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Dopamine is the chemical that normally inhibits prolactin secretion, so clinicians may treat prolactinoma with drugs that act like dopamine such as bromocriptine and cabergoline. [12] This type of drug is called a dopamine agonist. [12] These drugs shrink the tumor and return prolactin levels to normal in approximately 80% of patients.
Dopamine agonists are mainly used to treat Parkinson's disease, but also hyperprolactinemia and restless legs syndrome. [15] The side effects are predominantly collected from studies of Parkinson's disease, where dopamine agonists are commonly used as a first-line treatment with levodopa. [16]
[58] [59] If the prolactinoma does not initially respond to dopamine agonist therapy, such that prolactin levels are still high or the tumor is not shrinking as expected, the dose of the dopamine agonist can be increased in a stepwise fashion to the maximum tolerated dose. [3] Another option is to consider switching between dopamine agonists.
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.
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]
Dopamine agonists for infertility treatment are commonly administered to hyperprolactinemic anovulation patients. Both bromocriptine and cabergoline are the first-line dopamine agonist in hyperprolactinemia treatment. [46] Cabergoline is currently more preferred than bromocrptine due to its higher efficacy and fewer side effects like nausea. [53]
Cabergoline is a long-acting dopamine D 2 receptor agonist. In-vitro rat studies show a direct inhibitory effect of cabergoline on the prolactin secretion in the lactotroph cells of the pituitary gland and cabergoline decreases serum prolactin levels in reserpinized rats.
Dopamine receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS) and are implicated in many neurological processes, including motivational and incentive salience, cognition, memory, learning, and fine motor control, as well as modulation of neuroendocrine signaling.