questions 2

Endocrine Medications

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Topic updated on 06/07/17 7:04pm

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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(M2.PH.70) A 65-year-old type II diabetic gentleman presents to the emergency room with increasing left flank pain. Routine labs are reveal an increase in his serum creatinine from his previous baseline level. An arterial blood gas is drawn revealing: pH 7.30, HCO3 20, PCO2 37, PO2 82. What medication should be immediately stopped to prevent worsening of his acidosis? Topic Review Topic

1. Insulin glargine
2. Metformin
3. Glipizide
4. Rosiglitazone
5. Exetinide

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