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Updated: Dec 17 2021

Hypothalamic / Pituitary Drugs

  • Snapshot
    • A 67-year-old man who is a long time smoker is brought to the emergency room following a seizure episode. He has no previous seizure history and according to his wife, no clear precipitating factor triggered the event. The seizure lasted a total of 2 minutes but the patient had no head trauma. A routine laboratory panel demonstrates signficiant hyponatremia. A computed tomography scan shows a speculated lesion within the right lung. (SIADH secondary to small cell lung cancer)
  • Overview
    • Describes a group of drugs used in the treatment of various disorders affecting the hypothalamus and/or pituitary
  • Anti-Diuretic Hormone (ADH) Antagonists
    • Mechanism of action
      • selectively blocks the action of ADH at the V2 receptor, which are expressed peripherally and is involved in the modulation of kidney function
        • allows for aquaresis and increased sodium concentration
      • examples include conivaptan, tolvaptan, lixivaptan, mozavaptan, and satavaptan
    • Clinical use
      • euvolemic hyponatremia (e.g., SIADH)
      • hypervolemic hyponatremia (e.g., CHF)
    • Adverse effects
      • increased thirst and dry mouth
      • weakness
      • nausea/vomitting
  • Desmopressin Acetate
    • Mechanism of action
      • anti-diuretic that binds to V2 receptors at the renal collecting duct, leading to increase in aquaporin channels and thus water reabsorption from the urine
      • also stimulates the release of von Willebrand factor (vWF) from endothelial cells via the V2 receptor
    • Clinical use
      • central diabetes insipidis
      • sleep enuresis
      • von Willebrand disease
    • Adverse effects
      • facial flushing
      • headaches
      • hyponatremia that can lead to seizures
      • gastrointestinal upset
  • Growth Hormone
    • Mechanism of action
      • recombinant form of growth hormone (GH), which stimulates growth, cell reproduction, and regeneration (anabolic effects)
      • increases the production of insulin-growth factor-1 (IGF-1)
    • Clinical use
      • replacement therapy for patients with GH deficiency
      • Turner syndrome
        • allows for height growth in children with conditions associated with short stature
      • chronic renal failure
      • Prader-Willi syndrome
      • short bowel syndrome
    • Adverse effects
      • headaches
      • edema
      • myalgia
      • gynecomastic
      • scoliosis
  • Leuprolide
    • Mechanism of action
      • acts as a mimetic of gonadotrophin-releasing hormone (GnRH), leading to the secretion of luteinizing hormone (LH) and follicle stimulating hormone (FSH) and subsequent increases in estradiol and testosterone levels
    • Clinical use
      • idiopathic central precocious puberty
      • prostate cancer
      • breast cancer
      • endometriosis
      • uterine fibroids
    • Adverse effects
      • hot flashes
      • insomnia
      • headaches
      • unstable mood
  • Oxytocin
    • Mechanism of action
      • neuropeptide that facilitates milk letdown, uterine contractions, and bonding via binding to its receptors
      • receptors are expressed by neurons in many parts of the brain and spinal cord (e.g., amygdala)
    • Clinical use
      • labor stimulation
      • uterine hemorrhage management
      • milk let down
    • Adverse effects
      • cramping/stomach pain
      • nausea/vomiting
      • hypo/hypertension
      • arrhythmias
      • seizures
  • Somatostatin (Octreotide)
    • Mechanism of action
      • octapeptide that mimics naturally occurring somatostatin, which is a potent inhibitor of growth hormone, glucagon, and insulin
    • Clinical use
      • acromegaly and gigantism
      • bleeding esophageal varices
      • carcinoid syndrome
      • gastrinoma
      • glucagonoma
    • Adverse effects
      • headache
      • hypothyroidism
      • cardiac conduction changes (e.g., bradycardia)
      • gastrointestinal symptoms (e.g., cramping, diarrhea, or constipation)
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