Pharm 5 Androgens Flashcards

1
Q

Primary stimulator of testosterone synthesis and androgen-binding globulin

A

LH - testosterone (leydig cells)

FSH - ABG

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2
Q

LH, FSH stimulated by

A

GnRH (pulsatile)

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3
Q

LH, FSH inhibitors (male)

A

Testosterone, Estradiol

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4
Q

Site of female androgen synthesis

A

Corpus luteum

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5
Q

Testosterone metabolism

A
5a-reductase -> dihydrotestosterone
P450 aromatase (CYP19) -> estradiol
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6
Q

5a reductase & CYP19 locations

A

5a reductase - Skin, bone, liver, genitals

CYP19 aromatase - Fat, liver, bone

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7
Q

Testosterone action

A

A-R ->

  • Internal genitalia (Wolffian development)
  • Skeletal muscle (puberty)
  • Erythropoiesis
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8
Q

Dihydrotestosterone action

A

A-R ->

  • Eternal genitalia (differentiation and maturation)
  • Hair follicles (puberty)
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9
Q

Estradiol action

A

E-R ->

  • Bone density and epiphyses closure
  • Regulation of male reproductive tract fluid
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10
Q

Transdermal androgen Tx

A

Testosterone

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11
Q

IM deposit androgen Tx

A

Testosterone cypionate

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12
Q

Oral androgen Tx

A
  • Methyltestosterone
  • Oxandrolone
  • Danazol
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13
Q

Endometriosis androgen Tx

A

Danazol

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14
Q

Unusual clinical uses for androgens

A

Hereditary angioedema

  • AIDS muscle wasting
  • Severe anemia (stimulate erythropoiesis)
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15
Q

Androgen Tx tumor risk

A

Liver tumors

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16
Q

Androgen Tx contraindications (3)

A

Pregnancy
Prostate/Breast cancer
Infants/Young children

17
Q

-Danazol-
MOA
indications

A

Weak androgen, progestin, glucocorticoid

  • INHIBITS gonadal steroidogenesis
  • Endometriosis, Fibrocystic breast disease
18
Q

-Ketoconazole-

indication

A

Inhibits P450 required for steroid synthesis

-Prostate cancer

19
Q

-Finasteride-
MOA
indication

A

5a-reductase inhibitor

  • Blocks dihydrotestosterone production
  • Benign prostatic hyperplasia
20
Q

-Flutamide-

indication

A

Nonsteroidal competitive A-R antagonist

-Prostate cancer

21
Q

-Spironolactone-
MOA
indication

A

Blocks Aldosterone-R and Androgen-R

  • Inhibits 17a-hydroxylase
  • Hirsutism
22
Q

-Tetrahydrogestrinone-

indication

A

The “clear” - THG

-Designer steroid to avoid drug test detection

23
Q

Steroid abuse AE

A
  • Retention of sodium and water
  • CAD risk (+LDL, -HDL)
  • Severe acne
  • Hyperinsulinemia, altered glucose tolerance
  • Liver toxicity
  • Premature bone fusion
  • Testicular atrophy and gynecomastia