Androgens Flashcards
Testosterone is produced in
Leydig cells in men
Corpus Luteum and Adrenal cortex in women
Function of 5a reductase
converts Testosterone to DIhydrotestosterone and Estradial
Uses of Androgens
male hypogonadism
aplastic anemia
Osteoposrosis
Puberty for Testosterone deficient boys
incr. athletic performance: anabolic steroids
AEs of Androgens
Excessive masculinization
decr. sperm production
decr. testicular size
Gynecomastia
Virilization in females
Hepatotoxic
Aggressive behavior
Effects of Virilisation in females
Hyperandrogenism
Temporal balding
male body physique
muscle building
incr. clitoris size
Hirsutism
Admin of Testosterone derivatives
Implant as it undergoes extensive 1st pass metabolism when taken orally=inactivation
CIs of Testosterone impkant
Breast, prostate neoplasm
Effects of Testosterone implant
May cause premature closing of epiphyses if administered early in puberty
Stimulates endogenous EPO production
DIs of Testosterone Implant
Incr. effects of warfarin:=incr. bleeding
May decr blood glycose levels
Which are the Testosterone Esters
Testosterone Undecanoate: T deficiency
Enanthate: incr. muscle mass
Cypionate: T. deficiency
Uses of Testosterone Esters
improve sexual performance
libido
What is Methyltestosterone
17-a-alkyl derivative of T with an oral bioavailability>T.
*its an Ester of T
Uses of Methytestosterone
treats men with T. deficiency
Cautions with Methytestosterone
Prolonged periods of se
Hepatotoxic
What is Mesterolone
dihydroT. derivative that is not metabolised to estrogen
Has an oral bioavailability>T
Indications of Mesterolone
Patients with hepatic disease and those woth estrogenic synptoms of other testosterone
What is Nandrolone
An anabolic effec with hight anabolic effects and lower androgneic effects
Indications of Nandrolone
Treatment of Osteoporosis and Aplastic anemia
Effects of Nandrolone
incr. muscle growth
incr. appetite
incr. RBC production
incr. bone density
Larger doses of Nandrolone leads to
Gynecomastia
decr. libido
AEs of Nandrolone
Erectile dysfunction
CV damage
decr liver hepatic enzymes
liver tumors
cholestatic jaundice
Name an Antigonadotropin
Danazol
MOA of Danazol
binds to estrogen Rs–> inhibits Gonadotropin secretion
Activities of danazol
Weak pregestational, androgenic and glucocorticoid activities
Danazol induces
Endometrial atrophy
AEs of Danazol
greasy skin
acne
voice changes
weight gain
Clinical uses of Danazol
For Sex hormone dependent conditions:
Endometriosis
Breast dysplasia
Gynecomastia
What are Antiandrogens
are inhibitors of Testosterone synthesis
MOA of Antiandrogens
GNRH analogues that inhibit LH secretion thus they inhibit Testosterone synthesis
Name the Antiandrogens
Flutamide
Spironolactone
Cyproterone acetate
Goserelin
Leuprorelin
Triptorelin
Buserelin
What is Flutamide
potent androgen receptor antagonists
Indications of Flutamide
treats metastatic cancer: GnRH analogue
blocks action of adrenal glands
AEs of Fluatmide
Gynecomastia
Galactorrhea
NV
decr. libido
Hepatotoxic
What is Spironoloactone
Weak inhibitor of Androgen Rs thus weak testosterone inhibition
Aldosterone inhibitor
Competitive inhibitor of DHT at target organs
Indications of Spironolactone
Hirsutism in females
What is Cyproterone Acetate
its a competitve agonist to DHT
is a progestin
has antiandrogenic properties
Indications of Cyproterone Acetate
Hirsutism
Severe acne
AEs of Cyproterone Acetate
weight gain
decr. libido
dry vagina
CIs of Cyproterone Acetate
Pregnancy: teratogenic
What is Finasteride
A 5a-reductase inhibitor
–> blocks conversion of Testosterone to DHT (reversible within 4 months of therapy)
Indications of Finasteride
Treatment of BPH: shrinkage of prostate gland in 3-6monthes
Male pattern baldness
hisutism
AEs of Finasteride
infrequently causes impotence
RARE: decr libido, gynecomastia, erectile dysfunction, decr. ejaculation
Pulsatile admin of GnRH analogues cause
incr. circulating gonadotropines–> treats infertility
Sustained admin of GnRH analogues cause
reduction in steroid secretion–> treatment of hormone dependent cancer
Indications of Goserelin
Breast and prostate cancer
Dysfunctional uterine bleeding
AEs of Goserelin
Headache
depression
hot flushes
vaginal dryness
Indications of Leuprorelin
advanced and metastatic prostate cancer
Endometriosis
Infertility
AEs of Leuprorelin
Ovarian hyperstimulation
headache
mood disorders
visual disturbances
Indications of Triptorelin
Advanced prostate cancer
Central precocious Puberty
Endometriosis
Infertility
AEs of Triptorelin
Ovarian hyperstimulation
headache
mood disorders
visual disturbances
Indications of Buserelin
Decr. Testosterone production
Advanced and metastatic prostate cancer
Endometriosis
Infertility
AEs of Buserelin
hot flushes
loss of libido
