Endo & Repro

Question 1

Clomiphene

Answer 1

SERM that selectively inhibits the estrogen receptors of the hypothalamus, inhibiting negative feedback of estrogen on gonadotropin release, leading to upregulation of HPO

Used to induce ovulation

May cause hot flashes, ovarian enlargement, multiple simultaneous pregnancies, and visual disturbances

Question 2

Leuprolide

Answer 2

GnRH analog with agonist properties when used in a pulsatile fashion and antagonist properties when used continuously

Treats infertility (pulsatile), prostate cancer (continuous, used w/ flutamide), uterine fibroids (continuous), precocious puberty (continuous)

Question 3

Ethinyl estradiol, DES, mestranol

Answer 3

Estrogen analogs used to treat hypogonadism or ovarian failure, menstrual abnormalities, post-menopausal symptoms, or androgen-dependent prostate cancer

Increased risk of endometrial cancer and thrombi

Contraindicated in patients with ER+ breast cancer or a history of DVTs

Question 4

Raloxifene

Answer 4

SERM that acts as ER agonist in bone, and ER antagonist in endometrium

Treats osteoporosis

Increased risk of thromboembolic events

Question 5

Tamoxifen

Answer 5

SERM that acts as ER antagonist in breast tissue, and ER agonist in bone and endometrium

Treats ER+ breast cancer

Risk of endometrial cancer, thromboembolic events

Question 6

Anastrazole/exemestane

Answer 6

Aromatase inhibitors

Treat breast cancer in postmenopausal women

Question 7

Progestins

Answer 7

Progesterone analogs; decrease growth and increase vascularization of endometrium

Treat endometrial cancer and abnormal uterine bleeding

Question 8

Mifepristone (RU-486)

Answer 8

Competitive antagonist of PRs

Used with mistoprostol (PGE₁) to terminate pregnancy

Question 9

Danozol

Answer 9

Synthetic androgen that acts as partial agonist at androgen receptors, resulting in hypoestrogenic hyperandrogenic effects

Treats endometriosis and hereditary angioedema

Toxicity: acne, hirsutism, masculinization, edema, decreased HDL levels, hepatotoxicity

Question 10

Flutamide

Answer 10

Nonsteroidal competitive inhibitor of androgens at testosterone receptor

Treats prostate carcinoma

Question 11

Finasteride

Answer 11

5-alpha-reductase inhibitor

Treats BPH and male-pattern baldness

Question 12

Ketoconazole

Answer 12

Inhibits steroid synthesis via inhibition of 17,20-desmolase

Treats Cushing’s syndrome and prevents hirsutism in PCOS

Side effects: gynecomastia, amenorrhea

Question 13

Spironolactone

Answer 13

K⁺-sparing diuretic with antimineralocorticoid and antiandrogen properties. Inhibits aldosterone-binding, 17-alpha-hydroxylase activity, and 17,20-desmolase

Prevents hirsutism in PCOS

Side effects: gynecomastia, amenorrhea

Question 14

Tamuslosin

Answer 14

Selective for a_1A,D receptors (found on prostate) vs. vascular a_1B receptors

Treats BPH without hypotensive effects

Question 15

Sildenafil, vardenafil

Answer 15

Inhibit phosphodiesterase 5, leading to increased cGMP and smooth muscle relaxation in the corpus cavernosum

Treats ED

Toxicity: headache, flushing, dyspepsia, impaired blue-green color vision, life-threatening hypotension when used with nitrates

Question 16

Metformin

Answer 16

Biguanide that increases peripheral glucose uptake (insulin sensitivity), decreases gluconeogenesis, and increases glycolysis.

First-line therapy in T2DM. Can be used in patients without islet function.

Toxicities: Lactic acidosis (contraindicated in renal failure), GI upset

Question 17

Tolbutamide, Chlorpropamide (1st-generation)

Glyburide, Glimepiride, Glipizide (2nd-generation)

Answer 17

Sulfonylureas that increase insulin release by closing K channels in B-cell membrane, leading to depolarization and Ca influx.

Stimulates release of endogenous insluin in T2DM. Requires some islet function so useless in T1DM

Toxicities: hypoglycemia (increased risk in renal failure and with 2nd-generation SUs), disulfiram-like effects (Tolbutamide, Chlorpropamide)

Question 18

Pioglitazone, Rosiglitazone

Answer 18

Glitazones/thiazolidinediones

Bind PPAR-gamma nuclear transcription regulator (increases insulin sensitivity and levels of adiponectin, which is decreased in obesity)

Monotherapy or combined therapy for T2DM

Toxicities: weight gain, edema, hepatotoxicity, HF

Question 19

Acarbose, Miglitol

Answer 19

alpha-glucosidase inhibitors (alpha-glucosidases are located on the intestinal brush border)

Decrease glucose absorption leading to decreased postprandial hyperglycemia

May cause GI disturbances

Question 20

Pramlintide

Answer 20

Amylin analog that decreases gastric emptying and decreases glucagon, which decreases post-prandial spikes in glucose

Amylin is normally co-released with insulin by the B-cells

Treats T1DM and T2DM

Question 21

Exenatide, Liraglutide

Answer 21

GLP-1 analogs that increase insulin and decrease glucagon release

GLP-1 is normally secreted by ileal L-cells in reseponse to carbs, proteins, and lipids

Treat T2DM

Toxicities: pancreatitis

Question 22

Linagliptin, Saxagliptin, Sitagliptin

Answer 22

DPP-4 inhibitors that decrease the normal degredation of incretins such as GLP-1. Results in increased insulin and decreased glucagon release

Treats T2DM

Toxicities: mild UTIs and URIs