Androgens-valentovic Flashcards
(35 cards)
Testosterone
Not through oral route, why?
Extensive first pass
Low bioavailability
Testosterone
Topical
Application
24 h depot release (applied to shoulder and upper arm)
Testosterone
Patch
Application
Applied daily
Local irritation causes compliance issues
Testosterone
Patch
Application
Not to scrotum- to much testosterone absorption
Testosterone
Patch
Caution…
Acne or abnormal hair growth in female partner
Testosterone
Black box for gels and topicals
Virilization can occur in children exposed to topical testosterone
Testosterone esters
Testosterone cypionate and enanthate
Testosterone esters
Application
Administered IM: longer duration (2-4 wks)
Testosterone esters
Indicated for
Hypogonadism
Metastatic breast cancer
17a-alkylate testosterone
Types and application
Orally effective
Methyltestosterone, fluoxymesterone
17a-alkylated testosterone
Methyltestosterone, fluoxymesterone
Indications
Hypogonadism and metastatic breast cancer
17a-alkylated testosterone
Methyltestosterone, fluoxymesterone
Risk
High abuse potential for anabolic activity
17a-alkylated testosterone
Methyltestosterone, fluoxymesterone
Contraindications
Male breast cancer
Prostate cancer
Pregnancy
17a-alkylated testosterone
Methyltestosterone, fluoxymesterone
ADR
Cholestatic hepatitis
HIGHEST RISK OF HEPATOTOXICITY
Liver cancer
Bleeding (dec clotting factors)
Contraindications for all testosterone analogs
Prostate cancer
Male breast cancer
Pregnancy
ADR for all testosterone analogs
Salt and water retention (hypertension)
GREATEST RISK OF JAUNDICE WITH 17A-ALKYLATED TESTOSTERONE METHYLTESTOSTERONE AND FLUOXYMESTERONE
Danazol
MOA
Depresses preovulatory surge in output of FSH and LH
Reduces ovarian estrogen and progesterone production
Suppresses FSH and LH surge=>anovulation
Danazol
Uses
Endometriosis
Danazol
ADR
Weight gain
Acne
Danazol
Contraindications
Pregnancy
Breast feeding
Stanazolol
MOA
Inc mRNA levels and protein levels of C1, INH, and C4
Stanazolol
Use
Hereditary angioedema
Stanazolol
ADR
Hepatic toxicity
Stanazolol
Contraindications
Pregnancy
Male breast or prostate cancer
Female breast cancer with hypercalcemia