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Uses and Administration
Lisuride maleate, an ergot derivative, is a dopamine D2-agonist with actions and uses similar to those of bromocriptine (Refer to). It is also reported to have serotonergic activity. It is used similarly in the management of Parkinson's disease ( Refer to ) and has been used in disorders associated with hyperprolactinaemia ( Refer to ), including amenorrhoea, galactorrhoea, and infertility. It is also used to suppress puerperal lactation for medical reasons; it is not recommended for the routine suppression of physiological lactation or for the treatment of postpartum breast pain and engorgement that can be adequately relieved with simple analgesics and breast support. Lisuride has been used in some countries for the treatment of acromegaly, and for the prophylaxis of migraine. It is normally given orally; doses should be taken with food.
In the management of Parkinson's disease, lisuride maleate has been added to treatment with levodopa or other antiparkinsonian drugs. Initially 100 micrograms is taken at bedtime and additional doses of 100 micrograms may be added, at intervals of one week, first in the morning and then at midday. Further increases are made, until an optimum response is obtained, by adding 100 micrograms each week using the same sequence of increases, starting with the bedtime dose; dosage should not normally exceed 2 mg daily given in 3 or 4 divided doses.
When used to suppress lactation, the usual dose of lisuride maleate is 200 micrograms two or three times daily for 14 days; treatment should be started within the first 24 hours of delivery.
In the treatment of disorders associated withhyperprolactinaemia, 100 micrograms of lisuride maleate may be given in the evening of the first day, followed by 100 micrograms at midday and in the evening of the second day, and 100 micrograms in the morning, at midday, and in the evening of the third day; thereafter doses may be adjusted according to prolactin levels. Similar doses are also used in acromegaly with adjustments made according to growth hormone levels (see also Refer to ).
(last reviewed 2010-09-02; last modified 2010-05-15)
Acromegaly
Dopaminergics can produce a paradoxical reduction in growth hormone secretion and may be used in the treatment of acromegaly as adjunctive therapy to surgery, radiotherapy, or somatostatin analogues to reduce circulating growth hormone levels, although they are less effective than somatostatin analogues ( Refer to ). While bromocriptine and cabergoline have been the main dopamine agonists used, lisuride has been used in some countries.
(last reviewed 2010-09-02; last modified 2011-10-24)
Hyperprolactinaemia and prolactinomas
Dopamine agonists have been widely used for the treatment of hyperprolactinaemia secondary to a prolactinoma ( Refer to ). Lisuride has been used as an alternative to bromocriptine. There is a report of plasma-prolactin concentrations being reduced to normal in 4 female patients with macroprolactinomas given lisuride 400 to 800 micrograms daily for 2 years.1 Subsequent dosage reduction in 3 was followed by a rise in prolactin values. In the fourth patient prolactin remained in the normal range when the dose was progressively reduced from 400 to 50 micrograms daily, although complete withdrawal was followed by an increase in prolactin concentration within 3 months.
Vaginal dosage of lisuride has been studied in an attempt to avoid adverse effects associated with oral therapy. In a study2 involving 40 women with hyperprolactinaemia a 200-microgram standard oral tablet placed in the vagina at night produced a similar reduction in prolactin concentrations to that obtained with 400 micrograms taken orally and was better tolerated.
(last reviewed 2010-09-02; last modified 2010-08-27)
References
1. Liuzzi A, et al.. Low doses of dopamine agonists in the long-term treatment of macroprolactinomas.N Engl J Med. 1985; 313: 656–9. PubMed
2. Tasdemir M, et al.. Vaginal lisuride for hyperprolactinaemia.Lancet. 1995; 346: 1362. PubMed
Lactation inhibition
Lisuride is used in some countries for the prevention of puerperal lactation ( Refer to ). However, the routine use of dopaminergics is not recommended for the suppression of physiological lactation.
References.
(last reviewed 2010-09-02; last modified 2006-12-06)
References
1. Venturini PL, et al.. Effects of lisuride and bromocriptine on inhibition of lactation and on serum prolactin levels: comparative double-blind study.Eur J Obstet Gynecol Reprod Biol. 1981; 11: 395–400. PubMed
Mastalgia
In a small placebo-controlled study,1 lisuride 200 micrograms daily was effective in the treatment of cyclical mastalgia. However, since mastalgia ( Refer to ) can improve spontaneously, treatment should rarely be considered unless pain has been present for about 6 months.
(last reviewed 2010-09-02; last modified 2008-08-26)
References
1. Kaleli S, et al.. Symptomatic treatment of premenstrual mastalgia in premenopausal women with lisuride maleate: a double-blind placebo-controlled randomized study.Fertil Steril. 2001; 75: 718–23. PubMed
Migraine
Although lisuride has been used in some countries for the prophylaxis of migraine ( Refer to ) it is not usually considered to be the drug of choice or even one of the main alternatives.
(last reviewed 2010-09-02; last modified 2006-01-13)
Parkinsonism
While some neurologists use dopamine agonists such as lisuride early in the treatment of parkinsonism ( Refer to ) in an attempt to delay therapy with levodopa, others reserve them for adjunctive use when levodopa is no longer effective alone or cannot be tolerated. They are sometimes useful in reducing 'off' periods with levodopa and in ameliorating other fluctuations in mobility in the later stages of the disease.
References.
