Endocrine - Male Gonadal Pharm

Front 1

Testosterone replacement therapy

-expected therapeutic effects (4)

Back 1

1. Treat hypogonadism
2. Treat catabolic states (illness or post-surgery)
3. Athletic performance - muscle growth - lean body mass - strength
4. Eryhtropoesis (not anymore)

Front 2

Testosterone replacement therapy

-adverse effects (9)

Back 2

1. Inhibit secretion of pituitary gonadotropins (FSH,LH) - feedback inhibition
2. Inhibit endogenous testicular production of testosterone
3. Reduce spermatogenesis and fertility
4. Erythrocyosis
5. Gynecomastia
6. Virilization of women and children
7. Edema (sodium retention) or Jaundice
8. Lipid imbalance - high LDL/low HDL
9. Dilated cardiac myopathy

Front 3

Testosterone delievery system - pro's and con's

-testosterone esters - enanthate, cypionate, undecanoate

Back 3

Injectable, long-acting esters of testosterone.
- esters are more lipophilic than testosterone, preparations are in oil
-IM injection every 2 weeks
-fluctuating levels in the body

Front 4

Testosterone delievery system - pro's and con's

-alkylated testosterone - used for postpubertal hypodonadism

Back 4

Oral form of testosterone

PROS:
-short acting, taken daily
-less hepatic metabolism than when given IM
-reduced androgenicity

CONS
-potential for hepatotoxicity
-not easily detectable via immunoassay - difficult to monitor therapy

Front 5

Testosterone delievery system - pro's and con's

-transdermal patch/gel

Back 5

PROS
-provide stable level of testosterone throughout the day

CONS
-patches may cause rash, are visible
-gel can virilize women and children if they come in contact, must allow to dry and cover with clothing

Front 6

Testosterone replacement therapy - pros and cons

-buccal testosterone

Back 6

Small, tablet like product adheres to the gum surface above the incisor.

PROS
-absorbed through the gum and directly into the bloodstream
-bypasses liver metabolism

CONS
-must take twice a day

Front 7

Anti-androgens

-which drugs (2) are used to treat alopecia and BPH?

Back 7

5-alpha reductase inhibitors
-Finasteride
-Dutasteride

Front 8

Anti-androgens

-which drugs (2) are used to treat prostate cancer?
-which drugs is better? why?

Back 8

Non-steroidal androgen receptor antagonists
-Flutamide (hepatotoxicity, gynomastia, 4/d dosing)
-Bicalutamide (fewer SE, daily dosing)


Usually combined with GnRH agonists for combined androgen blockade

Front 9

GnRH receptor agonists

-MOA
-drugs (2)

Back 9

MOA: superactive GnRH analogs down regulate GnRH receptor over time - initial surge in testosterone

1. Leuprolide
2. Goserelin

Front 10

GnRH receptor antagonists

-MOA
-drug

Back 10

MOA: Block the action of the GnRH receptor - blocks LH production - no transient increase in testosterone level

1. Plenaxis

Front 11

Nonsteroidal androgen receptor antagonists

-MOA
-drugs (2)

Back 11

MOA: compete with androgens for rececptor site - used in prostate cancer

1. Flutamide
2. Bicalutamide (better)

Front 12

5-alpha reductase inhibitors

-MOA
-drugs

Back 12

MOA: block conversion of testosterone to dihydrotestosterone (active form) - used in BPH and alopecia

1. Finasteride
2. Dutasteride

Front 13

Ketoconazole

-MOA

Back 13

MOA: inhibits glucocorticoid and androgen synthesis in adrenal glad - never used on its own

Front 14

Spironolactone

-MOA

Back 14

MOA: competitive androgen receptor antagonist - treat female hirsutism, PCOS