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🄼💊MSY2 Pharm (Endocrine/Repro/Thyroid) > Androgens > Flashcards

Androgens Flashcards

1
Q

Name the natural androgens (4)

A
  • Testosterone
  • Dihydrotestosterone (DHT)
  • Androstenedione
  • Dehydroepiandroesterone (DHEA)
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2
Q

Most potent natural androgen

A

DHT

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3
Q

Benefit of synthetic androgens

A

Longer half-life (like all synthetic hormones)

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4
Q

Metabolic conversions of Testosterone (2)

A
  • 5 alpha reductase –> DHT
  • Aromatase –> Estrogen
  • Aromatase might change androstenedione into estrogen instead of testosterone
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5
Q

Basic Mechanism of Action of Androgen (3 steps)

A
  • Testosterone diffuses into cell and binds to intracellular androgen receptor
  • Hormone receptor complex dimerizes in cell nucleus and binds to specific hormone-response elements on DNA, along with a complex of co-activator or co-repressor proteins
  • Promotion or inhibition of transcription of specific genes, resulting in physiologic effect.
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6
Q

Reproductive actions of Androgens (4)

A
  • primary and secondary sex male characteristics
  • Early stages of breast and pubertal development in girls (adrenarche)
  • spermatogenesis (with help of FSH)
  • Stimulate libido
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7
Q

Anabolic actions of Androgens (3)

A
  • Increase protein synthesis
  • Increased lean body mass
  • DEC Fat

*similar to GH

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8
Q

Effect of Androgens on growth (2)

A
  • Skeletal growth and closure of epiphyses of long bones during puberty and adolescence
  • Growth of larynx –> Voice Deepening
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9
Q

Metabolic/hematologic actions of androgens (6)

A
  • Erythropoiesis
  • Decreased clotting factors production (opposite of estrogen)
  • Increased skin sebum
  • Decrease HDL but INC LDL :-(
  • Androgenic alopecia (male pattern baldness)
  • Increases bone density
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10
Q

Consequences of androgen deficiency in men (6)

A
  1. Decreased libido; erectile dysfunction
  2. Decreased lean muscle mass w/INC Fat
  3. Decreased axillary / pubic hair
  4. Anemia
  5. Osteoporosis
  6. Decreased energy, sense of well being
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11
Q

Therapeutic uses of androgens (3)

A

-HRT in primary or secondary hypogonadism
(gonads must be responsive)
-Delayed puberty
-Male Osteoporosis

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12
Q

Which androgens are used in hormone replacement therapy? (2)

A
  • Testosterone enanthate

- Testosterone cypionate

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13
Q

Clinical indication of Testosterone enanthate and Testosterone cypionate

A

hypOgonadism

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14
Q

Effect of Testosterone enanthate and Testosterone cypionate (2)

A
  • [Primary and Secondary Sex Characteristics]

- Alterations in body musculature such as Fat distribution

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15
Q

SEs of Testosterone enanthate and Testosterone cypionate (7)

A

CLAP for (H)arry (B)arry

  • Cholestatic jaundice sundrome (protein synthesis in liver)
  • Liver carcinoma
  • Benign prostatic hyperplasia
  • Prostate CA
  • Gynecomastia
  • Acne
  • Headache
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16
Q

Contraindication of Testosterone enanthate and Testosterone cypionate (3)

A
  • Breast cancer in men
  • Prostate cancer
  • Pregnancy when used in women
17
Q

Delivery routes and formulations of Testosterone enanthate and Testosterone cypionate (4)

A
  • Intramuscular
  • Transdermal
  • Topical gel
  • Oral

*The transdermal is preferred to prevent first pass hepatic metabolism

18
Q

[Drug class/MOA] of Flutamide

A

[Androgen R Blocker] –> prevents DHT & Testosterone from binding

19
Q

Clinical indications of Flutamide (2)

A
  • Metastatic Prostate Cancer

- BPH

20
Q

Side Effects of Flutamide (4)

A
  • Hepatotoxicity
  • Hematopoietic disorders
  • Rash
  • Constitutional (HA/Nausea)
21
Q

Contraindication of Flutamide

A

Severe Liver Dz

22
Q

Compare efficacy between Flutamide and other tx in prostate cancer

A

Flutamide > [DES and Leuprolide] which shut down LH and FSH to block androgen synthesis

23
Q

Effectiveness of Flutamide

A

Excellent when combined with medical or surgical castration

24
Q

[Drug class/MOA] of spironolactone (2)

A

Androgen R Blocker & Aldosterone R Blocker

25
Q

Drug indications of spironolactone (7)

A

“Spironolactone (H)as (P)owerful HACEK “

  • Hirsutism
  • HTN
  • Acne vulgaris
  • Edema 2º to heart failure
  • Cirrhosis or nephrotic syndrome
  • Kalemia (hypOkalemia)
  • Primary aldosteronism
26
Q

Side Effects of spironolactone (6)

A

“Spironolactone speared at me like a DHAGGA”

  • Dyspepsia
  • Hyperkalemic metabolic acidosis
  • [Agranulocytosis systemic lupus erythematosus]
  • Gynecomastia
  • GI Hemorrhage
  • Abnormal menstruation

and also…

  • Lethargy
  • Impotence
  • Rash
  • Breast cancer - not yet established
27
Q

Contraindications of spironolactone (3)

A
  • Anuria
  • Hyperkalemia
  • Acute renal insufficiency
28
Q

[Drug class/MOA] of Finasteride

A

[5 alpha reductase II inhibitor] –> Inhibits Peripheral Testosterone conversion to DHT

29
Q

Drug indications of Finasteride (2)

A
  • BPH

- Androgenic alopecia

30
Q

Side Effects of Finasteride (4)

A

“Finesse too much –> BLEP”

  • Breast CA in males
  • Libido DEC
  • Erectile Dysfunction & Ejaculation problems
  • Breast TTP
31
Q

Contraindications of Finasteride (2)

A
  • Known or suspected pregnancy

- Women and children

32
Q

Effects of Finasteride on the prostate

A

-Improves urine flow (especially in large prostates)

  • alternative to transurethral resection of prostate (TRUP)
  • up to 25% reduction in prostate size when consistently used for one year
33
Q

Which organs can [5 alpha reductase II] be found? (3)

A
  • Prostate
  • Liver
  • Skin

🄼💊MSY2 Pharm (Endocrine/Repro/Thyroid) (6 decks)

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