ergoloid mesylates (Rx)

Brand and Other Names:Hydergine
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 1mg

Age-Related Mental Decline & Alzheimer's Dementia

1 mg PO q8hr

May administer up to 4.5-12 mg/day therapeutic trial should be 6 months in duration

Safety & efficacy not established

Age-Related Mental Decline & Alzheimer's Dementia

1 mg PO q8hr

May administer up to 4.5-12 mg/day therapeutic trial should be 6 months in duration

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Interactions

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            Contraindicated (31)

            • almotriptan

              ergoloid mesylates, almotriptan. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Additive vasospasm. Sep. by 24h.

            • atazanavir

              atazanavir will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • clarithromycin

              clarithromycin will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • conivaptan

              conivaptan will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • darunavir

              darunavir will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • eletriptan

              ergoloid mesylates, eletriptan. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Additive vasospasm. Sep. by 24h.

            • elvitegravir/cobicistat/emtricitabine/tenofovir DF

              elvitegravir/cobicistat/emtricitabine/tenofovir DF increases levels of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Cobicistat is a CYP3A4 inhibitor; contraindicated with CYP3A4 substrates for which elevated plasma concentrations are associated with serious and/or life-threatening events.

            • frovatriptan

              ergoloid mesylates, frovatriptan. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Additive vasospasm. Sep. by 24h.

            • glyceryl trinitrate pr

              ergoloid mesylates decreases effects of glyceryl trinitrate pr by pharmacodynamic antagonism. Contraindicated.

            • indinavir

              indinavir will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • itraconazole

              itraconazole will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • ketoconazole

              ketoconazole will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • levoketoconazole

              levoketoconazole will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • lopinavir

              lopinavir will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • mifepristone

              mifepristone will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • naratriptan

              ergoloid mesylates, naratriptan. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Additive vasospasm. Sep. by 24h.

            • nitroglycerin IV

              ergoloid mesylates decreases effects of nitroglycerin IV by pharmacodynamic antagonism. Contraindicated.

            • nitroglycerin sublingual

              ergoloid mesylates decreases effects of nitroglycerin sublingual by pharmacodynamic antagonism. Contraindicated.

            • nitroglycerin topical

              ergoloid mesylates decreases effects of nitroglycerin topical by pharmacodynamic antagonism. Contraindicated.

            • nitroglycerin transdermal

              ergoloid mesylates decreases effects of nitroglycerin transdermal by pharmacodynamic antagonism. Contraindicated.

            • nitroglycerin translingual

              ergoloid mesylates decreases effects of nitroglycerin translingual by pharmacodynamic antagonism. Contraindicated.

            • posaconazole

              posaconazole will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • pseudoephedrine

              ergoloid mesylates increases effects of pseudoephedrine by pharmacodynamic synergism. Contraindicated. Ergot derivatives may enhance the vasoconstricting effect of pseudoephedrine and eventually significantly increasing blood pressure.

            • ritonavir

              ritonavir will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • rizatriptan

              ergoloid mesylates, rizatriptan. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Additive vasospasm. Sep. by 24h.

            • saquinavir

              saquinavir will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • sumatriptan

              ergoloid mesylates, sumatriptan. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Additive vasospasm. Sep. by 24h.

            • sumatriptan intranasal

              ergoloid mesylates, sumatriptan intranasal. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Additive vasospasm. Sep. by 24h.

            • tipranavir

              tipranavir will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • voriconazole

              voriconazole will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • zolmitriptan

              ergoloid mesylates, zolmitriptan. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Additive vasospasm. Sep. by 24h.

            Serious - Use Alternative (53)

            • abametapir

              abametapir will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

            • amyl nitrite

              amyl nitrite increases effects of ergoloid mesylates by decreasing metabolism. Avoid or Use Alternate Drug. Risk of increased SBP, angina pectoris.

            • apalutamide

              apalutamide will decrease the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.

            • atazanavir

              atazanavir increases levels of ergoloid mesylates by decreasing metabolism. Contraindicated.

            • benzphetamine

              ergoloid mesylates, benzphetamine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • bromocriptine

              ergoloid mesylates, bromocriptine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. The concomitant use of bromocriptine with ergot alkaloids may potentially lead to ergot toxicity; therefore the combination should be avoided.

            • clarithromycin

              clarithromycin increases levels of ergoloid mesylates by decreasing metabolism. Contraindicated.

            • darunavir

              darunavir increases levels of ergoloid mesylates by decreasing metabolism. Contraindicated.

