Abstract
We studied the effects of the new non-ergot D2-dopamine agonist roxindol for the treatment of human prolactinomas. Roxindol is a non-ergot drug with additional 5-hydroxytryptamine type 1 A agonist and serotonin reuptake inhibitory activity. Ten patients with prolactin-secreting pituitary adenomas received roxindol three times daily at a dosage of 7.5–30 mg/day for at least 4 weeks according to a prospective protocol. All patients but one had received oral bromocriptine previously without normalization of prolactin levels. Serum prolactin profiles were analyzed once a week during the first month of therapy and at 4-week intervals thereafter. Mean baseline serum prolactin was suppressed from 23000±13 600 mU/1 (range 1500–141000 mU/1; 20 mU/l=1 μg/1) by 37 ± 11 % after 1 week, by 49±9% after 4 weeks, and by 65±11% (n = 8) after 24 weeks of treatment. Serum prolactin was normalized in two patients. A tumor volume reduction of 20–25% was obtained in two subjects. Compared with previous treatment with oral bromocriptine the decrease in serum prolactin was comparable. In contrast, tolerance of roxindol was superior in five of seven patients with major side effects with bromocriptine, including three subjects who had discontinued bromocriptine because of adverse reactions. Four subjects spontaneously reported improvement of psychological and physical performance. One patient had a transient increase of serum transaminases. Thus, for the first time we could show a suppressive effect of roxindol on prolactin secretion in human prolactinomas. Due to its good tolerance roxindol may provide a useful alternative to bromocriptine.
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Abbreviations
- MRI:
-
magnetic resonance imaging
- PRL:
-
prolactin
References
Besser GM, Parke L, Edwards CRW, Forsyth IA, McNeilly AS (1972) Galactorrhoea: successful treatment with reduction of plasma prolactin levels by brom-ergocryptine. Br Med J 3:669–672
Chiodini PG, Liuzzi A, Cozzi R, Verde G, Oppizzi G, Dallabonzana D, Spelta B, Silvestrini F, Borghi G, Luccarelli G, Rainer E, Horowski R (1981) Side reduction of macroprolactinomas by bromocriptine or lisurid treatment. J Clin Endocrinol Metab 53:737–743
Ciccarelli M, Mazza E, Ghigo E, Guidoni F, Barberis A, Massara F, Camani F (1987) Long term treatment with oral single administration of bromocriptine in patients with hyperprolactinaemia. J Endocrinol Invest 10:51–53
Ciccarelli E, Cammani F, Miola C, Besser GM, Avantaneo T, Grossman A (1989) A long-term treatment with a new repeatable injectable form of bromocriptine, Parlodel LAR, in patients with tumorous hyperprolactinaemia. Fertil Steril 52:930–935
Ciccarelli E, Giusti M, Miola C, Potenzoni F, Sghedoni D, Camanni F, Giordano G (1989) Effectiveness and tolerability of long term treatment with carbergoline, a new long-lasting ergoline derivative, in hyperprolactinemic patients. J Clin Endocrinol Metab 69:725–743
Crosignani PG, Ferrari C, Liuzzi A, Benco R, Mattei A, Rampini P, Dallabonzana D, Scarduelli C, Spelta B (1982) Treatment of hyperprolactinemic states with different drugs: a study with bromocriptine, metergoline and lisuride. Fertil Steril 37:61–67
Dallabonzana D, Liuzzi A, Oppizzi G, Cozzi R, Verde G, Chiodini P, Reiner E, Dorow R, Horowski R (1986) Chronic treatment of pathological hyperprolactinemia and acromegaly with the new ergot derivative terguride. J Clin Endocrinol Metab 63:1002–1007
