Repro-Endo: Pituitary / Hypothalamic Flashcards
1
Q
Leuprolide (Goserelin)
A
- 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
Q
Somatotropin
A
- 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
Q
Octreotide
A
- 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
Q
Bromocriptine, Cabergoline
A
- 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
Q
Desmopressin
A
- 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
Q
Oxytocin
A
- 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
Q
Rx for Women w/ Amenorrhea who desire fertility?
A
Pulsatile Leuprolide
(GnRH agonist –> LH / FSH)
8
Q
Rx for Prostate cancer?
A
Continous Leuprolide
(GnRH agonsit)
9
Q
Rx for Leiomyomas (Smooth Muscle Tumor)?
A
Continuous Leuprolide
(GnRH agonist)
10
Q
Rx for Endometriosis?
A
Continuous Leuprolide
(GnRH agonist)
11
Q
Rx for Precocious Puberty?
A
Continuous Leuprolide
(GnRH agonist)
12
Q
Rx for Dwarfism?
A
Somatotropin
(GH analog)
13
Q
Rx for Wasting a/w AIDS or Malignancy?
A
Somatotropin
(GH analog)
14
Q
Rx for Esophageal varices?
A
Octreotide
(Somatostatin analog)
15
Q
Rx for VIPomas?
A
Octreotide
(Somatostatin analog)
16
Q
Rx for Carcinoid Syndrome?
A
Octreotide
(Somatostatin analog)
17
Q
Rx for Acromegaly?
A
Octreotide
(Somatostatin analog)
18
Q
Rx for Zollinger-Ellison Syndrome?
A
Octreotide
(Somatostatin analog)
19
Q
Rx for Prolactinomas?
A
Bromocriptine, Cabergoline
(Dopamine receptor agonists)
20
Q
Rx for Parkinson Disease?
A
Bromocriptine, Cabergoline
(Dopamine receptor agonists)
21
Q
Rx for Central Diabetes Insipidus?
A
Desmopressin
(Vasopressin analog: ADH)
22
Q
Rx for von Willebrand Disease?
A
Desmopressin
(Vasopressin analog: ADH)
23
Q
Rx for Inducing labor and Stimulating Breast Milk?
A
Oxytocin
(Posterior Pituitary Hormone)
24
Q
Demeclocycline
A
- 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
31
Rx for Hirsuitism in Women?
* **Spironolactone** and **Cyproterone Acetate**
* Weak antagonists at androgen receptor
* Spironolactone is also a weak inhibitor of Testosterone production
32
Rx for Benign Prostatic Hyperplasia (BPH)?
* **Finasteride, Dutasteride, PDE5 inhibitors**
* **Finasteride** Blocks Type II (prostate specific) 5α-reductase and prevents the conversion of Testosterone to DHT
* Also approved for the Tx of Male Patterend Baldness
* **Dutasteride** blocks both Type I and Type II forms of 5α-reductase --\> works in all tissues.
* **PDE5 inhibitors** - relax smooth muscle in the Urogenital tract and be be used to Tx BPH
33
Sildenafil
* Inhibits Phosphodiesterase 5 (PDE5) that is expressed in the Genital tissue
* PDE5 causes the hydrolysis of cGMP, Sildenafil causes a large increase in cGMP --\> enhanced and prolonged erection
* Nerves must be initially functional for Sildenafil to work
* Se: Priapism (long erection), Hypotension
* Sildenafil may increase the risk of Melanomas
34
Alprostadil
* A Prostaglandine E1 agonist
* Simulate a PGE1 receptor and cause an increase in cAMP
* Cyclic AMP also causes a relaxation of Cavernosal Smooth muscle and causes erection w/out functional neurons
* Must be injected
35
Papavarine
* Non-selective Phosphodiesterase Inhibitor that inhibits that breakdown of both cGMP
* Injected directly into the Penis
36
Phentolamine
* Nonselective Alpha adrenergic receptor agonsit
* Prevents NorEpi from causing Constrction of Arterioles supplying blood to the Corpor Cavernosa
- -\> Promotes erection
* Injected directly into the Penis
