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Year 2 Endo Repro > Pharmacology of Estrogens/Progestins > Flashcards

Pharmacology of Estrogens/Progestins Flashcards

1
Q

Estradiol 17B (E2)

A

most estrogenic action

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2
Q

Synthetic Steroidal Estrogens

A
  • Ethinyl estradiol
  • Mestranol
  • Quienestrol
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3
Q

Synthetic Non-steroidal Estrogens

A
  • Diethylstilbestrol (DES)
  • Chlorotrianisene
  • Methallenestril
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4
Q

Pathway of GnRH secretion

A

hypothalamic-pituitary portal system to gonadotrophs of anterior pituitary to increase LH and FSH

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5
Q

LH actions in females

A

LH –> Thecal cells to synthesize androgen –> estrone E1/Estradiol (E2) in the Granulosa cells via FSH

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6
Q

LH actions in males

A

LH –> testicular Leydig cells to increase synthesis of Testosterone –> diffuses to neighboring Sertoli cells

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7
Q

What do Sertoli and Granulosa cells synthesize and secrete?

A

Inhibit A/Inhibin B and Activin

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8
Q

What does Inhibin/Activin regulate?

A

FSH

-do not regulate LH release

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9
Q

Where does hormone-receptor complex act?

A

Dimerizes in nucleus binds to specific regions of DNA; complex with co-activators and co-repressors and different transcription factors

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10
Q

What are three actions of Estrogen?

A
  • Growth, development, structural maintenance of primary and secondary female sex characteristics
  • Growth of uterine endometrium during cycle
  • Secretion of thin mucus
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11
Q

What are the metabolic action of estrogen?

A
  • Increase circulating HDL, decrease LDL
  • Inc. cholesterol saturation of bile
  • Inc. BP via renin substrate
  • Promote thrombosis
  • Decrease bone reabsorption
  • Inc. liver protein synthesis
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12
Q

Major clinical uses of Estrogens

A
  • component of oral contraceptives
  • HRT during menopause
  • HRT for delayed puberty;hypogonadism in women
  • Rx of perimenopause (menopause transition years), dysmenorrhea (painful menstruation), oligomenorrhea (infer. uterine bleeding)
  • Rx for acne
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13
Q

Drug indications for Estrogen preparations

A
  • Vasomotor symptoms of menopause
  • Vulvar vaginal atrophy
  • Female hypoestrogenism secondary to hypogonadism castration or primary ovarian failure
  • In combination with other therapeutic measures to retard bone loss and osteoporosis in post menopausal women
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14
Q

Side effects of Estrogen preparations

A
  • Nausea Vomiting
  • Edema
  • Headache
  • Breast tenderness
  • Venous thrombosis
  • Breakthrough bleeding
  • Estrogen alone (without progesterone) causes endometrial hyperplasia and possible endometrial carcinoma
  • Increased incidence of adenocarcinoma of vagina in female offsprings of patients who taken DES
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15
Q

Contraindication of Estrogen preparations

A
  • Breast and Endometrial cancers
  • Cerebral vascular coronary artery disease
  • Benign or malignant liver tumors
  • Severe hypertension
  • Pregnancy
  • Female smokers over 35 years of age
  • Thrombotic disorders
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16
Q

Name three Selective use of Estrogen Receptor Modulator (SERMs)

A

Tamoxifen
Clomiphene
Raloxifene

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17
Q

What is the indication for Tamoxifen (SERM)?

A

used for prevention, palliative, and as an adjuvant therapy for breast cancer

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18
Q

Mechanism of Action for Tamoxifen (SERM)

A

acts as an estrogen receptor antagonist in breast tissue and as a partial agonist in endometrium and bone

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19
Q

Side effects of Tamoxifen (SERM)

A
  • malignant neoplasm of endometrium
  • cataracts
  • pulmonary embolism
  • Hot flashes
  • Abnormal menstruation
  • Vaginal discharge
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20
Q

Contraindication of SERM

A
  • History of deep vein thrombosis or pulmonary embolism

- Pregnancy

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21
Q

Therapeutic Considerations for Tamoxifen (SERM)

A
  • Tamoxifen administration is associated with 4 - 6 fold increase incidence of endometrial cancer
  • Administered for no more than 5 years, to minimize the risk of endometrial cancer
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22
Q

Drug Indications for Clomiphene

A

-used for female infertility due to ovulatory disorder

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23
Q

Mechanism of Action for Clomiphene

A
  • estrogen receptor antagonist in hypothalamus and pituitary gland, and partial agonist in ovaries
  • disinhibits GnRH release and inc. level of LH and FSH
  • inc. FSH stimulates follicle growth, LH surge and ovulation
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24
Q

Side effects of Clomiphene

A
  • Thromboembolism
  • Ovarian cysts and hypertrophy
  • Flushing and vasomotor symptoms
  • Abdominal discomfort
25
Q

Indications for Raloxifene

A

Osteoporosis prevention and treatment

26
Q

Mechanism of Action of Raloxifene

A

Estrogen receptor agonist in bone and estrogen receptor antagonist in uterus and breast

27
Q

Side effects of Raloxifene

A
  • Retinal vascular occlusion
  • Venous thromboembolism
  • Hot flashes
  • Leg cramps
28
Q

