Androgens -12 Flashcards
Testosterone
- testosterone is secreted by the ___
- in men, there is a constant ___ of testosterone produced daily (95% ___ cells, 5% by adrenal glands)
- testosterone plasma levels: men - ___ mcg/dL after puberty. women - ___ mcg/dL
- circulating testoserone is bound to ___ (65%), ___ (33%), ___ (2%)
- testis
- 8 mg, Leydig
- 0.6 mcg/dL, 0.3 mcg/dL
- sex-hormone binding globulin (SHBG)
- albumin
- free
Regulation of testosterone synthesis
- the hypothalamus releases ___
- anterior pituitary releases ___ and ___
- LH triggers ___ cells in the testis to produce ___. FSH triggers ___ cells to produce ___.
- Testosterone is responsible for the development of sex organs and also inhibits the ___ and ___ through negative feed back.
- GnRH (Gonadotropin-releasing hormone)
- LH (luteinizing hormone) and FSH (follicle stimulating hormone), sperm
- hypothalamus and anterior pituitary
Testosterone metabolism
- in target tissues, testosterone is broken down into ___ by 5α-reductase
- testosterone can also be broken down into ___ by aromatase
- 5α-Dihydrotestosterone
- 17β-Estradiol
T or F: 5α-Dihydrotestosterone is a more potent major active androgen
True
better binding/more activity than testosterone
Testosterone excretion
- occurs in the ___
- inactivated to ___ and ___
- then conjugated and excreted to the ___
- liver
- androsterone and etiocholanolone
- urine
Adrenal androgens
3 intermediates of testosterone
* ___, ___, and ___
* have ___ androgen effects
* large amounts produced in the ___
- androstenedione, dihydroepiandrosterone (DHEA), dihydroepiandrosterone sulfate (DHEAS)
- weak
- adrenal glands
Physiologic effects
- penile and scrotal growth
- ___ and ___ skin
- pubic, axillary, and beard hair
- deepening of voice
- skeletal growth followed by ___ closure
- increase in lean body mass → positive ___ balance
- stimulation and maintenance of sexual function
- stimulation of ___ production
- decrease in ___ levels
- oily and thick
- epiphyseal
- nitrogen
- erythrocyte
- HDL
clinical uses
Androgen replacement therapy in men
* Male ____ (testosterone deficiency)
* Hypopituitarism - promote production of ___ to produce sperm
- hypogonadism
- FSH
clinical use
Gynecologic disorders
* endometriosis (___)
* replacement therapy for ___ women (in combo with estrogens) (controversial)
* eliminates ___ bleeding
* enhances ___
- danazol
- postmenopausal
- endometrial
- libido
must be used with great caution due to adverse effects
clinical use
Protein anabolic agents
* reverse ___ loss after trauma/surgery/prolonged immobilization. Promotes ___ growth.
- can also be used for ___pause
- protein
- andropause
Synthetic androgens
- when administered ___, testosterone is readily absorbed but largely ___.
- ___ forms are more active orally. Example: ___
- ___ forms have prolonged absorption time and greater activity for intramuscular administration. Examples: ___, ___, and ___
- orally, inactivated
- 17-alkyl, methyltestosterone
- ester, propionate, enanthate, cypionate
Anabolic steroids in sports
- doses ___ times larger than the daily normal production
- harmful changes in ___ levels
- acne
- high ___
- hepatic dysfunction in case of ___ steroids
- large doses of anabolic steroids suppress the secretion of ___ → testicular ___
- 10-200
- cholesterol
- high blood pressure
- 17-alkyl
- gonadotropins, atrophy
Adverse effects in women
- hirsutism
- acne
- amenorrhea
- clitoral enlargement
- deepening of voice
Adverse effects in men
- acne
- sleep apnea
- gynecomastia
- azoospermia and testicular atrophy
- increased aggresiveness adn psychotic symptoms
Antiandrogens
___ inhibitors
* block the conversion from testosterone to 5α-dihydrotestosterone.
5α-reductase
Antiandrogens
Androgen receptor inhibitors
* block the binding of ___ androgens or inhibit the activation of the ____
* steroidal and non-steroidal inhibitors
- endogenous
- receptors
5α-reductase inhibitors
Finasteride
* Proscar: used to treat ___
* Propecia: used to treat ___
* for women: ___
- benign prostatic hyperplasia
- male pattern baldness
- hirsutism
5α-reductase inhibitors
Dutasteride
* used for ___ and ___
BPH and male pattern baldness
Steroidal androgen receptor inhibitors
Cyproterone and cyproterone ester
* for women: ___
* for men: ___
- hirsutism
- excessive sexual drive
Steroidal androgen receptor inhibitors
Spironolactone
* for women: ___
* ___ (in pup this was not an FDA approved use)
- hirsutism
- acne
Non-steroidal androgen receptor inhibitors
Flutamide
* ___ anti-androgen used for ___
non-steroidal, prostate cancer
Non-steroidal androgen receptor inhibitors
Enzalutamide
* ___anti-androgen used for ___
non-steroidal, Metastatic castration-resistant prostate cancer
What is this?
5a-dihydrotestosterone
What is this?
17B-Estradiol
What is this?
Androstenedione
What is this?
Androsterone
What is this?
Cyproterone
What is this?
Dihydroepiandrosterone (DHEA)
What is this?
Dihydroepiandrosterone Sulfate (DHEAS)
What is this?
Dutasteride
What is this?
Enzalutamide
What is this?
Finasteride
What is this?
Flutamide
What is this?
Methyltestosterone
What is this?
Spironolactone
What is this?
Testosterone
What is this?
Testosterone cypionate
What is this?
Testosterone enanthate
