Estrogens & Progestins Flashcards by Ashley Wong

Conjugated Estrogen, Estradiol, Transdermal Estradiol, Ethinyl estradiol, Diethylstilbertrol/DES- Mech of Action

acts as estrogen

How well did you know this?

Not at all

Perfectly

Conjugated Estrogen, Estradiol, Transdermal Estradiol, Ethinyl estradiol, Diethylstilbertrol/DES- Clinical Use

Vasomotor symptoms of menopause
vulvar and vaginal atrophy
female hypoestrogenism secondary to hypogonadism, castration, or primary ovarian failure
in combination to retard bone loss in osteoporosis

How well did you know this?

Not at all

Perfectly

Conjugated Estrogen, Estradiol, Transdermal Estradiol, Ethinyl estradiol, Diethylstilbertrol/DES- Adverse Effects/Contraindications

Nausea, vomiting, edema, headache, breast tenderness, venous thrombosis, breakthrough bleeding

Estrogen alone causes endometrial hyperplasia and increases risk of carcinoma

Contraindicated in breast and endometrial cancer, cerebral vascular coronary artery disease, benign or malignant liver tumors, severe hypertension, pregnancy, smokers over 35, thrombotic disorders

How well did you know this?

Not at all

Perfectly

Selective Estrogen Receptor Modulators- SERMS- Available Drugs

Tamoxifen
Clomiphene
Raloxifene

How well did you know this?

Not at all

Perfectly

Estrogens- Available Drugs

Conjugated estrogen
Estradiol
Transdermal estradiol
Ethinyl estradiol (steroidal synthetic)
Diethylstilbertrol/DES (non-steroidal synthetic)

How well did you know this?

Not at all

Perfectly

Tamoxifen- Mech of Action

Estrogen receptor antagonist in breast tissue

Estrogen receptor partial agonist in endometrium and bone

How well did you know this?

Not at all

Perfectly

Tamoxifen- Clinical Use

prevention, palliative, and adjuvant therapy for breast cancer

not given for any more than 5 years to reduce the chance of causing cancer

How well did you know this?

Not at all

Perfectly

Tamoxifen- Adverse Effects/Contraindications

malignant neoplasm of endometrium
cataracts
pulmonary embolism
hot flashes
abnormal menstruation
vaginal discharge

Contraindicated in hx of DVT or PE, pregnancy

How well did you know this?

Not at all

Perfectly

Comiphene- Mech of Action

Estrogen receptor antagonist in hypothalamus and pituitary

Partial agonist in ovaries

Disinhibits GnRH, FSH, and LH release

How well did you know this?

Not at all

Perfectly

Comiphene- Clinical Use

female infertility due to ovulatory disorder

How well did you know this?

Not at all

Perfectly

Comiphene- Adverse Effects/Contraindications

Thromboembolism
ovarian cysts and hypertrophy
flushing and vasomotor symptoms
abdominal discomfort

Contraindicated in pregnancy, thyroid or adrenal dysfunction, liver disease, endometrial carcinoma, ovarian cysts organic intracranial lesion

How well did you know this?

Not at all

Perfectly

Raloxifene- Mech of Action

Estrogen receptor agonist in bone

Antagonist in uterus and breast

How well did you know this?

Not at all

Perfectly

Raloxifene- Clinical Use

prevention and treatment of osteoporosis

How well did you know this?

Not at all

Perfectly

Raloxifene- Adverse Effects/Contraindications

retinal vascular occlusion
venous thromboembolism
hot flashes
leg cramps

Contraindicated in pregnancy and history of venous thromboembolism

How well did you know this?

Not at all

Perfectly

Fulvestrant- Mech of Action

Complete estrogen receptor antagonist

NO agonist activity

How well did you know this?

Not at all

Perfectly

Fulvestrant- Clinical Use

treatment of estrogen receptor positive metastatic breast cancer in post-menopausal women with disease progression following anti-estrogen therapy (Tamoxifen)

How well did you know this?

