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PPP 249 SPRING QUARTER 2023 > Sex Hormone Pharmacology > Flashcards

Sex Hormone Pharmacology Flashcards

1
Q

Estrogens :

  1. Estradiol or E2
    - primary systemic ___
    -Avail in many formulations (4) ?
  2. estrone or E1
    - how active?
    -Available as a component of ? (2)
  3. Ethinyl estradiol
    -synthetically modified to have?
    - how potent?
    -available in ?
  4. Estriol or E3
    - not a __
    -Less potent than ?
A
  1. estrogen
    tablet, cream, patch, ring
  2. 1/3 as active as estradiol
    - conjugated estrogens like premarin , esterified estrogens (Menest)
  3. slower hepatic metab
    - 15-20x more potent than e2
    - combo products
  4. drug
    E2
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2
Q

MOA OF ESTROGEN
1. Slow effects are transcription mediated. describe 3 steps

  1. rapid effects are transcription INDEPENDENT (three steps)
A
  1. estrogen binds receptor in cytoplasm or nucleus. E-R complex dimerizes and initiates transcription . protein synthesis mediates cell growth, function and differentiation
  2. E binds R in cytoplasm or cell membrane
    E-R complex activates kinases and other proteins
    2nd messengers mediate rapid cellular effects
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3
Q

Developmental effects of ESTROGEN :
F, G, S

Excess = incr risk of?

A

female genitalia
growth like puberty growth spurt and epiphyseal closure of long bones
secondary sex traits like body contours, hair growths, skin pigmentation, breast devel

excess = incr risk of breast cancer

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4
Q

Estrogen Nervous System Effects : B, M, S

A

behavior
mood –> menopause causes mood swings and depression
sympathetic tone -> menopause causes vasomotor sx’s like hot flashes

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5
Q

Cardio Effects of Estrogen
- Coagulation . helps incr factors (5) and decrease ? (3)
If excess leads to increased?

-Cholesterol
incr __ decr _(3)__, menopause causes __

Smooth musc relaxation and vasodilation
incr __ and __, decr __ and __
-menopause causes hot flashes
-excess causes ? (3)

A

2, 7, 9,10, 12
protein s and C, antithrombin
thrombosis risk like : stroke, MI, DVT, PE

HDL, LDL LPA and total cholesterol , dyslipidemia

nitric oxide, prostacyclin
angiotensin, endothelin

paradoxical HTN, edema, bloating

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6
Q

Metabolic and Hepatic Effects :
-Increases T_____
-Incr B____
-Incr Synthesis of ___
-___ resistance

Oral admin increases __ and decr __

A

triglycerides, bile concentration leading to gallstones, clotting factors , insulin

Toxicity, bioavailability

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7
Q

Repro Effects
-Increases __ growth
proliferative phase. Menopause causes __

Progesterone required for ?
Secretory phase
an imbalance results in ?

Enhances progesterone’s suppression of ___
-combined with progestins in OC’s

A

endometrial growth
abnormal uterine bleeding

endometrial maturation
endometriosis, endometr cancer

GnRH

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8
Q

Skeletal effects of Estrogen :
Increases ___ by inhibiting __ stimulating __ incr ___ survival
Menopause causes : ___

Epiphyseal closure ! (men and women)

A

bone mineral density
osteoclasts (major effect)
osteoblasts
osteocyte
osteoporosis

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9
Q

Avoid contraindications for giving HRT!
What are 6 CI’s?

Select the right drug !

Uterus intact –>
Uterus absent –>
Moderate CVD Risk –>

A

breast cancer, liver disease, stroke, DVT, CVD, High CVD Risk

estrogen + progestin
estrogen only
Avoid oral route

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10
Q

Progestins

MOA?

Many progestins act on receptors for other hormones such as (3)?

A

nuclear/cytoplasmic receptors similar to estrogen

estrogen, androgen, mineralocorticoid

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11
Q

Nervous System effects of Progestins
1. D__
2. INCR ___
3. INCR ___ (weight gain possible ae)

A

drowsiness, take oral contra’s at night
body temp, used for fertility monitoring
appetite

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12
Q

Repro effects : Contraceptive effect by 3 mechs

  1. Decreases transit of ___
    -thickens ___ and impairs ___ through __
  2. Suppresses ___
    - decr ___ by neg feedback
    -effect enhanced by combining with estrogen
  3. Matures ____
    -secretory phase
    -continuous admin impairs ___
    -Abrupt withdrawal triggers ___
    -Deficiency : may trigger ___
A
  1. sperm
    cervical mucus, motility, fallopian tubes
  2. ovulation , GnRH
  3. endometrial lining
    - implantation
    menstruation
    breakthrough bleeding LATE CYCLE
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13
Q

Estrogen Deficiency :
Causes? (3)

Progestin deficiency?
Causes (2)?

Progestin Excess causes ? (2)

What can cause hypertension?

A

Early cycle breakthru bleeding
HYPOmenorrhea, or amenorrhea

LATE CYCLE breakthru bleeding
HYPERmenorrhea

HYPOmenorrhea or AMENORRHEA

estrogen excess

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14
Q

Estrogen + Progestin
-Contraindicated in women with risk factors for ___ like ?

Progestin only
-PO more difficult to take and can be less reliable
-less ___
Half life of ?
-Requires?
-Same ____
-What forms avoid these issues?

A

thrombosis (CVD, DVT/PE, Afib, Stroke, smokers >35 yo)

pituitary suppression
8 hrs
perfect adherence
time daily plus or minus three hrs

parenteral

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15
Q

Dosage forms for Estrogen + progestin (3)

for progestin only? (4)

What’s the most effect dosage form?

