Androgens Drugs Flashcards
Synthetic
Methyltestosterone
Testosterone Cypionate
Testosterone Enanthate
(addition on the 17 carbon)
Methyltestosterone
Synthetic
More active orally (17 methyl group)
Cannot be broken down
Testosterone Cypionate
Synthetic
IM
More hydrophobic
Prodrug
activated slowly in body
Prolonged absorption time
Testosterone enanthate
Synthetic
IM
More hydrophobic
Prodrug
activated slowly in body
Prolonged absorption time
5a-Reductase inhibitors
Finasteride
Dutasteride
(Add cross on top of addition of 17 carbon)
5a-Reductase inhibitors MOA
Block the conversion from testosterone to 5a-dihydrotestosterone
Finasteride
5a-Reductase inhibitor
TX: Benign prostatic hyperplasia
Male pattern baldness
Hirsutism in women
Dutasteride
5a-Reductase inhibitor
Tx: Benign prostatic hyperplasia
Male pattern baldness
Androgen receptor antagonists MOA:
Block the binding of endogenous androgens to the receptor or inhibit the activation of the receptors
Steroidal androgen receptor antagonists:
Cyproterone acetate
Spironolactone
(Additions at C 6-7)
Cyproterone acetate
Steroidal androgen
Tx: Hirsutism in women
Excessive sex drive in men
Spironolactone
Steroidal androgen
Tx: Hirsutism in women
Acne
Non-steroidal receptor antagonists:
Flutamide
Enzalutamide
(Looks nothing like testosterone; fully conjugated rings)
Flutamide
Non-steroidal receptor antagonist
Tx. Prostate cancer
Enzalutamide
Non-steroidal receptor antagonist
TX. of Metastatic castration resistant prostate cancer
