Endo & Repro Flashcards
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
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)
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
Raloxifene
SERM that acts as ER agonist in bone, and ER antagonist in endometrium
Treats osteoporosis
Increased risk of thromboembolic events
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
Anastrazole/exemestane
Aromatase inhibitors
Treat breast cancer in postmenopausal women
Progestins
Progesterone analogs; decrease growth and increase vascularization of endometrium
Treat endometrial cancer and abnormal uterine bleeding
Mifepristone (RU-486)
Competitive antagonist of PRs
Used with mistoprostol (PGE1) to terminate pregnancy
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
Flutamide
Nonsteroidal competitive inhibitor of androgens at testosterone receptor
Treats prostate carcinoma
Finasteride
5-alpha-reductase inhibitor
Treats BPH and male-pattern baldness
Ketoconazole
Inhibits steroid synthesis via inhibition of 17,20-desmolase
Treats Cushing’s syndrome and prevents hirsutism in PCOS
Side effects: gynecomastia, amenorrhea
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
Tamuslosin
Selective for a1A,D receptors (found on prostate) vs. vascular a1B receptors
Treats BPH without hypotensive effects
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
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
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)
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
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
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
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
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
