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 Quinagolide hydrochloride

Deacription of Quinagolide: Quinagolide (Norprolac) is a selective, D2 receptor agonist that is used for the treatment of elevated levels of prolactin. Quinagolide (Norprolac) was approved in European Community, but not in USA as of December, 2011.  Quinagolide (Norprolac) is a selective, D2 receptor agonist (also called dopamine receptor stimulant) that is used for the treatment of elevated levels of prolactin, and Quinagolide prevents the production of a chemical called prolactin. Prolactin is involved in many processes within the body, such as milk production after childbirth and altering levels of hormones involved with controlling the menstrual cycle and fertility. Quinagolide is therefore helpful in reducing prolactin levels to reduce milk production for certain medical reasons and to treat some types of infertility, breast problems and menstrual disorders.

Current developer:  Ferring Pharmaceuticals Inc.

1. Quinagolide on endometriotic lesions in patients with endometriosis-associated hyperprolactinemia. Quinagolide induced a 69.5% reduction in the size of the lesions, with 35% vanishing completely. Histologic analysis showed tissue degeneration, which was supported by down-regulation of VEGF/VEGFR2, three proangiogenic cytokines (CCL2, RUNX1, and AGGF1) and plasminogen activator inhibitor (PAI) 1, a potent inhibitor of fibrinolysis in the L2 lesions. CONCLUSION(S): By interfering with angiogenesis, enhancing fibrinolysis, and reducing inflammation, quinagolide reduces or eliminates peritoneal endometriotic lesions in women with endometriosis. [source: Fertil Steril. 2011 Mar 1;95(3):882-888.e1.]

2. Quinagolide in prevention of early ovarian hyperstimulation syndrome in IVF patients: a randomized, double-blind, placebo-controlled trial.  Quinagolide appears to prevent moderate/severe early OHSS while not affecting treatment outcome. The effect is more marked in patients who did not achieve a clinical pregnancy. Quinagolide administered in high doses without dose-titration is associated with poor tolerability. ClinicalTrials.gov Identifier: NCT00329693. [source:  Hum Reprod. 2010 Apr;25(4):995-1004.]

3. Quinagolide--a valuable treatment option for hyperprolactinaemia. Quinagolide may improve patient compliance to treatment owing to its reduced side effect profile, simple and rapid titration over just 7 days, once-daily dosing regimen and easy to use starter pack (available in some countries). Quinagolide offers an additional benefit for patients wishing to become pregnant, as it can be used until the point of confirmation of pregnancy. Therefore, as a well tolerated and effective therapy, with a simple dosing regimen, quinagolide should be considered as a first-line therapy in the treatment of hyperprolactinaemia. [source:  Eur J Endocrinol. 2006 Feb;154(2):187-95.]

PD and PK properties of quinagolide

1. Pharmacodynamic properties of Quinagolide

Pharmacotherapeutic group: prolactin inhibitors (ATC code G02C B04). Quinagolide, the active ingredient of NORPROLAC, is a selective dopamine D2-receptor agonist not belonging to the chemical classes of ergot or ergoline compounds. Owing to its dopaminergic action, the drug exerts a strong inhibitory effect on the secretion of the anterior pituitary hormone prolactin, but does not reduce normal levels of other pituitary hormones. In some patients the reduction of prolactin secretion may be accompanied by short-lasting, small increases in plasma growth hormone levels, the clinical significance of which is unknown. As a specific inhibitor of prolactin secretion with a prolonged duration of action, NORPROLAC has been shown to be effective and suitable for once-a-day oral treatment of patients presenting with hyperprolactinaemia and its clinical manifestations such as galactorrhoea, oligomenorrhoea, amenorrhoea, infertility and reduced libido.

2. Pharmacokinetic properties of Quinagolide

After oral administration of radiolabelled drug, quinagolide is rapidly and well absorbed. Plasma concentration values obtained by a non-selective radio-immunoassay (RIA), measuring quinagolide together with some of its metabolites, were close to the limit of quantification and gave no reliable information. The apparent volume of distribution of quinagolide after single oral administration of radiolabelled compound was calculated to be approx. 100L. For the parent drug, a terminal half-life of 11.5 hours has been calculated under single dose conditions, and of 17 hours at steady state.

