Pharmacology of Sex Hormones Flashcards
What are the female gonadal hormones?
Estrogen and Progesterone
What is the flow of the Hypothalamic Pituitary Gonadal Axis?
Hypothalamus = GnRH –> Pituitary = LH and FS –> Ovary = Inc or Dec Estrogen and Progesterone
What are the forms of Estrogen?
Estradiol E2 = ovaries
Estrone E1 = postmenopause
Estriol E3 = pregnancy
What is Progesterone?
Precursor for estrogen, androgen, and andrenocortical hormones
What is the Follicular Phase?
Development of the follicle
What is the Luteal Phase?
After ovulation until menstruation or fertilization
Testosterone is the precursor to what?
Estrogens via Aromatase Conversion
Sex Hormones are bound to what to travel across membranes as lipids?
SHBG
Where are steroid binding receptors found?
Cytoplasm, CYTOPLASMIC not cell surface
What are the physiological roles of estrogens?
- Females sexual maturation
- Menstruation the building up of endometrium
- CV protection
- Increased blood clotting
What are the pharmacological uses for estrogens?
- Contraception
- Hypogonadism
- Hormone Replacement postmenopause
What are the adverse effects of estrogens/
- Uterine bleeding
- Cancer risks
- Nausea
- Breast tenderness
- Migraine/HA
- Gallbladder malfunction
- HTN
What produces progesterone?
Corpus Luteum
Embyro/Placenta
What produces estrogen?
Ovaries
Developing Follicle
Corpus Luteum
What are the physiological roles of progestin?
- Endometrial changes following ovulation (secretory)
- Stimulates lipoprotein lipase and favors dat deposition
- Increases basal insulin
- Increase sodium reabsorption
- Increases body temp
- Increases sensitivity to P(CO2)
What are the pharmacological uses of progestins?
- Hormone replacement postmenopause
- Contraception
- Delay premature labor
What are the adverse effects of progestins?
- Increase BP
- Lower HDL
- Edema due to sodium retention
What is the follicular phase?
Development of follicles in ovary
What is ovulation?
LH Surge
What is luteal phase?
Corpus luteum to pregnancy or menstruation
What is menses?
Onset at drop in Progesterone
What do Ovulation Predictor kits track?
Rise in LH
Can give up to 2 day warning
What do Fertility Monitors track?
Rise in Estrogen and LH
Can give 2-4 days before LH peak
What is essential for the maintenance of pregnancy?
Progesterone
How long will the corpus luteum supplement progesterone?
10 weeks, corpus luteum is kept healthy by hCG
>10 wks placenta takes over
What are the qualities of the progestin generations?
1st: Norethindrone Acetate
2nd: Norgestrel, Levongrestrel more androgen
3rd: Desogestrel, Norgestimate less androgen
4th: Drospirenone, Dienogest mineralocorticoid and low androgen
What formulations are progestin only?
Norethindrone Acetate and Drospirenone
What is the MOA for Combined Estrogen and Progestin?
INHIBIT OVULATION
Increase cervical mucus
Decrease endometrium lining
Decrease flow in fallopian tubes
What is the MOA of Progestin Only?
May Inhibit Ovulation
Increase cervical mucus
Decrease endometrium
Decrease flow in fallopian
What are the dose related A/E of Contraceptives?
- Cardiovascular (HTN, DVT, Stroke)
- Cancer
- Endo/Metabolic
- Migraines/HA
- Nausea
- Edema
- Weight Gain
What are the endocrine and metabolic A/Es of contraceptives?
Fluid retention
Increase LDL and decrease HDL
Glucose
Acne or Hirsutism
What are the Contraindications for Hormonal Contraceptives?
- Clotting history (estrogen only)
- Uncontrolled cholesterol/HTN
- Pregnancy
- Estrogen postive cancer
- Smokers
- Migraines
- Gallbladder
What is the MOA of Emergency Contraception?
INHIBITS OVULATION
What is Ulipristal Acetate (Ella) and its MOA?
EC, selective progesterone receptor modulator, partial agonist at PG receptors, weak antagonist at GC receptors
What product is an Abortifacient and its MOA?
Mifepristone RU486
Progesterone receptor ANTAGONIST
What do you use with Mifepristone RU486 to induce abortion?
Misoprostol, prostaglandin E1 analog
What are there SERMS?
Tamoxifen
Raloxifene
Clomiphene
What is the MOA of Tamoxifen?
Estrogen ANTAGONISST in breast, treats breast cancer
What is the MOA of Raloxifene?
Estrogen AGONIST in bone, treats osteoporosis
What is the MOA of Clomiphene?
Estrogen PARTIAL AGONIST, induces ovulation for infertility
What SERMS are used for Menopause?
Ospemifene
Medroxyprogesterone
Estrogens
Ospemifene is used for what?
AGONIST, for vaginal dryness
Medroxyprogesterone is used for what?
Hyperplasia of endometrium
Estrogens SERM is used for what?
Relieve VMS and Urogenital Atrophy
