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What are the transport mechanisms of Androgens?
- Testosterone-Estrogen binding protein (30%)
- Albumin bound (68%)
- Free (2%)
- Active fraction = free + albumnin-bound
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What are the actions of Testosterone?
- Androgen receptors
- Converted to DHT via 5a-reductase
- Converted to estrogen via aromatase
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What's the treatment for Hypogonadism?
Testosterone supplement
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what's the cause of congenital adrenal hyperplasia?
Tx?
- 21-Hydroxylase deficiency
- Tx: hydrocortisone & fludrocortisone
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What's the clinical presentation of Andropause?
Decreased testosterone concentration from 30-70 y/o
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What are disorders with testosterone replacement as a treatment?
Andropause, Catabolic (AIDS) Wasting, Anemia
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What kind of drug is Flutamide?
- Androgen receptor antagonist
- Sequential rise in LH --> testosterone increase
- More toxic
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What kind of drug is Bicalutamide?
- Androgen receptor antagonist
- Sequential rise in LH --> testosterone increase
- Less toxic
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What kind of drug is Cyproterone Acetate?
- Weak androgen recpetor antagonist
- Tx for hitsutism in women
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What kind of drug is Finasteride?
- Block type II 5a-reductase --> inhibit DHT production in prostate
- Tx for BPH
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What kind of drug is Dutasteride?
Block type I &II 5a-reductase --> inhibit DHT production in prostateTx for BPH
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What kind of drugs are:
Estradiol-17, Estriol, Estrone, Premarin
- Estradiol-17: is the main estrogen produced by the ovary
- Estriol: a weak estrogen
- Estrone: a weak estrogen
- Premarin: from pregnant mare urine
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What kind of drug is 17a ethunyl estradiol?
Orally active estrogen therapy
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What kind of drug is equilin?
- Equine estrogen therapy
- Conjugation with SO4 results in avoidance of first pass metabolism
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What kind of drug is ethinyl estradion/ norethindrone acetate? What's the clinical result?
- Estrogen and Progesterone combined
- Decreased risk of colon CA, bone fracture
- Increased risk of MI, CVA, clots, breast CA
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What kind of drug is Tamoxifen?
- Partial estrogen receptor agonist
- Agonist: endometrium & Bone
- Antagonist: Breast
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What kind of drug is Raloxifene?
- Partial estrogen receptor agonist
- Agonist: Bone
- Antagonist: Breast & endometrium
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What kind of drug is Letrozole?
- Aromatase inhibitor
- Tx for breast CA to block local production of estrogen
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