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Pharm II > Pharm 2 Unit 3 Endocrine drugs > Flashcards

Pharm 2 Unit 3 Endocrine drugs Flashcards

(75 cards)

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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
What would keep you from prescribing gonadotropins
sex-steroid dependent cancers
26
What are the major endogenous estrogens and what is their mechanism. Are they orally active
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
27
How are estrogens metabolized
- conjugated by liver (excreted in bile) | - enterohepatic circulation, reverses conjugation and increases bioavailability
28
What is ovarian hyperstimulation syndrome
sudden ovarian enlargement, increased vascular permeability, rapid accumulation of fluid in peritoneal/pleural/pericardial cavities, hypovolemia, fever, shock
29
Estrogen function on the ovary, uterus, and endocervical gland?
ovary: prepare follicle cells for ovulation w/ FSH Uterus: inuce ENDOMETRIAL CELL DIVISION AND GROWTH during follicular phase endocervical gland: mucous
30
how does estrogen influence breast, puberty and growth
Breasts: growth (pregnancy and puberty) Puberty: CLOSES EPIPHYSES Bone: MAINTENANCE
31
how does estrogen influence blood, and metabolism
Blood: SYN OF CLOTTING PROTEINS, ^ PLATELET ADHESIVENESS ``` Metabolic: liver - clotting factors, HORMONE BINDING PROTEINS, INCREASES HDL and DECREASES LDL, Na/H20 retention ```
32
Are naturally occuring estrogens orally active? if not, what have we done
``` not orally active we developed forms: 1. synthetic (contraceptives) 2. Conjugated (postmeno HRT) 3. Estradiol (creams/patches) ```
33
what are exogenous estrogens used for
contraception, postmeno HRT, stimulating pubertal development, decrease uterine bleeding, suppress ovulation in dysmenorrhea
34
SE of estrogen include
1. endometrial hyperplasia 2. Nausea/ breast tender 3. **MIGRAINES (vasodilation in brain) 4. gallbladder dz 4. HTN 5. **THROMBOEMBOLISM, accl blood CLOTTING MIGRAINES, THROMBOEMBOLISM, CLOTTING
35
primary SE of estrogen to know
migraines, thromboemolism, accelerated blood clotting
36
Contraindicated to rx estrogen when
- estrogen dep breast cancer** - uncontrolled HTN - liver dz - THOMBOEMBOLIC disorders - smoking and >35 - preg (excess estrogen increases baby's risk for cancer)
37
``` Tamoxifen (Nolvadex) *class and Use ```
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
Instead of tamoxifen, what other antiestrogen SERM is better for reducing likelihood of uterine cancer
Raloxifene (Evista) *antagonist of uterine cancer also antagonizes breast cancer and is good for osteoporosis Raloxifene: decrease uterine/breast cancer, helps osteoporosis
39
Instead of tamoxifen which may decrease HDL, what other antiestrogen SERM is better for HDL
Toremifene (Fareston) | this SERM is similar to Tamoxifen but INCREASES HDL as well
40
``` Clomiphene (Clomid) *class and MOA ```
Antiestrogen: SERM *antagonizes neg feedback of estrogen in hypothalamus *Fertility drug: stimulates LH and FSH, induces Ovulation *MULTIPLE PREGNANCIES (clomiphene, clone, mult preg)
41
main use for Raloxifene (Evista) SERM
decrease uterine/breast cancer, OSTEOPOROSIS
42
``` Fulvestrant (faslodex) class and MOA ```
``` Antiestrogen FULL estrogen receptor antagonist *use when want to fully antagonize estrogen -not used much Fulvestrant FULL EST antagonist ```
43
what is aromatase
final converting enzyme for estrogen production
44
aromatase inhibitors generally speaking do what
inhibit estrogen synthesis
45
Anastrozole (Arimidez) | class, use
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
Letrozole (femara) | class, use
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
Exemastane (Aromasin)
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
SE of aromatase inhibitors
essentially menopause sx | -Diarrhea, abdominal pain, N/V, hot flashes, joint pain
49
Contraindication aromatase inhibitors
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
What is progesterone produced by and what mechanism does it use
Progesterone: - produced by CL - produced by fetal/placenta in pregnant women MOA: nuclear receptor
51
what are the biological functions of progesterone
Uterus: converts endometrium to secretory state, maintains pregnancy (suppresses contractility) - regulates cervical mucus, lobulolveolar development in mammary duct, increases body temp (thermogenic)
52
is natural progesterone orally active? if not, what have we done medically
not orally active so we made Progestins: * 19-nortestosterone (progestin& andogenic activity) * Progesterone derivatives (varying levels of androgen activity)
53
Use of Progestins
Contraception, prevent endometrial hyperplasia in HRT SE: HTN, reduced HDL (19-nortestos), depression, drowsiness
54
in general, antiprogestins are
abortion like drugs
55
Mifepristone (RU 486) | *class, use, SE
Antiprogestin: *progesterone/glucocorticoid receptor antagonist USE - terminate pregnancy (w/ prostglandin) SE: vomiting, dirrhea, pelvic pain, vaginal bleeding
56
Danazol (Danocrine) | *class, use, SE
Antiprogestin: *weak progestin and androgen, suppresses ovarian function USE: ENDOMETRIOSIS**** SE: lots
57
Contraception options
combination of estrogen and progestin | *DROSPIRENONE/ETHINYL ESTRADIOL
58
Drospirenone/ethinyl estradiol use, MOA - Yasmin?
99. 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
what contraception combo tx is typically used and how is it dosed
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
Seasonal | class, cycle time
newer combination oral contraceptive | 84 d on, 7 d off
61
Seasonique | class, timing
New combo oral contraceptive | 84 d on, 7 d estrogen only (to minimize bleeding)
62
Lybrel | class, timing
New combo oral contraceptive | ALWAYS on
63
Adverse SE of new oral contraceptivies
increased breakthrough bleeding (esp 1st yr), hard to tell if you are pregnant or just missing period
64
Yasmin (Yaz) | class, use, advantages
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
Natazia | class, use, info
Newest oral combination contraceptive * uses estradiol valerate to produce E2 in vivo (bioidentical hormone0 * uses dienogest as progestin, weird 4 cycle regimen
66
Nuvaring | class, info
Vaginal ring contraceptive | *3 wk supply etonogesterel and ethinyl estradiol
67
Progestin only contraception options include
1. Mini pills 2. Depo-provera 3. Implanon 4. Mirena
68
what are mini-pills
progestin only contraception * 87-98% effective * adolescents and breast feeding
69
what is depo-provera
Progestin only contraception 3 mth depot injection of medroxyprogesterone
70
what is implanon
Progestin only contraception - single silastic tube implanted in art >99% effective 3 yr
71
What is mirena
Progestin only IUC containing levonorgesterel | 99.9% effective up to 5 yr
72
What are Post-Coital contraceptive options
1. Plan B 2. Preven 3. Mifeprisotone (RU 486, Mifeprix)
73
Plan B | class, use
Post-coital emergency contraceptive option * levonorgestrel only pill * take w/in 72 hr (sooner=better) * available to 18+ w/o rx
74
``` Preven class use ```
similar to Plan B post coital emergency contraceptive option, but also has ethyinyl estradiol
75
Mifepristone (RU-486)
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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