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Pharmacology > Androgen Pharmacology > Flashcards

Androgen Pharmacology Flashcards

1
Q

Describe the function and location of
FSH
Testosterone
LH

A

FSH from pituitary controls spermatogenesis in seminiferous cells

Testosterone produced in Leydig cells is also required for spermatogenesis

LH from pituitary stimulates androgen (testosterone) production in Leydig cells.

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2
Q
  • Pituitary begins to secrete LH and FSH at ___
  • After (__) levels of testosterone are regulated by ___
  • Episodic firing of peptidergic neurons in arcuate nucleus results in pulsatile release of ___ –> pulsatile release of LH (lesser amounts of FSH) from the pituitary
A

puberty / puberty

negative feedback at level of pituitary via testosterone interaction with pituitary receptors

GnRH

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3
Q
  • Pituitary begins to secrete LH and FSH at ___
  • After (__) levels of testosterone are regulated by ___
  • Episodic firing of peptidergic neurons in arcuate nucleus results in pulsatile release of ___ –> pulsatile release of LH (lesser amounts of FSH) from the pituitary
A

puberty / puberty

negative feedback at level of pituitary via testosterone interaction with pituitary receptors

GnRH

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4
Q

Most important androgen in muscle and liver

A

testosterone

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5
Q

Hypogonadal levels of testosterone are

A

<200 ng/dl

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6
Q

DHT is predominant androgen mediator in some tissues including

A
  • prostate
  • reproductive tissue (penis-scrotum)
  • hair
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7
Q
  • Conversion to DHT blocked by the enzyme inhibitors __ and ___
  • Converted to estrogen by ___ in peripheral tissues
A

finasteride (type II)

  • (Proscar® [prostate cancer],
  • Propecia® [hair loss])

Dutasteride (type I and II)
-(Avodart® [prostate cancer])

CYP19 aromatase

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8
Q

Function of testosterone

A
  1. puberty associated changes in males (secondary sex characteristics)
  2. essential in utero
  3. Growth-promoting properties (increase muscle mass, skeletal growth)
  4. closing of epiphysis via conversion to estrogen
  5. psychologic/behavioral changes via direct effects on CNS
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9
Q

Describe the clinical uses of physiological testosterone replacement

A
  1. Hypogonadal boys (HD if def. occurs prior to sexual maturation)
  2. Osteoporosis (+/- estrogens)
  3. muscle wasting associated with AIDS
  4. HRT in aging med in controversial (only for T def. NOT impaired spermatogenesis)
  5. Abuse in sports via anabolic effect
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10
Q

Androgen deficiency related symptoms

A
  1. low libido
  2. decreased ED
  3. small testes
  4. low bone mineral density
  5. Gynecomastia
  6. Non-specific: fatigue, depression, anemia reduced muscle strength, increased fat
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11
Q 
Symptoms related specifically to androgen deficiency in aging males include: 
A.  Fatigue 
B.  Increased fat 
C.  Low libido 
D.  Depression 
E.  Low bone mineral density
A

C.  Low libido**

E.  Low bone mineral density

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12
Q

All anabolic hormones tested also have ____ type of side effects including:

A

Androgenic side effects

  1. block of LH-FSH release
  2. promotion of prostate growth
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13
Q

Consequences of Steroid abuse

A
  1. Infertility
  2. Gynecomastia
  3. testicular atrophy
  4. baldness and excessive body hair
  5. short stature
  6. tendon rupture
  7. increased LDL and decreased HDL
  8. HTN
  9. MI and CVA
  10. increased risk of hepatitis/HIV/infection
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14
Q 
Which of the following natural or synthetic steroids has both anabolic activity and androgenic activity in humans? 
A.  Testosterone
B.  Methyltestosterone 
C.  Oxandrolone 
D.  Nandrolone 
E.  Stanozolol 
F.   All of the above
A

F.   All of the above

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15
Q

Why has modifying the T molecule and/or changing administration routes so important for T meds?

