Progestins, Estrogens and Androgens Flashcards
Estradiol
- Estrogens
- Rapidly inactivated when given orally - Prevent ovulation by inhibiting pituitary and hypothalamus, decrease amount and increase viscosity of cervical mucus
- Contraception
Ethinyl estradiol
- Estrogens
- Prevent ovulation by inhibiting pituitary and hypothalamus, decrease amount and increase viscosity of cervical mucus
- Nausea, headaches, CV effects, decreased glucose tolerance, weight gain
- Combination OCP (continuous or discontinuous), ovarian dysfunction, PM symptoms
Tamoxifen
- SERMs
- Breast antagonist, agonist at other tissues (Raloxifene neutral at endometrium/vagina)
- Estrogen dependent breast cancer, relief of PM symptoms, osteoporosis
Ospemifene
- SERMs
- Breast antagonist, agonist at other tissues, neutral at endometrium
- Breast cancer, vaginal atrophy
Clomiphene
Fluvestrant
- Estrogen receptor antagonists
- Give in early follicular phase to antagonize inhibitory effects of estrogen on pituitary and hypothalamus
- Ovulation induction
Anastrozole (non-steroid)
Exemestane (steroid)
- Aromatase inhibitors
- Inhibit conversion of androgens to estrogens
- Hot flashes, effects on plasma lipids and bone resorption
- Breast cancer, ovulation induction
Drospirenone
- Progestins
- Enhanced activity as mineralocorticoid and androgen antagonist - prevent ovulation by inhibiting hypothalamus and pituitary, prevent fertilization by decreasing amount and increasing viscosity of cervical mucus,
- Nausea, headaches, CV effects, decreased glucose tolerance, weight gain
- Combination OCP (continuous or discountinous), ovarian dysfunction, PM symptoms
Progesterone
- Progestins
- Rapidly inactivated when given orally –prevent fertilization by decreasing amount and increasing viscosity of cervical mucus, prevent ovulation by inhibiting hypothalamus and pituitary
- Headaches, abnormal menstrual bleeding (irregular periods)
- Contraception (continuous), dysmenorrhea, endometriosis
Medroxyprogesterone acetate
- Progestins – IM injection
- Prevent fertilization by decreasing amount and increasing viscosity of cervical mucus, prevent ovulation by inhibiting hypothalamus and pituitary
- Headaches, abnormal menstrual bleeding (irregular periods)
- Progestin only IM injections (every 3 months)
Norethindrone
- Progestins – oral or IUD
- Prevent fertilization by decreasing amount and increasing viscosity of cervical mucus, prevent ovulation by inhibiting hypothalamus and pituitary
- More cross reactivity – headaches, abnormal menstrual bleeding
Combination - Nausea, headaches, CV effects, decreased glucose tolerance, weight gain
*Progestin only OCP and IUD (continuous)
Combination OCP (continuous or discontinuous), ovarian dysfunction, PM symptoms
Norgestrel
- Proogestins – oral or IUD
- Prevent fertilization by decreasing amount and increasing viscosity of cervical mucus, prevent ovulation by inhibiting hypothalamus and pituitary (emergency)
- Progestin - headaches, abnormal menstrual bleeding
Emergency – nausea and vomiting, headache, dizziness, breast tenderness, abdominal/leg cramps
*Progestin only OCP and IUD, dysmenorrhea, endometriosis
Emergency contraception (take within 72 hours – no prescription)
Ulipristal
- SPRMs – more effective than norgestrel
- Inhibits ovulation by antagonizing actions of progesterone on granulosa cell progesterone receptor
- Emergency contraception within 5 days (oral, prescription required)
RU 486
- Progestin receptor antagonists
- Inhibits ovulation by antagonizing actions of progesterone on granulosa cell progesterone receptor
- Emergency contraception within 5 days (oral, prescription required)
FSH
- Gonadotropins
- Used to induce follicular growth
- In vitro fertilization
CG
- Gonadotropins
- Used to induce ovulation
- Diagnostic for pregnancy, IVF
Gonadorelin
- GnRH analog
- Stimulate gonadotropin secretion (single injection or with a pump)
- Delayed puberty, anovulatory disorders
Luprolide
- GnRH agonist (long acting)
- Suppress gonadotropin secretion
- Desensitization - injectable
Cetrorelix
- GnRH antagonist
- Injectable – stop gonadotropin secretion in ovulation-induction protocols
- Precocious puberty, androgen excess, endometriosis, dysmenorrhea
Testosterone
Testosterone propionate
*Androgen
*Inactive when given orall but can be given transdermally or as buccal tablets
Propionate given IM
*Virilization feminization, suppression of HPG axis, edema, jaundice, hepatic carcinoma
*Male hypogonadism, muscle wasting in AIDS
Methyltestosterone
Danazol
- 17a-alkylated androgen
- Given orally
- More severe - virilization feminization, suppression of HPG axis, edema, jaundice, hepatic carcinoma
- Male hypogonadism, muscle wasting in AIDS
Dutasteride
Finasteride
- 5a-reductase inhibitor (oral)
* Benign prostatic hyperplasia, prostate cancer, hirsutism, CAH, male precocious puberty
Bicalutamide
Flutamide
Nilutamide
- Androgen receptor antagonist (oral)
* Benign prostatic hyperplasia, prostate cancer, hirsutism, CAH, male precocious puberty
