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Pharmacology > Reproductive > Flashcards

Reproductive Flashcards

1
Q

Leuprolide (mechanism, use [5])?

A

Mechanism:

  • GnRH analog
  • Agonist when used pulsatile
  • Antagonist when used continuously (down regulates GnRH receptors in pituitary → ↓ FSH/LH

Use:

  • Uterine fibroids
  • Endometriosis
  • Precocious puberty
  • Prostate cancer
  • Infertility (agonist)
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2
Q

Estrogens agonists (names, mechanism, use [3])?

A

Names: Ethinyl estradiol, DES, Mestranol
Mechanism: Agonist at estrogen receptors
Use:
- Hypogonadism or Ovarian failure
- Hormone replacement therapy in postmenopausal women
- Men with androgen-dependent prostate cancer

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3
Q

Ethinyl estradiol, DES, Mestranol (adverse effects [4], contraindications [2])?

A

AEs:

  • Increased risk of endometrial cancer
  • Bleeding in postmenopausal women
  • Clear cell adenocarcinoma of vagina in females exposed to DES in utero
  • Prothrombotic

Contraindications:

  • ER + breast cancer
  • History of DVTs
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4
Q

Selective Estrogen Receptor Modulators (SERMs)?

A

Clomiphene, Tamoxifen, Raloxifene

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5
Q

Clomiphene (mechanism, use, adverse effects [4])

A

Mechanism:
Estrogen receptor antagonist at hypothalamus → Prevents normal feedback inhibition → ↑ LH and FSH release → Stimulates ovulation

Use:
Infertility due to anovulation (PCOS)

AEs:

  • Hot flashes
  • Ovarian enlargement
  • Multiple simultaneous pregnancies
  • Visual disturbances
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6
Q

Tamoxifen (mechanism, use, adverse effects)

A

Mechanism:
Estrogen receptor antagonist at breast; agonist at bone and uterus

Use:
Prevents recurrence of and treats ER/PR + breast cancer

AEs:
↑ risk of thromboembolic events and endometrial cancer

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7
Q

Raloxifene (mechanism, use, adverse effects)

A

Mechanism:
Estrogen receptor antagonist at breast and uterus; agonist at bone

Use:
Treats osteoporosis

AEs:
↑ risk of thromboembolic events but no increased risk of endometrial cancer (vs. tamoxifen)

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8
Q

Aromatase inhibitors (names)

A

Anastrozole, letrozole, exemastane

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9
Q

Anastrozole, letrozole, exemastane (mechanism and use)?

A

Mechanism: Inhibit peripheral conversion of androgens to estrogen
Use: ER + breast cancer in postmenopausal women

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10
Q

Hormone replacement therapy (all)?

A
  • Relief/prevention of menopausal symptoms (hot flashes, vaginal atrophy)
  • Osteoporosis (since ↑ estrogen causes ↓ osteoclast activity)

Note: Unopposed estrogen replacement therapy ↑ risk of endometrial cancer so progesterone added.

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11
Q

Anastrozole (class)?

A

Aromatase inhibitor

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12
Q

Letrozole (class)?

A

Aromatase inhibitor

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13
Q

Exemastane (class)?

A

Aromatase inhibitor

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14
Q

Levonorgestrel (class)?

A

Progestin

* -gest-

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15
Q

Medroxyprogesterone (class)?

A

Progestin

* -gest-

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16
Q

Etonogestrel (class)?

A

Progestin

* -gest-

17
Q

Norethindrone (class)?

A

Progestin

* Nor ethinyl!!!

18
Q

Megestrol (class)?

A

Progestin

* -gest-

19
Q

Progestins (mechanism, use [3])?

A

Mechanism:
Bind progesterone receptors → ↓ growth and ↑ vascularization of endometrium + thickens cervical mucus

Use:

  • Contraception (pill, IUD, etc.)
  • Endometrial cancer
  • Abnormal uterine bleeding
20
Q

Progestin challenge?

A

Give to patient with amenorrhea to determine cause.

Remember, estrogen causes growth of endometrium. It is the giving and removing of progesterone that induces menses.

Suppose you are suspicious of Asherman syndrome. Give progesterone and remove.
- If withdrawal bleeding occurs, you know they don’t have that because they grew a thickened endometrium.

Suppose you are suspicious of anovulation due to low levels of estrogen. Without estrogen, there will be no growth of endometrium.
- If withdrawal bleeding occurs here, you know they have sufficient estrogen on board because they grew a thickened endometrium.

