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Block 1.12 > Pharmaology Of Androgen Drugs > Flashcards

Pharmaology Of Androgen Drugs Flashcards

1
Q

How are androgens defined pharmacologically? What are some of the related hormones?

A

Their biding and activation of the androgen receptor

Testosterone

Dihydroxytestosterone (DHT)

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2
Q

Can androgens be converted to estrogen?

A

Yes, by using aromatase

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3
Q

What are the anabolic steroid effects of androgens?

A

They are the primary male sec hormone

  1. Development of male reproductive tissues, testes and prostate
  2. Inc secondary male characteristics (inc muscle and bone mass, body hair)
  3. Health and well-being (mood, memory)
  4. Prevent osteoporosis (gets turned into estrogen
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4
Q

What happens to testosterone if it goes thro the 5a reductase route?

A

it will be converted into DHT

It will then bind to androgen receptors and increase
1. Facial and body hair

  1. Acne
  2. Scalp hair loss
  3. Prostate growth
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5
Q

What happens with testosterone is it doesn’t go thro aromatase or 5-a reductase?

A

It will bind to androgen receptors and cause

  1. Inc muscle mass
  2. Inc skeletal growth
  3. Inc spermatogenesis
  4. Inc sexual function
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6
Q

What happens to testosterone if it goes thro aromatase?

A

It will be converted into estradiol (E2) then bind to estrogen receptors

  1. Inc bone formation
  2. Inc growth of breast tissue
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7
Q

What are the steps for synthesis of testosterone and regulation of testosterone activities?

A
  1. The hypothalamus releases GnRH which goes to the pituitary
  2. The pituitary will release FHS and LH into the blood
  3. LH will enter the testicles and bind to LEYDIG CELL which will cause the production of testosterone from cholesterol
  4. The new testosterone produced will go to the SERTOLI CELL which will cause a production of new sperm cells.
  5. The FSH from the pituitary will bind to the SERTOLI CELL in the testicles and cause production of new sperm cells
  6. The testosterone produced by the LEYDIG CELL Wiccan be converted by aromatase to estrogen in adipose tissue

REGULATION

  1. Testosterone produced from LEYDIG CELL will be a negative feedback loop and bind at the hypothalamus (stops GnRH) and pituitary (stop LH and FSH)
  2. Exogenous androgens will block pituitary and hypothalamus (topical or injectable testosterone)
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8
Q

What are the clinical uses of androgens?

A

Hormonal
1. Androgen deficiency - testosterone replacement

  1. Endometriosis (when tissue that normally lines the uterus grows outside of the uterus) and breast disease in women
  2. Breast cancer
  3. Gender reassignment
Anabolic uses(build up muscle) 
1. Can be abused by body builders
  1. Used for people with burns (body will break down muscle and other tissues to try and repair itself)
  2. Used for HIV/AIDs with wasting states
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9
Q

What are the testosterone esters and what is their route and what are they used for?

A

They are non-Po (mostly injections)

Preferred for testosterone replacement therapy

  1. Testosterone enanthate
  2. Testosterone cypionate
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10
Q

What are the synthetic androgens and their route and what are used for?

A

They are usually Po and are preferred for anabolic effects

These are HEPATOTOXIC

  1. 17a-alkylate androgens - PO (has lots of side chain options)

OXANDROLONE ( most anabolic but also most hepatotoxic)

  1. 19-demethylated androgens- Injection

Used by athletes to enhance abilities

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11
Q

Do androgens have other hormonal effects?

A

Yes

  1. It can act like estrogen because it can be converted to estrogen and it can also bind to estrogen receptors
  2. It can have progestin properties as well as anti-progestin properties
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12
Q

What are the contraindications of androgen replacement therapy?

A
  1. Prostate or breast cancer (the androgen therapy can cause an increase in growth)
  2. Pregnancy (androgens may disturb fetal sexual differentiation)
  3. Liver dysfunction
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13
Q

What are the side effects for men when you have administered androgens?

A
  1. Infertility
  2. Shrinkage of testicles
  3. Breast development (gynecomastia)
  4. Priapism, ED
  5. Testicular atrophy
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14
Q

What are the ADR for women how use androgen replacements?

A
  1. Deepened voice
  2. Enlargement of clitoris
  3. Breast reduction
  4. Excessive growth of body hair
  5. Menstrual disturbances
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15
Q

What side effects happen to everyone who takes androgen replacement?

A
  1. Precocious puberty (boys, get it early), delayed puberty (girls) short stature in adolescents
  2. Male-pattern baldness, acne
  3. Muscle hypertrophy, tendon rupture
  4. Inc LDL, dec HDL
  5. Inc BP
  6. CV risks
  7. Cancer (breast , prostate)
  8. Liver toxicity, jaundice
  9. Mood changes; rage, mania
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16
Q

What happens to when exogenous testosterone is given to a male in terms of normal hormone levels?

A
  1. Get mood changes
  2. Get a drop in GnRH levels being released from hypothalamus
  3. LH and FSH elven drop (leads to infertility with less sperm production)
  4. Decreased testosterone synthesis
  5. Testes will atrophy
17
Q

What leads to benign prostate hypertrophy (BPH)?

A

The excessive growth of the prostate is often promoted by DHT (5a reductase, causes testosterone to become this) this leads to urinary symptoms (urinary incontinence)

18
Q

What are the 5a reductase inhibitors and what are they used to treat?

A
  1. Finasteride (proscar) type 2 enzyme inhibitor
  2. Dutasteride (advodart) Type 1 and 2 enzyme inhibitor

Used with or after alpha-1 blockers or PDE5 inhibitors to treat BPH. May take up to 6 months to show effect

19
Q

What are the side effects of 5a reductase inhibitors?

A
  1. Decreased libido
  2. ED
  3. Breast swelling and breast tenderness
  4. Hisutism in males (hair growth in unwanted places, face, back, chest)

NOT USED IN PREGO WOMEN!!!!

20
Q

What are the anti-androgen drugs and what are they used for?

A

Used for Prostate Cancer

  1. GnRH agonists

Leuprolide
Goserelin
Triptorelin
Histrelin

These will cause a flair ( get a lot of LH and FSH at the start, which leads to an initial increase in testosterone). It will then lead to receptor down-regulation and lower LH and FSH secretion eventually

  1. GnRH antagonists

Degarelix

Does not cause flair and can cause liver toxicity

Act to be receptor blocker and will decrease LH and FSH secretion immediately

21
Q

What are the Anti-androgens that are newer for prostate cancer 2?

A
  1. Androgen receptor antagonists (ARR)

1st gen:
Bicalutamide, used as an add on agent. This drug can change from antagonist activity to an agonist activity

2nd gen
Enzalutamide
Apalutamide
These are add on agents but DO NOT change from agonist to antagonist activity

  1. CYP17A1 Inhibitor
    Abiraterone (blocks the normal physiologic production of steroids, including androgens), this is the enzyme that produces testosterone

Block 1.12 (5 decks)

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