Ergot
alkaloids are the mainstay of therapy. In 1985, bromocriptine was approved for use in the United
States to treat hyperprolactinemia caused by a pituitary adenoma. These
agents act as strong dopamine agonists, thus decreasing prolactin levels.
Effects on prolactin levels occur within hours, and lesion size may decrease
within 1 or 2 weeks. Bromocriptine decreases prolactin synthesis, DNA
synthesis, cell multiplication, and overall size of prolactinomas,
bromocriptine treatment results in normal prolactin blood levels or return of
ovulatory menses in 80% to 90% of patients.
Because
ergot alkaloids, like bromocriptine, are excreted via the biliary tree, caution
is required when using it in the presence of liver disease. The major adverse
effects include nausea, headaches, hypotension, dizziness, fatigue and
drowsiness, omitting, headaches, nasal congestion, and constipation. Many
patients tolerate bromocriptine when the dose is increased gradually, by 1.25
mg (one-half tablet) daily each week until prolactin levels are normal or a
dose of 2.5 mg twice daily is reached. A proposed regimen is as follows:
one-half tablet every evening (1.25 mg) for 1 week, one-half tablet morning and
evening (1.25 mg) during the second
week, one-half tablet in the morning (1.25 mg) and a full tablet every evening
(2.5 mg) during the third week, and one tablet every morning and every evening
during the fourth week and thereafter (2.5 mg twice a day). The lowest dose
that maintains the prolactin level in the normal range is continued (1.25 mg
twice daily often is sufficient to normalize prolactin levels in individuals
with levels less than 100 ng/dL. Pharmacokinetic studies show peak serum levels
occur 3 hours after an oral dose, with a nadir at 7 hours. Because little
detectable bromocriptine is in the serum by 11 to 14 hours, twice-a-day
administration is required. Prolactin levels can be checked soon (6 to 24
hours) after the last dose.
One
rare, but notable, adverse effect of bromocriptine is a psychotic reaction.
Symptoms include auditory hallucinations, delusional ideas, and changes in mood
that quickly resolve after discontinuation of the during .
Many
investigators report no difference in fibrosis, calcification, prolactin
immunoreactivity, or the surgical success in patients pretreated with
bromocriptine compared to those not receiving bromocriptine .. An alternative
to oral administration is the vaginal administration or bromocriptine tablets,
which is well tolerated, and actually results in increased pharmacokinetic
measures . Cabergoline, another ergot alkaloid, has a very long half-life and
can be given orally twice per week. Its long duration of action is attributable
to slow elimination by pituitary tumor tissue, high affinity binding to
pituitary dopamine receptors, and extensive enterohepatic recirculation.
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