(last reviewed 2010-09-02; last modified 2010-08-27)
References
1. Rinne UK. Lisuride, a dopamine agonist in the treatment of early Parkinson's disease.Neurology. 1989; 39: 336–9. PubMed
2. Clarke CE, Speller J. Lisuride for levodopa-induced complications in Parkinson's disease. Available in The Cochrane Database of Systematic Reviews; Issue 1. Chichester: John Wiley; 1999 (accessed 16/02/06). PubMed
3. Clarke CE, et al.. Lisuride versus bromocriptine for levodopa-induced complications in Parkinson's disease. Available in The Cochrane Database of Systematic Reviews; Issue 1. Chichester: John Wiley; 1999 (accessed 16/02/06). PubMed
4. Allain H, et al.. Five-year follow-up of early lisuride and levodopa combination therapy versus levodopa monotherapy in de novo Parkinson's disease.Eur Neurol. 2000; 44: 22–30. PubMed
Administration
Lisuride has been of benefit when given by continuous intravenous or subcutaneous infusion in patients having fluctuations in mobility with levodopa therapy1-4 but severe psychiatric effects have been associated with the use of these routes.3Transdermal lisuride has also been investigated for the treatment of Parkinson's disease and restless legs syndrome.5,6
(last reviewed 2010-09-02; last modified 2010-08-27)
References
1. Obeso JA, et al.. Intravenous lisuride corrects oscillations of motor performance in Parkinson's disease.Ann Neurol. 1986; 19: 31–5. PubMed
2. Obeso JA, et al.. Lisuride infusion pump: a device for the treatment of motor fluctuations in Parkinson's disease.Lancet. 1986; i: 467–70. PubMed
3. Critchley P, et al.. Psychosis and the lisuride pump.Lancet. 1986; i: 349. PubMed
4. Stocchi F, et al.. Prospective randomized trial of lisuride infusion versus oral levodopa in patients with Parkinson's disease.Brain. 2002; 125: 2058–66. PubMed
5. Woitalla D, et al.. Transdermal lisuride delivery in the treatment of Parkinson's disease.J Neural Transm Suppl. 2004; 68: 89–95. PubMed
6. Benes H. Transdermal lisuride: short-term efficacy and tolerability study in patients with severe restless legs syndrome.Sleep Med. 2006; 7: 31–5. PubMed
Adverse Effects, Treatment and Precautions
Adverse Effects and Precautions
As for Bromocriptine, Refer to . Infusion of lisuride in parkinsonian patients has been associated with severe psychiatric adverse effects.
(last reviewed 2010-09-02; last modified 2004-03-30)
Effects on mental function
For reports of daytime somnolence occurring in patients receiving dopamine agonists including lisuride, see under Levodopa, Refer to .
For reference to disturbed behaviour includingexcessive gambling reported in patients with Parkinson's disease receiving dopamine agonists, see under Levodopa, Refer to .
For reference to dopamine dysregulation syndrome reported in patients with Parkinson's disease receiving dopamine agonists, see Abuse, under Precautions of Levodopa, Refer to .
(last reviewed 2010-09-02; last modified 2018-11-08)
Fibrosis
For reports of fibrotic reactions occurring in patients with Parkinson's disease receiving ergot derivative dopamine agonists including lisuride, see under Adverse Effects of Bromocriptine, Refer to .
(last reviewed 2010-09-02; last modified 2008-08-26)
Interactions
As for Bromocriptine, Refer to .
(last reviewed 2010-09-02; last modified 1998-08-24)
Pharmacokinetics
Plasma concentrations varied widely after a single oral dose of lisuride maleate 300 micrograms in 11 patients with Parkinson's disease.1 Absorption was rapid and the mean plasma elimination half-life was 2.2 hours. Only a mean of 0.05% of the dose was excreted unchanged in the urine in 24 hours. The mean oral bioavailability of lisuride maleate has been reported2 to be 10% after a 100-microgram dose and 22% after a 300-microgram dose.
A single dose of lisuride 25 micrograms given by intravenous, intramuscular, or subcutaneous injection reduced plasma-prolactin concentrations by up to 60% in 11 of 12 healthy subjects, the effect lasting for about 10 hours.3 Plasma-lisuride concentrations after intravenous injection fell in 2 phases with half-lives of 14 minutes and 1.5 hours, respectively. Peak plasma concentrations after subcutaneous and intramuscular injection were obtained after 12 and 15 minutes, respectively.
(last reviewed 2010-09-02; last modified 2010-08-27)
References
1. Burns RS, et al.. Disposition of oral lisuride in Parkinson's disease.Clin Pharmacol Ther. 1984; 35: 548–56. PubMed
2. Hümpel M, et al.. Radioimmunoassay of plasma lisuride in man following intravenous and oral administration of lisuride hydrogen maleate; effect on plasma prolactin level.Eur J Clin Pharmacol. 1981; 20: 47–51. PubMed
3. Krause W, et al.. The pharmacokinetics and pharmacodynamics of lisuride in healthy volunteers after intravenous, intramuscular, and subcutaneous injection.Eur J Clin Pharmacol. 1991; 40: 399–403. PubMed
Preparations: Single-Ingredient
The following preparations list represents a compilation of all available salt forms or related substances for this drug product.
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.
ARGENTINA: Dopagon¤;AUSTRIA: Dopergin¤; Prolacam¤;BELGIUM: Dopergine¤;BRAZIL: Dopergin¤;FRANCE: Arolac; Dopergine¤;GERMANY: Cuvalit¤; Dopergin¤;GREECE: Dipergon¤;ISRAEL: Dopergin¤;ITALY: Cuvalit¤; Dopergin;MEXICO: Dopergin;NETHERLANDS: Dopergin¤;NEW ZEALAND: Dopergin;SPAIN: Dopergin¤;SWITZERLAND: Dopergin¤;THAILAND: Dopergin¤;TURKEY: Dopergin;UNITED KINGDOM: Revanil¤;
Therapeutic Use
- Antiparkinsonian Drugs
Last Updated 1/21/20
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