics]] has been associated with serious adverse events; for this reason, these drugs should not be given concomitantly with ergotamine. While these reactions have not been reported with less potent [[CYP3A4]] inhibitors, there is a potential risk for serious toxicity including [[vasospasm]] when these drugs are used with ergotamine. Examples of less potent [[CYP3A4]] inhibitors include: [[saquinavir]], [[nefazodone]], [[fluconazole]], [[fluoxetine]], grapefruit juice, [[fluvoxamine]], [[zileuton]], [[metronidazole]], and [[clotrimazole]]. These lists are not exhaustive, and the prescriber should consider the effects on [[CYP3A4]] of other agents being considered for concomitant use with ergotamine.

=====Fibrotic Complications=====
*There have been a few reports of patients on ergotamine tartrate and [[caffeine]] therapy developing [[retroperitoneal]] and/or [[pleuropulmonary fibrosis]]. There have also been rare reports of fibrotic thickening of the [[aortic valve]], [[mitral valve]], [[tricuspid valve]], and/or [[pulmonary valve]] with long-term continuous use of ergotamine tartrate and caffeine. Ergomar Sublingual Tablets should not be used for chronic daily administration
|clinicalTrials=====Cardiovascular Effects==== 
*[[Vasoconstriction]]
**[[Ischemia]] 
**[[Cyanosis]] 
**[[Absence of pulse]] 
**[[Cold extremities]] 
**[[Gangrene]] 
**[[Precordial distress]] 
**[[Precordial pain]] 
**[[EKG]] changes 
**[[Muscle pain]] 
*[[Transient tachycardia]] 
*[[Bradycardia]] 
*[[Hypertension]]

=====Gastrointestinal Effects===== 
*[[Nausea and vomiting]]

=====Neurological Effects===== 
*[[Paresthesias]] 
*[[Numbness]] 
*[[Weakness]] 
*[[Vertigo]]

=====Allergic Effects=====
*Localized [[edema]] and [[itching]].

=====Fibrotic Complications=====
*[[Retroperitoneal]]
*[[Pleural]]
|drugInteractions=*Pharmacokinetic interactions (increased blood levels of ergotamine) have been reported in patients treated orally with ergotamine and [[macrolide antibiotics]] (e.g., [[troleandomycin]], [[clarithromycin]], [[erythromycin]]), and in patients treated orally with ergotamine and [[protease inhibitors]] (e.g. [[ritonavir]]) presumably due to inhibition of [[cytochrome P450]] 3A metabolism of ergotamine. Ergotamine has also been shown to be an inhibitor of [[cytochrome P450]] 3A catalyzed reactions. No pharmacokinetic interactions involving other [[cytochrome P450]] isoenzymes are known.
|FDAPregCat=X
|useInPregnancyFDA=*There are no studies on the placental transfer or teratogenicity of Ergomar. Ergotamine crosses the [[placenta]] in small amounts, although it does not appear to be [[embryotoxic]] in this quantity. However, prolonged [[vasoconstriction]] of the [[uterine vessels]] and/or increased [[myometrial tone]] leading to reduced myometrial and placental blood flow may have contributed to [[fetal growth retardation]] observed in animals.
|useInLaborDelivery=*Ergomar is contraindicated in pregnancy due to its oxytocic effect which is maximal in the third trimester.
|useInNursing=*Ergot drugs are known to inhibit [[prolactin]] but there are no reports of decreased lactation with Ergomar. Ergotamine is excreted in breast milk and may cause symptoms of [[vomiting]], [[diarrhea]], weak pulse and unstable [[blood pressure]] in nursing infants. Because of the potential for serious adverse reactions in nursing infants from Ergomar, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
|useInPed=*Safety and effectiveness in pediatric patients have not been established.
|administration=*Sublingual tablets
|overdose=*Symptoms include [[vomiting]], [[numbness]], [[tingling]], [[pain]] and [[cyanosis]] of the extremities associated with diminished or absent [[peripheral pulses]]; [[hypertension]] or [[hypotension]]; [[drowsiness]], [[stupor]], [[coma]], [[convulsions]] and [[shock]]. A case has been reported of reversible bilateral [[papillitis]] with ring [[scotomata]] in a patient who received five times the recommended daily adult dose over a period of 14 days. Treatment consists of removal of the offending drug. Maintenance of adequate pulmonary ventilation, correction of [[hypotension]], and control of [[convulsions]] and [[blood pressure]] are important considerations. Treatment of peripheral vasospasm should consist of warmth, but not heat, and protection of the ischemic limbs. Vasodilators may be beneficial but caution must be exercised to avoid aggravating an already existent [[hypotension]].
|drugBox=[[file:ErgotamineDB2.png|thumb|none|600px]]
|mechAction=*Ergotamine is a alpha adrenergic blocking agent with a direct stimulating effect on the smooth muscle of peripheral and cranial blood vessels and produces depression of central vasomotor centers. The compound also has the properties of [[serotonin]] antagonism. In comparison to hydrogenated ergotamine, the adrenergic blocking actions are less pronounced and vasoconstrictive actions are greater.
|structure=*D.H.E. 45® is ergotamine hydrogenated in the 9, 10 position as the mesylate salt. D.H.E. 45® is known chemically as ergotaman-3´,6´,18-trione,9,10-dihydro-12´-hydroxy-2´-methyl-5´-(phenylmethyl)-,(5´α)-, monomethanesulfonate. Its molecular weight is 679.80 and its empirical formula is C33H37N5O5•CH4O3S.
*The chemical structure is:

[[file:Ergotamine Structure432.png|none|400px]]
|howSupplied======Ergotamine Tartrate Sublingual Tablets=====
*Ergomar® Sublingual Tablets are round, green tablets each containing 2 mg of ergotamine tartrate. They are debossed with the product identification code "LB2" on one side, and are supplied in individual foil strips packaged in a plastic child resistant canister containing 20 tablets (5 – 2 × 2 foil strips) NDC 10802-12020
|storage=*Store at 20°- 25°C (68° - 77°F); excursions permitted to 15° - 30°C (59° - 86°F). Protect from light and heat. Keep out of reach of children.
|packLabel=[[file:FDA label.png|thumb|none|450px]]
|fdaPatientInfo=There is limited information regarding <i>Patient Counseling Information</i> of {{PAGENAME}} in the drug label.
|alcohol=Alcohol-Ergotamine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
|brandNames=*Ergomar®<ref>{{Cite web | title = ERGOMAR- ergotamine tartrate tablet, orally disintegrating | url = http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1bfd4827-5123-4dbb-8f94-7b097f5bfd5c}}</ref>
}}
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|fileName=CP2.png
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