Pharmacology of Gonadal Hormones 4 Flashcards

Describe the relationship of the psychological effects of androgens, estrogens, and progestins to their therapeutic applications and side effects.

1
Q

What are the therapeutic uses of androgens?

A
  • Replacement
    • pre- and post-pubertal hypogonadism
    • some cases of cryptorchidism
  • Anabolic
    • premature infants
    • postoperative
    • anemia
  • Palliative
    • hormone-dependent breast cancer
    • fibrocystic breast disease
    • endometriosis
  • Treatment
    • hereditary angioneurotic edema
      • inhibitor of complement deficient
      • androgens decrease the abnormal capillary permeability
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2
Q

What are the non-therapeutic (ab)uses of androgens?

A
  • Used at ~100x replacement dose
  • Post-pubertal males, effects mediated through receptors are limited because they may be saturated
  • more marked in prepubertal males or elderly males with lower androgens, and females
  • Antagonism of anti-anabolic effects of glucocorticoids
    • provide androgen-receptor independent effects
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3
Q

What are the major side effects of androgens?

A
  • Adult male
    • infertility
      • excessive feedback inhibition leads to impotence and sterility
      • azoospermia
  • Prepubertal male
    • precocious puberty
    • premature epiphyseal closure
  • Female
    • masculinization
      • muscle
      • voice
      • hair
      • clitoral enlargement
  • Other
    • promote growth of prostatic tumors
    • decreases HDL
    • increases LDL
    • acne
    • jaundice, possibly hepatocellular carcinoma (methyltestosterone)
    • CV effects
      • MI
      • stroke
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4
Q

What are the major uses of estrogen?

A
  • Replacement therapy for ovarian or pituitary failure
  • With SERM for menopausal symptoms
  • As androgen antagonist
    • prostate cancer
    • acne
    • hirsutism
  • Contraception
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5
Q

What are the major uses of progestin by itself?

A
  • Dysfunctional uterine bleeding
  • Endometriosis
  • Endometrial cancer
  • Prevention of premature labor
  • Some types of oral contraceptives
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6
Q

What are the major uses of progesterone combined with estrogen?

A
  • Hormonal replacement therapy (HRT) for menopausal symptoms
  • Treat dysmenorrhea
  • Suppress lactation
  • Limit excessive growth
  • Contraception
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7
Q

What are the major adverse effects of estrogens?

A
  • Nausea
  • Na retention, edema
  • Weight gain
  • Breast tenderness
  • Endometrial hyperplasia
  • Thromboembolism
  • Hypertension
  • Decreased glucose tolerance
  • Increased breast cancer risk in post-menopausal women
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8
Q

What are the representative progestins?

A
  • Progesterone
    • physiological progestin
    • first pass metabolism
    • effective orally when micronized
  • Medroxyprogesterone
    • orally effective synthetic analog
    • also used as depot
  • Norethindrone, levonorgestrel
    • synthetic
    • orally effective
    • 19-nortestosterone derivatives (gonanes)
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9
Q

What are the major adverse effects of progestins?

A
  • Na retention, edema
  • Weight gain
  • Depression
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10
Q

What agents are used to induce ovulation?

A
  • GnRH
  • Gonadotropins
  • Clomiphene
    • selective estrogen receptor modulator (SERM)
    • selectively blocks estrogen feedback inhibition
    • promotes ovulation
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11
Q

What agents are used for breast cancer chemoterapy, especially ER+ breast cancer?

A
  • Tamoxifen
    • SERM that acts as an antiestrogen on the mammary gland
      • also has estrogen agonist activity on bone and uterus
    • approved as breast cancer preventative
    • can have initial stimulatory effects
  • Fulvestrant
    • SERM that is a pure estrogen antagonist
    • lacks the initial stimulatory effects elicited by tamoxifen
  • Anastrozole
    • aromatase inhibitor, blocks estrogen synthesis
    • used for ovarian and prostate cancer
    • used in sequence with tamoxifen to prevent breast cancer recurrence
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12
Q

What agents are used for endometriosis?

A
  • Danazole
    • weak androgen that binds progestin receptors
    • also used for fibrocystic breast disease
  • Leuprolide
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