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Pharm II > Pharm 2 Unit 3 Endocrine drugs > Flashcards

Pharm 2 Unit 3 Endocrine drugs Flashcards

1
Q

Leuprolide (Lupron)

A

long acting GnRH agonist

*inhibit HPG axis (initial surge, then @ 3 wk ultimate inhibition)

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2
Q

Goserelln (Zoladex)

A

long acting GnRH Agonist

*inhibit HPG axis (initial surge, then @ 3wk ultimate inhibition)

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3
Q

Cetrorelix (cetrolide)

A

GnRH Antagonist

*inhibit HPG axis from onset (4-5d)

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4
Q

Ganirelix (Antagon)

A

GnRH Antagonist

*inhibit HPG axis from onset (4-5d)

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5
Q

Purpose of both GnRH agonist and GnRH antagonists

A
  • ART tx (so full control over exogenous GnRH and thus FSH, LH)
  • sex steroid dependent cancers
    • note: if using GnRH agonist, also give antiandrogen to protect against initial surge
  • precocious puberty
  • endometriosis
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6
Q

difference bw GnRH agonist and GnRH antagonist

A

3 wk for suppression of gotro vs 4-5 days

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7
Q

SE of both GnRH agonist and GnRH antagonists

A

Menopausal sx, testicular atrophy

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8
Q

What happens in the follicular phase (what drives folliculognenesis and what does this result in) and what is another name for this phase

A

aka proliferative phase:

  • FSH drives folliculogenesis –> increase estrogen (FSH eventually inhibited as estrogen levels increase)
  • estrogen causes endometrial development
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9
Q

What happens during ovulation

A

Sustained and high amts of estrogen –> positive feedback on LH –> LH surge = ovulation and lutenization (LH controls progesterone secretion from corpus luteum)

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10
Q

What happens during the luteal phase (what maintains the CL and endometrium) and what is another name for this phase

A

Luteal phase aka Secretory Phase

  • LH maintains the corpus luteum (CL)
  • CL secretes progesterone and estrogen, maintain the endometrium
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11
Q

How does menstruation occur

A

no pregnancy, loss of LH –> CL degenerates and is shed during menstuation–> loss of progesterone and estrogen

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12
Q

how does progesterone influence FSH, LH and GnRH

A

progesterone neg inhibits FSH, LH and GnRH (overrides estrogen)

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13
Q

FSH in males stimulates

A

spermatogenesis

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14
Q

FSH in females stimulates

A

ovarian follicular development

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15
Q

LH in males stimulates

A

steroid (testosterone) synthesis

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16
Q

LH in females stimulates

A

ovulation, lueiinization of follicules, steroid (progesterone) production

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17
Q

hMG (human Menopausal Gonadotropin)

A

Gonadotropin: FSH
*used for infertility, ART (stimulates ovaries and estrogen production 9-12 d), spermatogenesis (takes months)

*made of LH and LH (menotropins)

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18
Q

Urofollitropin (uFSH, Bravelle)

A

Gonadotropin: purified FSH

*used for infertility, ART (stimulates ovaries and estrogen production), spermatogenesis

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19
Q

hCG (Pregnyl)

A

Gonadotropin: LH

*Ovulation, luteinization of follicules aka maintains corpus luteum, steroid (progesterone, testosterone up to 1 yr)

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20
Q

In general, what are gonadotropins used for

A

reversing infertility

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21
Q

in males specifically, how are gonadotropins used

A

Inducing spermatogenesis
LH: increases testosterone (up to a yr)
FSH: induces spermatogenesis (about 2-3 mth)

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22
Q

In females, how are gonadotropins used

A

IVF (ART)
FSH: stimulate ovaries and estrogen production (9-12 d)
LH: single dose to induce ovulation

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23
Q

What are the steps for Ovarian hyperstimulation for ART

A

Begin a baseline GnRH agonist (longer) or GnRH antagonist (shorter)

  • Once woman starts Menses
  • initiate gonadotropin, FSH 9-12 d
  • single dose hCG (LH) to induce ovulation
  • retrieve oocyte and fertilize with male sperm
  • give progesterone
  • implant 3 embryos (embryo transfer)
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24
Q

What are the side effects of Gonadotropins

A

ovarian enlargment
OVARIAN HYPERSTIMULATION SYNDROME* (life threatening)
*multiple births (20%)
*Gynecomastia (men)
*HA/depression, edema, precocious puberty

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25
Q

What would keep you from prescribing gonadotropins

A

sex-steroid dependent cancers

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26
Q

What are the major endogenous estrogens and what is their mechanism. Are they orally active

A
  1. Estradiol
  2. Estriol
  3. Estrone
    * not orally active

Mechanism: nuclear receptors (lipophilic/hydrophobic, crosses through CM and binds to receptors in cytoplasm or nucleus, interacts with DNA - protein synthesis)
*enterohepatic circulation

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27
Q

How are estrogens metabolized

A
  • conjugated by liver (excreted in bile)

- enterohepatic circulation, reverses conjugation and increases bioavailability

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28
Q

What is ovarian hyperstimulation syndrome

A

sudden ovarian enlargement, increased vascular permeability, rapid accumulation of fluid in peritoneal/pleural/pericardial cavities, hypovolemia, fever, shock

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29
Q

Estrogen function on the ovary, uterus, and endocervical gland?

