Drugs affecting fertility and reproduction 1

Question 1

Estrogens - MoA

Answer 1

Hypertensive effect by increased angiotensinogen synthesis.
Thromboembolic effect by increased hepatic synthesis of clotting factors.
Gallbladder disease by increased cholesterol excretion in bile.

Question 2

Estrogens - Clinical use

Answer 2

Primary hypogonadism, including cases caused by surgical oophorectomy, menopause

Question 3

Estrogens - Contraindications and Special consideration

Answer 3

CONTRAINDICATED: pregnancy, uterine fibroids.

Use with caution if hepatic diseases, endometriosis, thromboembolic diseases, hypercalcemia

Question 4

Estrogens - Adverse effects

Answer 4

Breast tenderness, headache, edema, nausea, vomiting, anorexia, change in libido
HT, thromboembolic disorders, gallbladder disease

Question 5

Conjugated equine estrogens - Clinical use

Answer 5

HRT in postmenopausal women

Estrone can be adm IM

Question 6

Conjugated equine estrogens - Special consideration

Answer 6

Hydrolyzed to estrone and equilin before absorption from the gut.
Converted in the liver to sulfate and glucuronide conjugates

Question 7

Ethinyl estradiol and Mestranol - Clinical use

Answer 7

Oral estrogen-progestin contraceptives
Acne vulgaris
Dysmenorrhea

Question 8

Micronized estradiol and Trandermal estradiol - Clinical use

Answer 8

HRT in postmenopausal women

Question 9

Long-lasting ester of estradiol + Route of adm

Answer 9

Estradiol cypionate and Estradiol valerate

IM: both Oral: estradiol valerate

Question 10

Estradiol valerate - Clinical use

Answer 10

Contraceptive, Heavy or prolonged menstrual bleeding

Question 11

Estrogens

Answer 11

Conjugated eqine estrogens
Ethinyl estradiol
Mestranol
Micronized estradiol
Vaginal estradiol tablets
Estradiol cypionate
Estradiol valerate
Transdermal estradiol

Question 12

Progesterone esters

Answer 12

Suppress ovarian function in the treatment of dysmenorrhea, endometriosis, and uterine bleeding.

In HRT, the progesterone esters are used in combination with estrogens to decrease the incidence of estrogen-induced irregular bleeding and to prevent uterine hyperplasia and endometrial cancer.

Question 13

Progesterone esters - Special consideration

Answer 13

Extend oral bioavailability and half-life of progesterone

Question 14

Esters of progesterone + Route of dam

Answer 14

Megestrol - Oral
Hydroxyprogesterone caproate - IM
Medroxyprogesterone acetate - IM + oral

Question 15

Hydroxyprogesterone caproate - Clinical use

Answer 15

Reduce the risk of preterm delivery in women with a history of at least one spontaneous preterm birth.

Question 16

What is the progestin- only contraceptive?

Answer 16

Medroxyprogesterone acetate

Question 17

Synthetic progestins

Answer 17

Norgestrel
Desogestrel
Norgestimate
Norethindrone
Drospirenone

Question 18

Which synthetic progestin is a spironolactone derivative?

Answer 18

Drospirenone

Question 19

Synthetic progestins - are mostly derivatives of?

Answer 19

nortestosterone

Question 20

Synthetic progestins - MoA

Answer 20

Estrogenic, antiestrogenic and androgenic activities

Question 21

Synthetic progestins - Clinical use

Answer 21

Oral contraceptives

Dysmenorrhea, endometriosis, uterine bleeding

Question 22

Which synthetic progestin has more androgenic activity than other progestins?

Answer 22

Norgestrel

Question 23

Which synthetic progestins has less androgenic and more pro gestational activity?

Answer 23

Desogestrel and Norgestimate

Question 24

Which synthetic progestin has an intermediate androgenic potency?

Answer 24

Norethindrone

Question 25

Which synthetic progestin is an aldosterone antagonist?

Answer 25

Drospirenone

Question 26

Drospirenone - Special considerations

Answer 26

Antiandrogenic effect | Less incidence of weight gain, mood changes and acne

Question 27

Norgrestrel - Adverse effects

Answer 27

Increased incidence of acne, hirsutism, increased libido, oily skin.

