Pharmacology of Gonadal Hormones 2 Flashcards

Describe why and how gonadotropins are used therapeutically in males and females.

1
Q

List and describe the structures of gonadotropins and their recombinant forms.

A
  • FSH, LH, hCG
  • Glycoproteins with alpha and beta subunits
    • beta subuint confers specificity
  • Recombinant FSHs (follitropin alpha and follitropin beta) differ in their carbohydrate components.
  • LH and hCG are available as recombinant proteins (lutropin alpha, chorionogonadotropin alpha) or as the biological material (urine derived)
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2
Q

What is the mechanism of gonadotropins?

A
  • Acts through G protein-coupled membrane receptors in testis
  • cAMP is the principle 2nd messenger
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3
Q

What cells do FSH primarily act on in the male? What is the effect? What about LH?

A
  • FSH acts on Sertoli cells
    • promotes spermatogenesis
    • peromotes secretion of Androgen Binding Protein
  • LH acts on Leydig cells
    • stimulates side-chain cleavage of cholesterol
      • rate limiting step in testosterone synthesis
    • crossover between effects of FSH and LH
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4
Q

What are the diagnostic uses of gonadotropins in males?

A
  • Determine whether delayed puberty is due to primary gonadal failure
  • Evaluate Leydig cell function
    • hCG injected and testosterone measured
    • normal response indicates a problem at the hypothalamus or pituitary rather than primary gonadal failure
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5
Q

What are the therapeutic uses are gonadotropins in males?

A
  • Induce spermatogenesis in men with hypogonadotropic hypogonadism from hypothalamic or pituitary disease
    • FSH and LH given by injection
    • Response is slow, 4-6 months
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6
Q

What are the uses of FSH, LH, and hCG in the female?

A
  • Sequentially to induce ovulation and infertility treatment
    • FSH - induce follicular development
    • hCG/LH - induce oocyte maturation
    • success rate ~75%
  • Used together with GnRH agonists to generate oocytes for in vitro fertilization
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7
Q

What are the adverse effects of gonadotropin use.

A
  • Gynecomastia in men
  • Ovarian enlargement and multiple births in women
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