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USMLE Step 1 > Repro Drugs > Flashcards

Repro Drugs Flashcards

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USMLE® Step 1 flashcards
1
Q

Leuprolide: Mechanism

A

GnRH analog with agonist properties when used in a pulsatile fashion.
ANTAGONIST when used in a continuous fashion (downregulates GnRH receptor in pituitary –> decreased FSH/LH)

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2
Q

Leuprolide: Clinical Use

A

Pulsatile – infertility

Continuous – Prostate cancer, Uterine fibriouds, Precocious puberty

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3
Q

For prostate cancer, use continuous or pulsatile leuprolide? Also, with what other drug

A

Treat prostate cancer with continuous leuprolide and co-administer with flutamide (competitive inhibitor of androgens)

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4
Q

Leuprolide: Toxicity

A

Antiandrogen, nausea, vomiting

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5
Q

Testosterone, Methyltestosterone: Mechanism

A

Agonist at androgen receptors

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6
Q

Testosterone: Clinical Use

A

Treats hypogonaidism and promotes development of secondary sex characteristics; stimulation of anabolism to promote recovery after burn or injury

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7
Q

Testosterone: Toxicity

A

Causes masculinization in females; reduces intratesticular testosterones in males by inhibiting release of LH (via negative feedback), leading to gonadal atrophy. Premature closure of epiphyseal plates.

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8
Q

Testosterone effect on cholesterol

A

Increased LDL; Decreased HDL

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9
Q

Enzyme for conversion of testosterone to DHT

A

5-alpha reductase. DHT is more potent than testosterone

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10
Q

Finasteride

A

5-alpha reductase inhibitor (decreases conversion of testosterone to DHT).

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11
Q

Finasteride Uses

A

Useful for BPH (as DHT is primary mediator that causes hyperplasia in prostate). Also promotes hair growth - used to treat male pattern baldness

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12
Q

Flutamide

A

A non steroidal competitive inhibitor of androgens at the testosterone receptor. Used in prostate carcinoma.

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13
Q

Ketoconazole

A

Inhibits steroid synthesis (inhibits 17, 20 desmolase).

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14
Q

Spironolactone

A

Inhibits steroid binding.

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15
Q

Rx for polycystic ovarian syndrome to prevent hirsuitism

A

Spironolactone and Ketoconazole. Can cause gynecomastia and amenorrhea

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16
Q

Estrogens - name them

A

Ethinyl, Estradiol, DES, mestranol

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17
Q

Estrogen: Mechanism

A

Bind estrogen receptors

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18
Q

Estrogen: Clinical Use

A

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

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19
Q

Estrogen: Toxicity

A

Increased risk of endometrial cancer

  • bleeding in postmenopausal women
  • clear cell adenocarcinoma of vagina in females exposed to DES in utero
  • increased risk of thrombi
20
Q

Contraindications of Estrogen use

A
  • ER-positive breast cancer

- history of DVTs

21
Q

Selective Estrogen Receptor Modulators (SERMs)

A

Clomiphene, Tamoxifen, Raloxifene

22
Q

Clomiphine

A

SERM - partial agonist at estrogen receptors in hypothalamus.
Prevents normal feedback inhibition and increases release of LH and FSH from pituitary which stimulates ovulation

23
Q

Clomiphine: Use

A

Treat infertitility and polycystic ovarian syndrome. May cause hot flashes, ovarian enlargement. Multiple simultaneous pregancies, and visual disturbances

24
Q

Raloxifene

A

SERM. Agonist on bone; Reduces resorption of bone; Used to treat osteoporosis.

25
Q

Tamoxifen

A

Antagonist at breast tissue; Used to treat and prevent recurrence of ER-positive breast cancer.

26
Q

Hormone replacement therapy

A

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

27
Q

Discuss risks of HRT of cancer, CV dises

A

Unopposed estrogen replacement therapy (ERT increases risk of endometrial cancer, so progesterone is added. Possible INCREASED CV risk

28
Q

Anastrozole/ Exemestane

A

Aromatase inhibitors used in postmenopausal women with breast cancer

29
Q

Progestins : Mechanism

A

Bind progesterone receptors, reduce growth and increase vascularization of endometrium.

30
Q

Progestin: Clinical Use

A

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

31
Q

Mifepristone (RU-486): Mechanism

A

Competitive inhibitor of progestins at progesterone receptors

32
Q

Mifepristone (RU-486): Clinical Use

A

Termination of pregnancy. Administered with misprostol (PGE1)

33
Q

Mifepristone (RU-486): Toxicity

A

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

34
Q

Oral contraception (synthetic progestins, estrogen)

A

Estrogen and progestins inhibit LH/FSH and thus prevent estrogen surge. No estrogen surge –> no LH surge –> no ovulation

35
Q

Discuss progestins and pregnancy prevention

A

Progestins cause thickening of cervical mucus, thus limiting access of sperm to uterus. Also inhibit endometrial proliferation, thus making endometrium less suitable for implantation of an embryo.

36
Q

Contraindications of OCP

A

Smokers > 35 y.o
Increased risk of CV events
Patients with a hx of thromboembolism and stroke or hx of estrogen dependent tumor

37
Q

Terbutaline

A

B2 agonist that relaxes the uterus; reduces premature uterine contractions

38
Q

Tamsulosin

A

Alpha 1 antagonist used to treat BPH by inhibiting smooth muscle contraction. Selective alpha 1AD receptors (found on prostate) vs. vascular alpha 1 B receptors `

39
Q

Sildenafil, vardenafil

A

Phosphodiesterase inhibitors

40
Q

Sildenafil, Vardenafil: Mechanism

A

Inhibit phosphodiesterase 5, causing increase in cGMP smooth muscle relaxation in the corpus canvernosum, increased blood flow and penile erection

41
Q

Sildenafil, Vardenafil: Clinical Use

A

Treatment of erectile dysfunction

42
Q

Sildenafil, Vardenafil: Toxicity

A

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

“Hot and sweaty”, but then “Headache”, “Heartburn, “Hypotension”

43
Q

Danazol: Mechanism

A

Synthentic androgen that acts as partial agonist at androgen receptors.

44
Q

Danazol: Clinical Use

A

Endometriosis and hereditary angiodema

45
Q

Danazol: Toxicity

A

Weight fain, edema, acne, hirsuitism, masculinization. Decreased HDL levels, hepatotoxicity

USMLE Step 1 (34 decks)

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