Quinagolide is extensively metabolised during its first pass. Studies performed with 3H-labelled quinagolide revealed that more than 95% of the drug is excreted as metabolites. About equal amounts of total radioactivity are found in faeces and urine. In blood, quinagolide and its N-desethyl analogue are the biologically active but minor components. Their inactive sulphate or glucuronide conjugates represent the major circulating metabolites. In urine, the main metabolites are the glucuronide and sulphate conjugates of quinagolide and the N-desethyl, N,N-didesethyl analogues. In the faeces the unconjugated forms of the three components were found. The protein binding of quinagolide is approximately 90% and is non-specific. The results, obtained in pharmacodynamic studies, indicate that with the recommended therapeutic dosage a clinically significant prolactin-lowering effect occurs within 2 hours after ingestion, reaches a maximum of 4 to 6 hours and is maintained for about 24 hours. A definite dose-response relationship could be established for the duration, but not for the magnitude of the prolactin-lowering effect which, with a single oral dose of 50 micrograms  was close to maximum. Higher doses did not result in a considerably greater effect but prolonged its duration.

 1: Broekhof R, Gosselink MJ, Pijl H, Giltay EJ. The effect of aripiprazole and quinagolide, a dopamine agonist, in a patient with symptomatic pituitary prolactinoma and chronic psychosis. Gen Hosp Psychiatry. 2011 Aug 25. [Epub ahead of print] PubMed PMID: 21872335.

2: Lacasse P, Lollivier V, Bruckmaier RM, Boisclair YR, Wagner GF, Boutinaud M. Effect of the prolactin-release inhibitor quinagolide on lactating dairy cows. J Dairy Sci. 2011 Mar;94(3):1302-9. PubMed PMID: 21338795.

3: Gómez R, Abad A, Delgado F, Tamarit S, Simón C, Pellicer A. Effects of hyperprolactinemia treatment with the dopamine agonist quinagolide on endometriotic lesions in patients with endometriosis-associated hyperprolactinemia. Fertil Steril. 2011 Mar 1;95(3):882-8.e1. Epub 2010 Nov 5. PubMed PMID: 21055747.

4: Lakatos G, Szücs N, Kender Z, Czirják S, Rácz K. [Macroprolactinemia associated with pituitary macroadenoma: treatment with quinagolide]. Orv Hetil. 2010 Jun 27;151(26):1072-5. Hungarian. PubMed PMID: 20558354.

5: Busso C, Fernández-Sánchez M, García-Velasco JA, Landeras J, Ballesteros A, Muñoz E, González S, Simón C, Arce JC, Pellicer A. The non-ergot derived dopamine agonist quinagolide in prevention of early ovarian hyperstimulation syndrome in IVF patients: a randomized, double-blind, placebo-controlled trial. Hum Reprod. 2010 Apr;25(4):995-1004. Epub 2010 Feb 6. PubMed PMID: 20139430; PubMed Central PMCID: PMC2839910.

6: Vinkers DJ, van der Wee NJ. A case of mania after long-term use of quinagolide. Gen Hosp Psychiatry. 2007 Sep-Oct;29(5):464. PubMed PMID: 17888817.

7: Hrycek A, Pochopień-Kenig G, Scieszka J. Selected acute phase proteins and interleukin-6 in systemic lupus erythematosus patients treated with low doses of quinagolide. Autoimmunity. 2007 May;40(3):217-22. PubMed PMID: 17453721.

8: Hrycek A, Kusmierz D, Dybała T, Swiatkowska L. Expression of messenger RNA for transforming growth factor-beta1 and for transforming growth factor-beta receptors in peripheral blood of systemic lupus erythematosus patients treated with low doses of quinagolide. Autoimmunity. 2007 Feb;40(1):23-30. PubMed PMID: 17364494.

9: Barlier A, Jaquet P. Quinagolide--a valuable treatment option for hyperprolactinaemia. Eur J Endocrinol. 2006 Feb;154(2):187-95. Review. PubMed PMID: 16452531.

10: Hair WM, Wu FC, Lincoln GA. An investigation of the effectiveness of testosterone implants in combination with the prolactin inhibitor quinagolide in the suppression of spermatogenesis in men. Hum Reprod. 2003 Apr;18(4):749-55. PubMed PMID: 12660266.

11: Hrycek A, Kokocińska D, Kośmider J, Konieczny B. Tissue-polypeptide-specific antigen in SLE patients treated with low doses of quinagolide. Lupus. 2003;12(2):149-52. PubMed PMID: 12630763.

