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MSII Pharmacology > Unit 1 - Pharmacology of Reproduction > Flashcards

Unit 1 - Pharmacology of Reproduction Flashcards

1
Q

early follicular phase happenings

A

days 1-7

  • menstruation occurs at the beginning of the follicular phase
  • FSH and LH levels are increased relative to baseline
  • estrogen and progesterone levels are low
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2
Q

late follicular phase happenings

A

days 7-14

  • growth, maturation of ovarian follicles, and one follicle becomes dominant in growth and hormone escretion
  • FSH levels decrease due to negative feedback
  • estrogen levels increase due to positive feedback
  • progesterone levels remain low
  • endometrial lining continues to grow and thicken
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3
Q

pre-ovulation and ovulation happenings

A

days 13-14

-LH surge stimulates follicular rupture and ovulation occurs within 48 hours

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4
Q

luteal phase happenings

A

ruptured follicle develops into corpus luteum that makes large amounts of progesterone and estrogen

  • progesterone facilitates thickening of endometrial lining and development of blood vessels
  • absence of fertilization, the corpus luteum begins to degenerate and ceases hormone production
  • thus levels of estrogen and progesterone drop, and menstruation occurs
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5
Q

what are the different levels of estrogens?

A
  1. natural estrogens (E1/2/3)
  2. synthetic estrogens
    - steroidal synthetic estrogens
    - nonsteroidal synthetic estrogens

all differ by their R2/3 side chains (C3/17)

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6
Q

what is the primary source of estradiol in premenopausal women?

A

ovary

  • granulosa cells of ovarian follicles make estrogens
  • estradiol can be converted to estrone and estriol in liver
  • estrogens converted from androstenedione and testosterone in ovaries or in other tissues
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7
Q

what are examples of synthetic steroidal estrogens in use?

A
  1. estradiol esters - estradiol valerate, estradiol cypionate
  2. conjugated estrogens - estrone sulfate, equilin sulfate
  3. aklyl estrogens - ethinyl estradiol, mestranol
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8
Q

what is the major circulating estrogen in premenopausal women, men, and postmenopausal women?

A

pre: estradiol

men/post: estrone

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9
Q

where is aromatase expressed?

A

estrogen-producing cells of ovaries, placenta, adrenal gland, adipose tissue, testicles, and brain

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10
Q

what are examples of nonsteroidal synthetic estrogens?

A
  1. diethylstilbestrol (DES) was reported to increase risk of clear cell adenocarcinoma in vagina and cervix
  2. chlorotrianisene
  3. methallenestril
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11
Q

pharmocokinetics of estrogens

A

absorbed through skin, mucous membranes, and GIT

-in circulation, bind to SHBG (sex-hormone binding globulin), and albumin with lower affinity

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12
Q

pharmacokinetics of E2

A

mainly metabolized in liver to E1

  • significant amounts of estrogens and active metabolites are excreted in bile and reabsorbed from intestine
  • estradiol is not used orally frequently due to extensive first pass effect
  • -micronization increases t 1/2 of E2 and reduces GIT destruction
  • excretion of inactive metabolites occurs via urine
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13
Q

effects of estrogen on female maturation and reproductive system

A

develpoment of secondary sexual characteristics and sexual organs

  • stimulates proliferation of endometrium and follicular growth
  • stimulates breast cell growth
  • induces synthesis of progesterone receptors
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14
Q

negative feedback of estrogen

A

high estrogen causes negative feedback loop on anterior pituitary and hypothalamus to slow release of FSH and estrogen

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15
Q

positive feedback of estrogen

A

high concentrations at end of follicular phase to positively regulate pituiary to trigger FSH and LH release that causes ovary to produce more estrogen
-high estrogen and LH cause ovulation

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16
Q

cardiovascular effects of estrogen

A

“estrogen-alone” hormone therapy has no effect on CHD, but increases the risk of stroke and deep vein thrombosis in postmenopausal women

17
Q

effects of estrogen on lipoprotein

A

increase HDL and decrease LDL levels

18
Q

how is estrogen used as contraception

A

synthetic estrogen like ethinyl estrodiol (steroidal alkyl estrogen) is used with progestin to prevent pregnancy

19
Q

postmenopausal hormone therapy?

A

give estrogen to reduce postmenopause symptoms like hot flashes, atrophic vaginitis, and osteoporosis

20
Q

what are common adverse effects of estrogen therapy?

A

nausea, breast tension/pain, vaginal bleeding, headache, weight gain, HTN

21
Q

relationship between estrogen therapy and breast/cervical/endometrial cancers

A

breast: controversial; previous showed increased risk with >5 year use, but recently no increase with estrogen alone
cervical: may increase
endometrial: may increase

22
Q

relationship between estrogen therapy and HA, stroke, GB disease

A

increases risk of all

23
Q

contraindications of estrogen therapy

A

strongly contraindicated if breast/endometrial cancer, endometriosis, and undiagnosed vaginal bleeding
-generally contraindicated if pregnant, thromboembolic disease, HTN, hepatic disease, or family history of breast/uterine cancer

24
Q

what are antiestrogen therapeutics and example?

A

compounds that are estrogen receptor competitive antagonists (or partial agonists in some setting)
-include tamoxifen citrate and clomiphene citrate

25
Q

affinity of tamoxifen for ER?

A

estrogen has much higher binding affinity for its receptor than Tamoxifen

  • must be used in concentration much higher than estrogen to maintain inhibition of breast cancer cells
  • given orally, 10-20 mg 2x daily, with 7-14 hour halflife
26
Q

clomiphene citrate isomers

A

cis: zuclomiphene (weak estrogen agonist)
trans: enclomiphene (potent antagonist)

27
Q

where is progesterone made?

A

secreted in females by CL of ovary
-in pregnancy, high levels are made and secreted by placenta
males make it in the testes
-adrenal cortex makes it in both sexes
-production is stimulated by LH and gonadotropin

28
Q

physiological functions of progesterone

A

stimulates endometrium to develop secretory glands and support fertilized egg implantation

  • low levels in first several weeks lead to miscarriage
  • can suppress endometrial cancers b/c long-term use atrophies emdometrium
  • high levels trigger negative FB on hypothalamus to stop releasing gonadotropin and suppress ovulation
29
Q

what are the 2 general uses of progestins?

A
  1. contraception - used in combo with estrogens or in progestin-only methods
  2. hormone replacement therapy - postmenopausal women
    - counters endometrial stimulatory effects of estrogen and reduces risk of endometrial cancer
30
Q

what are the two types of progestins?

A
  1. natural (micronized and transvaginal)

2. synthetic

MSII Pharmacology (43 decks)

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