Brainscape's Knowledge GenomeTM

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


See full index

Pharm > Androgens > Flashcards

Androgens Flashcards

1
Q

DHEA

A

Androgenic precusor

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

Androstenedione

A

Androgenic precursor, adrenal cortex

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

Most potent natural androgen

A

DHT
Targets cells and tissues, acting in paracrine and autocrine manner

Binds 5x more strongly to the AR

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

Testosterone is released by the

A

Leydig cells

Critical for Spermatogenesis in seminiferous tubules

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

What does the Leydig Cells express?

A

17B HSD

Converts: DHEA -> Androstenediol
Converts: Androstenedione -> Testosterone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What converts testosterone to DHT?

A

5alpha reductase

5alpha reductase is found predominantly in androgen-responsive tissues

  • like the prostate
  • most DHT production occurs outside of the testes
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are the OBLIGATE precursors to estrone/estradiol?

A

Aromatase (CYP19)

Males who carry more fat tend to have higher circulating levels of estrone and estradiol

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

Where does LH from pituitary act?

A

Leydig cells

Testosterone production negatively feedbacks to the hypothalamus, which stops production of GnRH

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

What stimulates the seminiferous tubulues?

A

FSH

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

What localizes to the nuclear membrane in tissues in response to testosterone?

A

DHT

Kd of DHT is less than Kd of Testosterone

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

What results in AR to the ARE in genome?

A

Masculinization of internal/external male genitalia

Sexual differentiation of the male brain

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

What maintains the prostate?

A

DHT

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

Testosterone influences in the male fetal development….

A

Wolffian Duct development

Genital Tubercle/Urogenital Sinus (penis, scrotum, urethra, prostate)

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

Testosterone in females…

A

Body hair growth
Libido
Maintain bone density

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

Metabolic actions of testosterone…

A

Maintains and strengthens bone mass by osteoblasts proliferation and decrease bone resorption by osteoclasts

Increase protein synthesis
Increase LDL, decrease HDL - implications for CV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Therapeutic uses of androgens:

A 
Male hypogonadism - defect in testosterone
Andropause - Late onset Hypogonadism
Delayed Puberty
Improve Protein Balance
Osteoporosis
Anemia
Female Hypogonadism/Hypoadrenalism
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Male contraception hormones

A

Androgen + Progestogen

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

What are the contraindications for Androgen use?

A

Male pts with prostate disorders
Male patients with cardiac, renal or liver disorders
Pregnant or lactating females
Infants and very young children

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

What are the pros of androgen-replacement therapy with older males?

A 
Improvement in:
Mood
Libido
Bone density
Corrects Anemia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What are risks for ART?

A

Build up of plaque in coronary arteries
Increased risk of heart attack
Increased risk of stroke
Accelerate incidence of prostate cancer

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What is safe hormonal contraceptive in men?

A

Testosterone

Synthetic Progestogen

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

How is androgen administered?

A

Not usually orally, as rapidly degraded in liver!

  1. slow continuous absorbed form (gel, transdermal patch, subcutaneous)
  2. chemically modified testosterone derivative that bypasses metabolism in body
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Type A chemical modifications for androgen:

A

Esterification of C17 hydroxyl

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Type B androgen modification:

A

Alkylation of C17alpha position

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Type C chemical modification:

A

Modification of the A, B or C rings!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

What are the pure anabolic steroids?

A

Stanozolol
Oxandrolone

Type B and C modifications

27
Q

Esterification of C17 hydroxyl group is…

A

Type A modification

  • renders the molecule more soluble in fat/lipid, such that it can be slowly and continuously released into the blood stream
  • longer the ester chain, the more prolonged the action!
  • must be hydrolyzed in vivo to be considered biologically active
28
Q

Alkylation of the C17 alpha position

A

Type B modification

  • inhibits hepatic catabolism, inhibits first-pass metabolism in liver!
  • more suitable for oral administration -> higher oral bioavailability

Methyltestosterone = type B modification

29
Q

What is the draw back of Methyltestosterone?

