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Pharmacology- Test 4 Material > Progestins, Estrogens, Androgens > Flashcards

Progestins, Estrogens, Androgens Flashcards

1
Q

follicular phase

A
  • phase of the menstrual cycle in which female follicles develop and mature
  • ends with ovulation around day 14 of the cycle
  • main hormone controlling this phase is estradiol
  • progesterone levels are low during this phase
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2
Q

luteal phase

A
  • phase of menstrual cycle that occurs after ovulation
  • formation of corpus luteum and ends with pregnancy or menstruation
  • brought on by stimulatory effects of estradiol midway through cycle which stimulates LH spike
  • LH spike stimulates production of progesterone
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3
Q

androstenedione

A
  • androgen precursor to estrone
  • produced in female theca cells
  • converted to estrone in granulosa cells via action of aromatase
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4
Q

granulosa cells

A

-cells in a female required to convert androgens to various estrogens via action of aromatase

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5
Q

theca cells

A

-cells located outside of ovarian follicle who’s primary function is the conversion of cholesterol to androgens through the action of various CYP enzymes

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6
Q

estriol

A

-form of estrogen produced in the ovary

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7
Q

DHT (dihydrotestosterone)

A

-more potent form of androgen produced by the action of 5a-reductase which converts testosterone to DHT in other tissues outside of testes

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8
Q

aromatase

A

-enzyme responsible for conversion of androgens to estrogens in the granulosa cells of a female and the testes of a male

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9
Q

5a-reductase

A

-enzyme responsible for the conversion of testosterone to DHT in tissues outside of the testes

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10
Q

drospirenone

A

Progestin

  • used in combo progestin/estrogen oral contraceptives
  • has enhanced activity as MC antagonist and androgen antagonist
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11
Q

progesterone

A

Progestin

  • most important progesterone in humans
  • rapidly inactivated when given orally
  • decreases the amount of cervical mucous and increases its viscosity
  • main determinant of onset of menstruation
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12
Q

medroxyprogesterone acetate (Depo-Provera)

A

Progestin analog

  • commonly used in progestin only contraceptives
  • given as IM injections q 3 months
  • MOA: prevents fertilization by dec. amount and inc. the viscosity of cervical mucous (mimics normal progesterone, but at higher doses and without interruption)
  • Secondary MOA: prevents ovulation by inhibiting gonadotropin secretion (mimics inhibitory effects of progesterone on gonadotropin secretion)
  • S/Fx: headaches, abn. menstrual bleeding, dec. bone density with depo-provera
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13
Q

norethindrone (Micronor)

A

Progestin

  • commonly used in progestin only contraceptives or in combo oral progestin/estrogen contraceptives (monophasic to triphasic)
  • given as daily oral treatment or in IUDs implanted for 1-5 years (among most effective methods)
  • main MOA when progestin only: prevents fertilization by dec. amount and inc. the viscosity of cervical mucous (mimics normal progesterone, but at higher doses and without interruption)
  • main MOA when combo: prevents ovulation by inhibiting gonadotropin secretion (mimics inhibitory effects of progesterone and estrogen on gonadotropin secretion)
  • S/Fx: nausea, headaches, CV risks such as MI and thrombus (not recommended for smokers 35 and older), dec. glucose tolerance, weight gain, acne
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14
Q

norgestrel (Ovrette)

A

Progestin

  • commonly used in progestin only contraceptives
  • given as daily oral treatment or in IUDs implanted for 1-5 years (among most effective methods)
  • MOA: prevents fertilization by dec. amount and inc. the viscosity of cervical mucous (mimics normal progesterone, but at higher doses and without interruption)
  • Secondary MOA: prevents ovulation by inhibiting gonadotropin secretion (mimics inhibitory effects of progesterone on gonadotropin secretion)
  • S/Fx: headaches, abn. menstrual bleeding, dec. bone density with depo-provera
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15
Q

ulipristal (Ella)

A

Selective Progestin Response Modulator (SPRM)

  • effective oral emergency contraceptive if used within 5 days of intercourse (prescription required)
  • more effective then norgestrel (plan-b)
  • inhibits ovulation by antagonizing the actions of progesterone on the granulosa cell progesterone receptor (this action needed for follicular rupture)
  • also a progesterone agonist in the pituitary/hypothalamus and it delays LH surge
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16
Q

RU 486 (mifepristone)

A

Progestin Receptor Antagonist

  • oral, used for abortions (followed by oral prostaglandin)
  • used for post-coital contraception due to antagonizing effects of progesterone receptors everywhere including endometrium (progesterone normally required for implantation and maintenance of pregnancy)
  • also GC antagonist and is approved to be used as such in tx of Cushings and DM type II
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17
Q

FSH (Gonal-F)

A

Gonadotropin

  • IM injection used to induce follicular growth
  • commonly used prior to in vitro fertilization
18
Q

CG (Pregnyl)

A

Gonadotropin

  • IM injection used to induce ovulation
  • time sensitive admin based on growth of follicle
19
Q

gonadorelin

A

Synthetic GnRH

  • stimulate gonadotropin secretion
  • Tx: delayed puberty and anovulatory D/O in women.
  • Single injection or pulsatile pump
20
Q

luprolide

A

Long acting GnRH Agonist
-causes initial increases in androgen production, followed by a suppression of release of androgens (remember: give with flutamide)

21
Q

cetrorilex

A

GnRH antagonist

  • stop gonadotropin secretion
  • Prepercocious puberty in boys, endometriosis and dysmenorrhea.
22
Q

testosterone

A

Androgen

  • product of the hypothalamus-pituitary-testicular axis.
  • ineffective PO
  • Use: replacement for hypogonadism
  • Adverse: Virilization, feminization (males), azoospermia, small BALLS, edema, jaundice, hepatic carcinoma.
23
Q

testosterone proprionate

A

Androgen

-testosterone with a carboxy group (ester form).