            • dexfenfluramine

              dexfenfluramine, ergoloid mesylates. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Risk of serotonin syndrome.

              ergoloid mesylates, dexfenfluramine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • dexmethylphenidate

              ergoloid mesylates, dexmethylphenidate. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • dextroamphetamine

              ergoloid mesylates, dextroamphetamine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • diethylpropion

              ergoloid mesylates, diethylpropion. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • dobutamine

              ergoloid mesylates, dobutamine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • dopamine

              ergoloid mesylates, dopamine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • efavirenz

              efavirenz increases levels of ergoloid mesylates by decreasing metabolism. Avoid or Use Alternate Drug. Competitive inhibition of CYP3A4 might lead to vasospasm and ischemia.

            • ephedrine

              ergoloid mesylates, ephedrine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • epinephrine

              ergoloid mesylates, epinephrine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • fenfluramine

              fenfluramine, ergoloid mesylates. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Risk of serotonin syndrome.

              ergoloid mesylates, fenfluramine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • fexinidazole

              fexinidazole will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

            • fosamprenavir

              fosamprenavir increases levels of ergoloid mesylates by decreasing metabolism. Contraindicated.

            • glyceryl trinitrate pr

              glyceryl trinitrate pr increases effects of ergoloid mesylates by decreasing metabolism. Avoid or Use Alternate Drug. Risk of increased SBP, angina pectoris.

            • idelalisib

              idelalisib will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates

            • indinavir

              indinavir increases levels of ergoloid mesylates by decreasing metabolism. Contraindicated.

            • isoproterenol

              ergoloid mesylates, isoproterenol. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • isosorbide dinitrate

              isosorbide dinitrate increases effects of ergoloid mesylates by decreasing metabolism. Avoid or Use Alternate Drug. Risk of increased SBP, angina pectoris.

            • isosorbide mononitrate

              isosorbide mononitrate increases effects of ergoloid mesylates by decreasing metabolism. Avoid or Use Alternate Drug. Risk of increased SBP, angina pectoris.

            • ivosidenib

              ivosidenib will decrease the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternate therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.

            • lisdexamfetamine

              ergoloid mesylates, lisdexamfetamine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • methamphetamine

              ergoloid mesylates, methamphetamine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • methylenedioxymethamphetamine

              ergoloid mesylates, methylenedioxymethamphetamine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • methylphenidate

              ergoloid mesylates, methylphenidate. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • midodrine

              ergoloid mesylates, midodrine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • nicorandil

              nicorandil increases effects of ergoloid mesylates by decreasing metabolism. Avoid or Use Alternate Drug. Risk of increased SBP, angina pectoris.

            • nitroglycerin IV

              nitroglycerin IV increases effects of ergoloid mesylates by decreasing metabolism. Avoid or Use Alternate Drug. Risk of increased SBP, angina pectoris.

            • nitroglycerin PO

              nitroglycerin PO increases effects of ergoloid mesylates by decreasing metabolism. Avoid or Use Alternate Drug. Risk of increased SBP, angina pectoris.

            • nitroglycerin sublingual

              nitroglycerin sublingual increases effects of ergoloid mesylates by decreasing metabolism. Avoid or Use Alternate Drug. Risk of increased SBP, angina pectoris.

            • nitroglycerin topical

              nitroglycerin topical increases effects of ergoloid mesylates by decreasing metabolism. Avoid or Use Alternate Drug. Risk of increased SBP, angina pectoris.

            • nitroglycerin transdermal

              nitroglycerin transdermal increases effects of ergoloid mesylates by decreasing metabolism. Avoid or Use Alternate Drug. Risk of increased SBP, angina pectoris.

            • nitroglycerin translingual

              nitroglycerin translingual increases effects of ergoloid mesylates by decreasing metabolism. Avoid or Use Alternate Drug. Risk of increased SBP, angina pectoris.

            • norepinephrine

              ergoloid mesylates, norepinephrine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • phendimetrazine

              ergoloid mesylates, phendimetrazine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • phentermine

              ergoloid mesylates, phentermine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • phenylephrine

              ergoloid mesylates, phenylephrine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • phenylephrine PO

              ergoloid mesylates, phenylephrine PO. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • propylhexedrine

              ergoloid mesylates, propylhexedrine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • ritonavir

              ritonavir increases levels of ergoloid mesylates by decreasing metabolism. Contraindicated.

            • saquinavir

              saquinavir increases levels of ergoloid mesylates by decreasing metabolism. Contraindicated.

            • serdexmethylphenidate/dexmethylphenidate

              ergoloid mesylates, serdexmethylphenidate/dexmethylphenidate. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • tipranavir

              tipranavir increases levels of ergoloid mesylates by decreasing metabolism. Contraindicated.

