(ER goe loid MES i lates)
Mental capacity decline: Treatment of signs and symptoms of an idiopathic decline in mental capacity.
Note: Individuals who do respond come from groups of patients who would be considered clinically to suffer from some ill-defined process related to aging or to have some underlying dementing condition (ie, primary progressive dementia, Alzheimer dementia, senile onset, multi-infarct dementia).
Hypersensitivity to ergoloid mesylates, ergot, or any component of the formulation; acute or chronic psychosis; concurrent use with potent inhibitors of cytochrome P450 (CYP-450) 3A4 (includes protease inhibitors, azole antifungals, and some macrolide antibiotics).
Canadian labeling: Additional contraindications (not in US labeling): Severe bradycardia; severe hypotension.
Documentation of allergenic cross-reactivity for ergot alkaloids is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.
Mental capacity decline: Oral:
US labeling: 1 mg 3 times daily; results may not be observed until 3 to 4 weeks.
Canadian labeling: 1 mg 3 to 4 times daily with food; discontinue if no improvement is seen within 3 to 4 weeks.
Avoid use in this age group due to lack of efficacy (Beers Criteria).
There are no dosage adjustments provided in the manufacturers labeling.
There are no dosage adjustments provided in the manufacturers labeling.
Store at 20 ‚ °C to 25 ‚ °C (68 ‚ °F to 77 ‚ °F).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Generic: 1 mg
Analgesics (Opioid): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy
Antiemetics (5HT3 Antagonists): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy
Antihepaciviral Combination Products: May increase the serum concentration of Ergot Derivatives. Avoid combination
Anti-Parkinson Agents (Monoamine Oxidase Inhibitor): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity if selegiline or rasagiline is combined with a serotonin modulator. Use of transdermal selegiline with serotonin modulators is contraindicated. Consider therapy modification
Antipsychotic Agents: Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy
Aprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Beta-Blockers: May enhance the vasoconstricting effect of Ergot Derivatives. Consider therapy modification
Boceprevir: May increase the serum concentration of Ergoloid Mesylates. Avoid combination
Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Avoid combination
CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Monitor therapy
CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates. Consider therapy modification
Dapoxetine: May enhance the adverse/toxic effect of Serotonin Modulators. Avoid combination
Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination
Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination
Itraconazole: May increase the serum concentration of Ergoloid Mesylates. Avoid combination
Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Ketoconazole (Systemic): May increase the serum concentration of Ergoloid Mesylates. Avoid combination
Linezolid: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Management: Due to a risk of serotonin syndrome/serotonin toxicity, discontinue serotonin modulators 2 weeks prior to the administration of linezolid. If urgent initiation of linezolid is needed, discontinue serotonin modulators immediately and monitor closely. Consider therapy modification
Lorcaserin: May enhance the adverse/toxic effect of Ergot Derivatives. Specifically, use of these drugs together may increase the risk of developing valvular heart disease. Lorcaserin may enhance the serotonergic effect of Ergot Derivatives. This could result in serotonin syndrome. Avoid combination
Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Macrolide Antibiotics: May increase the serum concentration of Ergot Derivatives. Cabergoline and Clarithromycin may interact, see specific monograph for full details. Exceptions: Azithromycin (Systemic); Fidaxomicin; Spiramycin. Consider therapy modification
Metaxalone: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy
Methylene Blue: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Avoid combination
Metoclopramide: Serotonin Modulators may enhance the adverse/toxic effect of Metoclopramide. This may be manifest as symptoms consistent with serotonin syndrome or neuroleptic malignant syndrome. Monitor therapy
MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates. Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Consider therapy modification
Netupitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Nitroglycerin: Ergot Derivatives may diminish the vasodilatory effect of Nitroglycerin. This is of particular concern in patients being treated for angina. Nitroglycerin may increase the serum concentration of Ergot Derivatives. Avoid combination
Osimertinib: May increase the serum concentration of CYP3A4 Substrates. Osimertinib may decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
Palbociclib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Posaconazole: May increase the serum concentration of Ergoloid Mesylates. Avoid combination
Protease Inhibitors: May increase the serum concentration of Ergot Derivatives. Avoid combination
Reboxetine: May enhance the hypertensive effect of Ergot Derivatives. Monitor therapy
Roxithromycin: May increase the serum concentration of Ergot Derivatives. Avoid combination
Serotonin 5-HT1D Receptor Agonists: Ergot Derivatives may enhance the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists. Serotonin 5-HT1D Receptor Agonists may enhance the vasoconstricting effect of Ergot Derivatives. Avoid combination
Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Exceptions: Nicergoline; Tedizolid. Monitor therapy
Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy
Stiripentol: May increase the serum concentration of CYP3A4 Substrates. Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification
Tedizolid: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy
Telaprevir: May increase the serum concentration of Ergoloid Mesylates. Avoid combination
TraMADol: Serotonin Modulators may enhance the adverse/toxic effect of TraMADol. The risk of seizures may be increased. TraMADol may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy
Voriconazole: May increase the serum concentration of Ergoloid Mesylates. Avoid combination
Frequency not defined. Adverse effects are minimal.
Cardiovascular: Bradycardia, flushing, orthostatic hypotension
Dermatologic: Skin rash
Gastrointestinal: Gastrointestinal distress (sublingual administration), nausea (sublingual administration; transient)
Local: Local irritation (sublingual administration)
Ophthalmic: Blurred vision
Respiratory: Nasal congestion
Concerns related to adverse effects:
- Cardiac valvular fibrosis: Ergot alkaloids have been associated with fibrotic valve thickening (eg, aortic, mitral, tricuspid); usually associated with long-term, chronic use.
- Pleural/retroperitoneal fibrosis: Rare cases of pleural and/or retroperitoneal fibrosis have been reported with prolonged daily use.
Concurrent drug therapy issues:
- Drug-drug interactions: Additional potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult Drug Interactions for more detailed information.
Other warnings/precautions:
- Appropriate use: Careful diagnosis should be attempted before prescribing. Because target symptoms are of unknown etiology, exclude potentially reversible and treatable conditions; particular care should be taken to exclude delirium and dementiform illness secondary to systemic disease, primary neurological disease, or primary disturbance of mood.
Ergoloid mesylates do not have the vasoconstrictor effects of the natural ergot alkaloids; exact mechanism in dementia is unknown; originally classed as peripheral and cerebral vasodilator, now considered a metabolic enhancer"; there is no specific evidence that clearly establishes the mechanism by which ergoloid mesylate preparations produce mental effects, nor is there conclusive evidence that the drug particularly affects cerebral arteriosclerosis or cerebrovascular insufficiency.
Rapid yet incomplete
Hepatic, including first-pass metabolism
Serum: 1.5 to 3 hours
Serum: ~2.6 to 5.1 hours
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience abdominal pain. Have patient report immediately to prescriber severe nausea or severe vomiting (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.