A

T has excellent oral absorption but rapid hepatic degradation –> therefore difficult to maintain normal T levels

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16
Q

Parenteral/IM T type and MOa

A

T ethanate
T cypionate esters

Increased lipophilicity - after IM dose sequestration with gradual release from vehicle

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17
Q

Parenteral T

A

T ethanate

T cypionate esters

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18
Q

Advantages and disadvantages of IM T.

A

Advantage: will initiate and maintain normal virilzation in hypogonadal men given every 1-3 weeks

Disadvanatage: less frequent injections an d greater fluctuations in serum T, which can result in fluctuations in energy, mood and libido

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19
Q

Advantages and disadvantages of oral T

A

Advantage: 17-a-alkylated androgens have reduced 1st pass metabolism

Disadvantage: hepatic SE diminished use

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20
Q

Advantages and disadvantages of transdermal patch T

A

Advantage: Once daily use normalizes T levels in most men

Disadvantage: severe skin rash necessitating discontinuation in up to 1/3rd of pts

21
Q

Advantages and disadvantages of transdermal gel T

A

Advantage: given every 24 hrs and maintains relatively stable T levels throughout the dosing period–> maintenance of mood, energy, and libido

Disadvantage: most expensive T formulations

22
Q

How often do buccal and nasal gel T need to be given

A

Buccal: BID tablets

Nasal gel: TID to nostrils

23
Q

Adverse effects of supraphysiologic or pharmacologic doses of androgens

A
  1. Decreased spermatogenesis
  2. Reversible cholestatic jaundice (higher w/ oral agents, hepatic carcinoma)
  3. Edema–> wt. gain/ exacerbate CHF
  4. Increased susceptibility to ARTERIAL thrombosis (decreased HDL, increase LDL and platelet aggregation)
  5. Psychiatric sx–> hypomania “-roid rage”
  6. Prostate adverse effects?
  7. testicular atrophy via decrease LH/FSH release
  8. conversion of androgens to estrogens– gynecomastia
    * return of normal fxn after continuation
24
Q 
Adverse effects associated with androgen use can include all of the following EXCEPT:
A.  Anemia 
B.  Decreased spermatogenesis 
C.  Testicular enlargement 
D.  Prostate enlargement 
E.  Gynecomastia 
F.   Hepatotoxicity
A

A.  Anemia

C.  Testicular enlargement

25
Q

Adverse effects of androgens when used in male hypogonadism- physiological doses

A
  • *Testosterone itself has no “side effects” when used for male hypogonadism but some undesirable effects can be seen in certain situations.
  • Raising serum T from prepubertal to adult levels at any age could result in effects seen at puberty:
    1. acne,
    2. gynecomastia,
    3. aggressive sexual behavior
  • Presence of concomitant illnesses
    1. Stimulation of erythropoiesis could raise hematocrit above normal if predisposed (e.g., chronic pulmonary disease)
    2. Mild Na+ and fluid retention could exacerbate heart failure
26
Q

What is the target and MOA of keoconazole

A

Target: CYP17 (17α-hydroxylase) –> inhibition of testosterone synthesis

27
Q

What is the target and MOA of finesteride

A

5α-reductase –> inhibition of dihydrotestosterone (DHT) synthesis

28
Q

What is the target and MOA of flutamide

A

Target: Androgen receptor –> inhibition of androgen binding at its receptor

29
Q

Finasteride has efficacy in the prevention of male-pattern baldness by virtue of its ability to:
A.  Competitively antagonize androgen receptors
B.  Decrease the release of gonadotropins
C.  Increase the serum concentration of sex hormone- binding globulin (SHBG)
D.  Inhibit the synthesis of testosterone
E.  Reduce the production of dihydrotestosterone

A

E.  Reduce the production of dihydrotestosterone

30
Q

What is the target and MOA of GnRH antagonists?