Ferrari C, Barbieri C, Caldara R, Mucci M, Codedasa F, Parachi A, Romano C, Boghen M, Dubini A (1986) Long-lasting prolactin-lowering effect of carbergoline, a new dopamine agonist, in hyperprolactinemic patients. J Clin Endocrinol Metab 63:941–945
Grossman A, Bouloux PMG, Loneragan R, Rees LH, Wass JAH, Besser GM (1985) Comparison of the clinical activity of mesulergine and pergolide in the treatment of hyperprolactinaemia. Clin Endocrinol 22:611–616
Haase R, Jaspers C, Schulte HM, Lancranjan I, Pfingsten H, Orri-Fend M, Reinwein D, Benker G (1993) Control of prolactin-secreting macroadenomas with parenteral, long-acting bromocriptine in 30 patients treated for up to 3 years. Clin Endocrinol 32:565–571
Khalfallah Y, Claustrat B, Grochowicki M, Flocard F, Horlait S, Serusclat P, Sassolas G (1990) Effects of a new prolactin inhibitor, CV 205–502, in the treatment of human macroprolactinomas. J Clin Endocrinol Metab 71:354–359
Lamberts SWJ, Quik RFP (1991) A comparison of the efficacy and safety of pergolide and bromocriptine in the treatment of hyperprolactinemia. J Clin Endocrinol Metab 72:635–641
Molitch HE, Elton RL, Blackwell RE, Caldwell B, Chang RJ, Jaffe R, Joplin G, Robbins RJ, Tyson J, Thorner MO and the Bromocriptine Study Group (1985) Bromocriptine as a primary treatment of prolactin-secreting macroadenomas: results of a prospective multicenter study. J Clin Endocrinol Metab 60:698–705
Pellegrini I, Rasolonjanahary R, Gunz G, Bertrand P, Delivet S, Jedynak CP, Kordon C, Peillon F, Jaquet P, Enjalbert A (1989) Resistance to bromocriptine in prolactinomas. J Clin Endocrinol Metab 69:500–509
Seyfried CA, Greiner HE, Haase AF (1989) Biochemical and functional studies on EMD 49980: a potent, selectively presynaptic D-2 dopamine agonist with actions on serotonin systems. Eur J Pharmacol 160:31–41
Vance ML, Evans WS, Thorner MO (1984) Drugs five years later: bromocriptine. Ann Intern Med 10:78–91
Van der Lely AJ, Brownnell J, Lamberts SWJ (1991) The efficacy and tolerability of CV 205–502, a nonergot dopaminergic drug, in macroprolactinoma patients and in prolactinoma patients intolerant to bromocriptine. J Clin Endocrinol Metab 72:1136–1141
Van't Verlaat JW, Lancranjan I, Hendriks MJ, Croughs RJM (1988) Primary treatment of macroprolactinomas with Parlodel LAR. Acta Endocrinol 119:51–55
Verhelst JA, Froud LA, Touzel R, Wass JAH, Besser GM, Grossman AB (1991) Acute and long-term effects of once-daily oral bromocriptine and a new long-acting non-ergot dopamine agonist, quinagolide, in the treatment of hyperprolactinemia: a double-blind study. Acta Endocrinol 125:385–391
Wass JAH, Williams J, Charlesworth M, Kingsley DPE, Halliday AM, Doniach I, Rees LH, McDonald WI, Besser GM (1982) Bromocriptine in the management of large pituitary tumours. Br Med J 284:1908–1911
Webster J, Piscitelli G, Polli A, D'Alberton A, Falsetti L, Ferrari C, Fioretti P, Giordano G, L'Hermite M, Ciccarelli E, Crosigani PG, DeCecco L, Fadini R, Faglia G, Flamigni F, Tamburrano G, Scanlon MF (1992) Dose-dependent suppression of serum prolactin by carbergoline in hyperprolactinaemia: a placebo controlled, double blind, multicenter study. Clin Endocrinol 37:534–541
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Jaspers, C., Benker, G. & Reinwein, D. Treatment of prolactinoma patients with the new non-ergot dopamine agonist roxindol: first results. Clin Investig 72, 451–456 (1994). https://doi.org/10.1007/BF00180520
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DOI: https://doi.org/10.1007/BF00180520