Not at all

Perfectly

Fulvestrant- Adverse Effects/Contraindications

nausea
asthenia
pain
vasodilation (hot flashes)
headache

Contraindicated in pregnancy

Aromatase Inhibitors- Available Drugs

Anastrozole
Letrozole
Exemestane
Formestane

Anastrozole, Letrozole- Mech of Action

competitive inhibitor of aromatase

prevent estrogen formation from androgens

Aromatase Inhibitors- Clinical Use

treatment and prevention of estrogen receptor positive breast cancer (early stage, locally advanced, and metastatic)

may be more effective than SERMs

Aromatase Inhibitors- Adverse Effects/Contraindications

OSTEOPOROTIC FRACTURES
thrombophlebitis
hypercholesterolemia
profuse vaginal bleeding
peripheral edema
rash 
nausea
arthralgia
bone pain
headache 
depression
dyspnea

Contraindicated in hypersensitivity

Exemestane, Formestane- Mech of Action

Irreversible inhibitors of aromatase

prevent estrogen formation from androgens

Progestin Only Contraceptives- Available Drugs

Norgestrel
Norethindrone
Medroxyprogesterone acetate (injectable)
Etonogestrel (implant)
Levonorgestrel

Norgestrel, Norethindrone, Medroxyprogesterone acetate, Etonogestral- Mech of Action

alter frequency of GnRH pulsing and decrease anterior pituitary responsiveness to GnRH

alter tubal peristalsis, endometrial receptivity, and cervical mucus secretions

Norgestrel, Norethindrone, Medroxyprogesterone acetate, Etonogestral- Clinical Use

contraception

Norgestrel, Norethindrone, Medroxyprogesterone acetate, Etonogestral- Adverse Effects/Contraindications

``` irregular periods breast tenderness nausea dizziness headaches ``` Contraindicated in acute liver disease, liver tumors, known or suspected breast cancer, pregnancy

Levonorgestrel- Mech of Action

Block LH surge, disrupt normal ovulation, produce endometrial changes to prevent implantation

Levonorgestrel- Absorption, Distribution

Two doses separated by 12 hrs First dose w/i 72 hrs of intercourse

Levonorgestrel- Clinical Use

Emergency Contraception

Levonorgestrel- Adverse Effects/Contraindications

``` Nausea vomiting headache dizziness mastalgia ```

Combination Oral Contraceptives- Available Drugs

Estrogens: Ethinyl estradiol Mestranol ``` Progestins: Norgestrel Levonorgestrel Norethindrone Norethindrone acetate Ethynodiol Norgestimate Gestodene Desogestrel Drospirenone ```

Combination Oral Contraceptives- Mech of Action

Suppress GnRH, LH, and FSH secretion and follicular development, thus inhibiting ovulation Alter tubal peristalsis, endometrial receptivity, and cervical mucus secretions

Combination Oral Contraceptives- Absorption, Distribution

PO patches vaginal rings

Combination Oral Contraceptives- Clinical Use

contraception

Combination Oral Contraceptives- Adverse Effects/Contraindications

``` thromboembolism PE cerebral thrombosis gallbladder menstruation breakthrough bleeding breast tenderness bloating migraine weight change ``` contraindicated in breast or endometrial cancer, cerebral vascular or coronary artery disease, jaundice, liver tumors, severe hypertension, prolonged immobilization, pregnancy, smokers over 35, thrombotic disorders

Progesterone Receptor Antagonist- Available Drugs

Milfepristone (RU-486)

Milfepristone (RU-486)- Mech of Action

inhibit progesterone binding to receptor

Milfepristone (RU-486)- Clinical Use

abortion administered w/ Misoprostol to stimulate uterine contractions

Milfepristone (RU-486)- Adverse Effects/Contraindications

``` prolonged bleeding time bacterial infections sepsis nausea vomiting diarrhea cramps headache ``` contraindicated in adrenal failure, ectopic pregnancy, hemorrhagic disorders, anticoagulation therapy, inherited porphyrias, IUD, undiagnosed adnexal mass

Hormone Replacement Therapy- Available Drugs

``` conjugated equine estrogen micronized estradiol conjugated synthetic estrogens transdermal estrogens vaginal rings medroxyprogesterone micronized progesterone combinations ```

Hormone Replacement Therapy- Clinical Use

vasomotor instability mood changes urogenital atrophy osteoporosis

Hormone Replacement Therapy- Adverse Effects/Contraindications

``` Estrogens: nausea mastalgia headache fluid retention cancer (?) ``` Progestins: weight gain headache contraindicated in breast or endometrial cancer, cerebral vascular or coronary artery disease, jaundice, liver tumors, severe hypertension, prolonged immobilization, pregnancy, smokers over 35, thrombotic disorders