A

ovary: prepare follicle cells for ovulation w/ FSH

Uterus: inuce ENDOMETRIAL CELL DIVISION AND GROWTH during follicular phase

endocervical gland: mucous

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30
Q

how does estrogen influence breast, puberty and growth

A

Breasts: growth (pregnancy and puberty)

Puberty: CLOSES EPIPHYSES

Bone: MAINTENANCE

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31
Q

how does estrogen influence blood, and metabolism

A

Blood: SYN OF CLOTTING PROTEINS,
^ PLATELET ADHESIVENESS

Metabolic: 
liver - clotting factors, 
HORMONE BINDING PROTEINS, 
INCREASES HDL and DECREASES LDL, 
Na/H20 retention
32
Q

Are naturally occuring estrogens orally active? if not, what have we done

A 
not orally active
we developed forms:
1. synthetic (contraceptives)
2. Conjugated (postmeno HRT)
3. Estradiol (creams/patches)
33
Q

what are exogenous estrogens used for

A

contraception, postmeno HRT, stimulating pubertal development, decrease uterine bleeding, suppress ovulation in dysmenorrhea

34
Q

SE of estrogen include

A
  1. endometrial hyperplasia
  2. Nausea/ breast tender
  3. **MIGRAINES (vasodilation in brain)
  4. gallbladder dz
  5. HTN
  6. **THROMBOEMBOLISM, accl blood CLOTTING

MIGRAINES, THROMBOEMBOLISM, CLOTTING

35
Q

primary SE of estrogen to know

A

migraines, thromboemolism, accelerated blood clotting

36
Q

Contraindicated to rx estrogen when

A
  • estrogen dep breast cancer**
  • uncontrolled HTN
  • liver dz
  • THOMBOEMBOLIC disorders
  • smoking and >35
  • preg (excess estrogen increases baby’s risk for cancer)
37
Q 
Tamoxifen (Nolvadex)
*class and Use
A

Antiestrogen:

  • SERM (selective estrogen receptor modulator)
  • antagonist: breast cancer (palliative, prophylactic)
  • agonist: bone (limits bone loss) uterus (may increase risk uterune cancer)

*might decrease HDL :(

tami’s happy bc helps breast cancer and osteoporosis but her HDL is now lower and her uterus has cancer

38
Q

Instead of tamoxifen, what other antiestrogen SERM is better for reducing likelihood of uterine cancer

A

Raloxifene (Evista)
*antagonist of uterine cancer
also antagonizes breast cancer and is good for osteoporosis

Raloxifene: decrease uterine/breast cancer, helps osteoporosis

39
Q

Instead of tamoxifen which may decrease HDL, what other antiestrogen SERM is better for HDL

A

Toremifene (Fareston)

this SERM is similar to Tamoxifen but INCREASES HDL as well

40
Q 
Clomiphene (Clomid)
*class and MOA
A

Antiestrogen: SERM
*antagonizes neg feedback of estrogen in hypothalamus
*Fertility drug: stimulates LH and FSH, induces Ovulation
*MULTIPLE PREGNANCIES
(clomiphene, clone, mult preg)

41
Q

main use for Raloxifene (Evista) SERM

A

decrease uterine/breast cancer, OSTEOPOROSIS

42
Q 
Fulvestrant (faslodex)
class and MOA
A 
Antiestrogen
FULL estrogen receptor antagonist
*use when want to fully antagonize estrogen
-not used much
   Fulvestrant FULL EST antagonist
43
Q

what is aromatase

A

final converting enzyme for estrogen production

44
Q

aromatase inhibitors generally speaking do what

A

inhibit estrogen synthesis

45
Q

Anastrozole (Arimidez)

class, use

A

Aromatase inhibitor
(inhibit estrogen but NOT adrenal steroid synthesis)

DOC: breast cancer tx POSTMENO (CI in premeno)
*2nd line adv breast cancer tx after tamoxifen failure in postmeno women

46
Q

Letrozole (femara)

class, use

A

Aromatase Inhibitor:
(inhibits estrogen syn but not adrenal steroid synth)

DOC: breast cancer in postmeno (CI in premeno)
*2nd line breast cancer tx after tamoxifen failure in postmeno women

47
Q

Exemastane (Aromasin)

A

Aromatase Inhibitor:
(inhibits estrogen syn but not adrenal steroid synth)
*Exemastane is an irreversible aromatase inhibitor**

