Cabergoline

(BAN, USAN, rINN)
Cabergoline Chemical formula
Synonyms: Cabergolina; Cabergolinum; FCE-21336; Kabergoliini; Kabergolin; Kabergolina. 1-[(6-Allylergolin-8 ylamino)propyl]-3-ethylurea; (8R)-6-AllylN-[3-(dimethylamino)propyl]N-(ethylcarbamoyl)ergoline-8-carboxamide.
Cyrillic synonym: Каберголин.

💊 Chemical information

Chemical formula: C26H37N5O2 = 451.6.
CAS — 81409-90-7.
ATC — G02CB03; N04BC06.
ATC Vet — QG02CB03; QN04BC06.

Pharmacopoeias.

In Eur..

Ph. Eur. 6.2

(Cabergoline). A white or almost white, crystalline powder. It exhibits polymorphism. Practically insoluble in water; freely soluble in alcohol; very slightly soluble in n-hexane. It is slightly soluble in 0.1M hydrochloric acid. Protect from light.

💊 Adverse Effects and Precautions

1. European Multicentre Study Group for Cabergoline in Lactation Inhibition. Single dose cabergoline versus bromocriptine in inhibition of puerperal lactation: randomised, double blind, multicentre study. BMJ 1991; 302: 1367–71
2. Webster J. A comparative review of the tolerability profiles of dopamine agonists in the treatment of hyperprolactinaemia and inhibition of lactation. Drug Safety 1996; 14: 228–38. Correction. ibid.; 342.

Parkinsonism.

Cabergoline is used as a long-acting dopamine agonist in Parkinson’s disease. Dopamine agonists are often used to begin treatment in an attempt to delay therapy with levodopa, particularly in younger patients. They also have an adjunctive use when levodopa is no longer effective alone or cannot be tolerated, and may sometimes be useful in reducing ‘off’ periods with levodopa and in ameliorating other fluctuations of mobility in the later stages of the disease.
1. Inzelberg R, et al. Double-blind comparison of cabergoline and bromocriptine in Parkinson’s disease patients with motor fluctuations. Neurology 1996; 47: 785–8
2. Geminiani G, et al. Cabergoline in Parkinson’s disease complicated by motor fluctuations. Mov Disord 1996; 11: 495–500
3. Hutton JT, et al. Multicenter, placebo-controlled trial of cabergoline taken once daily in the treatment of Parkinson’s disease. Neurology 1996; 46: 1062–5
4. Marsden CD. Clinical experience with cabergoline in patients with advanced Parkinson’s disease treated with levodopa. Drugs 1998; 55 (suppl 1): 17–22
5. Rinne UK, et al. Early treatment of Parkinson’s disease with cabergoline delays the onset of motor complications: results of a double-blind levodopa controlled trial. Drugs 1998; 55 (suppl 1): 23–30
6. Clarke CE, Deane KHO. Cabergoline for levodopa-induced complications in Parkinson’s disease. Available in The Cochrane Database of Systematic Reviews; Issu
1. Chichester: John Wiley; 2001 (accessed 16/02/06)
7. Clarke CE, Deane KHO. Cabergoline versus bromocriptine for levodopa-induced complications in Parkinson’s disease. Available in The Cochrane Database of Systematic Reviews; Issu
1. Chichester: John Wiley; 2001 (accessed 16/02/06)
8. Bracco F, et al. The long-acting dopamine receptor agonist cabergoline in early Parkinson’s disease: final results of a 5-year, double-blind, levodopa-controlled study. CNS Drugs 2004; 18: 733–46. Correction. ibid. 2005; 19: 633
9. Curran MP, Perry CM. Cabergoline: a review of its use in the treatment of Parkinson’s disease. Drugs 2004; 64: 2125–41
10. Odin P, et al. Efficacy and safety of high-dose cabergoline in Parkinson’s disease. Acta Neurol Scand 2006; 113: 18–24.

Restless legs syndrome.

The aetiology of restless legs syndrome is obscure and treatment has been largely empirical but dopaminergic therapy has emerged as a common first-line choice. Long-acting drugs such as cabergoline may be preferred in order to avoid the complications associated with levodopa therapy. Results from a 12-week open-label pilot study1 in 9 patients with idiopathic RLS given cabergoline after insufficient response to levodopa therapy were promising; doses of cabergoline ranged from 1 to 4 mg. A later randomised multicentre study2 in 85 patients concluded that a single evening dose of cabergoline for 5 weeks markedly reduced symptoms during the night and the next day compared with placebo. Results from the follow-up analysis of 66 patients after 1 year of treatment suggested that cabergoline at a median dose of 2 mg daily has a high rate of remission and is well tolerated. The authors recommended an initial dose of cabergoline 500 micrograms in the evening increased in increments of 500 micrograms weekly according to response.
1. Stiasny K, et al. Treatment of idiopathic restless legs syndrome (RLS) with the D2-agonist cabergoline—an open clinical trial. Sleep 2000; 23: 349–54
2. Stiasny-Kolster K, et al. Effective cabergoline treatment in idiopathic restless legs syndrome. Neurology 2004; 63: 2272–9.

💊 Preparations

Proprietary Preparations

Arg.: Cabaser; Caberpar; Cieldom; Dostinex; Lac Stop; Lactamax; Triaspar; Austral.: Cabaser; Dostinex; Austria: Cabaseril; Dostinex; Belg.: Dostinex; Sostilar; Braz.: Dostinex; Canad.: Dostinex; Chile: Dostinex; Cz.: Cabera; Dostinex; Denm.: Cabaser; Dostinex; Fin.: Cabaser; Dostinex; Fr.: Dostinex; Ger.: Cabaseril; Dostinex; Gr.: Dostinex; Hong Kong: Dostinex; India: Caberlin; Camforte†; Irl.: Cabaser; Dostinex; Israel: Cabaser; Dostinex; Ital.: Actualene; Cabaser; Dostinex; Malaysia: Dostinex; Mex.: Dostinex; Neth.: Dostinex; Norw.: Cabaser; Dostinex; NZ: Dostinex; Pol.: Dostinex; Port.: Dostinex; Rus.: Dostinex (Достинекс); S.Afr.: Dostinex; Singapore: Dostinex; Spain: Dostinex; Sogilen; Swed.: Cabaser; Dostinex; Switz.: Cabaser; Dostinex; Turk.: Cabaser; Dostinex; UK: Cabaser; Dostinex; USA: Dostinex†; Venez.: Dostinex.
Published October 31, 2018.