B14-1 Hypothalamic & Pituitary Hormones

Question 1

GnRH MOA? Where is it released from?

Answer 1

• Controls the release of FSH & LH

- released from the Hypothalamus

Question 2

How are GnRH Agonists used therepeutically?

Answer 2

1. Pulsatile
   - as replacement therapy
   - used for infertility or Dx of LH insufficiency in Hypogonadism
2. Continuous
   - suppression therapy (reversible castration)
   - “Biphasic Response” where it acts as an agonist for the first 7-10 days (flare) followed by inhibtion as the receptor becomes desensitized
   - Tx: Endometrious, prostate cancer, central precocious puberty (puberty before 8 years of age)

Question 3

Name 4 GnRH antagonists

Answer 3

“Ant needs to relix” - Ganirelix, Cetorelix, Abarelix, Degarelix

Question 4

Name some advantages to GnRH antagonists compared to continuous use of GnRH agonists

Answer 4

• No initial “flare” in hormone levels

- More rapid onset of antagonistic effects

Question 5

What are GnRH antagonists used to Tx?

Answer 5

Prostate cancer (atlernative to GnRH agonists)

Question 6

Name a Growth Hormone (GH) agonist

Answer 6

Somatropin

Question 7

Therepeutic use for Somatropin?

Answer 7

• GH deficiency

- Diseases of growth failure like Prader-Willi or Turner Syndrome

Question 8

Name 2 Growth Hormone (GH) antagonists, aka _______________?

Answer 8

Octreotide and Lanreotide, a “Somatostatin Analog”

Question 9

Octreotide/Lanreotide MOA?

Answer 9

Inhibits GH

Question 10

Name 3 therapeutic uses of Octreotide & Lanreotide?

Answer 10

1. Acromegaly or Gigantism
2. Carcinoid syndrom or other hormone-secreting tumors (gastrinoma)
3. Bleeding esophageal varices

Question 11

Menotropin contains what? What is it used for?

Answer 11

• “Meno-“ means mixed, so contains both FSH & LH

- infertility, induces spermatogenesis or ovulation

Question 12

Urofollitropin contains what? Used for what?

Answer 12

• FSH only

- same as Menotropins: Infertility

Question 13

Lutropin (recombinant hCG) contains what? Used for what?

Answer 13

• LH only

- LH replacement therapy

Question 14

Prolactin is the principle hormone for what? Where is it released from? How is it regulated?

Answer 14

• Lactation
• Anterior pituitary
• regulated by Hypothalamic inhibitory effects of dopamine

Question 15

Name 2 prolactin antagonists. How do these work?

Answer 15

• Bromocriptine and Cabergoline
• “it’s dope to go online with my bro’s”
• They’re directly Dopamine agonists, and since dopamine provides inhibitory affects on the anterior pituitary release of Prolactin, direct dopamine agonists are indirect Prolactin Antagonists

Question 16

What are prolactin antagonists used for?

Answer 16

Hyperprolactinemia, which inhibits ovuation and causes menstraul irregularities

Question 17

In summary, name the Anterior Pituitary Hormones we discussed

Answer 17

• Growth Hormone
• Gonadotropins: FSH and LH
• Prolactin

Question 18

Name the posterior pituitary hormone we discussed

Answer 18

• Vasopressin (ADH)

Question 19

Name the vasopressin (ADH) agonist. What is it used to treat & how does it work?

Answer 19

• Desmopressin
• DOC for Central Diabetes Insipidus via V1b receptor
• Also can be used for Von Willebrand’s Disease, primary nocturnal enuresis, and Hemophilia A

Question 20

Name the Vasopressin Antagonists (and what receptor they block). What are they used to treat? What is often preferred over these drugs?

Answer 20

• Conivaptan (V1 & V2 blocker) and Tolvaptan (V2 blocker)
• Tx for SIADH (Syndrome of Inappropriate ADH secretion)
• Sometimes called aquaretics
• Demeclocycline

Question 21

Name the two GnRH agonists

Answer 21

Leuprolide & Goserelin