A

Prolonged used is associated with liver toxicity

  • cholestasis
  • Peliosis
  • hepatic cysts
  • hepatic neoplasms
  • liver carcinoma
30
Q

Modifications of A, B or C ring and C17alpha-alkylation

A

Enhances the androgenic potency of the molecule
Increases the oral bioavailability of the drug

Not due to stronger binding affinity for the AR
Increases the drug half-life

31
Q

Side effects of androgenic therapy

A 
High cholesterol
Acne
Thinning of hair
Fluid retention
High blood pressure
Liver damage
Erthrocytosis

Male: decreased size of testes, decreased sperm, impotence, gynecomastia
Female: infertility, hirsutism, changes in fat deposition, decreased breast size

32
Q

Side effect of androgenic therapy

A

Liver damage: especially the C17alpha-alkylate derivative

33
Q

What are anti-androgens used for?

A

Prostate cancer
Benign Prostate Hyperplasia
Male Pattern Hair Loss
Hirsutism

34
Q

What are the two types of anti androgens?

A

Drugs that block the androgen synthesis

Drugs that block the androgen receptor

35
Q

What is dependent on androgens for growth and survival?

A

Prostate cancer

36
Q

Leuprolide

A

GnRH receptor agonist

- inhibitor of hypothalamic-pituitary-testes signally

37
Q

Goserelin

A

GnRH receptor agonist

38
Q

Buserelin

A

GnRH receptor agonist

39
Q

Histrelin

A

GnRH receptor agonist - disrupts the pulse signaling

40
Q

Estradiol

A

Used for estrogen treatment, along with DES

41
Q

Ketoconazole

A

First generation inhibitor of androgen biosynthesis!

42
Q

Abiraterone

A

Second generation inhibitor of androgen biosynthesis

43
Q

Finesteride

A

Inhibitor of DHT synthesis

44
Q

Dutasteride

A

Inhibitor of DHT synthesis

45
Q

What inhibits the release of GnRH and LH?

A

Estrogen treatment

  • DES
  • Estradiol

Negatively feedbacks at the hypothalamus

46
Q

What is castration level?

A

Less than 50ng/dL of testosterone

47
Q

What is an orchlectomy?

A

Surgical removal of testes

Surgical castration

48
Q

What is the chemical castrator at the level of the Hypothalamus?

A

GnRH receptor agonist

Leuprolide
Goserelin

49
Q

Ketoconazole

A

Inhibits 3 out of 4 of the enzymes involved in testosterone synthesis in leydig cells

Inhibits CYP34A - drug metabolism!

Androgen biosynthesis antagonist - first-generation

50
Q

Abiraterone

A

Selective inhibitor of CYP17 in the testes
Androgen biosynthesis inhibitor

PYRIDINE MOIETY
Does not inhibit CYP3A4, unlike Ketoconazole

51
Q

Ketoconazole

A

Inhibits four enzymes involved in adrenocortical steroid biosynthesis

  • not only blocks androgen precursor biosynthesis but cortisol and aldosterone synthesis
  • inhibits CYP3A4 in liver -> affecting drug metabolism
52
Q

Finasteride

A

DHT reduction

Inhibitor of 5alpha reductase

53
Q

Dutasteride

A

99% DHT reduction

Inhibits 5-alpha reductase

54
Q

What is used to treat benign prostate hyperplasia?

A

Finasteride, Dutasteride

Androgen-responsive tissue:
- scalp, prostate

Blocks DHT action here

55
Q

Flutamide

A

AR antagonist

56
Q

Bicalutmide

A

AR antagonist

57
Q

Nilutamide

A

AR antagonist

1st generation

58
Q

Enzalutamide

A

2nd generation AR antagonist

59
Q

Apalutamide

A

2nd generation AR antagonist

60
Q

Enzalutamide vs 1st generation AR antagonists

A 
Higher binding affinity
No:
- nuclear import
- DNA binding
- coactivator recruitment
61
Q

Bicalutamide

A 
Low binding affinity to AR
Slight:
- import into nucleus
- DNA binding
- coactivator recruitment
62
Q

Common side effects of enzalutamide:

A

Seizures
Dizziness
High BP

63
Q

Apalutamide and Enzalutamide for treatment of:

A

Prostate cancer

64
Q

What are some types of androgen deprivation therapies?

A

Surgical castration (orchiectomy)
Chemical castration
Estrogen treatment

Goal: to lower testosterone to “castrate” levels - 50ng/dL

Pharm (6 decks)

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