L 11 androgens Flashcards

1
Q

testosterone

A

-Most important androgen secreted by the testis
Binds to the androgen receptor and alters the rate of transcription

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2
Q

In men, ~8 mg of testosterone is produced daily

A

-95% by the Leydig cells in the testis
-5% by the adrenal glands

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2
Q

Plasma levels of testosterone

A

-In men, 0.6 μg/dL after puberty; decreases after age 50
-In women, 0.03 μg/d

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3
Q

circulating testosterone

A

-Bound to sex hormone-binding globulin (SHBG) (65%)
-Bound to albumin (33%)
-Free (2%

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4
Q

GnRH

A

gonadrotropin-releasing hormone

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5
Q

LH

A

luteinizing hormone

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6
Q

FSH

A

follicle stimulating hormone

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7
Q

excretion of testosterone

A

-occurs in the liver
-inactivated and conjugated, then excreted to the urine

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8
Q

adrenal androgens

A

-Intermediates of the testosterone synthesis pathway
-Produced in significant amounts, largely in the adrenal glands.
-Weak androgen effects
-Physiological functions are not known
-androstenedione, DHEA, DHEAS

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9
Q

physiologic effects of testosterone

A

-Responsible for many changes at puberty
-Growth-promoting properties
-Stimulation and maintenance of sexual function
-Stimulation of erythrocyte production
-Decrease in HDL levels

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10
Q

growth promoting properties

A

-Penile and scrotal growth
-Change in the skin (thicker and oilier)
-pubic, axillary, and beard hair
-Deepening of the voice
-Skeletal growth followed by epiphyseal closure
-Increase in lean body mass  positive nitrogen balance

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11
Q

androgen replacement therapy in men

A

-Male hypogonadism (testosterone deficiency)
-Hypopituitarism

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12
Q

gynecological disorders

A

-Must be used with great caution due to adverse effects
-Endometriosis (danazol)
-In combination with estrogens for replacement therapy in the postmenopausal period (controversial)
-Eliminates the endometrial bleeding.
-Enhances libido

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13
Q

protein anabolic agents

A

Reverses protein loss after trauma, surgery, or prolonged immobilization in conjunction with dietary measures and exercises

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14
Q

clinical uses of androgens

A

-andropause
-protein anabolic agents
-gynecologic disorders
-androgen replacement therapy in men

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15
Q

synthetic androgens

A

-When administered orally, testosterone is readily absorbed but inactivated largely.
-17-alkyl forms (ex. methyltestosterone) are more active orally.
-Ester forms (ex. propionate, enanthate, cypionate) have prolonged absorption time
and greater activity for intramuscular administration

16
Q

anabolic steroids in sports

A

-Used in doses 10 – 200 times larger than the daily normal production to increase
strength and aggressiveness.
-Such effects have been proven only in women
-Large doses of anabolic steroids suppress the secretion of gonadotropins. –> testicular atrophy

17
Q

significant health risks by long term use of anabolic steroids

A

-Harmful changes in cholesterol levels (Low HDL and high LDL)
-Acne
-High blood pressure
-Hepatic dysfunction in case of 17-alkyl steroid

18
Q

adverse effects of androgen in women

A

-Hirsutism
-Acne
-Amenorrhea
-Clitoral enlargement
-Deepening of the voice
-should not be used in infants or pregnant women because there is significant disturbances in sexual development

19
Q

adverse effects of androgens in men

A

-Acne
-Sleep apnea
-Gynecomastia
-Azoospermia and testicular atrophy
-Increased aggressiveness and psychotic symptom

20
Q

antiandrogens

A

-5a reductase inhibitor
-androgen receptor antagonist

21
Q

5a reductase inhibitors

A

-block the conversion from testosterone to 5a dihydrotestosterone
-Finasteride (Proscar ®, Propecia® )
-Dutasteride (Avodart®

22
Q

synthetic androgens

A

-Methyltestosterone (Android®, Metandren®, Testred®)
-testosterone enanthate (Delatestryl®)
-testosterone cypionate (Depo-Testosterone®

23
Q

androgen receptor antagonist

A

-Block the binding of endogenous androgens to the receptor or inhibit the activation of the receptors
-Steroidal inhibitors
-Non-steroidal inhibitors

24
Q

finasteride

A

-Benign prostatic hyperplasia (Proscar®)
-Male pattern baldness (Propecia ®)
-Hirsutism in women

25
Q

dutasteride

A

-Benign prostatic hyperplasia
-Male pattern baldnes

26
Q

cyproterone acetate

A

-Hirsutism in women
-Excessive sexual drive in men

27
Q

spironolactone

A

-Hirsutism in women
-Acne

28
Q

steroidal androgen receptor antagonist

A

Cyproterone acetate (Androcur®)
 Spironolactone (Aldactone®)

29
Q

flutamide

A

-Non-steroidal antiandrogen
-Prostate cancer

30
Q

enzalutamide

A

-Non-steroidal antiandrogen
-Metastatic castration-resistant prostate cancer

31
Q

nonsteroidal androgen receptor antagonist

A

flutamide (Eulexin®)
 Enzalutamide (Xtandi®)