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Flashcards in Endo & Repro Deck (22):
1

Clomiphene

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

2

Leuprolide

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)

3

Ethinyl estradiol, DES, mestranol

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

4

Raloxifene

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

Treats osteoporosis

Increased risk of thromboembolic events

5

Tamoxifen

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

6

Anastrazole/exemestane

Aromatase inhibitors

Treat breast cancer in postmenopausal women

7

Progestins

Progesterone analogs; decrease growth and increase vascularization of endometrium

Treat endometrial cancer and abnormal uterine bleeding

8

Mifepristone (RU-486)

Competitive antagonist of PRs

Used with mistoprostol (PGE1) to terminate pregnancy

9

Danozol

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

10

Flutamide

Nonsteroidal competitive inhibitor of androgens at testosterone receptor

Treats prostate carcinoma

11

Finasteride

5-alpha-reductase inhibitor

Treats BPH and male-pattern baldness

12

Ketoconazole

Inhibits steroid synthesis via inhibition of 17,20-desmolase

Treats Cushing's syndrome and prevents hirsutism in PCOS

Side effects: gynecomastia, amenorrhea

 

13

Spironolactone

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

14

Tamuslosin

Selective for a1A,D receptors (found on prostate) vs. vascular a1B receptors

Treats BPH without hypotensive effects

15

Sildenafil, vardenafil

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

16

Metformin

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

17

Tolbutamide, Chlorpropamide (1st-generation)

Glyburide, Glimepiride, Glipizide (2nd-generation)

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)

18

Pioglitazone, Rosiglitazone

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

19

Acarbose, Miglitol

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

Decrease glucose absorption leading to decreased postprandial hyperglycemia

May cause GI disturbances

20

Pramlintide

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

21

Exenatide, Liraglutide

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

22

Linagliptin, Saxagliptin, Sitagliptin

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