Updated: 5/21/2019

Hypothalamic / Pituitary Drugs

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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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