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Lisuride: An 8-Alpha-Ergoline with Ergot Antagonistic Properties

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NeuroPsychopharmacotherapy

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Abstract

Lisuride (usually as hydrogen maleate) is the second oldest dopamine (DA) agonist in clinical use (after bromocriptine) and the most potent one.

Initially it has been registered by former Schering AG/West-Berlin/Germany as a peripheral serotonin (5-HT) antagonist for the prevention of migraine attacks, similar to methysergide, at effective oral dosages of 0.025 mg 3x/day.

Subsequently, at higher dosages it was found also to possess long-lasting prolactin (PRL)-lowering effects, and thus it has been approved for inhibition of post-partum lactation and treatment of mastitis, mastopathy, and hyperprolactinemic fertility disorders (anovulation, luteal insufficiency or amenorrhea without or with galactorrhea), which often are caused by micro- or macroprolactinomas of the anterior pituitary and also, rarely, a subgroup of acromegaly. During long-term treatment of these PRL-producing pituitary tumors, effects are becoming stronger with time, and it also was observed that treatment with lisuride could cause the majority of these tumors to shrink and, at least in some cases, to disappear completely.

Furthermore, as the prolactin-lowering effect was proof of dopaminergic activity, lisuride was also tested in Parkinson’s Disease (PD), where it also has shown good efficacy at very low oral dosages ranging from 0.6 to 2.4 mg/day especially when combined with levodopa.

On this basis, lisuride has been approved and until recently marketed as an oral prolactin-lowering and anti-PD drug in most European countries, but also in South-American and Asian countries. In view of a highly variable first-pass effect, parenteral forms (subcutaneous infusion, patch or patch pump) are preferred.

Much later, lisuride has also been found to be a most potent unsurmountable 5-HT2B antagonist and thus, to possess – in contrast to chemically related drugs such as pergolide and cabergoline, which cause fibrotic cardiac valvulopathies – strong anti-fibrotic effects to be investigated in a number of fibrotic conditions. For this reason, it is also expected to be effective in carcinoid syndrome.

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Authors and Affiliations

  1. Antaxios GmbH, Michendorf, Germany

    Reinhard Horowski

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  1. Reinhard Horowski
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Correspondence to Reinhard Horowski .

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Editors and Affiliations

  1. Dept Psychiatry , Psychosomatics & Psychotherapy, University of Würzburg, Medical School Clinical Neurochemistry, Würzburg, Germany

    Peter Riederer

  2. Inst für Psychologische Medizin, Haag, Bayern, Germany

    Gerd Laux

  3. Fujita Health University School Medicine, Toyoake, Aichi, Japan

    Toshiharu Nagatsu

  4. Center Translational Res Neurol Diseases, Dalian Med Uni Shanghai Inst Health Sc Center Translational Res Neurol Diseases, Dalian, China

    Weidong Le

  5. Würzburg, Bayern, Germany

    Christian Riederer

Section Editor information

  1. Center for Research Promotion and Support, Fujita Health University School of Medicine, Toyoake, Aichi, Japan

    Toshiharu Nagatsu

  2. Department of Physiological Chemistry, Fujita Health University School of Medicine, Toyoake, Aichi, Japan

    Akira Nakashima

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Horowski, R. (2021). Lisuride: An 8-Alpha-Ergoline with Ergot Antagonistic Properties. In: Riederer, P., Laux, G., Nagatsu, T., Le, W., Riederer, C. (eds) NeuroPsychopharmacotherapy. Springer, Cham. https://doi.org/10.1007/978-3-319-56015-1_287-1

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