Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharmacology > Gonadal Hormones > Flashcards

Gonadal Hormones Flashcards

1
Q

Ethinyl Estradiol
Mestranol (pro-drug converted to ^)

A

Synthetic Estrogens

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Main effects of estrogen

A
  • Female Maturation
    • 2° sex characteristics
  • Endometrial proliferation
  • Metabolic
  • Protein Synthesis
    • Increase in hepatic production of binding proteins eg. SHBG
  • Vasculature
    • Increase production of NO and prostacyclin
  • Fluid Balance: Na+ and H20 retention
  • Other Effects
    • Reproductive Function
    • Sexual Behavior
    • GI Tract
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

describe Estrogen use in Postmenopausal Hormonal Therapy

A
  • Decreases risk of osteoporosis (does not treat osteoporosis)
  • Reestablishes feedback on hypothalamic control of NE secretion, leading to decreased frequency of hot flashes
  • Reverses postmenopausal atrophy of the vulva, vagina, urethra, and trigone of the bladder
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

describe other clinical uses’ of estrogen

A
  • Primary hypogonadism
    • Progestin added after first uterine bleeding
  • Treatment of androgen-dependent prostate cancer
  • OCPs
  • Menstrual abnormalities
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

List minor AEs of estrogen

A
  • Uterine bleeding
  • Nausea
  • Breast tenderness
  • Melasma
  • Peripheral edema
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

List moderate/severe AEs of estrogen

A
  • ↑ risk of endometrial cancer
    • ​offset by combining estrogen with progestin
  • ↑ migraine frequency
  • Cholestasis and gallbladder disease
  • HTN
  • Thromboembolism
  • Depression
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

estrogen contraindications

A

Cytochrome inducers → reduction in efficacy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Selective Estrogen Receptor Modulators

A

Tamoxifen Raloxifene Clomiphene

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Tamoxifen MOA

A

Antagonist @ breast

Agonist everywhere else (endometrium, liver, bone)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Raloxifene MOA

A

Antagonist @ uterus & breast

Agonist in bone (inhibits resorption)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Clomiphene MOA

A

Antagonist @ hypothalamus - prevents feedback inhibition, increasing estrogen

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Tamoxifen clinical use

A

hormone-responsive breast cancer

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Raloxifene clinical use

A

Prevention of hormone-responsive breast cancer

Prevention and treatment of osteoporosis in postmenopausal women (agonist @bone)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Clomiphene clinical use

A

Treatment of infertility associated with anovulatory cycles (eg. PCOS)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Compare tamoxifen and raloxifene AEs

A

Endometrial hyperplasia (increased risk of cancer) with tamoxifen, no risk with raloxifene

  • Hot flashes and nausea
  • Thromboembolism
  • Raloxifene: leg cramps
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Clomiphene AEs

A
  • Hot flashes, nausea, vomiting, weight gain, breast tenderness
  • Ovarian hyperstimulation
  • Multiple simultaneous pregnancies (10%)
  • Visual disturbances
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

SERD

A

Fulvestrant

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Fulvestrant MOA

A

bind to estrogen receptors → degrades receptor and downregulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Fulvestrant clinical use

A

Adjuvant treatment of hormone-receptor + metastatic breast cancer resistant to first-line tamoxifen therapy

20
Q

Fulvestrant AEs

A
  • Hot flashes
  • Arthralgias
  • Myalgias
21
Q

Aromatase Inhibitors

A

Anastrozole, Letrozole (non-steroidal, reversible)

Exemestrane (steroidal, irreversible)

22
Q

AI clinical use

A

adjuvant chemotherapy in ER+ breast cancer

23
Q

AI AEs

A
  • Hot flashes
  • Nausea
  • Fatigue
  • Alopecia
  • Dermatitis
24
Q

Synthetic Progestins

A
  • Medroxyprogesterone
  • Norgestrol
  • Norethindrone
  • Norgestimate
  • Desogestreol
  • Drospirenone
25
Q

Progestins MOA

A

enter cell & bind progesterone receptors → lipid-receptor complex binds to a progesterone response element (PRE) and activates gene expression

