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RGU Exam 3 > Pharmacology of Androgens > Flashcards

Pharmacology of Androgens Flashcards

1
Q

Major Male Androgens

A
  • Testosterone
  • Androstenedione
  • Dehydroepiandrosterone (DHEA)
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2
Q

Androgen Biochemical Synthesis Graph

A
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3
Q

Organs that produce androgens

A
  • Testis

*Leydig cells

  • Adrenal glands
  • Ovary

*theca cells

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4
Q

Cytochrome P450 role in testosterone production

A
  • Progesterone is converted to androstenedione by cytochrome P450
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5
Q

Testosterone metabolization product

A
  • 5-alpha dihydrotestosterone (DHT) in prostate

*the end product; the form of testosterone this will actually make changes occur

  • Unchanged in onther tissues

*muscle

*kidney

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6
Q

DHT Synthesis

A
  • Dihydrotestosterone; Androstanolone
  • Most potent androgen required for sex development
  • Synthesized from testosterone in the prostate gland, testes, hair follicles and adrenal glands by 5-alpha reductase
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7
Q

Androgens production is regulated by

A
  • Luteinizing Hormone (LH)

*LH synthesized by anterior pituitary

  • Leydig cells contain receptors for LH
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8
Q

Hormonal Control of Testicular Function Graph

A
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9
Q

Androgen Release Process

A
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10
Q

Sertoli Cells are primarily regulated by what hormone?

A
  • FSH
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11
Q

Sertoli Cells factors released

A
  • Release androgen-binding (transferrin) and inhibin
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12
Q

Adrenal glands secrete

A
  • Dehydroepiandrosterone
  • Androstenedione
  • Testosterone
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13
Q

Adrenocorticotropin stimulates adrenal to secrete

A
  • Cortisol
  • Sex steroids
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14
Q

Sex Hormone Binding Globulin (SHBG)

A
  • Serum glycoprotein

*88,000 daltons

  • Derived from liver
  • Strong binding of testosterone
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15
Q

Sex Hormone Binding Globulin (SHBG) is increased by

A
  • Estrogens

*females 2-3x more than males

  • Thyroxine
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16
Q

Sex Hormone Binding Globulin decreased by

A
  • Androgens
  • Growth hormone
  • Insulin
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17
Q

Androgens Pharmacological Actions

A
  • Stimulates production of sperm
  • Erythropoiesis
  • Pos. nitrogen balance
  • Growth/development of:

*hair

*bone

*muscle

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18
Q

Testosterone Injections

A

Intramuscular injections

  • Cypionate

*DEPO-testost.

  • Enanthate

*Delatestryl

  • Propinate
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19
Q

Androgen Products (Drugs)

A
  • Fluoxymesterone (Halotestin)
  • Oxandrolone (Anavar)
  • Oxymetholone (Anadrol)
  • Methyltestost. (Metandren)
  • Nandrolone (Durabolin)
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20
Q

Anabolic Steroids Effects

A
  • Synthetic derivatives of testost.
  • Anabolic action > Androgenic
  • Increases:

*muscle mass

*physical performance

*linear growth: children

21
Q

Anabolic Steroids

A
  • Anabolic action > Androgenic

- Oxandrolone

  • Oxymetholone
  • Stanozolol
22
Q

Androgens Therapeutical Uses

A
  • Primary testicular failure

*Increases expression of secondary sex characteristics

*does not fix infertility

  • Secondary testicular failure

*insufficient stimulation of testes by pituitary gonadotropins

*hypogonadotropic hypogonadism

  • Short children and teenagers to increase height
  • Aplastic anemia

*erythropoiesis

  • Inoperable breast cancer
  • Postpartum:

*breat pain

*engorgement

  • Malnutrition
23
Q

Androgen Therapy for short children/teenagers

A
  • Controversial
  • Role of androgens not completely established
  • ADRs

*premature closure of epiphyseal plates

*virilization

  • Preferable combined w/ growth hormone
24
Q

Danazol (Danocrine)

A
  • Weak androgen
  • Treatment of:

*endometriosis

*fibrocystic breast disease

*PMS

25
Q

Androgens ADRs

A

Usually dose-related

  • Priapism
  • Suppression of gonadotropin
  • Gynecomastia
  • Decreased size of testis and spermatogenesis
  • Weight gain
  • Na+ retention (edema, hypertension)
  • Decreased HDLs (possible atherogenesis)
  • Hepatotoxic (jaundice, peliosis hepatitis, hepatocellular carcinoma)
26
Q

Androgens specific ADRs in females

A
  • Virilization (discontinue when appears since it may become irreversible)
  • Pregnancy category X
27
Q

Anabolic drugs ADRs

A

All the same ADRs as androgens as well as…

  • Benign prostatic hyperplasia
  • Prostatic cancer
  • Increased risk of atheroslcerosis and peliosis hepatitis
  • Acne conglobata
  • Atherosclerosis and CV pathology

