The Effects of CV205-502 in Patients withHyperprolactinaemia Intolerant and/or Resistant to Bromocriptine

razzaq, riadh abdul; O’Halloran, Domhnall J; Beardwell, Colin G; Shalet, Stephen M

doi:10.1159/000182739

Cited by 26 publications

(12 citation statements)

References 9 publications

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“…There are only sporadic reports of using pergolide in bromocriptine-resistant patients which show only modest efficacy [84,85]. Quinagolide (CV 205-502) has been shown to be effective in reducing PRL levels to normal in about 50% of patients resistant to bromocriptine [86][87][88][89][90] but this drug is not available in the U.S. An even greater efficacy in such patients has been shown with cabergoline, studies showing that about 80% of such patients could obtain normalization of PRL levels with this drug [79,91]. Furthermore, Colao et al [91] showed that 85% of 20 patients resistant to both bromocriptine and quinagolide responded with a normalization of PRL levels and 70% responded with some tumor size change.…”

Section: Treatment Approaches For Patients Resistant To Dopamine Agonmentioning

confidence: 99%

Pharmacologic Resistance in Prolactinoma Patients

2005

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Pharmacologic resistance to dopamine agonists is defined here as failure to normalize PRL levels and failure to decrease macroprolactinoma size by >or=50%. Failure to normalize PRL levels is found in about one-quarter of patients treated with bromocriptine and 10-15% of those treated with pergolide or cabergoline. Failure to achieve at least a 50% reduction in tumor size occurs in about one-third of those treated with bromocriptine and 10-15% of those treated with pergolide or cabergoline. The cause of dopamine resistance is primarily a decrease in D(2) receptors but the receptors have normal affinity for dopamine. Treatment approaches for patients resistant to dopamine agonists include changing to another dopamine agonist and increasing the dose of the drug as long as there is continued response to the dose increases and no adverse effects with higher doses. Transsphenoidal surgery is also an option. Clomiphene, gonadotropins, and GnRH can be used if fertility is desired. For those not desiring fertility, estrogen replacement may be used unless there is a macroadenoma, in which case control of tumor growth is also an issue and dopamine agonists are generally necessary. In many patients modest or even no reduction in tumor size may be acceptable as long as there is not tumor growth. Hormone replacement (estrogen or testosterone) may cause a decrease in efficacy of the dopamine agonist so that it must be carried out cautiously. Reduction of endogenous estrogen, use of selective estrogen receptor modulators, and aromatase inhibitors are potential experimental approaches.

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Section: Treatment Approaches For Patients Resistant To Dopamine Agonmentioning

confidence: 99%

Pharmacologic Resistance in Prolactinoma Patients

2005

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“…One definition is the absence of serum PRL level normalisation and/or tumour shrinkage after at least 3 months of treatment with bromocriptine at a dose of 15 mg, or quinagolide at a dose of 0.6 mg [31, 32, 33]. These doses are rather high for the treatment of hyperprolactinaemia.…”

Section: Prolactin-secreting Pituitary Adenomasmentioning

confidence: 99%

“…Treatment with quinagolide has also been demonstrated to be more effective than bromocriptine in several poorly responding patients [14, 16]. Not all patients responded satisfactorily to cabergoline and quinagolide although the response to cabergoline was better in some cases [32, 33, 40, 41]. One explanation was that cabergoline binds the receptor significantly longer than quinagolide [42]and induces less severe and shorter lasting side effects [43].…”

Section: Prolactin-secreting Pituitary Adenomasmentioning

confidence: 99%

New Medical Approaches in Pituitary Adenomas

et al. 2000

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Recently, the medical approach to patients with secreting and clinically non-functioning pituitary adenomas has received great impulse thanks to the availability of new, selective and long-lasting compounds with dopaminergic activity, such as cabergoline, and of somatostatin analogues provided in slow-release formulations, such as lanreotide and octreotide long acting release (LAR). In particular, the use of cabergoline has induced control of hyperprolactinaemia and tumour shrinkage in the great majority of patients with micro- and macroprolactinomas. Cabergoline treatment restores fertility both in women and men, and partially improves osteoporosis, one of the major complications of hyperprolactinaemia. In acromegaly, disease control (growth hormone [GH] <2.5–1.0 μg/l as a fasting or glucose-suppressed value, respectively, together with age-normalised insulin-like growth factor [IGF]-I) is achievable in more than half of patients receiving treatment with lanreotide or octreotide-LAR. Improvement in cardiomyopathy, sleep apnoea and arthropathy has been reported during GH/IGF-I suppression after pharmacotherapy. A synthetic GH analogue, B2036-PEG, that antagonises endogenous GH binding to its receptor-binding sites and a GH-releasing hormone antagonist that blocks the effect of this releasing factor on the hypothalamus and pituitary are presently under investigation in acromegaly. Preliminary studies have clearly demonstrated the effectiveness of the GH receptor antagonist in suppressing IGF-I levels in acromegalic patients previously unresponsive to somatostatin analogues. Beneficial effects of subcutaneous octreotide and lanreotide have also been reported in adenomas secreting thyroid-stimulating hormone, while the results of treatment with dopamine agonists or somatostatin analogues remain disappointing in patients with clinically non-functioning adenomas. In these patients the possibility of visualising in vivo the expression of D₂ receptors using specific radiotracers such as ¹²³I-methoxybenzamide has allowed selection of patients likely to respond to cabergoline. Scant effects of pharmacotherapy have also been reported in patients with adenomas secreting adrenocorticotropic hormone. However, some preliminary data suggest a potential use of cabergoline in combination with ketoconazole, or alone, in selected cases of Cushing’s disease or Nelson’s syndrome.

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“…By the end of the 24 weeks there was no difference between the drugs in terms of serum prolactin concentrations or clinical effects. In two studies involving 37 patients with hyperprolactinaemia resistant to bromocriptine, quinagolide (75-500µg daily) lowered prolactin levels in most patients,13 , 14 returning levels to normal in about one third 13. In patients with macroprolactinomas13 , 15–17 quinagolide reduced prolactin levels, and in over half reduced prolactinoma size by more than 25%.…”

Section: Clinical Studiesmentioning

confidence: 99%

“…Some patients intolerant of bromocriptine can take quinagolide;14–16 whether the reverse is true is not known.…”

Section: Unwanted Effectsmentioning

confidence: 99%

New drugs for hyperprolactinaemia

1995

DTB

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In 1976 we heralded the introduction of bromocriptine (Parlodel - Sandoz) as "an important advance" for the treatment of patients with hyperprolactinaemia.1 Now two new drugs are available for treating hyperprolactinaemia; cabergoline (▼Dostinex - Pharmacia) which the manufacturer claims offers "a significant advance in prolactin control" and quinagolide (▼Norprolac - Sandoz) for which the claim is of a "significant advance in the therapy of hyperprolactinaemia". Do these newer products hold real advantages?

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The Effects of CV205-502 in Patients withHyperprolactinaemia Intolerant and/or Resistant to Bromocriptine

Cited by 26 publications

References 9 publications

Pharmacologic Resistance in Prolactinoma Patients

Pharmacologic Resistance in Prolactinoma Patients

New Medical Approaches in Pituitary Adenomas

New drugs for hyperprolactinaemia

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