Lisuride

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Genes that may be involved
  • Substrate of
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics

Brand Names

Europe

Austria: Dopergin; France: Arolac, Dopergine; Germany: Dopergin; Greece: Dipergon; Italy: Dopergin; Poland: Lysenyl; Spain: Dopergin.

Latin America

Mexico: Dopergin.

Drug combinations

Chemistry

Lisuride: C~20~H~26~N~4~O. Mw: 338.45. 3-(9,10-Didehydro-6-methylergolin-8α-yl)-1,1-diethylurea. CAS-18016-80-3.

Pharmacologic Category

Antiparkinsonian Agents; Ergot-derivative Dopamine Receptor Agonists. Antimigraine Agents, Miscellaneous. (ATC-Code: G02CB02; N02CA07).

Mechanism of action

Displays dopaminergic, and consequently prolactin-reducing properties. Active substance lisuride has pronounced affinity for dopamine receptors in striatum and pituitary.

Therapeutic use

Parkinson’s disease, postencephalitic parkinsonism, parkinsonism of other origin (except medicine-induced form). Prevention of onset of lactation in puerperium (primary ablactation) only for clearly defined medical reasons. Galactorrhea, prolactin-induced amenorrhea, prolactin-induced infertility in women, prolactinomas, acromegaly.

Pregnancy and lactiation implications

Do not use during pregnancy. If cessation of milk production is desired, breast-feeding must be discontinued. In all other circumstances lisuride must not be used in breast-feeding mothers.

Unlabeled use

Contraindications

Hypersensitivity to lisuride and other ergot derivatives.

Warnings and precautions

In patients with past or present psychoses, deterioration or recurrence of symptoms is possible (must be considered very carefully in severe disorders of arterial circulation in periphery and heart (coronary failure)). High blood pressure, MI, convulsive fits and stroke (known symptoms of postpartum cerebral angiopathy) observed in rare cases in association with use of ergot-derived dopamine agonists as lactation inhibitor in puerperal period. Although no causal association between treatment and these events -which also occur spontaneously in puerperal period- has been confirmed, treatment should be discontinued immediately, as a precaution, on the occurrence of high blood pressure, persistent headache or other signs of disturbance of CNS in women taking lisuride for ablactation. Before starting treatment of hyperprolactinemia with lusiride, cause of disorder must be clarified (e.g. medicines, hypothyroidism). Of particular importance is the question of whether there is an invasive, large adenoma of the pituitary gland. In the case of visual field defects or if the sella is significantly enlarged, either surgery or lisuride treatment alone can be applied. Pathological gambling, increased libido and hypersexuality reported in patients treated with dopamine agonists for Parkinson’s disease, including lisuride. Persons with impaired renal function, especially dialysis patients, are particularly sensitive to dopamine agonists. Use with caution in severe disturbances of liver function (lisuride is almost completely metabolized in liver). If pregnancy occurs in women with pituitary adenoma (prolactinoma), signs of renewed tumor growth (severe and sustained headaches, disturbed vision), must be very closely observed by adequate diagnostic measures. Development of cardiac fibrosis, pulmonary fibrosis, pleural fibrosis, pleural effusion or retroperitoneal fibrosis observed in isolated cases after long-term use of ergot-type dopamine agonists, including lisuride. Shortness of breath, persistent urge to cough or disturbances of kidney function occurring under treatment with lisuride must be clarified by appropriate diagnostic procedures; if necessary lisuride should be withdrawn.

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