ECE2022 Eposter Presentations Pituitary and Neuroendocrinology (211 abstracts)
Pharmacokinetic profile of cabergoline in patients with dopamine agonist resistant prolactinomas: a pilot study
Aleksandra Shutova 1 , Natalia Fedorova 1 , Svetlana Vorotnikova 1 , Vitalii Ioutsi 1 , Juriy Panov 2 , Ekaterina Pigarova 1 , Larisa Dzeranova 1 & Ekaterina Troshina 2
1Federal state Budgetary Institution ‘National Medical Research Centre of Endocrinology’ Ministry of Health of the Russian Federation, Department of neuroendocrinology, Moscow, Russian Federation; 2Federal State Budgetary Institution ‘National Medical Research Centre of Endocrinology’ Ministry of Health of the Russian Federation, Moscow, Russian Federation
Introduction: Approximately 20% of patients with prolactinomas do not respond satisfactory (resistant) even to high dose dopamine agonist treatment. Worth noticing that there are no clear prognostic signs of treatment’s resistance as well as its etiology is a subject of discussion.
Aim: The aim of our study was to assessabsorption and metabolism of cabergoline in patients with dopamine agonist-resistant prolactinomas.
Materials and methods: In patients (n=4) with resistant prolactinomas (no normalization of PRL, no menses with max tolerated dose of cabergoline more than 3 mg a week) and one with normal effect of the drug we conducted a pharmacokinetic test: 1) cabergoline was preliminary withdrawn 4 days before the test; 2) at 9:00 the blood was taken before and 30-, 60-, 90-, 120-minutes and 4 hours after taking the cabergoline in a fixed doze of 0.5 mg. The concentration of cabergoline substance in the serum was measured using LC-MS/MS.
Results: It is shown that the serum cabergoline concentration curve in 3 patients with resistance to treatment doesn’t represent expected pharmacokinetic peaks (the growth rate less than + 1-50%). The pharmacokinetic curve of 1 resistant patient represented a cabergoline concentration peak at 30 min point (the growth rate +175%) with subsequent decline to baseline levels. The serum cabergoline concentration curve of drug-sensitive patient is characterized by an already significant baseline concentration that becomes progressively higher reaching an outstanding peak (the growth rate +112%) at the end of the test period.
Conclusion: Our pilot results show that the patients with dopamine-resistant prolactinomas may have a defect in forming (absorption or metabolic abnormalities) an adequate blood concentrations of the drug. Understanding the underlying mechanisms will allow us to develop personalized treatment strategy.
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Endocrine Abstracts
ISSN 1470-3947 (print) | ISSN 1479-6848 (online)
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