Progestins, Estrogens, and Androgens Flashcards
What are the main actions of Estrogen/Estradiol?
- Promote endometrial proliferation during the follicular phase (1st half) of the menstrual cycle
- Negative feedback on GnRH and FSH/LH secretion
- Decrease bone resorption (Osteoclast activity)
- Increase clotting factors and risk for thromboembolism
- Increase endometrial and breast CA
What are the main actions of Progesterone?
- Promote endometrial development during the luteal phase (2nd half) of the menstrual cycle
- Decrease amount of cervical mucus and increase viscosity of cervical mucus
- Negative feedback on GnRH and FSH/LH secretion
- Important in placenta for maintenance of pregnancy
What types of drugs can be used for contraception?
Progesterone, Estrogen, Combinations, and Selective Progesterone Receptor Modulators (SPRMs)
What types of drugs can be used for suppression of the Hypothalamic-Pituitary-Gonadal (HPG) axis?
Progesterone and Estrogen
What types of drugs can be used for replacement therapy?
Progesterone, Estrogen, and Selective Estrogen Receptor Modulators (SERMs)
What types of drugs can be used for breast CA therapy?
SERMs and Aromatase Inhibitors
What types of drugs can be used for ovulation induction?
Estrogen Antagonists and Aromatase Inhibitors
What types of drugs can be used for Abortions?
Progesterone Antagonists
Estradiol or Ethinyl estradiol
1) Use
2) Mechanism of Action
3) Adverse Effects
1)Combination-type Contraceptive Agent w/Progestin
2)Prevent ovulation by inhibiting the hypothalamus and pituitary
Progestin decreases amount and increases viscosity of cervical mucus
3)Thromboembolism-mostly in smokers over 35 years old
Norethindrone or Norgestrel
1) Use
2) Mechanism of Action
3) Adverse Effect
1) Progestin-ONLY Contraception
2) Prevent fertilization by decreasing the amount and increasing the viscosity of cervical mucus
3) Abnormal menstrual bleeding
Medroxyprogesterone acetate (Depo-Provera)
1) Use
2) Mechanism of Action
3) Adverse Effect
1) Progestin-ONLY Contraception (IM injection)
2) Prevent fertilization by decreasing the amount and increasing the viscosity of cervical mucus
3) Decreased bone density
What drugs can decrease the efficacy of combination-type contraceptives?
- Rifampin
- Anticonvulsants (via CYP3A4)
What is another use of norgestrel when given in VERY high dose? What is the mechanism of action in high doses? What is the most common adverse effect?
- Emergency Contraceptive
- Suppression of the hypothalamic-pituitary-gonadal axis therefore inhibiting ovulation
- Nausea and Vomiting
Ulipristal
1) Use
2) Mechanism of Action
1)Emergency Contraceptive
2)Selective Progesterone Receptor Modulator (SPRM)-inhibits ovulation by antagonizing the actions of progesterone on the granulosa cell progesterone receptor
Also a Progesterone agonist in the pituitary/hypothalamus and therefore delays the LH surge
Estrone Sulfate
1)Use
1) Treatment of postmenopausal symptoms and postmenopausal osteoporosis
* Use lowest effective dose and shortest duration possible
Raloxifene
1) Use
2) Mechanism of Action
1) Relief of Postmenopausal symptoms, Osteoporosis, Estrogen-dependent breast CA in Postmenopausal women
2) Selective Estrogen Receptor Modulator (SERM) and Estrogen Receptor Antagonist
Tamoxifen
1) Use
2) Mechanism of Action
1) Relief of Postmenopausal symptoms, Osteoporosis, Estrogen-dependent breast CA
2) Selective Estrogen Receptor Modulator (SERM) and Estrogen Receptor Antagonist
Bazedoxifene
1) Use
2) Mechanism of Action
1)Postmenopausal symptoms
2)Selective Estrogen Receptor Modulator (SERM) and Estrogen Receptor Antagonist
Also has Agonist effects on bone
Clomiphene
1) Use
2) Mechanism of Action
1) Induction of ovulation
2) Estrogen Receptor Antagonist-Antagonizes the inhibitory effects of estrogen on the pituitary and hypothalamus
* Do NOT use long-term!
Exemestane
1) Use
2) Mechanism of Action
1) Breast CA in Postmenopausal women, Induce ovulation
2) Steroidal Aromatase Inhibitor-inhibits the conversion of androgens to estrogens
Letrozole
1) Use
2) Mechanism of Action
1) Breast CA in Postmenopausal women, Induce ovulation
2) Non-steroidal Aromatase Inhibitor-inhibits the conversion of androgens to estrogens
RU486/mifepristone
1) Use
2) Mechanism of Action
1) Abortions
2) Progesterone Receptor Antagonist-antagonizes progesterone actions everywhere including the endometrium
* Also has a glucocorticoid antagonist activity so can be used for Cushing syndrome and Type 2 DM
What are the main actions of Androgens?
- Puberty in males
- Maintenance of secondary sexual characteristics and accessory organs in males
- Promote anabolic reactions throughout the body
What are the uses of Androgen therapy?
- Replacement therapy in male hypogonadism (low androgen levels)
- Treatment of catabolic states such as muscle wasting associated w/AIDS
Finasteride
1) Use
2) Mechanism of Action
1) Syndromes of androgen excess like BPH, prostate CA, hirsutism, congenital androgen hyperplasia, male precocious puberty
2) 5-alpha Reductase Inhibitor-inhibit 5-alpha reductase enzyme to prevent conversion of testosterone to dihydrotestosterone
Flutamide
1) Use
2) Mechanism of Action
1) Syndromes of androgen excess like BPH, prostate CA, hirsutism, congenital androgen hyperplasia, male precocious puberty
2) Androgen Receptor Antagonists-directly bind to the androgen receptor and block all activity at the receptor
Bicalutamide
1) Use
2) Mechanism of Action
1) Syndromes of androgen excess like BPH, prostate CA, hirsutism, congenital androgen hyperplasia, male precocious puberty
2) Androgen Receptor Antagonists-directly bind to the androgen receptor and block all activity at the receptor
FSH
1)Use
1)Induce follicular growth prior to in vitro fertilization
CG
1) Use
2) Mechanism of Action
1) Induce ovulation (release of mature eggs) prior to in vitro fertilization
2) Acts on the LH receptor
Gonadorelin
1) Use
2) Mechanism of Action
1) Delayed puberty, Anovulatory disorders
2) Synthetic GnRH-stimulates gonadotropin secretion
* Administered in pulsatile fashion
Cetrorelix
1) Use
2) Mechanism of Action
1) Precocious puberty in boys, Endometriosis, Dysmenorrhea
2) GnRH Antagonist-shuts down hypothalamic-pituitary axis by blocking the GnRH receptor to reduce gonadotropin secretion
Luprolide
1) Use
2) Mechanism of Action
1) Precocious puberty in boys, Endometriosis, Dysmenorrhea
2) Long-acting Synthetic GnRH Agonist-initially stimulates gonadotropin secretion then suppresses it d/t long-acting desensitization
Methyltestosterone
1) Mechanism of Action
2) Adverse Effects
1) 17-alpha-Alkylated Androgen
2) Hepatic Toxicity
* Can be given orally unlike testosterone
Danazol
1) Mechanism of Action
2) Adverse Effects
1) 17-alpha-Alkylated Androgen
2) Hepatic Toxicity
* Can be given orally unlike testosterone
Testosterone
1)Route of Administration
1)Transdermal, Buccal tablets
