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Test 9 > Pharm 3 Estrogen/Progestin > Flashcards

Pharm 3 Estrogen/Progestin Flashcards

(47 cards)

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1
Q

Ovarian-pituitary cycle

A
  • Elevated FSH during 1st half stimulates follicle
  • Midcycle estradiol exerts positive feedback, triggers LH surge
  • LH surge induces ovulation, stimulates corpus luteum and progesterone production
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2
Q

Pregnancy hormone

A

hCG (chorionic gonadotorpin) identical to LH, maintains estrogen and progesterone production by maintaining corpus luteum

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3
Q

Hormones interacting with endometrium

A
  • Estrogen mediates proliferation

- Progesterone maintains secretory state

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4
Q

Base molecule for estrodiol/testosterone synthesis

A

Cholesterol

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5
Q

Hormone replacement therapy

A

Estradiol undergoes extensive first-pass metabolism, so use conjugated estrogens (estrone sulfate)

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6
Q

-Estrone sulfate-

indication

A

Conjugated estrogen absorbed in lower gut

-Hormone replacement therapy

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7
Q

-Ethinyl estradiol-

indication

A

Ethinyl substitution reduces first-pass metabolism, greater oral potency than conjugated estrogens
-Oral contraceptives

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8
Q

-Estradiol cypionate-

A

Insoluble in water

-Once monthly IM for HRT

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9
Q

-Medroxyprogesterone-

A

Breast and endometrial cancer

-Oral or IM

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10
Q

-Megestrol-

A

Endometrial cancer

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11
Q

-Norethindrone-

A

19-nortestosterone derivative Progestin

-Oral contraceptives

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12
Q

-Desogestrel-

A

Progesterone for oral contraceptive

-Lowest degree of androgenic activity

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13
Q

Estradiol/Progesterone transport

A
  • Estradiol bound to SHBG (sex hormone binding globulin) high affinity
  • Progesterone bound to CBG (corticosteroid binding globulin) with high affinity
  • Both bound to albumin with low affinity
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14
Q

Estradiol/Progesterone Metabolism

A

Hepatic conjugation

  • Estradiol -> estrone -> bile -> reabsorbed
  • Progesterone -> pregnanediol
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15
Q

Estrogen MOA

A

Binds to nuclear receptor (homodimer), regulates trasncription

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16
Q

Progestin MOA

A

Binds to response element similar to that of corticosteroids

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17
Q

Estrogen effects on bone

A
  • Prepubertal growth of long bones
  • Pubertal closure of epiphyses
  • Post pubertal decreased bone resorption
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18
Q

Estrogen effects on clotting

A
  • Increase clotting factors
  • Decrease antithrombin
  • Increase platelet adhesiveness
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19
Q

Estrogen effects on lipids

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A

Increase HDL, triglycerides

Decrease LDL

20
Q

Estrogen effect of sex behavior

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A

-Mediates testosterone’s effect on libido

21
Q

Estrogen other effects

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A
  • Maintain skin and blood vessel integrity
  • Increase CBG, TBG, SHBG
  • Increase cortisol
  • Increase Na and water retention
22
Q

Progesterone v Estrogen

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A

Antagonize estrogen

  • Decrease Na retention
  • Decrease HDL
  • Increase metabolism
  • Downregulate receptors
23
Q

Progesterone other effects

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A
  • Stimulate respiratory center
  • Increase insulin, reduce glucose tolerance
  • Acne
  • Weight gain
24
Q

Primary hypogonadic impaired development Tx

Study These Flashcards
A

-Start estrogen at 11-13, add progestin when growht is completed

25
Hysterectomy HRT
Unopposed estrogen (don't worry about progesterone)
26
Other clinical uses for Estrogen
- Ovarian suppression for hyperandrogenism - Ovulation suppression in dysmenorrhea - Androgen-dependent prostate cancer (suppress gonadotropin secretion)
27
Estradiol levels postmenopausal
1/4 that of males
28
Postmenopausal HRT alleviates (5)
``` Sleep disturbances Hot flashes Urogenital changes Osteoporosis High cholesterol ```
29
HRT contraindications
Liver disease | Breast or other estrogen-dependent cancer
30
Low dose combination OC
- All use ethinyl estradiol - Norgestrel for monophasic - Norethindrone for bi/triphasic
31
Monophasic v Triphasic
- Triphasic eliminates period for 90 days | - Triphasic reduces total dose of progestin (reduced SE)
32
OC MOA
Inhibit gonadotropin secretion, suppress ovulation (progestin only blocks ovulation 60-80%) - Thicken cervical mucus - Reduce tubal secretion/motility - Change uterine endometrium
33
OC mild AE
Breakthrough bleeding | -Tx with higher dose estrogen or different progestin
34
OC moderate AE
Acne with higher progestin doses | -Nausea, mastalgia, weight gain, headache
35
OC severe AE
- Thromboembolism (estrogen dependent) - Myocardial infarction - Cholestatic jaundice
36
OC neoplasm risk
Hepatic adenoma
37
OC contraindications
Impaired liver function, h/o thromboembolic disease, CAD, hyperlipidemia
38
OC caution with
Migraine, HTN, DM, gallbladder disease
39
OC drug interactions
- Decreased efficacy with antibiotics that affect GI absorption - Insulin efficacy reduced by OC
40
Tx for endometriosis
``` Medroxyprogesterone Acetate (IM injection every 3 months) -Amenorrhea side effect ```
41
-Clomiphene-
Antiestrogen (competitive) reduces negative feedback | -Induces ovulation
42
-Fulvestrant-
Pure estrogen receptor antagonist | -For treating hormone-responsive metastatic breast cancer in postmenopausal women
43
-Tamoxifen-
Anti-estrogen on breast - Pro-estrogen on lipids, bones, endometrium - Tx perimenopausal symptoms
44
-Raloxifene-
Anti-estrogen on breast, pro (1/2 strength) on bones - Tx post-menopausal osteoporosis, BRCA - No effect on perimenopausal symptoms
45
-Mifepristone (RU 486)- MOA Parent molecule Effect
Progesterone-R antagonist, glucocorticoid-R antagonist, prostaglandin dehydrogenase inhibitor - Norethindrone derivative - Stimulate uterine SM contractility
46
-Mifepristone- | other use
Glucocorticoid receptor antagonist | -Tx Cushing's secondary to ectopic ACTH secretion
47
Abortion regimen
Mifepristone in first 49 days | -Misoprostol (prostaglandin analog) 48 hours later to expel blastocyst

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