Lisuride

Lisuride
Clinical data
Trade namesDopergin, others
Other namesLysuride; Mesorgydin; Methylergol carbamide
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral[1]
Investigational: Subcutaneous implant, transdermal patch[1]
ATC code
Legal status
Legal status
  • BR: Class C1 (Other controlled substances)[2]
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability10–20%[3]
Protein binding60–70%[3]
MetabolismHepatic
MetabolitesMore than 15 known[3]
Elimination half-life2 hours[3]
ExcretionRenal and biliary in equal amounts
Identifiers
  • 1,1-Diethyl-3-(7-methyl-4,6,6a,7,8,9-hexahydro-indolo[4,3-fg]quinolin-9-yl)-urea
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.038.099 Edit this at Wikidata
Chemical and physical data
FormulaC20H26N4O
Molar mass338.455 g·mol−1
3D model (JSmol)
  • [H][C@@]12Cc3c[nH]c4cccc(C1=C[C@H](NC(=O)N(CC)CC)CN2C)c34
  • InChI=1S/C20H26N4O/c1-4-24(5-2)20(25)22-14-10-16-15-7-6-8-17-19(15)13(11-21-17)9-18(16)23(3)12-14/h6-8,10-11,14,18,21H,4-5,9,12H2,1-3H3,(H,22,25)/t14-,18+/m0/s1 checkY
  • Key:BKRGVLQUQGGVSM-KBXCAEBGSA-N checkY
  (verify)

Lisuride, sold under the brand name Dopergin among others, is a monoaminergic medication of the ergoline class which is used in the treatment of Parkinson's disease, migraine, and high prolactin levels.[1] It is taken by mouth.[1]

Side effects of lisuride include nausea and vomiting, dizziness, headache, fatigue or drowsiness, insomnia or sleep, gastrointestinal disturbances such as abdominal pain or diarrhea, nasal congestion or runny nose, and hypotension, hallucinations or confusion (particularly at higher doses). Rarely, serious side effects such as cardiac or pulmonary fibrosis have been reported with long-term use, but they are extremely uncommon.[3]

Lisuride acts as a mixed agonist and antagonist of dopamine, serotonin, and adrenergic receptors.[1][4][5][6] Activation of specific dopamine receptors is thought to be responsible for its effectiveness in the treatment of Parkinson's disease and ability to suppress prolactin levels,[1] while interactions with serotonin receptors are thought to be principally involved in its effectiveness for migraine.[7][8]

  1. ^ a b c d e f Horowski R, Löschmann PA (April 2019). "Classical dopamine agonists". Journal of Neural Transmission. 126 (4): 449–454. doi:10.1007/s00702-019-01989-y. PMID 30805732. S2CID 71144049.
  2. ^ Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
  3. ^ a b c d e Cite error: The named reference MoveDisord2002 was invoked but never defined (see the help page).
  4. ^ Cite error: The named reference pmid12388666 was invoked but never defined (see the help page).
  5. ^ Cite error: The named reference pmid12388667 was invoked but never defined (see the help page).
  6. ^ Cite error: The named reference pmid12388668 was invoked but never defined (see the help page).
  7. ^ Ramírez Rosas MB, Labruijere S, Villalón CM, Maassen Vandenbrink A (August 2013). "Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs". Expert Opinion on Pharmacotherapy. 14 (12): 1599–1610. doi:10.1517/14656566.2013.806487. PMID 23815106. S2CID 22721405.
  8. ^ Villalón CM, VanDenBrink AM (2017). "The Role of 5-Hydroxytryptamine in the Pathophysiology of Migraine and its Relevance to the Design of Novel Treatments". Mini Reviews in Medicinal Chemistry. 17 (11): 928–938. doi:10.2174/1389557516666160728121050. PMID 27465216.