A

GnRH Receptor–> competitive inhibition of GnRH receptors

31
Q

What is the target and MOA of spironolactone

A

Target: Androgen receptor –> inhibition of androgen binding at its receptor

*just like flutamide

32
Q

GnRH Analogs and adminstration

A

Leuprolide (Lupron)–

SC or IM depot implants duration of 1-3-4-6 months

33
Q

5-a-reductase inhibitors and adminstration

A
  1. Finesteride (Proscar)-
    (type II)-PO QD
  2. Dutasteride (Avodart)- (type I and II)-PO QD
34
Q

Androgen receptors antagonists and adminstratoin

A
  1. Bicalutamide (Casodex)-PO QD

2. Spironolactone (Aldactone) – PO BID

35
Q

Synthesis inhibitors

A

Ketoconazole (Nizoralz)

36
Q

Clinical uses of Anti-androgens

A
  1. Prostate Cancer
  2. BPH
  3. Androgenetic alopecia (male pattern baldness)
  4. Precocious puberty in boys
  5. Hirsutism of PCOS
37
Q

Describe the use of anti-androgens for prostate cancer

A
  1. GnRH agonists (Leuprolide/Lupron)
    • Androgen receptor blocker for disease flares (Bicalutamide
      * NO flare sx w/ antagonists
  3. GnRh antagonists (Degarelix) given monthly SC if advanced prostate CA
38
Q

Sx of disease flares with prostate CA

A
  1. worsen bone pain
  2. urinary tract sx

*no flare sx w/ antagonists

39
Q

Describe the tx and use of anti-androgens for BPH

A
  1. A1blockers (initial therapy
  2. 5-a-reductase inhibitors (oral- Finesteride or dutasteride)– for larger prostates or intolerance of A1blockers
  3. PDE-5 inhibitors if mild-mod sx + ED

**therapy must be continued to maintain efficacy

40
Q

Describe the use of anti-androgens for androgenetic alopecia (male pattern baldness)

A
  1. 5-a-reductase inhibitors (Finesteride-Propecia)
    * *use lower dose than for BPH (1mg vs 5mg)

**therapy must be continued to maintain efficacy

41
Q

Describe the use of anti-androgens for precocious puberty in boys

A
  1. GnRH agonist (Leuprolide-Lupron) continuous
42
Q 
A 60-year-old man is found to have a prostate lump and an elevated prostate-specific antigen. MRI suggests several enlarged lymph nodes in the lower abdomen, and an x-ray reveals 2 radiolucent lesions in the bony pelvis. This patient is likely to treated with which of the following
drugs? 
A.  Letrozole 
B.  Desogestrel 
C.  Bicalutamide
D.  Methyltestosterone 
E.  Oxandrolone 
F.   Leuprolide
A

C.  Bicalutamide

F.   Leuprolide

43
Q

Adverse Effects of Lueprolide (Lupron)

A
  1. HA
  2. nausea
  3. Injection site rxn
  4. hypogonadism* w/ prolonged tx
44
Q

Adverse Effects of Finesteride

A
  1. Decreased libido
  2. ejaculatory or ED (5-19%)
  3. Weakness 5%
45
Q

Adverse Effects of Dutasteride

A

similar to finasteride

  1. Decreased libido
  2. ejaculatory or ED (5-19%)
  3. Weakness 5%
46
Q

Adverse Effects of Bicalutamide

A
  1. Androgen deprivation effects**
    (2. decreased libido
  2. gynecomastia)
  3. Nausea 10%
  4. Transient abnormal LFTs
47
Q

Adverse Effects of Spironolactone

A
  1. Hyperkalemia

2. Gynecomastia*

48
Q

Benign prostatic hypertrophy (BPH) can be characterized by frequent urinary urgency, diminished urinary stream, urinary retention, and prostate-specific antigen (PSA) within normal limits for age. Which of the following best describes how an a1-adrenergic antagonist improves urinary flow?
A.  Decreases urine production
B.  Decreases the resistance of the urethral sphincter
C.  Promotes relaxation of the detrusor muscle
D.  Reduces formation of urethral nitric oxide
E.  Reduces formation of dihydrotestosterone

A

B.  Decreases the resistance of the urethral sphincter

Pharmacology (31 decks)

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