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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Questions (1)

(M2.EC.14.55) An 7-year-old girl is brought to the pediatrician by her concerned mother, because she is "more physically matured" than the rest of the girls in her class. On physical exam, she is noted to have breast development and pubic hair. On gonadotropin reseasing hormone (GnRH) stimulation, she has an increase in leutienizing hormone (LH) levels. Thyroid function tests and an MRI of the head are both within normal limits. Which of the following is the most appropriate treatment for this condition?

QID: 104380
1

Ketoconazole

0%

(0/19)

2

Leuprolide

79%

(15/19)

3

Finasteride

0%

(0/19)

4

Octreotide

11%

(2/19)

5

Anastrozole

5%

(1/19)

M 7 E

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Evidence (2)
EXPERT COMMENTS (6)
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