Pharm #3 - Androgens Flashcards
State the physiological actions of androgens on the reproductive system
REPRODUCTIVE
Growth, development, maintenance of primary and secondary male sex characteristics
Puberty in females
Promote spermatogenesis (w/ FSH)
Neuroendocrine regulation of gonadotropin secretion
State the physiological actions of androgens (anabolic)
ANABOLIC
Increase protein synthesis, lean body mass, skeletal muscle growth, reduce fat mass
State the physiological actions of androgens (growth)
GROWTH
Stimulates skeletal growth, epiphyseal closure
Growth of larynx at puberty, voice deepening
State the physiological actions of androgens (metabolic)
METABOLIC Erythropoiesis Decreased synthesis of clotting factors Increased sebum production in skin Decrease HDL; increase LDL Androgenic alopecia (male pattern baldness)
CONSEQUENCES OF ANDROGEN DEFICIENCY IN MEN -6
- Decreased libido, erectile dysfunction
- Decreased skeletal muscle mass; increased adipose tissue mass
- Decreased axillary and pubic hair
- Anemia
- Osteoporosis
- Decreased energy and sense of well being
THERAPEUTIC USES OF ANDROGENS (3)
HRT in primary or secondary hypogonadism
Induction of puberty in delayed maturation
Rx of osteoporosis in males (similar to estrogen on its action of bone)
What are the 2 androgens used in HRT
Testosterone enanthate
Testosterone cypionate
Testosterone enanthate
Testosterone cypionate
- INdication
- MOA
Hypogonadism
Replacement of testosterone produces androgenic effects, such as: Growth and maturation of prostate Seminal vesicles Penis & Scrotum Development of male hair distribution Laryngeal enlargement Vocal cord thickening Alterations in body musculature, and Fat distribution
Testosterone enanthate
Testosterone cypionate
Side effects -7 (main 1)
- Cholestatic jaundice syndrome***
(similar to estrogen - progesterone combo) - Liver carcinoma
- Benign prostatic hyperplasia
- Prostate cancer
- Gynecomastia (excess converted to estrogen)
- Acne (sebaceous gland d
evelopment) - Headache
Testosterone enanthate
Testosterone cypiona
Contraindications - 3
Breast cancer in men (androgen is converted to estrogen = bad)
Prostate cancer
Pregnancy when used in women (stimulate estrogen production)
Flutamide
MOA
Indication s(2)
Competitive inhibition of dihydrotestosterone & testosterone binding to the receptor
(androgen receptor antagonist)
Metastatic prostate cancer
Benign prostatic hypertrophy
Flutamide
SE (2 main)
COntra -1
Hepatotoxicity Hematopoietic disorders Diarrhea Nausea Rash Hot Flashes
Contra: Severe hepatic impairment
better for prostate cancer
- DES or -leuprolide or - flutamide
Flutamide is comparatively better than DES and leuprolide in treatment of prostate cancer
Highly effective when combined with medical or surgical castration
DES synthetic estrogen (non-aromatic)
half life is very long
offspring can result in adenocarcinoma
Leuprolide – GnRH antagonist
Spironolactone
MOA
Competitive inhibition of dihydrotestosterone & testosterone binding to the receptor
Spironolactone
indications - 6
Hirsutism Hypertension Acne vulgaris Edema associated with heart failure Cirrhosis or nephrotic syndrome Hypokalemia