12: Ilkko E, Tikkakoski T, Salmela P, Pyhtinen J, Kurunlahti M. MR imaging of pituitary adenomas treated with the prolactin inhibitor quinagolide. Acta Radiol. 2002 Mar;43(2):125-9. PubMed PMID: 12010287.

13: Mostafa AA, Bebawy LI, Refaat HH. Spectrophotometric determination of clobetasol propionate, halobetasol propionate, quinagolide hydrochloride, through charge transfer complexation. J Pharm Biomed Anal. 2002 Mar 1;27(6):889-99. PubMed PMID: 11836053.

14: Schultz PN, Ginsberg L, McCutcheon IE, Samaan N, Leavens M, Gagel RF. Quinagolide in the management of prolactinoma. Pituitary. 2000 Dec;3(4):239-49. PubMed PMID: 11788012.

15: De Luis DA, Lahera M, Botella JI, Valero MA, Varela C. [Efficacy of quinagolide in the treatment of a patient with hypophyseal resistance to thyroid hormones]. An Med Interna. 2001 May;18(5):259-61. Spanish. PubMed PMID: 11496561.

16: Hrycek A, Cieślik P, Tustanowski J, Nowak S, Jedynak P. Selected serum cytokines in systemic lupus erythematosus treated with quinagolide. Lupus. 2001;10(6):424-30. PubMed PMID: 11434578.

17: Ferone D, Pivonello R, Lastoria S, Faggiano A, Del Basso de Caro ML, Cappabianca P, Lombardi G, Colao A. In vivo and in vitro effects of octreotide, quinagolide and cabergoline in four hyperprolactinaemic acromegalics: correlation with somatostatin and dopamine D2 receptor scintigraphy. Clin Endocrinol (Oxf). 2001 Apr;54(4):469-77. PubMed PMID: 11318782.

18: Rohmer V, Freneau E, Morange I, Simonetta C. Efficacy of quinagolide in resistance to dopamine agonists: results of a multicenter study. Club de l'Hypophyse. Ann Endocrinol (Paris). 2000 Nov;61(5):411-7. PubMed PMID: 11084391.

19: Nobels FR, de Herder WW, van den Brink WM, Kwekkeboom DJ, Hofland LJ, Zuyderwijk J, de Jong FH, Lamberts SW. Long-term treatment with the dopamine agonist quinagolide of patients with clinically non-functioning pituitary adenoma. Eur J Endocrinol. 2000 Nov;143(5):615-21. PubMed PMID: 11078985.

20: De Luis DA, Becerra A, Lahera M, Botella JI, Valero, Varela C. A randomized cross-over study comparing cabergoline and quinagolide in the treatment of hyperprolactinemic patients. J Endocrinol Invest. 2000 Jul-Aug;23(7):428-34. PubMed PMID: 11005266.

21: Koloszár S, Keresztúri A, Kovács L. [Treatment of hyperprolactinemic anovulation with the dopamin-agonist quinagolide]. Orv Hetil. 2000 Jul 16;141(29):1621-3. Hungarian. PubMed PMID: 10962898.

22: Di Sarno A, Landi ML, Marzullo P, Di Somma C, Pivonello R, Cerbone G, Lombardi G, Colao A. The effect of quinagolide and cabergoline, two selective dopamine receptor type 2 agonists, in the treatment of prolactinomas. Clin Endocrinol (Oxf). 2000 Jul;53(1):53-60. PubMed PMID: 10931080.

23: Colao A, Ferone D, Lastoria S, Cerbone G, Di Sarno A, Di Somma C, Lucci R, Lombardi G. Hormone levels and tumour size response to quinagolide and cabergoline in patients with prolactin-secreting and clinically non-functioning pituitary adenomas: predictive value of pituitary scintigraphy with 123I-methoxybenzamide. Clin Endocrinol (Oxf). 2000 Apr;52(4):437-45. PubMed PMID: 10762286.

24: Webster J. Cabergoline and quinagolide therapy for prolactinomas. Clin Endocrinol (Oxf). 2000 Nov;53(5):549-50. PubMed PMID: 11106914.

25: Eijsbouts A, van den Hoogen F, Laan RF, Hermus RM, Sweep FC, van de Putte L. Treatment of rheumatoid arthritis with the dopamine agonist quinagolide. J Rheumatol. 1999 Oct;26(10):2284-5. PubMed PMID: 10529161.