Question 28

Drospirenone - Adverse effects

Answer 28

``` Decreased BP (decreased salt and water retention). In contraceptive: 2-3X increased risk of VTE compared to levonorgestrel (but still low risk) ```

Question 29

Estrogen - Progestin contraceptives - MoA

Answer 29

Synergistic suppression of ovulation, by feedback inhibition of GnRH secretion. Estrogen component: Decreased FSH secretion (no maturation of follicle). Progestin component: inhibit LH surge (no ovulation). Delayed maturation of endometrium, development of viscous cervical mucus

Question 30

Estrogen - Progestin contraceptives - Clinical use

Answer 30

Contraceptives Acne vulgaris Dysmenorrhea

Question 31

Estrogen - Progestin contraceptives - Special consideration and Contraindication

Answer 31

For dysmenorrhea: treatment is started some days before menstruation. NSAIDs are alternative treatment for dysmenorrhea. Smokers over 35 years should use other contraceptive methods. Caution if gall bladder disease. CONTRAIND: thromboembolic disease, history of MI, CAD, active liver disease, breast cancer, carcinoma of reproductive tract Reduce incidence of endometrial and ovarian cancer. Does not increase the risk of breast cancer. Low risk of hepatic adenoma

Question 32

Estrogen - Progestin contraceptives - Adverse effects

Answer 32

Hypertension, thromboembolic disorders, gallstones High dose: breast cancer Increases Risk of stroke, MI, DVT Increased Estrogen: breast enlargement, dizziness, dysmenorrhea, edema, headache, irritability, nausea, vomiting, weight gain (cyclic) Decreased Estrogen: Atrophic vaginitis, continuous bleeding, early bleeding, hypomenorrhea, vasomotor symptoms Increased Progestin: Acne, depression, fatigue, hirsutism, libido change, oily skin, weight gain (noncyclic) Decreased Progestin: Dysmenorrhea, hypermenorrhea, late-cycle bleeding

Question 33

Estrogen - Progestin contraceptives - Interactions

Answer 33

Carbemazepine, phenytoin: increased hepatic metabolism of oral contraceptives (may cause contraceptive failure). Antibiotics (penicillins, tetracyclines): Decreased enterohepatic cycling of contraceptives and decreased contraceptive effect. Estrogen cause increased potency of cyclosporine, antidepressants, glucocorticoids + increase antagonize warfarin effect + increased hepatotoxicity of dantrolene

Question 34

Difference between Monophasic and Triphasic estrogen- progestin contraceptives

Answer 34

Monophasic: Same amount of progestin throughout cycle. Triphasic: Increased amount of progestin after 7-14 days

Question 35

Monophasic estrogen-progestin contraceptives + Special considerations

Answer 35

Ethinyl estradiol + levonorgestrel: 84 days continuous use, then 7 inactive tablets. Drospirenone + ethinylestradiol: Available for 21-day and 24-day regimens (latter less rates of contraceptive failure)

Question 36

Ethinyl estradiol + levonorgestrel - Clinical use

Answer 36

Menstrual suppression

Question 37

Extended-cycle preparations contain

Answer 37

Ethinyl estradiol + levonorgestrel

Question 38

Norelgestromin/ethinylestradiol (ortho evra) - Special considerations and Adverse effects

Answer 38

4 week adm cycl. New patch same day each week for 3 weeks, week 4 is patch-free. Less effective in women weighting >198 pounds. Greater incidence of venous thromboembolism than oral contraceptives

Question 39

Progestin-only contraceptives - MoA

Answer 39

Decrease Frequency of GnRH pulse (Decrease LH surge). Thicken & decrease cervical mucus, create a thin, atrophic endometrium that is hostile to implantation of the blastocyst IUD: produces localized effects on the endometrium

Question 40

Progestin-only contraceptives - Clinical use

Answer 40

Suited as contraceptive for smokers, older women, or with contraindication for estrogen

Question 41

Progestin-only contraceptives - Special consideration

Answer 41

Increased Contraceptive failure risk compared to estrogen-progestin contraceptives. Must be taken daily without interruption

Question 42

Progestin-only contraceptives - Adverse effects

Answer 42

Frequent spotting, amenorrhea, increased risk of ectopic pregnancy. Irregular and unpredictable menstrual cycle

Question 43

Progestin-only contraceptives

Answer 43

Norethindrone Medroxyprogesterone Levonorgestrel Ulipristal acetate

Question 44

Medroxyprogesterone acetate - Clinical use

Answer 44

Castration agent in men convicted of pedophilia, serial rape, sex crimes.

Question 45

Emergency contraceptives

Answer 45

Levonorgestrel and Ulipristal acetate

Question 46

Levonorgestrel - Adverse effects

Answer 46

Usually nausea and vomiting (reduced by eg promethazine). | Headache, dizziness, leg cramps, abdominal cramps