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Endocrine Drug Introduction
  • Endocrine medications can be broken down into the following categories
    • diabetic agents
    • hormone agonists
    • hormone antagonists
Endocrine Drug Table
 
Diabetic Agents
Name Mechanism of Action  Key Indication(s)
 Key Toxicity
Sulfonylureas (1st Generation)
Chlorpropamide
  • Inhibits ATP-sensitive K+ channels resulting in β-cell depolarization and insulin release
  • Second-line treatment for type II diabetes
  • Hypoglycemia (long-lasting)
  • Renal failure
  • Disulfiram effects
Tolazamide
Tolbutamide
Sulfonylureas (2nd Generation)
Glipizide
  • Inhibits ATP-sensitive K+ channels resulting in β-cell depolarization and insulin release
  • Second-line treatment for type II diabetes
  • Hypoglycemia (long-lasting)
  • Renal failure
Glyburide
Biguinides
Metformin
  • Exact mechanism unknown
  • ↓ gluconeogenesis
  • ↑ insulin sensitivity
  • ↑ glycolysis
  • ↓ serum glucose levels
  • ↓ postprandial glucose levels
  • First-line treatment for type II diabetes and metabolic syndrome
  • Lactic acidosis in patients with poor renal function
Alpha-Glucosidase Inhibitor
Acarbose
  • Prevents breakdown of carbohydrates into single glucose molecules decreasing rate of absorption
  • Refractory type II diabetes mellitus
  • Osmotic diarrhea
  • Flatulence
Miglitol
Thiaglitazone
Pioglitazone
  • Stimulates PPAR-γ which controls insulin-sensitive genes resulting in increased insulin sensitivity in peripheral tissues
  • Type II diabetes combination therapy
  • Heart failure
  • Hepatotoxicity
  • Weight gain
Troglitazone
Rosiglitazone
Other
Repaglinide
  • Inhibits ATP-sensitive K+ channels resulting in β-cell depolarization and insulin release
  • Type II diabetes combination therapy
  • Hypoglycemia
Hormone Agonists
Estrogen
Polyestradiol
  • Inhibits actions of dihydrotestosterone
    • Blocks LH secretion by pituitary
    • Decreases testosterone synthesis
    • Blocks testosterone uptake into prostate cells
    • Inhibits 5α-reductase
    • Induces chemical castration
  • Palliative prostate cancer therapy
  • Feminization
  • Nausea
  • Headache
  • Water retention
Diethylstilbestrol
  • Inhibits HPG axis
  • Blocks testosterone synthesis
  • Induces chemical castration
  • Believed to decrease incidence of stillbirth
  • No longer used in the US
  • Clear cell carcinoma (of the fetus)
  • Vaginal adenosis
  • T-shaped uterus
Progestins
Megestrol acetate
  • Synthetic progestin suppresses leuteinizing hormone by inhibition of pituitary function
  • Anorexic mechanism unknown
  • Appetite stimulant
  • Anti-neoplastic agent
  • Weight gain
  • Nausea
  • Vomiting
Gonadotropin Releasing Hormones
Leuprorelin
  • Acts as a gonadotropin releasing hormone agonist which inhibits gonadotropin secretion
  • Hormone responsive cancer (non-pulsatile)
  • Fertility (pulsatile)
  • Flushing
  • Sweating
  • Fatigue
  • Edema
  • Skin reaction
Hormone Antagonists
Anti-Estrogens
Tamoxifen
  • Competitively binds to estrogen receptors inhibiting effects of estrogen
  • ER/PR positive breast cancer
  • Endometrial cancer
  • Growth plate fusion
  • Increased bone density
Anti-Androgens
Flutamide
  • Blocks action of testosterone by binding to adrogen receptors
  • Prostate cancer (used prior to GnRH analogues)
  • Gynecomastia
  • GI disturbance
Enzyme Inhibitors
Anastrozole
  • Inhibits aromatase
  • ER/PR positive breast cancer
  • Fertility
  • Osteoporosis
  • Bone fracture
 

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