26
Q

Main effects of Progestins

A
  • prevents endometrial hyperplasia by decreasing growth and increasing vascularization of endometrium
  • Thickening of cervical mucus - inhibits movement of sperm
  • ↑ body temperature
  • Maintenance of pregnancy
27
Q

Progestin clinical use

A
  • OCPs, HRT
  • endometrial cancer
  • abnormal uterine bleeding
  • infertility
  • dx test of estrogen secretion
28
Q

Progestin AEs

A
  • Uterine bleeding
  • Weight gain, Insulin resistance
  • Depression, headache
  • Changes in libido
  • Thromboembolic events (rare)
  • Decrease HDL levels (androgenic progestins)
29
Q

Antiprogestin

A

Mifepristone - competitive inhibitor at progesterone receptor and cortisol antagonist

30
Q

Mifepristone clinical use and AEs

A
  • Used in combination with misoprostol as abortifacient
  • AE: vomiting, diarrhea, abdominal/pelvic pain, uterine bleeding
31
Q

Androgens

A

Testosterone Methyltestosterone Danazol

32
Q

Androgens MOA

A

In skin, prostate seminal vesicles, and epididymis, testosterone is converted to 5a-dihydrotestosterone (DHT) by 5a-reductase and binds to the intracellular androgen receptor

33
Q

Androgens main effects

A
  • Male Maturation
    • male 2° sex characteristics
    • Increases lean body mass, stimulate body hair growth and serum secretion
  • Sexual function - increased libido
  • Metabolic
    • Reduction of hormone binding and other carrier proteins
    • Increased synthesis of clotting factors, triglyceride lipase,a1-antitrypsin, haptoglobin and sialic acid
34
Q

Methyltestosterone and danazol can be given ___

A

Methyltestosterone and danazol can be given orally

35
Q

Testosterone / Methyltestosterone clinical use

A
  • hypogonadism
  • Chronic wasting associated with HIV or cancer
  • Stimulate anabolism to promote recovery after burns or other injuries
  • Increase lean body mass and endurance in athletes (unapproved)
36
Q

___ also has anti-estrogen activity so it can be used for ___ and ___

A

Danazol also has anti-estrogen activity so it can be used for endometriosis and fibrocystic breast disease

37
Q

Androgen AEs

A

Females

  • Masculinization, acne, facial hair growth, deepening of the voice, male pattern baldness, excessive muscle development
  • Menstrual irregularities

Males

  • Priapism, impotence, decreased spermatogenesis
  • Gynecomastia
  • Gonadal atrophy
38
Q

Androgen AEs in children / generally

A
  • Children
    • Abnormal sexual maturation
    • Growth disturbances due to premature closing of the epiphyseal plates
  • General
    • Increase LDL and decrease HDL
    • Fluid retention → edema
39
Q

Androgen AEs on athletes

A
  • Reduction in testicular size (high doses)
  • Hepatic abnormalities
  • Increased aggression
40
Q

“-amide”, Spironolactone, Cyproterone

A

Androgen Receptor Antagonists

41
Q

Finasteride

A

5a-reductase Inhibitor

42
Q

Ketoconazole

A

Steroid Synthesis Inhibitor

43
Q

Flutamide MOA, use, AE

A
  • MOA: competitive androgen receptor inhibitor
  • Clinical use: Prostate carcinoma, hirsutism
  • AE: gynecomastia, hot flashes, reversible hepatotoxicity
44
Q

Spironolactone MOA, Use, AE

A
  • MOA: Mineralocorticoid receptor and androgen receptor antagonist
  • Clinical use: Reduction of androgenic symptoms due to PCOS (hirsutism), aldosteronism, diuretic
  • AE: Gynecomastia, amenorrhea, hyperkalemia
45
Q

which drug inhibits 5a-reductase, MOA, use, AE?

A
  • Finasteride
  • Decreases conversion of testosterone to DHT
  • Clinical use: BPH and male-pattern baldness
  • Adverse effects: Rarely impotence and gynecomastia
46
Q

Ketoconazole MOA, Use, AE

A
  • steroid synthesis inhibitor
  • CYP450 inhibitor
  • Clinical use: Cushings syndrome (non-operable), prostate cancer resistant to 1st line drugs
  • AE: Gynecomastia, amenorrhea, CYP 450 inhibitor

Pharmacology (19 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions