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Test 9 > Pharm 3 Estrogen/Progestin > Flashcards

Pharm 3 Estrogen/Progestin Flashcards

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

A

Increase HDL, triglycerides

Decrease LDL

20
Q

Estrogen effect of sex behavior

A

-Mediates testosterone’s effect on libido

21
Q

Estrogen other effects

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

Progesterone v Estrogen

A

Antagonize estrogen

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

Progesterone other effects

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

Primary hypogonadic impaired development Tx

A

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

25
Q

Hysterectomy HRT

A

Unopposed estrogen (don’t worry about progesterone)

26
Q

Other clinical uses for Estrogen

A
  • Ovarian suppression for hyperandrogenism
  • Ovulation suppression in dysmenorrhea
  • Androgen-dependent prostate cancer (suppress gonadotropin secretion)
27
Q

Estradiol levels postmenopausal

A

1/4 that of males

28
Q

Postmenopausal HRT alleviates (5)

A 
Sleep disturbances
Hot flashes
Urogenital changes
Osteoporosis
High cholesterol
29
Q

HRT contraindications

A

Liver disease

Breast or other estrogen-dependent cancer

30
Q

Low dose combination OC

A
  • All use ethinyl estradiol
  • Norgestrel for monophasic
  • Norethindrone for bi/triphasic
31
Q

Monophasic v Triphasic

A
  • Triphasic eliminates period for 90 days

- Triphasic reduces total dose of progestin (reduced SE)

32
Q

OC MOA

A

Inhibit gonadotropin secretion, suppress ovulation (progestin only blocks ovulation 60-80%)

  • Thicken cervical mucus
  • Reduce tubal secretion/motility
  • Change uterine endometrium
33
Q

OC mild AE

A

Breakthrough bleeding

-Tx with higher dose estrogen or different progestin

34
Q

OC moderate AE

A

Acne with higher progestin doses

-Nausea, mastalgia, weight gain, headache

35
Q

OC severe AE

A
  • Thromboembolism (estrogen dependent)
  • Myocardial infarction
  • Cholestatic jaundice
36
Q

OC neoplasm risk

A

Hepatic adenoma

37
Q

OC contraindications

A

Impaired liver function, h/o thromboembolic disease, CAD, hyperlipidemia

38
Q

OC caution with

A

Migraine, HTN, DM, gallbladder disease

39
Q

OC drug interactions

A
  • Decreased efficacy with antibiotics that affect GI absorption
  • Insulin efficacy reduced by OC
40
Q

Tx for endometriosis

A 
Medroxyprogesterone Acetate (IM injection every 3 months)
-Amenorrhea side effect
41
Q

-Clomiphene-

A

Antiestrogen (competitive) reduces negative feedback

-Induces ovulation

42
Q

-Fulvestrant-

A

Pure estrogen receptor antagonist

-For treating hormone-responsive metastatic breast cancer in postmenopausal women

43
Q

-Tamoxifen-

A

Anti-estrogen on breast

  • Pro-estrogen on lipids, bones, endometrium
  • Tx perimenopausal symptoms
44
Q

-Raloxifene-

A

Anti-estrogen on breast, pro (1/2 strength) on bones

  • Tx post-menopausal osteoporosis, BRCA
  • No effect on perimenopausal symptoms
45
Q

-Mifepristone (RU 486)-
MOA
Parent molecule
Effect

A

Progesterone-R antagonist, glucocorticoid-R antagonist, prostaglandin dehydrogenase inhibitor

  • Norethindrone derivative
  • Stimulate uterine SM contractility
46
Q

-Mifepristone-

other use

A

Glucocorticoid receptor antagonist

-Tx Cushing’s secondary to ectopic ACTH secretion

47
Q

Abortion regimen

A

Mifepristone in first 49 days

-Misoprostol (prostaglandin analog) 48 hours later to expel blastocyst

Test 9 (17 decks)

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