Fertility and reproduction drugs

Estradiol MOA

most predominant estrogen in the human body

Estradiol primary indication

• oral contraception

• treatment of primary hypogonadism

• treatment as hormone therapy in post-menopausal women

Estradiol side effects / notable aspects

• Estrogen has many formulations (transdermal, oral)

• hypertension

• thromboembolic disorders

• gallbladder disease

• giving estrogen along as HRT increases risk of endometrial cancer

Norethidrone MOA

progesterone formulation

• used to suppress ovarian function

Norethidrone primary indication

• oral contraception

• treatment of dysmenorrhea, endometriosis, uterine bleeding

• used in HRT to prevent uterine hyperplasia and reduce risk of endometrial cancer

Norethidrone side effects/notable aspects

• HRT with both estrogen + progesterone is recommended as first option, followed by decreasing dose of estrogen gradually

• HRT should not be used in women with endometrial cancer/breast cancer history

Etonogestrel/ethinyl estradiol vaginal ring (Nuvaring) MOA

• progesterone/estrogen combination

• estrogen - reduce FSH secretion

• progesterone - inhibits the midcycle LH surge required for ovualtion

Nuvaring primary indication

• contraception

• treatment of acne vulgaris

• treatment of dysmenorrhea

Nuvaring notable aspects

• inserts for 3 weeks

• removed for 1 week during which women will have normal menstrual cycle

Etongestrel implant (Nexplanon) MOA

progesterone only

Nexplanon primary indication

contraception

Nexplanon side effects/notable aspects

• implant approved up to 5 years

• progestin-only contraceptives suited for women who smoke, are older, and women whom estrogen is contraindicated

Depoprovera

progesterone only medication that is an injection every 3 months

Drospirenone and ethinyl estradiol (Yasmin)

progesterone/estrogen combination

• estrogen - reduces FSH secretion

• progesterone - inhibits the midcycle LH surge required for ovulation

Yasmin primary indication

• oral contraception

• treatment of acne vulgaris

• treatment of dysmenorrhea

Yasmin side effects / notable aspects

• available as 21 day or 24 day hormone regimen

• estrogen can produce side effects

• Drospirenone is an aldosterone antagonist with a weak antiandrogenic effect

• beware of interactions with drugs that increase hepatic metabolism of OCPs

Copper intrauterine device (Paragard) MOA

alters the viability and transport of both sperm and ovum, thus preventing pregnancy before fertilization

Paragard primary indication

contraception

Paragard notable aspect

can be used for up to 10 years

Levonorgestrel intrauterine device (Mirena) MOA

• progesterone

• prevent pregnancy by producing localized effects on endometrium

Mirena primary indication

contraception

Mirena notable aspect

can be used for up to 8 years

levonorgestrel (Plan B)

• progesterone formulation

• prevents fertilization by inhibition of ovulation

• unlikely to prevent implantation of a fertilized egg

Plan B primary indication

emergency contraception

Plan B side effects

nausea and vomiting

Clomiphene MOA

• weak estrogen agonist and moderate estrogen antagonist

• blocks estrogen receptors in the hypothalamus and pituitary, preventing estrogen feedback inhibition on gonadotropin secretion

• leads to an increase in FSH and LH

Clomiphene primary indication

treats anovulatory infertility

Clomiphene notable aspects

5-7% of women treated with Clomiphene have multiple births

Tamoxifen MOA

• prodrug that is absorbed form the gut and converted to active metabolites

• breast tissue - acts as estrogen receptor antagonist

Tamoxifen primary indication

used for prevention and treatment for breast cancer (tumor cells are estrogen receptor positive)

Tamoxifen side effects

can lead to increased risk of endometrial cancer

Mifepristone MOA

• glucocorticoid receptor antagonist AND

• progesterone receptor antagonist

• causes endometrial degeneration, leading to detachment of the blastocyst

Mifepristone primary indication

medical termination of pregnancy

Mifepristone side effects / notable aspects

after administration, followed up by giving a prostaglandin (misoprostol) 48 hours later to stimulate uterine contractions

• nausea, vomiting

Raloxifene MOA

• estrogen agonist effect on bone

• estrogen antagonist effect on breast

Raloxifene primary indication

used for prevention of osteoporosis and reduction of risk of breast cancer

Finasteride MOA

• 5-alpha-reductase inhibitors

• reduced DHT synthesis

Finasteride primary indication

• treats symptomatic BPH

• used to treat male pattern baldness

Finasteride side effect

erectile dysfunction

Flutamide MOA

androgen receptor antagonist

Flutamide primary indication

treats inoperable prostate cancer alongside GnRH analogs