26: Ioannidou-Mouzaka L, Niagassas M, Galanos A, Kalovidouris A. Pilot study on the treatment of cyclical mastodynia with Quinagolide. Eur J Gynaecol Oncol. 1999;20(2):117-21. PubMed PMID: 10376428.

27: Ferone D, Lastoria S, Colao A, Varrella P, Cerbone G, Acampa W, Merola B, Salvatore M, Lombardi G. Correlation of scintigraphic results using 123I-methoxybenzamide with hormone levels and tumor size response to quinagolide in patients with pituitary adenomas. J Clin Endocrinol Metab. 1998 Jan;83(1):248-52. PubMed PMID: 9435450.

28: Colao A, Lombardi G. Prolactinomas apparently resistant to quinagolide respond to cabergoline therapy. J Clin Endocrinol Metab. 1997 Aug;82(8):2756. PubMed PMID: 9253368.

29: Delgrange E, Donckier J. Prolactinomas apparently resistant to quinagolide respond to cabergoline therapy. J Clin Endocrinol Metab. 1997 Aug;82(8):2755-6. PubMed PMID: 9253367.

30: Guido R, Valenti S, Foppiani L, De Martini D, Cossu M, Giusti M. Prolactin decrease and shift to a normal-like isoform profile during treatment with quinagolide in a patient affected by an invasive prolactinoma. J Endocrinol Invest. 1997 May;20(5):289-93. PubMed PMID: 9258810.

31: Tabarin A, Catargi B. [Treatment of macroprolactinomas with quinagolide (Norprolac)]. Ann Endocrinol (Paris). 1997;58(2):87-94. Review. French. PubMed PMID: 9239226.

32: Jaquet P. [Quinagolide and macroprolactinomas a progress?]. Ann Endocrinol (Paris). 1997;58(2):83-5. Review. French. PubMed PMID: 9239225.

33: Morange I, Barlier A, Pellegrini I, Brue T, Enjalbert A, Jaquet P. Prolactinomas resistant to bromocriptine: long-term efficacy of quinagolide and outcome of pregnancy. Eur J Endocrinol. 1996 Oct;135(4):413-20. PubMed PMID: 8921822.

34: Bodmer CW, Atkin SL, Savage MW, Masson EA, White MC. Effects of quinagolide (CV 205-502), a selective D2-agonist, on vascular reactivity in patients with a prolactin-secreting adenoma. Clin Endocrinol (Oxf). 1995 Jul;43(1):49-53. PubMed PMID: 7641411.

35: Vilar L, Burke CW. Quinagolide efficacy and tolerability in hyperprolactinaemic patients who are resistant to or intolerant of bromocriptine. Clin Endocrinol (Oxf). 1994 Dec;41(6):821-6. PubMed PMID: 7889620.

36: Lévy L, Alvaro V, Dubray C, Joubert D. Ca(2+)-dependent protein kinase C isoforms in rat pituitary hyperplasia: effect of in vivo treatment with quinagolide. Eur J Pharmacol. 1994 Aug 16;268(3):327-34. PubMed PMID: 7528679.

37: Giusti M, Porcella E, Carraro A, Cuttica M, Valenti S, Giordano G. A cross-over study with the two novel dopaminergic drugs cabergoline and quinagolide in hyperprolactinemic patients. J Endocrinol Invest. 1994 Jan;17(1):51-7. PubMed PMID: 7911813.

38: Trouillas J, Chevallier P, Claustrat B, Hooghe-Peters E, Dubray C, Rousset B, Girod C. Inhibitory effects of the dopamine agonists quinagolide (CV 205-502) and bromocriptine on prolactin secretion and growth of SMtTW pituitary tumors in the rat. Endocrinology. 1994 Jan;134(1):401-10. PubMed PMID: 7903933.

39: Nickelsen T, Jungmann E, Althoff P, Schumm-Draeger PM, Usadel KH. Treatment of macroprolactinoma with the new potent non-ergot D2-dopamine agonist quinagolide and effects on prolactin levels, pituitary function, an the renin-aldosterone system. Results of a clinical long-term study. Arzneimittelforschung. 1993 Apr;43(4):421-5. PubMed PMID: 8098604.

40: Verhelst JA, Froud AL, Touzel R, Wass JA, Besser GM, Grossman AB. 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 (Copenh). 1991 Oct;125(4):385-91. PubMed PMID: 1683503.