Pituitary Macroadenomas Medication
- Author: James R Mulinda, MD, FACP, FACE; Chief Editor: George T Griffing, MD more...
Medication Summary
Medications are used to control excess hormone secretion or to replace deficient hormones.
Dopaminergic agents
Class Summary
These agents directly stimulate postsynaptic dopamine receptors. The dopaminergic neurons in the tuberoinfundibular process modulate the secretion of hormones from the anterior pituitary by secreting an inhibitory factor, believed to be dopamine.
Bromocriptine (Parlodel)
Dopamine agonist used to normalize serum prolactin levels. Semisynthetic, ergot alkaloid derivative. Strong dopamine D2-receptor agonist. Partial dopamine D1-receptor agonist. FDA approved as an adjunct to levodopa/carbidopa but less effective than other dopamine agonists.
Might relieve akinesia, rigidity, and tremor associated with Parkinson disease. Stimulates dopamine receptors in the corpus striatum. Approximately 28% absorbed from the GI tract and metabolized in the liver. Approximate elimination half-life is 50 h, with 85% excreted in feces and 3-6% eliminated in the urine.
Initiate at low dosage and slowly increase dosage to individualize therapy. Assess dosage titration q2wk. Gradually reduce dose in 2.5-mg decrements if severe adverse reactions occur.
Cabergoline (Dostinex)
Dopamine agonist used to normalize serum prolactin levels. Long-acting dopamine receptor agonist with high affinity for D2 receptors. Prolactin secretion by anterior pituitary is under hypothalamic inhibitory control exerted through dopamine.
Pergolide (Permax)
Pergolide was withdrawn from the US market March 29, 2007. Potent dopamine receptor agonist at both D1 and D2 receptor sites. Approximately 10-1000 times more potent than bromocriptine on a mg-per-mg basis. Inhibits secretion of prolactin. Causes a transient rise in serum concentrations of growth hormone and decrease in serum concentrations of LH.
Growth hormone receptor antagonists
Class Summary
Used for the treatment of acromegaly.
Pegvisomant (Somavert)
Genetically engineered growth hormone receptor antagonist used to treat acromegaly. Useful in patients not responding to somatostatin analogues. May be used concurrently with somatostatin analogues after surgery and radiation.
Somatostatin analogues
Class Summary
Used to control symptoms resulting from excess hormone secretion.
Octreotide (Sandostatin)
Somatostatin analogue used to normalize growth hormone levels. Acts primarily on somatostatin receptor subtypes II and V. Inhibits growth hormone secretion and has multiple other endocrine and nonendocrine effects, including inhibition of glucagon, VIP, and GI peptides.
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