Reproduction Drugs

Question 1

Name 4 estradiol esters (steroidal)

Answer 1

Estradiol (valerate and cypionate)
Estrone Sulfate
Equilin Sulfate
quinestrol

Question 2

What is the mechanism and applications of estradiol esters and alkyl estrogens

Answer 2

Absorbed though skin, mucous membranes, GI tract; body wide distribution via sex hormone binding globulin.
Contraception, primary hypogonadism, postemenopausal hormone therapy

Question 3

Name 2 alkyl estrogens

Answer 3

Ethinyl estradiol

Mestranol

Question 4

Name a non-steroidal synthetic estrogen

Answer 4

Diethylstilbestrol (DES)

Question 5

Name a non-steroidal anti estrogen; SERM

Answer 5

Tamoxifen citrate (Nolvadex)

Question 6

name a non-steroidal anti estrogen

Answer 6

Clomiphene citrate (Clomid)

Question 7

How does tamoxifen work and what is it used for?

Answer 7

Blocks estrogen from binding to ER and causing growth in ER+ breast cancers.

Question 8

What are the side effects of tamoxifen?

Answer 8

Pre-estrogenic effect on uterine epithelium increases the risk of endometrial cancers.

Question 9

How does clomiphene citrate work and what is it used for?

Answer 9

Blockes estrogen binding to hypothalamic receptors (no estradiol negative feedback on gonadotropins) –> increased secretion of gonadotropins and LH –> ovulation.
It is used to stimulate ovulation in patients who want to get preggers

Question 10

What are the side effects of clomiphene citrate

Answer 10

Hot flashes, multiple pregnancy

Question 11

Name two natural progesterone products

Answer 11

Micronized progesterone and transvaginal progesterone

Question 12

What is the mechanism and side effects of transvaginal progesteron

Answer 12

Binds to PR; vaginal gel (uterine effects without first pass metabolism and minimal systemic side effects
Fatigue and Drowsiness

Question 13

Name 4 synthetic progesterones

Answer 13

Medroxyprogesterone
norethindrone
norgestrel
Megestrol

Question 14

What are the side effects of synthetic progesterones?

Answer 14

Important: edema, abdominal bloating; less commonly strong androgenic effects (hirsutism, acne)
Others: Anxiety, irritability, depression, muscular pain; increased risk of thrombus and PE

Question 15

What are the applications of all progesterone products?

Answer 15

Contraception and hormone replacement therapy

Question 16

What are the 3 types of combination contraception pills? What are their mechanisms and what are their side effects

Answer 16

Monophasic, Biphasic, and triphasic orthonovum.
COnstant level of estrogen suppresses FSH and LH surge; progesterone suppresses LH surge, thickens cervical mucus and leads to endometrial atrophy.
Side effects are as with synthetic estrogens and progesterones

Question 17

What is the mini-pill? what are its indications and side effects?

Answer 17

It is progestin only.
It is less effective than combo pill but is use in patient with estrogen containdications, good in lactating women (estrogen reduces milk production)
It is more likely to produce irregular menstrual cycle

Question 18

What type of drug is levonogestrel (Plan B) how does it work?

Answer 18

synthetic progestogen.

Prevents implantation

Question 19

What is mifepristone ( RU-486, korlym) how does it work? what are its side effects

Answer 19

Anti-progestin; glucocorticoid receptor antagonist.
Competitively binds to progesterone receptor(leading to detachment of fetus)
Abortion, cushings syndrome

Question 20

What are 3 PDE-5 inhibitors?

Answer 20

Sidenafil citrate (Viagra t0.5 4hrs)
Vardenafil HCl (Levitra t0.5 4hrs)
Tadalafil (Cialis t0.5 17.5hrs)

Question 21

What are the side effects of PDE-5 inhibitors?

Answer 21

Headache, dizziness, change in vision

Question 22

When are PDE-5 inhibitors contarindicated

Answer 22

in patients on nitrates or alpha blockers.

Question 23

What is the mechanism of micronized progesterone and its side effects?

Answer 23

binds to PR; decreades first pass metabolism and enhances dissolution to micronization.
Fatigue and Drowsiness

Question 24

What are the side effects of etrogen products?

Answer 24

Weight gain, HTN; less commonly, may cause breast cancer, DVT, cervical and endometrial cancer.
Nausea breast tension/pain, vaginal bleeding, headache.