Sex Hormones Flashcards
Estradiol (E2)
- The primary systemic estrogen
- Available in many formulations (tablet, cream, patch, ring…)
Estrone (E1)
- 1/3 as active as estradiol
- Available as a component of conjugated estrogens (Premarin) and esterified estrogens (Menest)
Ethinyl estradiol
- Synthetically modified to have slower hepatic metabolism
- 15-20x more potent than E2
- Available in combo products
Estriol (E3)
- Not a drug
- Less potent than E2
Estrogens: Mechanism of Action
-Slow effects are transcription mediated (protein synthesis)
-Rapid effects are transcription independent (2nd messengers)
Nuclear receptors
Estrogen Effects
-Increase risk of breast cancer
-Mood swings/depression/hot flashes
-Increase risk of thrombosis (MI/DVT/PE/S)
-Dyslipidemia
-Paradoxical HTN, edema, bloating
-Uterine bleeding
-Osteoporosis
- Oral administration:
– ↑ Toxicity
– ↓ Bioavailability
Estrogen Contraindications
-Breast cancer
-Liver disease
-Stroke, DVT, CVD, High CVD risk
Uterus intact =
Uterus absent =
Moderate CVD risk =
-Estrogen + Progestin
-Estrogen
-Avoid oral route
Progestins Mechanism of Action
- Nuclear / cytoplasmic receptor (similar to estrogen)
- Many progestins act on receptors for other hormones
– Estrogen
– Androgen
– Mineralocorticoid
Progestin excess
Hypomenorrhea or amenorrhea
Progestin deficiency
- Late cycle breakthrough bleeding
- HYPERmenorrhea
Estrogen deficiency
- Early cycle breakthrough bleeding
- Hypomenorrhea or amenorrhea
When choosing contraceptives, Estrogen + Progestin vs Progestin Only
E + P
= CI in thrombosis RF (CVD/Smoker/Stroke/Any Heart)
P only
= requires perfect adherence, same time daily
Hypothyroid SX
-Fatigue
-Weight gain
-Cold intolerance
-Joint/muscle pain
-Dry skin/hair
-Slow HR
-Depression
Hyperthyroid SX
-Anxiety, hard concentrating
-Fatigue
-Frequent bowel movements
-Goiter
-Hair loss
-Weight loss
-Heat intolerance
-Tremor
-Fast HR
