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Medical therapy is the preferred treatment in prolactinomas. [3] In most cases, medications that are dopamine agonists, such as cabergoline, [52] quinagolide and bromocriptine (often preferred when pregnancy is possible), are the treatment of choice used to decrease prolactin levels and tumor size upon the presence of microadenomas or ...
Bromocriptine, originally marketed as Parlodel and subsequently under many brand names, [1] is an ergoline derivative and dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease, hyperprolactinaemia, neuroleptic malignant syndrome, and, as an adjunct, type 2 diabetes.
A prolactinoma is a tumor of the pituitary gland that produces the hormone prolactin.It is the most common type of functioning pituitary tumor. [1] Symptoms of prolactinoma are due to abnormally high levels of prolactin in the blood (hyperprolactinemia), or due to pressure of the tumor on surrounding brain tissue and/or the optic nerves.
Prolactin inhibitors are mainly used to treat hyperprolactinemia (high prolactin levels). [1] Agonists of the dopamine D 2 receptor such as bromocriptine and cabergoline are able to strongly suppress pituitary prolactin secretion and thereby decrease circulating prolactin levels, and so are most commonly used as prolactin inhibitors. [1]
Absorption of bromocriptine oral dose is approximately 28%; however, only 6% reaches the systemic circulation unchanged, due to a substantial first-pass effect. Bromocriptine reaches mean peak plasma levels after about 1–1.5 hours after a single oral dose. The drug has high protein binding, ranging from 90-96% bound to serum albumin.
Hypoprolactinemia can result from autoimmune disease, [2] hypopituitarism, [1] growth hormone deficiency, [2] hypothyroidism, [2] excessive dopamine action in the tuberoinfundibular pathway and/or the anterior pituitary, and ingestion of drugs that activate the D 2 receptor, such as direct D 2 receptor agonists like bromocriptine and pergolide, and indirect D 2 receptor activators like ...
In patients with hyperprolactinemia, the serum pattern of prolactin isoforms usually encompasses 60%–90% monomeric prolactin, 15%–30% big-prolactin (40–60 kDa: usually prolactin dimers or big-big degradation products) and 0%–10% big-big prolactin (>100 kDa). [7]
These side effects are noted in less than 2% of patients. They require immediate termination of treatment. Clinical improvement and normalization of X-ray findings are normally seen soon after cabergoline withdrawal. It appears that the dose typically used for treatment of hyperprolactinemia is too low to cause this type of side effects.