Estrogens, Progestins and Androgens Flashcards
How do hormones circulate through the body?
Hormones that are released from cells circulate in the blood largely bound to sex hormone binding globulin (SHBG) and albumin
Where are ER-beta receptors found?
Colon, vascular endothelium, lung, bladder and brain
17-beta estradiol and phytoestrogens bind
Where are PR-alpha receptors found?
Uterus and ovary
Binds progesterone
Where are AR receptors found?
Both male and female genitals, bones, muscles
Binds testosterone and dihydrotestosterone (more potent form of testosterone)
What are the physiological effects of estrogens?
Sexual maturation and growth, development of endometrial lining, maintain structure and function of skin and blood vessels, decrease rate of bone reabsorption, antioxidant, induce synthesis of both estrogen and progesterone receptors
What are the effects of estrogens on the liver?
Increased production of CBG, SHBG, thyroid binding globulin, transferrin and angiotensinogen
What is the effect of angiotensinogen?
Increased Na reabsorption and water retention (bloating) and increased blood pressure
What are the effects of estrogen on fats?
Increased HDL, lowered LDL, slight decreased plasma cholesterol and increased triglycerides
What are the effects of estrogen on coagulation?
Enhances the coagulation of the blood. Increases clotting factors, fibrinogen and plasminogen, decreases antithrombin III and platelet adhesiveness
What are the physiological effects of progesterone?
Precursor to estrogens and androgens, downregulates estrogen receptor and it’s stimulation of the endometrium, induce maturation and secretory changes in the endometrium in preparation for pregnancy, antagonizes the mineralcorticoid receptor to decrease Na resorption and water retention
What are the effects of progesterone metabolites?
Anxiolytic and hypnotic effects on the brain
What are the contraindications for estrogen containing estrogens?
> 35 and smoke >15 cigarettes/day, hypertension, diabetes with severe vascular disease, history of stroke, migraine headaches with an aura, multiple risk factors for CVD, women cancers, active liver disease, thromboembolic disorder and pregnancy.
What are the effects of estrogen in hormonal contraceptives?
Inhibition of development of dominant ovarian follicle and suppression of ovarian steroid production by suppression of FSH
What are the effects of progestin in hormonal contraceptives?
Atrophy of the endometrium, making it less suitable for implantation
Thickening of cervical mucus, impeding sperm transport
Impairment of normal tubual motility and peristalsis
What form of estrogen is in combined oral contraceptives?
10-35 mcg Ethinyl estradiol, a synthetic estrogen
Addition of ethinyl inhibits first-pass metabolism and increases potency
Mestranol is a pro-drug
What are some examples of 1st generation progestins?
Norethindrone, Norethindone acetate and ethynodiol diacetate
Medium androgen activity
What are some examples of 2nd generation progestins?
Levonorestrel, norgestrel
Strong androgen and anti-estrogen activity
What are some supposed additional effects of 2nd generation progestins?
Improved libido, negative lipid effects, increased acne and weight gain
Lower VTE risk
What are some examples of 3rd generation progestins?
Norgestimate, Desogestrel, Gestodene
Low androgen activity
What are the supposed additional effects of 3rd generation progestins?
Higher VTE risk, better for acne
What is drospirenone?
A spironolactone analogue, anti-androgenic/anti-mineralcorticoid activity
Improves PMDD symptoms, hirsutism and acne, higher VTE risk, increase s serum potassium
What is cyroterone?
An anti-androgen
How is ethinyl estradiol bound to proteins?
Highly bound to plasma albumin but not SHBG so unbound distribute rapidly and extensively
How are progestins bound to proteins?
Extensively but weakly bound to albumin and moderately but strongly bound to SHBG (can displace testosterone and lead to increased acne and lipid effects
Some strongly bound to CBG
What are the types of typical OC combinations?
21 days of monophasic, biphasic and triphasic (increased progestin), resulting in 13 bleeds each year unless taken continuously
What are the types of extended cycle OC combinations?
24 days, 26 days (estrogen)/24 days (progestin) resulting in 13 bleeds each year, 84 days resulting in 4 bleeds each year
What do progestin only pills contain and cause?
Norethindrone 0.35 mg taken continuously (no off days) resulting in 13 bleeds per year
What are the well-known benefits of oral contraceptive pills?
Prevent pregnancy, cycle regulation and decreased menstrual flow, decreased per-menopausal symptoms, decreased dysmenorrhea, relief of PMS and PMDD, improve hirsutism and acne, decreased risk of fibroids/fewer ovarian cysts, increased bone mineral density
What are the less known benefits of oral contraceptive pills?
Treat polycystic ovary syndrome, reduce PID, reduce ectopic pregnancy, improve symptoms of endometriosis, reduce risk of ovarian and endometrial cancer, possible reduction of benign breast disease, protective against colon cancer
What are some side effects of estrogen?
Too much: Nausea, breast tenderness (take at bedtime with food), headache, bloating
Too little: Spotting, breakthrough bleeding early/mid cycle (should improve with time)
What are some side effects of progestin?
Too much: Breast tenderness, headache, fatigue, mood changes, bloating
Too little: Breakthrough bleeding late cycle