Quinagolide Hydrochloride

(BANM, rINNM)
Synonyms: CV-205-502 (quinagolide); Hidrocloruro de quinagolida; Quinagolide, Chlorhydrate de; Quinagolidi Hydrochloridum; SD2-CV205-502 (quinagolide). (±)N,N-Diethyl-N′-[(3R * ,4aR * ,10aS * )1,2,3,4,4a,5,10,10a-octahydro-6-hydroxy-1-propylbenzo[g]quinolin-3-yl]sulfamide hydrochloride.
Cyrillic synonym: Хинаголида Гидрохлорид.

💊 Chemical information

Chemical formula: C20H33N3O3S,HCl = 432.0.
CAS — 87056-78-8 (quinagolide); 94424-50-7 ATC — G02CB04.
ATC Vet — QG02CB04.

💊 Adverse Effects and Precautions

As for Bromocriptine, although it is not an ergot derivative and does not seem to be associated with fibrotic reactions or vasoconstriction. Licensed product information contra-indicates the use of quinagolide in patients with hepatic or renal impairment; however, this is based on a lack of data in such patients.

Effects on mental function.

For reports of daytime somnolence occurring in patients receiving dopamine agonists including quinagolide, see Effects on Mental Function, under Adverse Effects of Levodopa.

💊 Interactions

As for Bromocriptine.

💊 Pharmacokinetics

Quinagolide is rapidly absorbed from the gastrointestinal tract and undergoes extensive first-pass metabolism to the N-desethyl analogue which is biologically active and the N,N-didesethyl analogue. Roughly equal amounts of a dose appear in the urine and the faeces; it is excreted in the urine as sulfate or glucuronide conjugates of quinagolide and its metabolites and in the faeces as the unconjugated forms. Protein binding has been reported to be about 90%. The elimination half-life of quinagolide at steady state is about 17 hours.

💊 Uses and Administration

Quinagolide is a non-ergot dopamine D2-agonist that has actions and uses similar to those of bromocriptine. It is used in the treatment of disorders associated with hyperprolactinaemia. Quinagolide is given as the hydrochloride, but doses are described in terms of the base; 27.3 micrograms of quinagolide hydrochloride is equivalent to about 25 micrograms of quinagolide. The initial dose, given once daily with food at bedtime, is 25 micrograms daily for 3 days. Doses are increased thereafter at 3-day intervals in steps of 25 micrograms until the optimal response is achieved, which is usually within the range of 75 to 150 micrograms daily. If doses greater than 300 micrograms daily are required, the daily dosage may be increased in steps of 75 to 150 micrograms at intervals of not less than 4 weeks. Quinagolide has also been investigated in the treatment of acromegaly and lactation inhibition.

Acromegaly.

Dopaminergics can produce a paradoxical reduction in growth hormone secretion and may be used in the treatment of acromegaly as adjunctive therapy to surgery, radiotherapy, or somatostatin analogues to reduce circulating growth hormone levels, although they are less effective than somatostatin analogues. Bromocriptine has been the main dopamine agonist used, but quinagolide has been tried and results of an open study1 in which quinagolide was given to 17 patients with acromegaly suggest that quinagolide has a more prolonged effect on suppression of growth hormone secretion than bromocriptine. However, it was ineffective in bromocriptine-resistant patients. In another study involving 34 patients, quinagolide was more effective than either cabergoline or a depot preparation of bromocriptine in normalising circulating growth hormone and insulin-like growth factor.2
1. Chiodini PG, et al. CV 205-502 in acromegaly. Acta Endocrinol (Copenh) 1993; 128: 389–93
2. Colao A, et al. Effect of different dopaminergic agents in the treatment of acromegaly. J Clin Endocrinol Metab 1997; 82: 518–23.

Hyperprolactinaemia and prolactinomas.

Dopamine agonists such as quinagolide are widely used for the treatment of hyperprolactinaemia secondary to a prolactinoma.
1. Rohmer V, et al. Efficacy of quinagolide in resistance to dopamine agonists: results of a multicenter study. Ann Endocrinol (Paris) 2000; 61: 411–17
2. Schultz PN, et al. Quinagolide in the management of prolactinoma. Pituitary 2000; 3: 239–49
3. Barlier A, Jaquet P. Quinagolide—a valuable treatment option for hyperprolactinaemia. Eur J Endocrinol 2006; 154: 187–95.

Lactation inhibition.

A small preliminary study1 has suggested that quinagolide is of similar efficacy to bromocriptine for prevention of puerperal lactation. However, the routine use of dopaminergics is not recommended for the suppression of physiological lactation.
1. van der Heijden PFM, et al. Lactation inhibition by the dopamine agonist CV 205-502. Br J Obstet Gynaecol 1991; 98: 270–6.

💊 Preparations

Proprietary Preparations

Austria: Norprolac; Canad.: Norprolac; Cz.: Norprolac; Fin.: Norprolac; Fr.: Norprolac; Ger.: Norprolac; Gr.: Norprolac; Hong Kong: Norprolac†; Hung.: Norprolac; Israel: Norprolac; Mex.: Norprolac; Neth.: Norprolac; Norw.: Norprolac; Pol.: Norprolac; Port.: Norprolac; Rus.: Norprolac (Норпролак); S.Afr.: Norprolac; Spain: Norprolac; Prodelion; Swed.: Norprolac; Switz.: Norprolac; UK: Norprolac.
Published May 08, 2019.