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Androgens Flashcards

1
Q

DHEA

A

Androgenic precusor

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2
Q

Androstenedione

A

Androgenic precursor, adrenal cortex

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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

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4
Q

Testosterone is released by the

A

Leydig cells

Critical for Spermatogenesis in seminiferous tubules

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5
Q

What does the Leydig Cells express?

A

17B HSD

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

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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
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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

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8
Q

Where does LH from pituitary act?

A

Leydig cells

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

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9
Q

What stimulates the seminiferous tubulues?

A

FSH

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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

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11
Q

What results in AR to the ARE in genome?

A

Masculinization of internal/external male genitalia

Sexual differentiation of the male brain

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12
Q

What maintains the prostate?

A

DHT

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13
Q

Testosterone influences in the male fetal development….

A

Wolffian Duct development

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

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14
Q

Testosterone in females…

A

Body hair growth
Libido
Maintain bone density

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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

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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
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17
Q

Male contraception hormones

A

Androgen + Progestogen

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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

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19
Q

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

A 
Improvement in:
Mood
Libido
Bone density
Corrects Anemia
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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

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21
Q

What is safe hormonal contraceptive in men?

A

Testosterone

Synthetic Progestogen

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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
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23
Q

Type A chemical modifications for androgen:

A

Esterification of C17 hydroxyl

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24
Q

Type B androgen modification:

A

Alkylation of C17alpha position

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25
Type C chemical modification:
Modification of the A, B or C rings!
26
What are the pure anabolic steroids?
Stanozolol Oxandrolone Type B and C modifications
27
Esterification of C17 hydroxyl group is...
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
Alkylation of the C17 alpha position
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
What is the draw back of Methyltestosterone?
Prolonged used is associated with liver toxicity - cholestasis - Peliosis - hepatic cysts - hepatic neoplasms - liver carcinoma
30
Modifications of A, B or C ring and C17alpha-alkylation
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
Side effects of androgenic therapy
``` 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
Side effect of androgenic therapy
Liver damage: especially the C17alpha-alkylate derivative
33
What are anti-androgens used for?
Prostate cancer Benign Prostate Hyperplasia Male Pattern Hair Loss Hirsutism
34
What are the two types of anti androgens?
Drugs that block the androgen synthesis | Drugs that block the androgen receptor
35
What is dependent on androgens for growth and survival?
Prostate cancer
36
Leuprolide
GnRH receptor agonist | - inhibitor of hypothalamic-pituitary-testes signally
37
Goserelin
GnRH receptor agonist
38
Buserelin
GnRH receptor agonist
39
Histrelin
GnRH receptor agonist - disrupts the pulse signaling
40
Estradiol
Used for estrogen treatment, along with DES
41
Ketoconazole
First generation inhibitor of androgen biosynthesis!
42
Abiraterone
Second generation inhibitor of androgen biosynthesis
43
Finesteride
Inhibitor of DHT synthesis
44
Dutasteride
Inhibitor of DHT synthesis
45
What inhibits the release of GnRH and LH?
Estrogen treatment - DES - Estradiol Negatively feedbacks at the hypothalamus
46
What is castration level?
Less than 50ng/dL of testosterone
47
What is an orchlectomy?
Surgical removal of testes Surgical castration
48
What is the chemical castrator at the level of the Hypothalamus?
GnRH receptor agonist Leuprolide Goserelin
49
Ketoconazole
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
Abiraterone
Selective inhibitor of CYP17 in the testes Androgen biosynthesis inhibitor PYRIDINE MOIETY Does not inhibit CYP3A4, unlike Ketoconazole
51
Ketoconazole
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
Finasteride
DHT reduction | Inhibitor of 5alpha reductase
53
Dutasteride
99% DHT reduction | Inhibits 5-alpha reductase
54
What is used to treat benign prostate hyperplasia?
Finasteride, Dutasteride Androgen-responsive tissue: - scalp, prostate Blocks DHT action here
55
Flutamide
AR antagonist
56
Bicalutmide
AR antagonist
57
Nilutamide
AR antagonist | 1st generation
58
Enzalutamide
2nd generation AR antagonist
59
Apalutamide
2nd generation AR antagonist
60
Enzalutamide vs 1st generation AR antagonists
``` Higher binding affinity No: - nuclear import - DNA binding - coactivator recruitment ```
61
Bicalutamide
``` Low binding affinity to AR Slight: - import into nucleus - DNA binding - coactivator recruitment ```
62
Common side effects of enzalutamide:
Seizures Dizziness High BP
63
Apalutamide and Enzalutamide for treatment of:
Prostate cancer
64
What are some types of androgen deprivation therapies?
Surgical castration (orchiectomy) Chemical castration Estrogen treatment Goal: to lower testosterone to “castrate” levels - 50ng/dL

Pharm (6 decks)

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