Androgens & Anti-Androgens:

Question 1

Testosterone:

Answer 1

• Mainly synthesized in the testis by Leydig Cells. It is converted in the periphery to DHT via 5alpha- reductase
• Orally ineffective

Question 2

17 alpha methyl testosterone:

Answer 2

• Synthetic Testosterone

- Oral or Sublingual preparations are available.

Question 3

Testosterone Propionate:

Answer 3

Androgenic ester

• Given via parental routes (SC/ IM routes)
• Administered for testosterone deficiency

Question 4

Stanozolol:

Answer 4

• Synthetic anabolic steroid

- -Decreases androgenic steroid production and increases anabolic activity

Question 5

Therapeutic Uses/ AE of Testosterone:

Answer 5

• To treat Hypogonadalism
• -Testosterone replacement stimulates the anterior pituitary to increase gonadotropins and promote secondary sex characteristics.
• To treat osteoporosis
• In trauma: To decrease protein loss and to promote positive nitrogen balance.
• In Post- Operative Patients/ Convalescence
• In the management of intractable anemia

AEs:

• Acne, Benign Prostatic Hyperplasia (BPH) and Hypertrophy
• Behavioural Changes
• Hepatic Dysfunction
• Cholestatic Jaundice

Question 6

Leuprolide:

Answer 6

• A synthetic GnRH peptide analogue agonist
• Decreases FSH/ LH production
• After an initial flare, it decreases male gonadal function.
• Useful in the management of prostate cancer by decreasing LH- dependent testosterone production
• Testosterone is responsible for the prostate hypertrophy and hyperplasia*
• Can be used for endometriosis

Question 7

Ganirelix:

Answer 7

• GnRH antagonist
• -Does not have the initial flare of gonadotropins
• Useful in the management of prostate cancer by decreasing LH- dependent testosterone production.
• Testosterone is responsible for the prostate hypertrophy and hyperplasia*
• Can be used to treat endometriosis.

Question 8

Finasteride:

Answer 8

5alpha- Reductase Inhibitor
-It is a steroid which prevents the conversion of testosterone to DHT- the active androgen in vivo

Therapeutic Uses:
-Prostate Cancer & Hirsutism in women

Question 9

Spironolactone:

Answer 9

• Synthetic steroid (competitive antagonist of aldosterone)
• K+ sparing diuretic/ a steroid antagonist that decreases the biosynthesis of testosterone in the Leydig cells of the testis
• It inhibits 17-alpha hydroxylase- thus, it decreases testosterone biosynthesis. It also blocks DHT receptors in the hair follicles- thus, inhibiting the action of testosterone at the hair follicles.

-It also blocks the DHT mediated androgenic responses (useful in treating Hirsutism for this reason, aside being used a K+ conserving diuretic.

Therapeutic Uses:

• ->Treatment and management of Hirsutism:
• Management of primary hyperaldosteronism
• Anti-hypertensive for volume overload hypertension
• It is also a K+ sparing diuretic

Question 10

Flutamide:

Answer 10

• DHT receptor antagonist (Anti- androgen)
• Non-steroid
• Competes with DHT for intracellular androgen receptors and blocks the action of testosterone (it is a competitive DHT antagonist)
• Main Adverse:
• Hepatotoxic
• –When Flutamide + Leuprolide are combined, there is a synergistic effect and there is no flare.

Question 11

Cyproterone Acetate:

Answer 11

DHT antagonist

• Is a steroid (Anti- Androgen Steroid)
• Is the most potent Progestin
• It blocks the testosterone (DHT) receptor

Use of Cyproterone:

• To treat hirsutism
• To decrease libido and aggressiveness in males (often sex offenders)