Pharm #3 - Androgens Flashcards

1
Q

State the physiological actions of androgens on the reproductive system

A

REPRODUCTIVE
Growth, development, maintenance of primary and secondary male sex characteristics
Puberty in females
Promote spermatogenesis (w/ FSH)
Neuroendocrine regulation of gonadotropin secretion

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2
Q

State the physiological actions of androgens (anabolic)

A

ANABOLIC

Increase protein synthesis, lean body mass, skeletal muscle growth, reduce fat mass

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3
Q

State the physiological actions of androgens (growth)

A

GROWTH
Stimulates skeletal growth, epiphyseal closure
Growth of larynx at puberty, voice deepening

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4
Q

State the physiological actions of androgens (metabolic)

A
METABOLIC
 Erythropoiesis
 Decreased synthesis of clotting factors
 Increased sebum production in skin
 Decrease HDL; increase LDL
 Androgenic alopecia (male pattern baldness)
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5
Q

CONSEQUENCES OF ANDROGEN DEFICIENCY IN MEN -6

A
  1. Decreased libido, erectile dysfunction
  2. Decreased skeletal muscle mass; increased adipose tissue mass
  3. Decreased axillary and pubic hair
  4. Anemia
  5. Osteoporosis
  6. Decreased energy and sense of well being
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6
Q

THERAPEUTIC USES OF ANDROGENS (3)

A

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)

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7
Q

What are the 2 androgens used in HRT

A

Testosterone enanthate

Testosterone cypionate

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8
Q

Testosterone enanthate
Testosterone cypionate

  • INdication
  • MOA
A

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
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9
Q

Testosterone enanthate
Testosterone cypionate

Side effects -7 (main 1)

A
  1. Cholestatic jaundice syndrome***
    (similar to estrogen - progesterone combo)
  2. Liver carcinoma
  3. Benign prostatic hyperplasia
  4. Prostate cancer
  5. Gynecomastia (excess converted to estrogen)
  6. Acne (sebaceous gland d
    evelopment)
  7. Headache
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10
Q

Testosterone enanthate
Testosterone cypiona

Contraindications - 3

A

Breast cancer in men (androgen is converted to estrogen = bad)

Prostate cancer

Pregnancy when used in women (stimulate estrogen production)

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11
Q

Flutamide

MOA

Indication s(2)

A

Competitive inhibition of dihydrotestosterone & testosterone binding to the receptor
(androgen receptor antagonist)

Metastatic prostate cancer
Benign prostatic hypertrophy

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12
Q

Flutamide

SE (2 main)

COntra -1

A
Hepatotoxicity
 Hematopoietic disorders
 Diarrhea
 Nausea
 Rash
 Hot Flashes

Contra: Severe hepatic impairment

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13
Q

better for prostate cancer

- DES 
or
-leuprolide
or
- flutamide
A

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

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14
Q

Spironolactone

MOA

A

Competitive inhibition of dihydrotestosterone & testosterone binding to the receptor

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15
Q

Spironolactone

indications - 6

A
Hirsutism
 Hypertension
 Acne vulgaris
 Edema associated with heart failure
 Cirrhosis or nephrotic syndrome
 Hypokalemia
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16
Q

Spironolactone

SE

(10)

A
  1. Gastrointestinal hemorrhage
  2. Hyperkalemic metabolic acidosis
  3. Agranulocytosis systemic lupus erythematosus
  4. Gynecomastia
  5. Dyspepsia
  6. Lethargy
  7. Abnormal menstruation
  8. Impotence
  9. Rash
  10. Breast cancer – not yet established
17
Q

3 contra for spironolactone

A

Anuria
Hyperkalemia
Acute renal insuffiency

*aldosterone receptor antagonist but also acts as an androgen receptor antagonist

18
Q

Finasteride

MOA

Indications -2

A

Selective inhibition of type II 5 α-reductase, the enzyme responsible for conversion of testosterone to dihydrotestosterone in prostate, liver & skin

  1. Benign prostatic hyperplasia
  2. Androgenic alopecia
19
Q

Finasteride

  • adverse - 5
A

All functions of DHT

  1. Neoplasm of male breast (rare and not yet investigated)
  2. Breast tenderness
  3. Decreased libido
  4. Erectile dysfunction
  5. Ejaculatory disorder
20
Q

Finasteride

Contra - 1

A

Known or suspected pregnancy

21
Q

Improves urine flow (smaller cells)

Can be used as alternative to transurethral resection of prostate (TRUP)

Up to 25% reduction in prostate size when consistently used for one year

Most effective in patients with large prostates

Women should not be treated with finasteride

A

Finasteride