Contraindication for Raloxifene

A

Pregnancy

-Hx or presence of venous thromboembolism

29
Q

Therapeutic considerations for raloxifene

A

Decreases risk of invasive breast cancer in post menopausal women with osteoporosis

30
Q

Name one Estrogen receptor antagonist

A

Fulvestrant

31
Q

Indication for Fulvestrant

A

Not first line
Tx of estrogen receptor positive metastatic breast cancer in post menopausal women with disease progression following anti-estrogen therapy

32
Q

Mechanism of Action of Fulvestrant

A

Competitively inhibit estrogen binding to receptor, blocking the action of estrogen on target tissue

33
Q

Side effects of Fulvestrant

A
  • Nausea
  • Asthenia (lack of strength)
  • Pain
  • Vasodilation (hot flashes)
  • Headaches
34
Q

Contraindication for Fulvestrant

A

Pregnancy

35
Q

Therapeutic consideration for Fulvestrant

A

Pure estrogen receptor antagonist with no agonist activity

36
Q

Name 4 Aromatase Inhibitors

A
  • Anastrozole
  • Letrozole
  • Exemestane
  • Formestane
37
Q

Indications for Aromatase Inhibitors

A

Treatment and prevention of estrogen receptor positive early stage, locally advanced and metastatic breast cancer

38
Q

Mechanism of Action for Aromatase Inhibitors

A

Anastrozole and Letrozole are competitive inhibitors of aromatase, the enzyme that catalyzes the formation of estrogens from androgen precursors. Exemestane and formestane are irreversible inhibitors of aromatase

39
Q

Side effects of Aromatase Inhibitors

A

A bunch of similar crap, see slide 32

40
Q

Therapeutic Considerations for Aromatase Inhibitors

A

Aromatase inhibitors may be more effective than SERMs for the treatment of breast cancer
-extreme suppression of estrogen action could lead to high risk of osteoporotic factors in women taking aromatase inhibitors

41
Q

Physiological actions of Progesterone (4)

A
  • neuroendocrine regulation of menstrual cycle
  • induces secretory uterine endometrium; necessary for implantation
  • Thick, viscous cervical mucus
  • Increases body temperature
42
Q

Clinical uses of Progestins

A
  • In OC’s, alone, or in combination with ethanol estradiol
  • Component of HRT in menopause
  • Rx of dysmenorrhea, oligomenorrhea, endometriosis, polycystic ovarian syndrome
43
Q

Name 4 Progestin-only Contraceptives

A
  • Norgestrel
  • Norethindrone
  • Medroxyprogesterone acetate (injectable)
  • Etonogestrel
44
Q

Indication for progestin-only contraceptives

A

Contraception

45
Q

Mechanism of action of progestin only contraceptives

A

Alter frequency of GnRH pulsing and decrease anterior pituitary gland responsiveness to GnRH. Secondary mechanisms of pregnancy prevention include alterations in tubal peristalsis, endometrial receptivity, and cervical mucus secretions, which together prevent the proper transport of both egg and sperm

46
Q

Side effects of Progestin only Contraceptives

A
  • Irregular periods
  • Breast tenderness
  • Nausea
  • Dizziness
  • Headaches
47
Q

Contraindications for Progestin only contraceptive

A

Acute liver disease
Benign or malignant liver tumors
Known or suspected breast cancer
pregnancy

48
Q

Classic regimen for COCs (combinations)

A

21 day on pill/ 7 days on placebo

49
Q

Efficacy of COCs (combinations)

A

approx. 0.1 incidence of accidental pregnancy in 1st year

50
Q

Mechanism of COCs (combination)

A

primarily neg. feedback on gonadotropin secretion; progestin may thicken cervical mucus

51
Q

Side effects of COC

A

-A and V / pulmonary thromboembolism or cerebral thrombosis
-Gall bladder dz
-Hypertension
-Hepatic neoplasm
-Abnormal menstruation
-Breakthrough bleeding
-breast tenderness
-bloating symptoms
migraine
-weight change

52
Q

Contraindication for COC

A
  • Breast cancer
  • Endometrial cancer or estrogen dependent neoplasms
  • cerebral vascular or coronary artery disease
  • cholestatic jaundice of pregnancy or jaundice with prior hormonal contraceptive use
  • benign or malignant liver tumors
  • severe hypertension
  • prolonged immobilization
  • pregnancy
  • female smokers over 35
  • thrombotic disorders
53
Q

which COC is used as a morning after contraception?

A

Levonorgestrel

54
Q

Name one Progesterone receptor antagonist

A

Mifepristone

55
Q

Indications for Mifepristone

A

Abortion (through day 49 of pregnancy)

56
Q

Mechanism of Action for Mifepristone

A

Inhibits progesterone binding to receptor

57
Q

Side effects of Mifepristone

A
  • Prolonged bleeding time
  • bact. infection
  • sepsis
  • nausea/vomiting/diarrhea
  • cramps
  • headache
58
Q

Contraindication for Mifepristone

A
  • chronic adrenal failure
  • ectopic pregnancy
  • hemorrhagic disorders
  • anticoagulation therapy
  • inherited porphyria
  • intrauterine device
  • undiagnosed adnexal mass

Year 2 Endo Repro (1 decks)

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