24
Q

danazol

A

Androgen: 17 alpha alkylated adrogen

  • product of the hypothalamus-pituitary-testicular axis.
  • Contains OH group making it orally active, but increased liver toxicity
  • Use: replacement for hypogonadism
  • Adverse: Virilization, feminization (males), azoospermia, small BALLS, edema, jaundice, hepatic carcinoma.
25
Q

methytestosterone

A

Androgen: 17 alpha alkylated adrogen

  • product of the hypothalamus-pituitary-testicular axis.
  • Contains OH group making it orally active, but increased liver toxicity
  • Use: replacement for hypogonadism
  • Adverse: Virilization, feminization (males), azoospermia, small BALLS, edema, jaundice, hepatic carcinoma.
26
Q

dutasteride

A

Anti-androgen: 5-alpha reductase inhibitor

  • Used to treat androgen excess or androgen dependent D/O: BPH, prostate CA, Hurtuism, CAH
  • S/E: persistent sexual dysfunction
27
Q

finasteride

A

Anti-androgen: 5-alpha reductase inhibitor

  • Used to treat androgen excess or androgen dependent D/O: BPH, prostate CA, Hurtuism, CAH
  • S/E: persistent sexual dysfunction
28
Q

bicalutamide

A

Anti-androgen: Androgen receptor antagonist

  • Used to treat androgen excess or androgen dependent D/O: BPH, prostate CA, Hurtuism, CAH
  • S/E: persistent sexual dysfunction
29
Q

flutamide

A

Anti-androgen: Androgen receptor antagonist

  • Used to treat androgen excess or androgen dependent D/O: BPH, prostate CA, Hurtuism, CAH
  • S/E: persistent sexual dysfunction
30
Q

nilutamide

A

Anti-androgen: Androgen receptor antagonist

  • Used to treat androgen excess or androgen dependent D/O: BPH, prostate CA, Hurtuism, CAH
  • S/E: persistent sexual dysfunction
31
Q

estradiol

A

estrogen

-rapidly inactivated when given orally

32
Q

ethinyl estradiol

A

estrogen
contraceptive agent often used in combination with northindrone
-Oral (21 days on, 7 days off)
prevent ovulation by inhibiting the hypothalamus & pituitary
-mimic inhibitory effects of estrogen on gonadotropin secretion in high doses
-adverse effects: nausea, headache, thromboembolism, MI, decreased glucose tolerance, weight gain, acne, hirstism
-health benefits: decreased incidience of ovarian cyst & benign fibrocystic breast disease, & endometrial/ovraian CA, increased HDL and decreased LDL

33
Q

estrone sulfate

A

estrogen

34
Q

diethylstilbestrol

A

estrogen

no longer on the market

35
Q

bazedoxifene

A

SERM
with conjugated estrogens, approved for the treatment of postmenopausal symptoms
-agonist effects on bone
-antagonist effect on breast and endometrium

36
Q

tamoxifen

A

SERM

  • relief of postmenopausal symptoms
  • treatment of osteoporosis
  • estrogen-dependent breast cancer
37
Q

raloxifene

A

SERM

  • relief of postmenopausal symptoms
  • treatment of osteoporosis
  • estrogen-dependent breast cancer
38
Q

ospemifene

A

SERM

  • treatment of vaginal atrophy in postmenopausal women
  • agonist effects on vaginal epithelium
39
Q

clomiphene

A

estrogen receptor antagonist

  • induce ovulation, when given early in the follicular phase of the menstrual cycle
  • antagonize the inhibitory effects of estrogen on the pituitary & hypothalamus
40
Q

fulvestrant

A

estrogen receptor antagonist

  • induce ovulation, when given early in the follicular phase of the menstrual cycle
  • antagonize the inhibitory effects of estrogen on the pituitary & hypothalamus
41
Q

anastrozole

A

aromatase inhibitor

  • oral, non-steroidal
  • inhibit conversion of androgens to estrogens
  • useful in the treatment of breast CA or disorders where estrogen action needs to be inhibited
  • only give to postmenopausal women
  • can induce ovulation
  • side effects: arthralgia, hot flashes, other postmenopausal symptoms
42
Q

exemestane

A

aromatase inhibitor

  • oral, steroidal
  • inhibit conversion of androgens to estrogens
  • useful in the treatment of breast CA or disorders where estrogen action needs to be inhibited
  • only give to postmenopausal women
  • can induce ovulation
  • side effects: arthralgia, hot flashes, other postmenopausal symptoms

Pharmacology- Test 4 Material (12 decks)

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