A
  1. oral, td patch, intravag ring
  2. oral, im injection, subdermal implant, intrauterine device
  3. Implant or IUD
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16
Q

Classification of Progestins : Progesterone derivs

  1. Progesterone has short ___ but low __
  2. Medroxyprogest is more __ and longer __
    acetate used as ?
  3. Megestrol
    -Unique effects at multiple receptors like ____
    -Used for ___ and __
A

half life, bioavail

potent, half life, long acting injection

mineralcorticoid, glucocorticoid
promotion of weight gain, breast cancer palliation

17
Q

Testosterone Derivs
1. first gen is ? It is moderately __ and the ONLY ___
2. second gen? it is the MOST ___

  1. third gen? ___ androgenic
  2. fourth gen is a ___ derivative called ?
    -It is ____ androgenic
A
  1. norethindrone
    androgenic
    progestin only OCP
  2. norgestrel, levonorgestrel , androgenic
  3. norgestimate. LESS
  4. spironolactone , drospirenone , ANTI
18
Q

Androgens :

  1. Primary systemic androgen?
    -available in ___ forms?
    -NOT ___
  2. DHT
    -more potent than?
    -Produced ___ in certain tissues
    -NOT a __
A
  1. testosterone
    parenteral (patch, gel, injection, implant)
    orally bioavail

Testosterone
locally (Skin and prostate)

drug

19
Q

Androgen Devel Effects
-___ genitalia , growth , secondary sex traits like?
-___ devel .
if pregnant woman exposed to androgen, can be __. pregnant woman dont touch drug products of androgens

A

male , deepening of voice
fetal
teratogenic , preg categ X

20
Q

Androgen Nervous System Effects
-Behavior, energy and mood
an excess causes? Deficiency?

Cardio effects
-Coag : Increases ? Excess causes?
-Cholest : DECR __, excess?
-Sodium/H2O retention : ____ stimulation?
Excess? (3)
-Red blood cell production : Stimulation of __
Deficiency?

A

Aggression (think body builders)
depression

clotting factor synthesis. incr risk of stroke, heart attack and DVT

HDL, dyslipidemia

mineralocorticoid receptor . edema, HTN, electrolyte imbalance

erythropoietin , anemia

21
Q

Metab and Hepatic Effects

-Metab of lipids, proteins, and carbs so an imbalance of the androgens causes ? (2)

-High first pass ___. (use parenteral routes)

-___ . incr risk of cholestasis and liver cancer especially with oral admin

A

insulin resistance, dyslipidemia

metabolism

hepatotoxicity

22
Q

Repro Effects : Incr ___ growth which can cause? (2)

-Sexual Function : Deficiency causes ?
-Spermatogenesis : Imbalance causes?

Also has endometrial effects in females so its combined with ___ for female __

A

prostate, BPH, Prostate cancer

decr libido

infertility

estrogen, hrt

23
Q

SKM effects
-Incr muscle __ and __. deficiency = ___. this is why its abused in performance enhancing drugs

-Incr ___ so a deficiency causes osteoporosis

Dermatological effects

“Male Pattern “ ____

Increases __ and ___ production so an excess causes ___

hair growth on face and body so an excess in females is known as ___

A

growth, strength. muscle weakness

bone mineral density

baldness
sweat , sebum, acne

hirsutism

24
Q

Modified Androgens have decreased ___ which allows for increased bioavail and ___ dosing
-increased half life allows for ____

  1. Methyltestosterone is used for?
  2. Oxandrolone used for ?
  3. Danazol used for?
A

hepatic metabolism
PO
once daily dosing

hypogonadism
weight gain
endometriosis

25
Q

Anti Hormonal Agents : GnRH Antag and Agonist

How do each work?

GnRH Antags : DEGARELIX
-Decreases ? Used for?

GnRH agonist : GOSERELIN
- decr ?
-FDA indications for hormone dep cancers but a drawback is?
if it’s used for cancer, initiate with a ?
Also used off label for?

A

Antag : blocks GnRH, no FSH and LH
Agonist : Continuously stimulates GnRH which in turn has an inhibitory effect on FSH and LH

FSH and LH –> decr sex hormones
hormone dependent cancers

FSH and LH and sex hormones

transient incr in hormone production ,tumor flare

2nd anti hormone drug

transgender therapy

26
Q

Synthesis Inhibs

For each target, state the drug and indication

  1. 17 HYDROXYLASE (TESTOSTERONE)
  2. 5 Alpha reductase (DHT)
  3. Aromatase (Estrogen)
A
  1. abiraterone (strong inhib) –> prostate cancer
    spironolactone (weak inhib) –> hirsutism
  2. Finasteride and dutasteride –> BPH and baldness
  3. Anastrazole, letrozole, exemestane –> breast cancer
27
Q

Abiraterone should always be given with? What would happen if you didnt?

A

Steroids (prednisone)

Decrease in Cortisol, INCR ACTH, INCR Aldost, hypertension and hypokalemia

28
Q

Major SERM’s : For the following drugs, state what their activity by site is (Agonist/antag at) and indications

  1. Tamoxifen
  2. Raloxifene

Other SERM’s such as :Clomiphene is an antag of?
Used for ?

A
  1. Agonist at bone, cholesterol, uterus
    antag at breast
    indication is breast cancer
  2. agonist at bone and cholesterol
    antag in breast and uterus

indic breast cancer and osteoporosis

hypothalamic negative feedback
infertility (stimulates ovulation)

29
Q

Hormone receptor antags : For the following drugs state which receptor is blocked and what its indication is?

Fulvestrant

Mifepristone

Bicalutamide

Spironolactone

A
  1. estrogen –> breast cancer
  2. progestin –> medical abortion combined with misoprostol
  3. Androgen –> prostate cancer , strong antags
  4. androgen –> hirsutism, weak antag

PPP 249 SPRING QUARTER 2023 (11 decks)

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