*case where a male abuser had to have legs amputated due to severe atherosclerotic development

28
Q

Acne Conglobata

A
  • Development of acne on the chest of anabolic steroid abusers
  • Can become very severe w/ lesions that include pauples, pustules, abscesses and deep ulcerations
  • Can be treated
29
Q

Androgens Contraindications

A
  • Male:

*breast carcinoma

*prostate carcinoma

  • Female:

*pregnancy (known/suspected)

  • All pts:

*serious cardiac, hepatic or renal disease

30
Q

Anti-androgens MOA

A
  • Suppress synthesis of androgen or blockade of androgen receptors
31
Q

Gonadotropin Releasing Hormone (GnRH) Agonist Analogues

A
  • Suppress synthesis of androgen by stimulating feedback inhibition
  • Goserelin
  • Leuprolide
  • Naferelin
32
Q

GnRH Agonist Analogues Therapeutic Uses

A
  • Primarily used to treat men w/ prostate cancer
33
Q

GnRH Agonist Analogues ADRs

A
  • Assoc. w/ small inc. risk for diabetes, heart attack, stroke, and sudden death
  • May cause initial inc. in testosterone lvls
34
Q

Leuprolide

A
  • Synthetic non-peptide analog of naturally occurring GnRH
  • Overstimulates production of androgens resulting in activation of neg. feedback resulting in dec. testosterone produciton
  • Inc. in testosterone lvls at start of treatment may produce new or worsening symptoms for a few wks
35
Q

Leuprolide Therapeutic Uses

A
  • Men: treat symptoms of prostate cancer; not the cancer itself
  • Women: treat symptoms of endometriosis (Pregnancy category X)
  • Children: treat precocious puberty
36
Q

Goserelin Acetate Implant (Zoladex)

A
  • Anti-androgen
  • Suppresses synthesis of androgen
  • Synthetic decapeptide analogue of LH releasing hormone (LHRH)
  • Also known as a GnRH agonist analogue
37
Q

Goserelin Acetate Implant Therapeutic Uses

A
  • Treatment of advanced prostatic carcinoma
38
Q

Nafarelin

A
  • Anti-androgen
  • Suppresses synthesis of androgen
  • Nasal spray
  • Powerful stimulant (agonist) analogue of GnRH
  • Stimulates release of the pituitary gonadotrophins, LH, and FSH
  • Initial inc. of gonadal steroidogenesis
  • At 4wks dec. gonadal steroidogenesis
39
Q

Nafarelin Therapeutic Uses

A
  • For hormonal management of endometriosis, including pain relief and reduction of endometric lesions
40
Q

Degarelix

A
  • Anti-androgen
  • Suppress synthesis of androgens
  • LHRH antagonist
  • Compared to LHRH agonists it dec. testosterone lvls more rapidly and no tumor flare
41
Q

Ketoconazole

A
  • Anti-androgen
  • Suppresses synthesis of androgen
  • Decreases cytochrome P450 in testicular microsomes
  • Dec. 17-hydroxylation of progesterone or pregnenolone
  • Less selective for fungal P450 than newer azoles/systemic ketoconazole rarely used as antifungal
42
Q

Ketoconazole ADRs

A
  • Gynecomastia
  • Impotence/oligospermia >400mg/day
  • Can block production of cortisol - may need to add corticosteroids (prednisone, hydrocortisone)
43
Q

Finasteride

A
  • Anti-androgen
  • Suppress synthesis of androgen
  • Steroid-like inhibitor of 5alpha-reductase
  • Orally active; t1/2 = ~8hrs (longer in elderly pts.)
  • Dec. dihydrotestosterone lvls within 8hrs
  • Duration: 24hrs
  • 40-50% metabolized
44
Q

Dutasteride

A
  • Anti-androgen
  • Suppresses synthesis of androgen
  • Steroid-like inhibitor of 5alpha-reductase
  • Slow onset of action
  • t1/2 > finasteride
45
Q

Abiraterone

A
  • Anti-androgen
  • Suppresses synthesis of androgen
  • Blocks CYP17
  • Dec. testicle production of androgens
  • Other cells including prostate cancer cells can still produce small amts. = cancer growth
46
Q

Flutamide

A
  • Anti-androgen
  • Blockade of androgen receptor
  • Nonsteroidal
47
Q

Flutamide Therapeutic Uses

A
  • Used w/ LHRH agonists in Tx of prostatic and metastatic carcinoma
48
Q

Flutamide ADRs

A
  • Hepatic injury
  • Not recommended when ALT > 2x ULN
49
Q

Enzalutamide

A
  • Anti-androgen
  • Blocks signals from androgens to cells for growth and division

RGU Exam 3 (19 decks)

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