Repro-Endo: Pituitary / Hypothalamic Flashcards Preview

Pharmacology > Repro-Endo: Pituitary / Hypothalamic > Flashcards

Flashcards in Repro-Endo: Pituitary / Hypothalamic Deck (36)
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1

Leuprolide (Goserelin)

  • GnRH agonist
  • GnRH analog w/ longer half-life
  • Pulsatile --> Increase LH / FSH
    • Women w/ Amenorrhea who desire fertility
  • Continuous --> Suppress LH / FSH
    • Prostate cancer
    • Leiomyomas (smooth muscle tumor)
    • Endometriosis
  • SE: Bone pain, Feet / Ankle swelling

2

Somatotropin

  • GH analog
  • Increases Lean muscle mass
  • Tx:
    • Turner syndrome
    • Dwarfism
    • Wasting a/w AIDS or Malignancy
  • SE: Hand / Foot edema, Thickening of Bones/Jaw, Carpel tunnel syndrome, Increased organ growth, Decreased insulin sensitivity, Hyperglycemia

3

Octreotide

  • Somatostatin analog
  • Longer half-life than Somatostatin
  • Hypothalamic hormone that normally inhibits the release of GH, Glucagon, Insulin, Gastrin, and Vasoactive Intestinal Peptide (VIP)
  • Tx: Acromegaly, Gastrinoma, Glucagonoma, Esophageal varices, VIPomas, Carcinode syndrome, Acromegaly, Zollinger-Ellison Syndrome
  • SE: Gallbladder disease, Pancreatitis, Hypo- or Hyer- thyroidism, Cardiac Arrhythmias

4

Bromocriptine, Cabergoline

  • Dopamine receptor agonsits
  • Dopamine inhibits Prolactin secretion from the Hypothalamus
  • Tx: Prolactinomas, Parkinson disease (High dose)
  • SE: Psychotic symptoms, Dizziness, Headache, Nausea, Lightheadedness, Confusion

5

Desmopressin

  • Vasopressin analog (ADH)
  • Minimal V1 activity on Smooth muscle
  • More V2 receptors --> Renal collecting tubules --> Water reabsorption and von Willebrand Factor (vWF) release
  • Tx: Central DI (NOT Nephrogenic), von Willebrand Disease
  • SE: Hyponatremia, Transient headache, flushing

6

Oxytocin

  • Posterior pituitary hormone --> Milk secretion and Uterine contractions during Labor
  • Tx: Induces labor, Decreases postpartum bleeding by inducing contractions, Stimulates breast milk letdown in new mothers
  • SE: Chest pain, Confusion, Excessive vaginal bleeding, Palpitations, Seizures

7

Rx for Women w/ Amenorrhea who desire fertility?

Pulsatile Leuprolide
(GnRH agonist --> LH / FSH)

8

Rx for Prostate cancer?

Continous Leuprolide

(GnRH agonsit)

9

Rx for Leiomyomas (Smooth Muscle Tumor)?

Continuous Leuprolide

(GnRH agonist)

10

Rx for Endometriosis?

Continuous Leuprolide

(GnRH agonist)

11

Rx for Precocious Puberty?

Continuous Leuprolide

(GnRH agonist)

12

Rx for Dwarfism?

Somatotropin

(GH analog)

13

Rx for Wasting a/w AIDS or Malignancy?

Somatotropin

(GH analog)

14

Rx for Esophageal varices?

Octreotide

(Somatostatin analog)

15

Rx for VIPomas?

Octreotide

(Somatostatin analog)

16

Rx for Carcinoid Syndrome?

Octreotide

(Somatostatin analog)

17

Rx for Acromegaly?

Octreotide

(Somatostatin analog)

18

Rx for Zollinger-Ellison Syndrome?

Octreotide

(Somatostatin analog)

19

Rx for Prolactinomas?

Bromocriptine, Cabergoline

(Dopamine receptor agonists)

20

Rx for Parkinson Disease?

Bromocriptine, Cabergoline

(Dopamine receptor agonists)

21

Rx for Central Diabetes Insipidus?

Desmopressin

(Vasopressin analog: ADH)

22

Rx for von Willebrand Disease?

Desmopressin

(Vasopressin analog: ADH)

23

Rx for Inducing labor and Stimulating Breast Milk?

Oxytocin

(Posterior Pituitary Hormone)

24

Demeclocycline

  • ADH antagonist
  • Member of the Tetracycline family
  • Tx: SIADH
  • SE: Nephrogenic DI, Photosensitivity, Bone and Teeth abnormalities

25

Flutamide

  • Prevents the binding of Endogenous Androgens to the Androgen receptor
  • Pure Androgen antagonist w/out Intrinsic steroidal activity
  • 3 x daily
  • 1 week increase in LH and FSH --> Testosterone surge
  • Tx: Metastatic prostate cancer, often combind w/ GnRH agonists
  • Se: Diarrhea, Gynecomastia, Hepatotoxicity (rare)
  • Flutamide, Bicalutamide, Enzalutamide

26

Bicalutamide

  • Nonsteroidal antiandrogen
  • More effective at Tx of Prostate cancer than Flutamide
  • Promotes translocation of Androgen receptors to the cell nucleus
  • Tx: Prostate cancer
  • Se: Less Diarrhea or other side effects

27

Enzalutamide

  • Non-steroidal antiandrogens
    • Acts as an Antagonist at the Adnrogen Receptor
  • Tx: Metastatic castration-resistant prostate cancer who have previosuly recieved Docetaxel
  • 5x higher affinity than Bicalutamide for Androgen receptor
  • Enzalutamide Does Not promotre translocation of Androgen receptors to the cell nucleus
  • BUT it does penetrate the BBB

28

GnRH Agonists and Antagonists

  • GnRH agonists (Leuprolide or Goserelin) and Androgen receptor antagonists (Bicalutamide or Flutamide) work together
  • The initial surge of FSH and LH and resulting elevation of Testosterone is blocked
  • Diethylstilbestrol is used because it inhibits LH and FSH but has Se (gynecomastia, nausea, thromboembolism, vomiting)
  • Abarelix - inhibits LH and FSH and inhibits Testosterone

29

Ketoconazole

  • Antifungal drug
  • Effective inhibitor of P450 enzymes involved in Steroid biosynthesis
  • 2nd line agent for Tx of Prostate cancer

30

Abiraterone acetate

  • Tx: Metastatic, castration-resistant prostate cancer
  • Inhibits biosynthesis of Androgens (& to a lesser extend, Glucocorticoids) by inhibiting CYP17
  • Combined w/ Prednisone (counter inhibition of Glucocorticoid synthesis)
  • Se: HTN, Hypokalemia, and Fluid retention due to Mineralocorticoid excess