Summary
The plasma concentration of lisuride and prolactin have been measured in twelve healthy male volunteers after IV, IM or SC injection of 25 μg lisuride hydrogen maleate as an aqueous solution.
After IV administration the plasma lisuride fell in two phases with half-lives of 14 min and 1.5 h. Total clearance was 13 ml·min−1·kg−1. After IM and SC injection the plasma concentrations peaked at 12 to 15 min and the profiles were similar to that found after IV administration. The systemic availabilities were 90% and 94%, respectively. Prolactin concentrations were reduced by a maximum of 60% relative to the normal circadian rhythm after all three routes of administration.
The treatments were well tolerated, the only adverse reactions reported by some of the volunteers being mild, transient dizziness, tiredness, and nausea.
Similar content being viewed by others
References
Horowski R (1976) Direct dopaminergic action of lisuride hydrogen maleate, an ergot derivative, in mice. Eur J Pharmacol 36: 373–383
Kehr W (1977) Effect of lisuride and other ergot derivatives on monoaminergic mechanisms in rat brain. Eur J Pharmacol 41: 261–273
Rogawski M, Aghajanian G (1978) Response of central monoaminergic neurons to lisuride: Comparison with LSD. Life Sci 22: 1615–1622
Battaglia G, Titeler M (1981) Direct binding of 3H-lisuride to adrenergic and serotonergic receptors. Life Sci 29: 909–916
Dorow R, Breitkopf M, Gräf KG, Korowski R (1983) Neuroendocrine effects of lisuride and its 9, 10-dihydrogenated analog in healthy volunteers, in Calne DB, Horowski R, McDonald RJ, Wuttke W (eds.). Lisuride and other dopamine agonists. Raven Press, New York
Liuzzi A, Chiodini P, Oppizzi G, Botalla L, Verde G, de Stefano L, Colussi G, Graf KJ, Horowski R (1978) Lisuride hydrogen maleate: Evidence for a long lasting dopaminergic activity in humans. J Endocrinol Metabol 46: 196–202
Bohnet HG, Hanker JP, Horowski R, Wiekings E, Schneider HPG (1979) Suppression of prolactin secretion by lisuride throughout the menstrual cycle and in hyperprolactinemic menstrual disorder. Acta Endocrinol 92: 8–19
Somerville BW, Herrmann WM (1976) Migraine prophylaxis with lisuride — A double blind study of lisuride versus placebo. Headache 16: 85–86
Verde G, Chiodini PG, Liuzzi A, Cozzi R, Fauales F, Batalla L, Spalta B, Valla Botanna D, Rainer E, Horowski R (1980) Effectiveness of the dopamine agonist lisuride in the treatment of acromegaly and pathological hyperprolactinemic states. J Endocrinol Invest 4: 405–414
Verde G (1979) Lisuride in acromegaly and pathological hyper-prolactinemia. Acta Endocrinol 91: 225
McDonald RJ, Horowski R (1983) Lisuride in the treatment of parkinsonism. Eur Neurol 22: 240–255
Hümpel M, Nieuweboer B, Hasan SH, Wendt H (1981) Radioimmunoassay of plasma lisuride in man following intravenous and oral administration of lisuride hydrogen maleate; effect on plasma prolactin level. Eur J Clin Pharmacol 20: 47–51
Hümpel M, Krause W, Hoyer GA, Wendt H, Pommerenke G (1984) The pharmacokinetics and biotransformation of 14C-lisuride hydrogen maleate in rhesus monkey and in man. Eur J Drug Metabol Pharmacokinet 9: 347–357
Luquin MR, Obeso JA, Martinez-Lage JM, Tresguerres J, Parada J, Nieuweboer B, Dorow R, Horowski R (1986) Parenteral administration of lisuride in Parkinson's disease. Yahr MD, Bergmann KJ (eds), In. Advances in Neurology, Vol 45, Raven Press, New York, pp 561–568
Kerr DJ, Singh VK, McConway MG, Beastall GH, Connell JM, Alexander WD, Davies DL (1987) Circadian variation of thyrotrophin determined by ultrasensitive immunoradiometric assay and the effect of low dose nocturnal dopamine infusion. Clin Sci 72: 737–741
Leblanc H, Lachelin GC, Abu Fadil S, Yen SS (1976) Effects of dopamine infusion on pituitary hormone secretion in humans. J Clin Endocrinol Metabol 43: 668–674
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Krause, W., Mager, T., Kühne, G. et al. The pharmacokinetics and pharmacodynamics of lisuride in healthy volunteers after intravenous, intramuscular, and subcutaneous injection. Eur J Clin Pharmacol 40, 399–403 (1991). https://doi.org/10.1007/BF00265851
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00265851