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Pharmacology > FA Reproductive > Flashcards

FA Reproductive Flashcards

1
Q

Leuprolide Mechanism

A

GnRH analog with agonist properties when used in pulsatile fashion; antagonist properties when used in continuous fashion (downregulates GnRH receptor in pituitary → ↓ FSH/LH).

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2
Q

Leuprolide Use

A

Infertility (pulsatile), prostate cancer (continuous - use with flutamide), precocious puberty (continuous).

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3
Q

Leuprolide Toxicity

A

Antiandrogen, nausea, vomiting.

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4
Q

Estrogens

A

Ethinyl estradiol, DES, mestranol

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5
Q

Estrogen Mechanism

A

Bind estrogen receptors

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6
Q

Estrogen Use

A

Hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women; use in men with androgen-dependent prostate cancer.

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7
Q

Estrogen Toxicity

A

↑ risk of endometrial cancer, bleeding in postmenopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, ↑ risk of thrombi. Contraindications - ER + breast cancer, history of DVTs.

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8
Q

Selective estrogen receptor modulators (SERMs)

A

Clomiphene, Tamoxifen, Raloxifene

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9
Q

Clomiphene Mechanism

A

Antagonist at estrogen receptors in hypothalamus. Prevents normal feedback inhibition and ↑ release of LH and FSH from pituitary, which stimulates ovulation.

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10
Q

Clomiphene Use

A

Treatment of infertility due to anovulation (e.g., PCOS).

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11
Q

Clomiphene Toxicity

A

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

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12
Q

Tamoxifen Mechanism

A

Antagonist on breast tissue; agonist at uterus, bone.

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13
Q

Tamoxifen Use

A

Primarily used to treat and prevent recurrence of ER + breast cancer.

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14
Q

Tamoxifen Toxicity

A

Associated with endometrial cancer, thromboembolic events.

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15
Q

Raloxifene Mechanism

A

Agonist on bone; antagonist at uterus.

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16
Q

Raloxifene Use

A

↓ resorption of bone → used to treat osteoporosis.

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17
Q

Raloxifene Toxicity

A

↑ risk of thromboembolic events

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18
Q

Anastrozole, Exemestane Mechanism

A

Aromatase inhibitors used in postmenopausal women with breast cancer

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19
Q

Anastrozole, Exemestane Use

A

Used in postmenopausal women with breast cancer

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20
Q

Hormone Replacement Therapy Use

A

Used for relief or prevention of menopausal symptoms (e.g., hot flashes, vaginal atrophy) and osteoporosis (↑ estrogen, ↓ osteoclast activity).

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21
Q

Hormone Replacement Therapy TOxicity

A

Unopposed estrogen replacement therapy (ERT) ↑ the risk of endometrial cancer, so progesterone is added. Possible increased cardiovascular risk.

22
Q

Progestin Mechanism

A

Bind progesterone receptors, ↓ growth and ↑ vascularization of endometrium.

23
Q

Progestin Use

A

Used in oral contraceptives and in the treatment of endometrial cancer and abnormal uterine bleeding.

24
Q

Mifepristone (RU-486) Mechanism

A

Competitive inhibitor of progestins at progesterone receptors.

25
Q

Mifepristone (RU-486) Use

A

Termination of pregnancy. Administered with misoprostol (PGE1)

26
Q

Mifepristone (RU-486) Toxicity

A

Heavy bleeding, GI effects (nausea, vomiting, anorexia), abdominal pain.

27
Q

Oral Contraception

A

Synthetic progestins, estrogen

28
Q

Oral Contraception Mechanism

A

Estrogen and progestins inhibit LH/FSH and thus prevent estrogen surge. No estrogen surge → no LH surge → no ovulation.
Progestins cause thickening of the cervical mucus, thereby limiting access of sperm to uterus. Progestins also inhibit endometrial proliferation, thus making endometrium less suitable for the implantation of an embryo.

29
Q

Oral Contraception Toxicity

A

Contraindications - smokers > 35 years old (↑ risk of cardiovascular events), patients with history of thromboembolism and stroke or history of estrogen-dependent tumor.

30
Q

Terbutaline Mechanism

A

β2-agonist that relaxes the uterus

31
Q

Terbutaline Use

A

Used to ↓ contraction frequency in women during labor.

32
Q

Danazol Mechanism

A

Synthetic androgen that acts as partial agonist at androgen receptors.

33
Q

Danazol Use

A

Endometriosis and hereditary angioedema.

34
Q

Danazol Toxicity

A

Weight gain, edema, acne, hirsutism, masculinization, ↓ HDL levels, hepatotoxicity.

35
Q

Testosterone, Methyltestosterone Mechanism

A

Agonist at androgen receptors.

36
Q

Testosterone, Methyltestosterone Use

A

Treats hypogonadism and promotes development of 2° sex characteristics; stimulation of anabolism to promote recovery after burn or injury.

37
Q

Testosterone, Methyltestosterone Toxicity

A

Causes masculinization in females; ↓ intratesticular testosterone in males by inhibiting release of LH (via negative feedback) → gonadal atrophy. Premature closure of epiphyseal plates. ↑ LDL, ↓ HDL.

38
Q

Antiandrogens

A

Finasteride, flutamide, ketoconazole, spironolactone

39
Q

Finasteride Mechanism

A

5α-reductase inhibitor (↓ conversion of testosterone to DHT).

40
Q

Finasteride Use

A

Useful in BPH. Also promotes hair growth - used to treat male-pattern baldness.

41
Q

Flutamide Mechanism

A

A nonsteroidal competitive inhibitor of androgens at the testosterone receptor.

42
Q

Flutamide Use

A

Used in prostate carcinoma.

43
Q

Ketoconazole Mechanism [Antiandrogen]

A

Inhibits steroid synthesis (inhibits 17,20-desmolase).

44
Q

Spironolactone Mechanism [Antiandrogen]

A

Inhibits steroid binding, 17α-hydroxylase, and 17,20-desmolase.

45
Q

Ketoconazole, Spironolactone Toxicity [Antiandrogen]

A

Gynecomastia and amenorrhea.

46
Q

Ketoconazole Use [Antiandrogen]

A

Treatment of polycystic ovarian syndrome to prevent hirsutism.

47
Q

Spironolactone Use [Antiandrogen]

A

Treatment of polycystic ovarian syndrome to prevent hirsutism.

48
Q

Tamsulosin Mechanism

A

α1-antagonist used to treat BPH by inhibiting smooth muscle contraction. Selective for α1A,D receptors (found on prostate) vs. vascular α1B receptors.

49
Q

Sildenafil, Vardenafil Mechanism

A

Inhibit phosphodiesterase 5, causing ↑ cGMP, smooth muscle relaxation in the corpus cavernosum, ↑ blood flow, and penile erection.

50
Q

Sildenafil, Vardenafil Use

A

Treatment of erectile dysfunction.

51
Q

Sildenafil, Vardenafil Toxicity

A

Headache, flushing, dyspepsia, impaired blue-green color vision. Risk of life-threatening hypotension in patients taking nitrates.

Pharmacology (14 decks)

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