21
Q

Mifepristone (class, mechanism, use)

A

Class: Antiprogestin (*prissy)
Mechanism: Competitive inhibitor of corpus luteum progestins at progesterone receptor
Use: Termination of pregnancy (mifepristone + misoprostol to ensure detached blastocyst is expelled)

22
Q

Ulipristal (class, mechanism, use)

A

Class: Antiprogestin (*prissy)
Mechanism: Competitive inhibitor of corpus luteum progestins at progesterone receptor
Use: Emergency contraception

23
Q

Combined contraception (contents, mechanisms [3], contraindications [4])

A

Contents: Progestins + Ethinyl estradiol (pill, patch, ring)
Mechanism:
- Estrogen and Progestin inhibit LH + FSH and thus prevent estrogen release → no LH surge → no ovulation
- Progestins cause thickening of cervical mucus, thereby limiting access of sperm to uterus
- Progestins inhibit endometrial proliferation so endometrium is less suitable for implantation of embryo

Contraindications:

  • Smokers > 35 yo (↑ risk of cardiovascular events)
  • Patients with ↑ risk of cardiovascular disease
    * History of thromboembolism
    * CAD
    * Stroke
  • Migraine
  • Breast cancer
24
Q

Copper IUD (mechanism, use [2], adverse effects [3])?

A

Mechanism:
Produces local inflammation toxic to sperm and ova, preventing fertilization and implantation; hormone free

Use:

  • Long-acting reversible contraception
  • Most effective emergency contraception

AEs:

  • Heavier menses
  • Dysmenorrhea
  • Risk of PID with insertion
25
Q

Terbutaline (mechanism, use)

A

Mechanism:
Beta-2 agonists that relax the uterus

Use: ↓ contraction frequency in women during (premature) labor

26
Q

Ritodrine (mechanism, use)

A

Mechanism: Beta-2 agonists that relax the uterus

Use: ↓ contraction frequency in women during (premature) labor

27
Q

Danazol (mechanism, use [2], adverse effects [7])

A

Mechanism: Androgen that acts as a partial agonist at androgen receptors

Use: Endometriosis and Hereditary angioedema

AEs:

  • Weight gain
  • Edema
  • Acne
  • Hirsutism
  • Masculinization
  • ↓ HDL
  • Hepatotoxicity
28
Q

Testosterone, Methyltestosterone (mechanism, use [2], adverse effects [4])?

A

Mechanism: Agonist at androgen receptors
Use:
- Treat hypogonadism to promote development of secondary sex characteristics
- Stimulate anabolism to promote recovery from burn or injury
AEs:
- Masculinization in females
- Inhibits release of LH → gonadal atrophy in males + ↓ intratesticular testosterone
- Premature closure of epiphyseal plates
- ↑ LDL, ↓ HDL

29
Q

Finasteride (class, mechanism, use [2])?

A

Class: Antiandrogen
Mechanism: Inhibits 5α-reductase → ↓ conversion of testosterone to DHT
Use: BPH and Male pattern baldness
*Old men must have too much DHT on board because they get both of these!

30
Q

Flutamide (class, mechanism, use)?

A

Class: Antiandrogen
Mechanism: Nonsteroidal competitive inhibitor at androgen receptor
Use: Prostate carcinoma

31
Q

Ketoconazole (class, mechanism, use, adverse effects [2])?

A

Class: Antiandrogen
Mechanism: Inhibits steroid synthesis by inhibiting 17,20-desmolase
Use: Reduces androgenic symptoms in PCOS
AEs: Gynecomastia (males); Amenorrhea (females)

32
Q

Spironolactone (class, mechanism [3], use, adverse effects [2])?

A 
Class: Antiandrogen
Mechanism: 
- Inhibits steroid binding
- Inhibits 17α-hydroxylase
- Inhibits 17,20-desmolase
Use: Reduces androgenic symptoms in PCOS
AEs: Gynecomastia (males); Amenorrhea (females)
33
Q

Tamsulosin (mechanism, use)?

A

Mechanism: Selectively antagonizes α1-A,D receptors on prostate and NOT α1-B receptors on vasculature
Use: BPH by inhibiting smooth muscle constriction (of the prostate around the urethra)

34
Q

Sildenafil, Vardenafil, Tadalafil (class, mechanism)?

*Read the whole answer!!!

A

Class: PDE-5 inhibitors
Mechanism: Inhibit PDE-5 breakdown of cGMP → ↑ cGMP → prolonged smooth muscle relaxation via NO → ↑ blood flow to corpus cavernosum of penis + ↓ pulmonary vascular resistance

35
Q

Sildenafil, Vardenafil, Tadalafil (use [3], adverse effects [5])?

A 
Use: 
- Erectile dysfunction
- Pulmonary hypertension
- BPH (Tadalafil ONLY)
AEs:
- Headache
- Flushing
- Dyspepsia
- Cyanopia (blue-tinted vision) *Viagra is the little blue pill patients always ask about*
- Life-threatening hypotension in patients taking nitrates!!!

*Hot and sweaty, but then Headache, Heartburn, and Hypotension

36
Q

Minoxidil (mechanism, use [2])?

A

Mechanism: Direct arteriolar vasodilator
Use:
- Androgenetic alopecia
- Severe, refractory hypertension

Pharmacology (5 decks)

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