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RGU 3 > Pharmacology of Androgens > Flashcards

Pharmacology of Androgens Flashcards

1
Q

What are the 3 androgens?

A
  1. Testosterone
  2. Androstenedione
  3. Dehydroepiandrosterone (DHEA)
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2
Q

What is the main difference between testosterone and estradiol?

A
  • methyl group on testosterone’s 4 ring structure
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3
Q

What produces androgens?

A
  • testis= leydig cells
  • adrenal glands
  • ovary= theca cells
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4
Q

Can production of testosterone come from progesterone?

A

YES via cytochrome P450 to androstenedione and then to testosterone.

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5
Q

To what is testosterone metabolized in the prostate?

A
  • 5-alpha dihydrotestosterone (DHT) via 5 alpha reductase.

* testosterone is unchanged in other tissues (muscle, kidney…)

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6
Q

What is the most potent androgen required for sex development?

A
  • DHT
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7
Q

What regulates androgen production?

A
  • LH from the anterior pituitary

* receptors for LH are found on Leydig cells in the testes.

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8
Q

Where else are androgens produced?

A
  • adrenal cortex
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9
Q

What regulates sertoli cells in the testes?

A
  • FSH from the anterior pituitary
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10
Q

What stimulates the adrenal glands to secrete cortisol and sex steroids?

A
  • adrenocorticotropin
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11
Q

What is sex hormone binding globulin (SHBG)?

A
  • serum glycoprotein derived from liver that binds testosterone in circulation
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12
Q

What INCREASES sex hormone binding globulin (SHBG)? (aka less free testosterone in the circulation)

A
  • estrogens

- thyroxine

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13
Q

What DECREASES sex hormone binding globulin (SHBG)? (aka more free testosterone in circulation)?

A
  • androgens
  • GH
  • insulin
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14
Q

What are the pharmacologic actions of androgens?

A
  • sperm production
  • erythropoiesis
  • positive nitrogen balance
  • growth/development of hair, bone, and muscle.
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15
Q

*** What is the major use for androgens?

A
  • replacement therapy in men who have reduced testosterone production (primary testicular insufficiency).
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16
Q

What are the available IM injection testosterones?

A
  • cypionate= 2-3 weeks
  • enanthate= 2-3 weeks
  • propionate= 1-3 days
17
Q

Where is a testosterone transdermal patch applied?

A
  • scrotal skin bc it’s thinner than other epidermis.
18
Q

What are the actions of anabolic steroids (synthetic derivatives of testosterone)?

A
  • increase muscle mass
  • increase physical performance
  • increase linear growth (children)
19
Q

** What is OXANDROLONE (anavar; oxandrin)?

A
  • anabolic steroid used for PRIMARY and SECONDARY testicular failure.
  • increases expression of secondary sex characteristics
20
Q

*** What is secondary testicular failure?

A
  • insufficient stimulation of testes by pituitary gonadotropins (hypogonadotropic hypogonadism).
21
Q

What is an ADR of using androgen therapy to increase height of short children?

A
  • premature closure of epiphyseal plates and virilization.

* best to combine with GH

22
Q

What are the therapeutic uses of androgens?

A
  • treatment of aplastic anemia (erythropoiesis)
  • inoperable breast cancer
  • postpartum breast pain
  • malnutrition
23
Q

** What is DANAZOL (danocrine)?

A

WEAK androgen used for the treatment of:

  • endometriosis
  • fibrocystic breast disease
  • PMS
24
Q

What was the result of using testosterone supplementation to treat men with multiple sclerosis (MS)?

A
  • improvement in cognitive performance
  • slowing of brain atrophy
  • increase in lean body mass
  • potential neuroprotective effects in men with relapsing-remitting MS
25
Q

What are some dose related ADRs of androgens (due to feedback inhibition as dose increases)?

A
  • priapism (sustained erection); not due to feedback inhibition.
  • suppression of gonadotropin
  • gynecomastia
  • decreased size of testis
  • decreased spermatogenesis
  • weight gain
  • Na+ retention (edema, HTN)
  • decreased HDL (atherosclerosis)
  • hepatotoxic (jaundice, carcinoma)
  • BPH
  • prostatic cancer
26
Q

What are some ADRs of androgen use in females?

A
  • virilization

- DO NOT use in pregnancy (category x)

27
Q

What is “Roid Rage”?

A
  • feeling of invincibility to physical challenges
28
Q

What must AndroGel and Testim now do on product labels?

A
  • include boxed warning of ADRs
29
Q

What are some toxic effects of anabolic steroids used by weightlifters?

A
  • acne conglobata= papules, pustules, abscesses, and deep ulcerations.
30
Q

What are contraindications for androgens?

A
  • breast carcinoma
  • prostate carcinoma
  • serious cardiac, hepatic, or renal disease
  • pregnancy (female)
31
Q

** How can we suppress synthesis of androgens (primarily used to treat SYMPTOMS of men with prostate cancer)?

A
  1. stimulate feedback inhibition= GnRH agonists (LEUPROLIDE; lupron), which decreases testosterone production over time.
  2. GOSERELIN ACETATE implant= LHRH analogue (GnRH analogue)
  3. NAFARELIN= GnRH analogue nasal spray.
  4. DEGARELIX= LHRH ANTagonist, which decreases testosterone rapidly.
  5. suppress synthesis of androgen= KETOCONAZOLE, which decreases cytochrome P450.
  6. 5 alpha-reductase inhibitors (FINASTERIDE and DUTASTERIDE)= suppress synthesis of androgen.
  7. CYP17 inhibitor (ABIRATERONE)= suppress androgen synthesis in other cells other than the prostate.
  8. blockade of androgen receptor= FLUTAMIDE, ENZALUTAMIDE, and SPIRONOLACTONE
32
Q

*** What is a problem with ketoconazole?

A
  • can block production of cortisol, so you may need to add corticosteroid when using this to suppress androgen synthesis.
33
Q

Does finasteride or dutasteride (5 alpha-reductase inhibitors) suppress synthesis of androgen more quickly?

A
  • finasteride

* dutasteride has a longer half-life though.

34
Q

Does spironolactone also inhibit cytochrome P450?

A

YES

RGU 3 (19 decks)

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