DOC: breast cancer Postmeno
*2nd line breast cancer tx after tamoxifen failure

48
Q

SE of aromatase inhibitors

A

essentially menopause sx

-Diarrhea, abdominal pain, N/V, hot flashes, joint pain

49
Q

Contraindication aromatase inhibitors

A

Premenopausal
CATX

*if tamoxifen fails and women is premeno and has breast cancer.. go in and do ovarian ablation to make woman postmeno so that aromatase inhibitor can be used

50
Q

What is progesterone produced by and what mechanism does it use

A

Progesterone:

  • produced by CL
  • produced by fetal/placenta in pregnant women

MOA: nuclear receptor

51
Q

what are the biological functions of progesterone

A

Uterus: converts endometrium to secretory state, maintains pregnancy (suppresses contractility)

  • regulates cervical mucus, lobulolveolar development in mammary duct, increases body temp (thermogenic)
52
Q

is natural progesterone orally active? if not, what have we done medically

A

not orally active so we made Progestins:

  • 19-nortestosterone (progestin& andogenic activity)
  • Progesterone derivatives (varying levels of androgen activity)
53
Q

Use of Progestins

A

Contraception, prevent endometrial hyperplasia in HRT

SE: HTN, reduced HDL (19-nortestos), depression, drowsiness

54
Q

in general, antiprogestins are

A

abortion like drugs

55
Q

Mifepristone (RU 486)

*class, use, SE

A

Antiprogestin:
*progesterone/glucocorticoid receptor antagonist
USE - terminate pregnancy (w/ prostglandin)
SE: vomiting, dirrhea, pelvic pain, vaginal bleeding

56
Q

Danazol (Danocrine)

*class, use, SE

A

Antiprogestin:
weak progestin and androgen, suppresses ovarian function
USE: ENDOMETRIOSIS***
SE: lots

57
Q

Contraception options

A

combination of estrogen and progestin

*DROSPIRENONE/ETHINYL ESTRADIOL

58
Q

Drospirenone/ethinyl estradiol use, MOA

  • Yasmin?
A
  1. 9% effective CONTRACEPTION
    * INHIBIT OVULATION bc no LH surge
    - change cervical mucus to block sperm
    - change endometrium to decrease implantation

*progestin w/drawal initiates bleeding

59
Q

what contraception combo tx is typically used and how is it dosed

A

estrogen: usu ethinyl estradiol or mestranol
Progestin: levonorgestrel or norethindrone

*used to due high estrogen, but had lots of SE
E:P ratio more important than amt (use minimal)
*vary E:P in 3 stages (in 21 d) to mimic normal hormonal cycle
*estrogen stays same throughout (20-35 ug or for HRT 5-10 ug), increase progestin each stage

60
Q

Seasonal

class, cycle time

A

newer combination oral contraceptive

84 d on, 7 d off

61
Q

Seasonique

class, timing

A

New combo oral contraceptive

84 d on, 7 d estrogen only (to minimize bleeding)

62
Q

Lybrel

class, timing

A

New combo oral contraceptive

ALWAYS on

63
Q

Adverse SE of new oral contraceptivies

A

increased breakthrough bleeding (esp 1st yr), hard to tell if you are pregnant or just missing period

64
Q

Yasmin (Yaz)

class, use, advantages

A

Combination oral contraceptive

  • ethinyl estradioal and drospirenone (mineralcorticoid antagonist)
  • advantage: less water retention, FDA approved for PMDD**, very little androgenic properties
  • think spironolactone, dospirenone
65
Q

Natazia

class, use, info

A

Newest oral combination contraceptive

  • uses estradiol valerate to produce E2 in vivo (bioidentical hormone0
  • uses dienogest as progestin, weird 4 cycle regimen
66
Q

Nuvaring

class, info

A

Vaginal ring contraceptive

*3 wk supply etonogesterel and ethinyl estradiol

67
Q

Progestin only contraception options include

A
  1. Mini pills
  2. Depo-provera
  3. Implanon
  4. Mirena
68
Q

what are mini-pills

A

progestin only contraception

  • 87-98% effective
  • adolescents and breast feeding
69
Q

what is depo-provera

A

Progestin only contraception 3 mth depot injection of medroxyprogesterone

70
Q

what is implanon

A

Progestin only contraception - single silastic tube implanted in art
>99% effective 3 yr

71
Q

What is mirena

A

Progestin only IUC containing levonorgesterel

99.9% effective up to 5 yr

72
Q

What are Post-Coital contraceptive options

A
  1. Plan B
  2. Preven
  3. Mifeprisotone (RU 486, Mifeprix)
73
Q

Plan B

class, use

A

Post-coital emergency contraceptive option

  • levonorgestrel only pill
  • take w/in 72 hr (sooner=better)
  • available to 18+ w/o rx
74
Q 
Preven
class use
A

similar to Plan B post coital emergency contraceptive option, but also has ethyinyl estradiol

75
Q

Mifepristone (RU-486)

A

post-coital emergency contraceptive option

  • also used to prevent implantation if admin 1/in 72 hr post intercourse
  • antiprogestin normally used to terminate preg

Pharm II (12 decks)

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