Endocrine

Question 1

Glitazones/ Thaiazolidinediones

Pioglitazone

Answer 1

MOA:
-Reduce insulin resistance, by binding to peroxisome proliferator activated receptor gamma (PPAR-gamma); requires alteration of in gene transcription and in protein synthesis (takes days-weeks)

Use:
-Glucose lowering agent

Tox:

• Fluid retention
• Wt gain (from fluid)
• Precipitation of CHF

Question 2

Flutamide

Answer 2

MOA:
-Non-steroid anti-androgen that competes with testosterone and DHT for testosterone receptors.

Use:
-Tx of prostate cancer in combination with GnRH agonists

Question 3

Leuprolide
Goserelin
Nafarelin
Histrelin

Answer 3

MOA:

• GnRH agonists that bind to GnRH receptors in the anterior pituitary and inhib synth of LH & FSH, if administered continuously.
• Decreased amt of LH leads to decreased Leydig cell stimulation and diminished testosterone synth.
• 1st see a transient increase, then decrease in both testosterone and DHT levels

Use:
-Enlarged prostate (cancer)

Question 4

Anastrozole

Answer 4

MOA:
-A nonsteroidal aromatase inhib which blocks estrogen production selectively

Use:
-An effected tx. for post menopausal women with breast cancer in whom the greatest source of estrogen is the conversion of androstenedione (produced in adrenal gland) to estrone (in liver, muscle, and fat) through aromatization

Question 5

SGLT2 inhibitors:
Canagliflozin
Dapagliflozin

Answer 5

MOA:
-Oral anti-diabetic agents that decrease proximal tubular resorption of glucose, thereby promoting urinary glucose loss

Use:
-DT2

Tox:

• Must monitor serum Cr b4 and after initiating therapy
• UTI and Genital mycotic infection due to glucosuria

Question 6

Ketoconazole

Answer 6

MOA:

-Anti-fungal that decreases androgen synthesis by inhibiting multiple enzyme pathways

Question 7

Tamoxifen

Answer 7

MOA:

• In breast tissue it antagonizes the estrogen R’s
• Partial agonist effect in bone, endometrium, and cardio tissues as well as procoag effects

Use:
-An adjuvant therapy for estrogen R positive breast cancer

Tox:

• DVT
• Thromboembolism
• Endometrial cancer

Question 8

Trastuzumab

Answer 8

MOA:

-Inhib of EGF and HER2/neu pathways, thereby leading to apoptosis of breast cancer cells

Question 9

Potassium Iodide

Answer 9

MOA:

-May prevent thyroid absorption of radioactive iodine isotopes by competitive inhibition.

Question 10

Tx’s for nephrogenic DI

Answer 10

HTZ–> has a paradoxical antidiuretic effect

Indomethacin–> increases water absorption by decreasing prostaglandin synthesis (PGE inhib’s ADH)

Question 11

Metyrapone

Answer 11

MOA:

-Inhibits last step of cortisol synthesis by blocking effects of 11-beta-hydroxylase.

Question 12

Drugs that decrease peripheral conversion of T4–>T3

Answer 12

• Propylthiouracil

- Beta blockers