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Pharma 2- Semmelweis > B-21. Androgens, anabolic steroids, antiandrogens. > Flashcards

B-21. Androgens, anabolic steroids, antiandrogens. Flashcards

1
Q

The testes main function? Controlled by? Main androgen secreted? Letter amount of DHEA secreted?

A
  • Gametogenic functions (controlled by FSH)
  • Endocrine functions:
    • The main androgen secreted by the testes is testosterone (Leydig cells – stimulated by LH)
    • Smaller amounts of dihydrotestosterone (potent), androstenedione and dehydroepiandrosterone (weak androgens) are also secreted
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2
Q

Testosterone pharmokinetics

A

Testosterone - IC receptor → gene activation

Good absorption, but low oral bioavailability (first pass metabolism) → injection of transdermal use

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3
Q

Testosterone Pharmacological actions

A
  • Testosterone Pharmacological actions:
    • In young men: development of secondary sex characteristics
    • In adult women: facial and body hair, deepening of voice, enlargement of the clitoris, frontal baldness etc.
    • In adult men: maintenance of libido, spermatogenesis
    • Anabolic effects:
      • Reduced nitrogen excretion, increased protein synthesis, decreased protein breakdown (more pronounced in women and children)
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4
Q

Steroids with androgenic/anabolic actions?

A

Testosterone

Nandrolone

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5
Q

Clinical uses of androgens and related steroids

A
  • Clinical uses of androgens and related steroids
    • Androgen replacement:
      • Hypogonadism in men, after castration
    • Protein anabolic agents after trauma, surgery, prolonged immobilization
    • Gynecologic disorders:
      • Danazol (weak androgen) for endometriosis
    • Illegal use (sports)
    • Danazol, stanozolol- for hereditary angioedema (long-term therapy- increased synthesis of C1-esterase-inhibitor in the liver)
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6
Q

Adverse effects of androgens and related steroids

A
  • Adverse effects of androgens and related steroids
    • Masculinizing action in women and children (hirsutism, acne, deepening of voice etc.)
    • Some androgens with progestational activity- increased cardiovascular risk, endometrial bleeding upon discontinuation in women
    • Sodium retention, edema
    • C-17-alkyl-substituted steroids (most anabolic agents) – hepatic dysfunction (AST, bilirubin, cholestasis, hepatic tumors)
    • Older males – prostate hyperplasia
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7
Q

Contraindications of steroids

A

Contraindications: Pregnancy, prostate cancer, infants and young children, breast cancer in males

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8
Q

Antiandrogen classes

A
  1. Androgenic suppression with GnRH-analogues
  2. Steroid synthesis inhibitors
  3. 5alpha-reductive inhibitors
  4. Androgen receptor antagonist
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9
Q

Steroid synthesis inhibitor drugs

A
  1. Ketoconazole
  2. 17-hydroxylase inhibitors
    • Abiraterone
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10
Q

Ketoconazole Function as a antiandrogen? Clinical trials? Side effects?

A
  • Antifungal drug, inhibitor of adrenal and gonadal steroid synthesis
  • Clinical trails in hirsutism (women) and prostate cancer are not encouraging
  • Causes sexual disturbances during the antifungal treatment
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11
Q

5alpha-reductase inhibitors drugs

A
  • Finasteride
  • Dutasteride
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12
Q

5alpha-reductive inhibitor effects? Useful in?

A

Moderately effective in reducing prostate size in men with benign prostate hyperplasia ▪ May be useful in male baldness and female hirsutism

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13
Q

Androgen receptor antagonist drugs

A

Flutamide Bicalutamide Nilutamide Enzalutamide Cyproterone acetate Spironolactone

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14
Q

Androgen receptor antagonist (Flutamide, bicalutamide, nilutamide, enzalutamide) Used in treatment of? Side effect?

A
  • Strong and pure androgen antagonists
  • Used in treatment of metastatic prostate cancer
  • Flutamide has a mild hepatotoxicity
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15
Q

Cyproterone acetate -Activity? Treatment of? Combined with?

A
  • Strong progestational activity
  • Treatment of hirsutism in women, decreases excessive sexual drive in men, useful in prostate cancer, and used in alopecia in women (combination therapy with ethynylestradiol)
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16
Q

Spironolactone use as an antiandrogen

A

Diuretic agent, aldosterone and androgen antagonist, inhibits testosterone synthesis, used in the treatment of hirsutism in women

17
Q

GnRH drugs

A
  1. Leuprolide
  2. Nafarelin
  3. Goserelin
  4. Histerelin
18
Q

GnRH analogues are what and produced where? Controls? Half life? Given?

A
  • Decapeptide, produced by the arcuate nucleus of the hypothalamus
  • Controls the release of the gonadotropins FSH and LH
  • GnRH analogs have a longer half-life (3 hours compared with GnRH – 4 minutes) and can be given intranasally
19
Q

GnRH (Leuprolide, Nafarelin, Goserelin, Histerelin) analogues diagnostic use

A
  • Diagnostic use:
    • Delayed puberty
      • Constitutional delay – normal LH response
      • Hypogonadotropic hypogonadism due to pituitary/hypothalamic disease – impaired LH response
20
Q

GnRH (Leuprolide, Nafarelin, Goserelin, Histerelin) analogues therapeutic uses

A
  • Therapeutic uses:
    • Stimulation – pulsatile GnRH (gonadorelin) therapy:
      • Every 90 minutes – infertility caused by hypothalamic hypogonadotropic hypogonadism in both sexes
    • Suppression – continuous therapy (GnRH analogs):
      • Prostate cancer, uterine fibroids, endometriosis, polycystic ovary syndrome, precocious puberty
    • In vitro fertilization programs:
      • Suppression followed by exogenous gonadotropins – synchronous follicular development
21
Q

GnRH antagonist and function

A
  1. Ganirelix
  2. Abarelix
  3. Degarelix
  4. Cetrorelix

Treatment of prostate cancer, in vitro fertilization programs

22
Q

FSH is? Stimulates?

A
  • Glycoproteins hormone produced in the anterior pituitary
  • Stimulates gametogenesis and follicular development in women and spermatogenesis in men
23
Q

FSH drugs

A
  • Follitropen Beta
    • Modified FSH for therapeutic use
  • Urofollitropin
    • Human FSH extracted from the urine of postmenopausal women without LH
  • hMF (menotropins)
    • FSH-LH combination
24
Q

FSH drugs indication

A

Pituitary or hypothalamic hypogondaism with infertility, in vitro fertilization programs

25
Q

LH produced by? Primarily responsible for?

A
  • Primarily responsible for regulation of gonadal steroid hormone secretion
    • No LH preparation in clinical use
    • Human chorionic gondotropin (hCG)- LH substitute
26
Q

Diagnostic use of LH

A

Prepubertal boys with undescended gonads- distinguished truly retained (cryptochid) testis from retracted (pseudocryptochid)

27
Q

Therapeutic use of LH

A
  • Therapeutic use
    • Induce ovulation (in combination with human menotropins)
    • Stimulate testosterone secretion (hypogonadotropic hypogonadism)
    • AIDs-related Kaposi’s sarcoma- injection into the lesions causes regression
28
Q
A

Pharma 2- Semmelweis (43 decks)

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