            • tucatinib

              tucatinib will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

            • voxelotor

              voxelotor will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

            • xylometazoline

              ergoloid mesylates, xylometazoline. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            • yohimbine

              ergoloid mesylates, yohimbine. Mechanism: pharmacodynamic synergism. Contraindicated. Additive vasospasm; risk of hypertension.

            Monitor Closely (38)

            • aripiprazole

              ergoloid mesylates, aripiprazole. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • asenapine

              ergoloid mesylates, asenapine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • belzutifan

              belzutifan will decrease the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.

            • cariprazine

              ergoloid mesylates, cariprazine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • cenobamate

              cenobamate will decrease the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

            • clozapine

              ergoloid mesylates, clozapine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • crofelemer

              crofelemer increases levels of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Crofelemer has the potential to inhibit CYP3A4 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.

            • dabrafenib

              dabrafenib will decrease the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.

            • duvelisib

              duvelisib will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration with duvelisib increases AUC of a sensitive CYP3A4 substrate which may increase the risk of toxicities of these drugs. Consider reducing the dose of the sensitive CYP3A4 substrate and monitor for signs of toxicities of the coadministered sensitive CYP3A substrate.

            • elagolix

              elagolix will decrease the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered.

            • encorafenib

              encorafenib, ergoloid mesylates. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.

            • fedratinib

              fedratinib will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

            • fenfluramine

              ergoloid mesylates decreases effects of fenfluramine by pharmacodynamic antagonism. Use Caution/Monitor. Potent serotonin receptor antagonists may decrease fenfluramine efficacy. If coadministered, monitor appropriately.

            • fluphenazine

              ergoloid mesylates, fluphenazine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • haloperidol

              ergoloid mesylates, haloperidol. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • iloperidone

              iloperidone increases levels of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4.

              ergoloid mesylates, iloperidone. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • istradefylline

              istradefylline will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

            • loxapine

              ergoloid mesylates, loxapine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • loxapine inhaled

              ergoloid mesylates, loxapine inhaled. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • lurasidone

              ergoloid mesylates, lurasidone. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • minocycline

              minocycline, ergoloid mesylates. Either increases toxicity of the other by Mechanism: unknown. Use Caution/Monitor. coadministration of ergot alkaloids and tetracyclines increases risk of ergotism.

            • mitotane

              mitotane decreases levels of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.

            • molindone

              ergoloid mesylates, molindone. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • olanzapine

              ergoloid mesylates, olanzapine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • paliperidone

              ergoloid mesylates, paliperidone. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • perphenazine

              ergoloid mesylates, perphenazine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • pimavanserin

              ergoloid mesylates, pimavanserin. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • pimozide

              ergoloid mesylates, pimozide. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • quetiapine

              ergoloid mesylates, quetiapine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • ribociclib

              ribociclib will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • risperidone

              ergoloid mesylates, risperidone. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • rucaparib

              rucaparib will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.

            • stiripentol

              stiripentol, ergoloid mesylates. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.

            • tazemetostat

              tazemetostat will decrease the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tecovirimat

              tecovirimat will decrease the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.

            • thiothixene

              ergoloid mesylates, thiothixene. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • trifluoperazine

              ergoloid mesylates, trifluoperazine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • ziprasidone

              ergoloid mesylates, ziprasidone. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            Minor (4)

            • acetazolamide

              acetazolamide will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • anastrozole

              anastrozole will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • cyclophosphamide

              cyclophosphamide will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • larotrectinib

              larotrectinib will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

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            Adverse Effects

            Frequency Not Defined

            Flushing

            Headache

            Rash

            Nausea

            Vomiting

            Nasal congestion

            Blurred vision

            Bradycardia or bradyarrhythmia

            Orthostatic hypotension

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            Warnings

            Contraindications

            Hypersensitivity, psychosis; consider other CNS disease before starting

            CYP3A4 inhibitors (azole anifungals, protease inhibitors, macrolide antibiotics)

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            Pregnancy & Lactation

            Pregnancy Category: N/A

            Lactation: unknown

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Contains derivatives of three naturally occurring ergot alkaloids which have some peripheral alpha blocking activity and also depress CNS vasomotor nerve activity resulting in slight decrease in BP and HR; mechanism of action in dementia is largely unknown

            Pharmacokinetics

            Half-Life elimination: 3.5 hr

            Onset: 3-4 wk

            Peak Plasma Time: ~1 hr

            Concentration: 576 pg/mL

            Bioavailability: 9%

            Metabolism: Liver

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            Images

            No images available for this drug.
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            Patient Handout

            A Patient Handout is not currently available for this monograph.
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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.