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Updated: Dec 31 2021

Endocrine Medications

  • Endocrine Drug Introduction
    • Endocrine medications can be broken down into the following categories
      • diabetic agents
      • hormone agonists
      • hormone antagonists
  • Endocrine Drug Table
    • Diabetic Agents
        • Sulfonylureas (1st Generation)
        • Name
        • Mechanism of Action
        • Key Indication(s)
        • Key Toxicity
        • Chlorpropamide
        • Tolazamide
        • Tolbutamide
        • 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
        • Sulfonylureas (2nd Generation)
        • Name
        • Mechanism of Action
        • Key Indication(s)
        • Key Toxicity
        • Glipizide
        • Glyburide
        • 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
        • Biguinides
        • Name
        • Mechanism of Action
        • Key Indication(s)
        • Key Toxicity
        • 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
        • Name
        • Mechanism of Action
        • Key Indication(s)
        • Key Toxicity
        • Acarbose
        • Miglitol
        • Prevents breakdown of carbohydrates into single glucose molecules decreasing rate of absorption
        • Refractory type II diabetes mellitus
        • Osmotic diarrhea
        •  Flatulence
        • Thioglitazones
        • Name
        • Mechanism of Action
        • Key Indication(s)
        • Key Toxicity
        • Pioglitazone
        • Troglitazone
        • Rosiglitazone
        • 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
        • Other
        • Name
        • Mechanism of Action
        • Key Indication(s)
        • Key Toxicity
        • Repaglinide
        • Inhibits ATP-sensitive K+ channels resulting in β-cell depolarization and insulin release
        • Type II diabetes combination therapy
        • Hypoglycemia
    • Hormone Agonists
        • Estrogen
        • Name
        • Mechanism of Action
        • Key Indication(s)
        • Key Toxicity
        • 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
        • Name
        • Mechanism of Action
        • Key Indication(s)
        • Key Toxicity
        • 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
        • Name
        • Mechanism of Action
        • Key Indication(s)
        • Key Toxicity
        • 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
        • Name
        • Mechanism of Action
        • Key Indication(s)
        • Key Toxicity
        • 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
        • Name
        • Mechanism of Action
        • Key Indication(s)
        • Key Toxicity
        • Flutamide
        • Blocks action of testosterone by binding to adrogen receptors
        • Prostate cancer (used prior to GnRH analogues)
        • Gynecomastia
        •  GI disturbance
        • Enzyme Inhibitors
        • Name
        • Mechanism of Action
        • Key Indication(s)
        • Key Toxicity
        • Anastrozole
        • Inhibits aromatase
        • ER/PR positive breast cancer
        •  Fertility
        • Osteoporosis
        • Bone fracture
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