P6 – PITUITARY TUMOR

- Drugs used to treat pituitary dysfunction

 Somatostatin Analogs

• Octreotide
• Route of administration: SC/IV
• Mechanism of action: agonist of somatostatin
receptors
• Effects: - GH, TSH, glucagon, insulin and gastrin
• Clinical applications: acromegaly + hormone-
secreting tumors ● bleeding from esophageal varices.
• Side effects: GI disturbances, gallstones, bradycardia
and cardiac conduction problems, pain at the site of
injection
 GH Receptor Antagonist

• Pegvisomant
• Route of administration: SC
• Mechanism of action: blocks GH receptors
• Effects: ameliorates the effects of ↑ GH
• Clinical applications: acromegaly
• Side effects: increased liver enzymes → liver failure
 GnRH analogs

• Leuprolide
• Route of administration: IV, SC, IM or intranasally
• Mechanism of action: agonists at GnRH receptors.
• Effects: intermittent: ↑ FSH & LH ● prolonged: ↓ FSH & LH
• Clinical applications: controlled ovarian stimulation, endometriosis,
uterine fibroids, prostate cancer & central precocious puberty.
• Side effects: headache, light-headeness, nausea, hypersensitivity
reactions, symptoms of menopause.
 Dopamine Agonists

• Bromocriptine
• Route of administration: orally/vaginally
• Mechanism of action: activates dopamine D2 receptors
• Effects: - prolactin secretion, GH (less)
• Clinical applications: hyperprolactinemia ● acromegaly ● Parkinson’s
disease
• Side effects: GI disturbances, headache, psychiatric disturbances,
vasospasm and pulmonary infiltrate (high dose)
 Vasopressin Receptor Antagonists

• Conivaptan
• Route of administration: IV
• Mechanism of action: antagonist of V1a and V2 receptors
• Effects: excretion of free water
• Clinical applications: hyponatremia
• Side effects: infusion site reactions