Androgens Flashcards
Name the natural androgens (4)
- Testosterone
- Dihydrotestosterone (DHT)
- Androstenedione
- Dehydroepiandroesterone (DHEA)
Most potent natural androgen
DHT
Benefit of synthetic androgens
Longer half-life (like all synthetic hormones)
Metabolic conversions of Testosterone (2)
- 5 alpha reductase –> DHT
- Aromatase –> Estrogen
- Aromatase might change androstenedione into estrogen instead of testosterone
Basic Mechanism of Action of Androgen (3 steps)
- Testosterone diffuses into cell and binds to intracellular androgen receptor
- Hormone receptor complex dimerizes in cell nucleus and binds to specific hormone-response elements on DNA, along with a complex of co-activator or co-repressor proteins
- Promotion or inhibition of transcription of specific genes, resulting in physiologic effect.
Reproductive actions of Androgens (4)
- primary and secondary sex male characteristics
- Early stages of breast and pubertal development in girls (adrenarche)
- spermatogenesis (with help of FSH)
- Stimulate libido
Anabolic actions of Androgens (3)
- Increase protein synthesis
- Increased lean body mass
- DEC Fat
*similar to GH
Effect of Androgens on growth (2)
- Skeletal growth and closure of epiphyses of long bones during puberty and adolescence
- Growth of larynx –> Voice Deepening
Metabolic/hematologic actions of androgens (6)
- Erythropoiesis
- Decreased clotting factors production (opposite of estrogen)
- Increased skin sebum
- Decrease HDL but INC LDL :-(
- Androgenic alopecia (male pattern baldness)
- Increases bone density
Consequences of androgen deficiency in men (6)
- Decreased libido; erectile dysfunction
- Decreased lean muscle mass w/INC Fat
- Decreased axillary / pubic hair
- Anemia
- Osteoporosis
- Decreased energy, sense of well being
Therapeutic uses of androgens (3)
-HRT in primary or secondary hypogonadism
(gonads must be responsive)
-Delayed puberty
-Male Osteoporosis
Which androgens are used in hormone replacement therapy? (2)
- Testosterone enanthate
- Testosterone cypionate
Clinical indication of Testosterone enanthate and Testosterone cypionate
hypOgonadism
Effect of Testosterone enanthate and Testosterone cypionate (2)
- [Primary and Secondary Sex Characteristics]
- Alterations in body musculature such as Fat distribution
SEs of Testosterone enanthate and Testosterone cypionate (7)
CLAP for (H)arry (B)arry
- Cholestatic jaundice sundrome (protein synthesis in liver)
- Liver carcinoma
- Benign prostatic hyperplasia
- Prostate CA
- Gynecomastia
- Acne
- Headache
Contraindication of Testosterone enanthate and Testosterone cypionate (3)
- Breast cancer in men
- Prostate cancer
- Pregnancy when used in women
Delivery routes and formulations of Testosterone enanthate and Testosterone cypionate (4)
- Intramuscular
- Transdermal
- Topical gel
- Oral
*The transdermal is preferred to prevent first pass hepatic metabolism
[Drug class/MOA] of Flutamide
[Androgen R Blocker] –> prevents DHT & Testosterone from binding
Clinical indications of Flutamide (2)
- Metastatic Prostate Cancer
- BPH
Side Effects of Flutamide (4)
- Hepatotoxicity
- Hematopoietic disorders
- Rash
- Constitutional (HA/Nausea)
Contraindication of Flutamide
Severe Liver Dz
Compare efficacy between Flutamide and other tx in prostate cancer
Flutamide > [DES and Leuprolide] which shut down LH and FSH to block androgen synthesis
Effectiveness of Flutamide
Excellent when combined with medical or surgical castration
[Drug class/MOA] of spironolactone (2)
Androgen R Blocker & Aldosterone R Blocker
Drug indications of spironolactone (7)
“Spironolactone (H)as (P)owerful HACEK “
- Hirsutism
- HTN
- Acne vulgaris
- Edema 2º to heart failure
- Cirrhosis or nephrotic syndrome
- Kalemia (hypOkalemia)
- Primary aldosteronism
Side Effects of spironolactone (6)
“Spironolactone speared at me like a DHAGGA”
- Dyspepsia
- Hyperkalemic metabolic acidosis
- [Agranulocytosis systemic lupus erythematosus]
- Gynecomastia
- GI Hemorrhage
- Abnormal menstruation
and also…
- Lethargy
- Impotence
- Rash
- Breast cancer - not yet established
Contraindications of spironolactone (3)
- Anuria
- Hyperkalemia
- Acute renal insufficiency
[Drug class/MOA] of Finasteride
[5 alpha reductase II inhibitor] –> Inhibits Peripheral Testosterone conversion to DHT
Drug indications of Finasteride (2)
- BPH
- Androgenic alopecia
Side Effects of Finasteride (4)
“Finesse too much –> BLEP”
- Breast CA in males
- Libido DEC
- Erectile Dysfunction & Ejaculation problems
- Breast TTP
Contraindications of Finasteride (2)
- Known or suspected pregnancy
- Women and children
Effects of Finasteride on the prostate
-Improves urine flow (especially in large prostates)
- alternative to transurethral resection of prostate (TRUP)
- up to 25% reduction in prostate size when consistently used for one year
Which organs can [5 alpha reductase II] be found? (3)
- Prostate
- Liver
- Skin
