Estrogens, Progestins & HRT Flashcards
Uses of Estradiol
Used in HRT and hypogonadism
Production and PK of Conjugated Estrogens
Produced (conjugated) in animals and extracted from urine
Given PO, IM, IV, or vaginally
Uses of Conjugated estrogens
Oral contraceptives or HRT
Mostly HRT
PK of Ethinyl estradiol
Estradiol synethetic analog
Increased potency, decreased rate of metabolism, and increased oral effectiveness
Uses for Ethinyl estradiol
HRT
Structure and use of progesterone
The exact same as endogenous progesterone
Not orally effective
Safer for long-term HRT than synthetics
Uses and properties of Medoxyprogesterone
Progesterone-like effects
HRT and contraceptive
Uses and properties of Norethindrone
Orally effective
Structurally similar to testosterone - may have unwanted androgen like side effects
Group used in oral contrapceptives
Properties of Norgestimate
No androgen effects
Used only in combination with oral contraceptives
What two main drug/drug categories are used in HRT
Conjugated estrogens with progestins
Medroxyprogesterone
Name the two Selective Estrogen Response Modifier Drugs
Roloxifene
Tamoxifen
Uses and effects of Raloxifene
Used to decrease osteoporosis
Used to decrease risk of breast and uterus cancer
Can induce hot flashes
Can increase clotting and thrombotic disease risks
Uses and effects of Tamoxifen
Used during breast CA treatment (Only Approval for use)
Beneficial for osteoporosis
Beneficial lipid profiles
Can increase risk of uterine CA
Increased risk of thrombotic disease
PK of Estradiol
Rapid first-pass metabolism
Many preparations for absorption based on need