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Pharm exam 4 > Androgens, Antiandrogens, Erectile Dysfxn > Flashcards

Androgens, Antiandrogens, Erectile Dysfxn Flashcards

1
Q

explain hypothalamic-pituitary-gonadal axis

A

Hypothalamus –> GnRH

GnRH –> Pituitary gonadotropes –> LH

LH –> Leydig cell –> testosterone

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2
Q

what do leydig cells express that converts androstenedione to testosterone

A

17B-hydroxysteroid dehydrogenase (17B-HSD)

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3
Q

___-bound testosterone is considered bioavailable

A

albumin

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4
Q

what converts testosterone to DHT

A

5alpha reductase

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5
Q

Anabolic effects of androgen:

Increases 1 synthesis and inhibits 2 breakdown

Stimulates 3 rate

Reduces bone 4 and enhances bone 5.

At puberty 6 facilitates closure of epiphyseal growth plate

Increases production of 7

A
  1. protein
  2. protein
  3. resting metabolic
  4. reabsorption
  5. formation
  6. estradiol
  7. erythropoietin
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6
Q

Primary or secondary androgen deficiency:

  1. hypergonadotropic hypogonadism
  2. hypogonadotropic hypogonadism
A
  1. primary

2. secondary

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7
Q

what are the non-steroidal anti-androgens?

A

flutamide and bicalutamides

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8
Q

MOA of nonsteroidal anti-androgens (flutamide and bicalutamides)

A

competitive antagonists at androgen receptor

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9
Q

what does flutamide and bicalutamides tx

A

tx prostate cancer

administered prior to GnRH analog tx to prevent testosterone surg

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10
Q

what anti-androgen is an AR antagonist

A

Enzalutamide

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11
Q

Enzalutamides MOA

A

*completely inhibits androgen binding to AR

inhibits nuclear translocation of AR

blocks DNA binding

blocks coactivator recruitment

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12
Q

what anti-androgens are GnRH receptor agonists?

what is the MOA

A

Leuprolide and goserelin

  • increase LH and testosterone production
  • leads to desensitization and downregulation of GnRH receptors on pituiary gonadotropes
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13
Q

what should you administer with Leuprolide and goserelin to decrease surge of LH and testosterone

A

AR antagonists (fluatmide, bicalutamide)

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14
Q

what does Leuprolide and goserelin tx

A

prostate cancer

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15
Q

what drug is a GnRH receptor antagonist

A

Degarelix

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16
Q

How does degarelix compare to leuprolide and goserlin tx?

A
  • Faster onset
  • No LH/testosterone surge
  • Reduce LH/FSH production and release
  • Decrease testosterone production
17
Q

which drug is an androgen biosynthetic inhibitor?

MOA?

A

Abiraterone

inhibits 17alpha hydroxylase and 17,20 lyase –> increase in aldosterone production –> can cause HTN, hypokalemia, fluid retention

18
Q

what are the 5a-reductase inhibitors

MOA?

A

Finasteride and Dutasteride (steroid like)

inhibit DHT activity and reduce levels

19
Q

what does abiraterone treat?

A

metastatic prostate cancer

20
Q

what does dutasteride treat

A

BPH

androgenic alopecia

21
Q

what are the erectile dysfunction drugs?

A

PDE5 inhibitors

  • Sildenfail
  • Vardenafil
  • Tadalafil
  • Avanafil
22
Q

of the PDE5 inhibitors for ED:

  1. longest T1/2
  2. fastest onset
  3. treat pulmonary HTN
  4. what else can they tx?
A
  1. Tadalafil
  2. Avanafil
  3. Sildenafil and Tadalafil
  4. BPH
23
Q

Testosterone ester:

1 conjugated to testosterone, increases 2 of molecule, dissolved in oil and given 3, slow release and catabolism, 4 duration

A
  1. FA
  2. lipophilicity
  3. IM
  4. long
24
Q

17a-alkylated derivatives (steroid like)

significantly 1 liver catabolism,
Administered 2,

3 toxicity and 4 cancer can occur (higher risk than ester or testosterone)

A
  1. slower
  2. orally
  3. Liver
  4. Hepatic
25
Q

SE of androgen preps

A
  • Musculoskeletal: premature epiphyseal closure, increase muscle and tendon injuries
  • Hepatic dysfunction (17-alkylated testosterone derivatives): cholestatic jaundice, peliosis, carcinoma
  • Edema, fluid retention (HTN) - renal dysfunction
  • Polycythemia
  • Mental disturbance: mood swings, aggression, depression, psychosis
26
Q

SE of antiandrogens: flutamide and bicalutamide

A

mild gynecomastia,

mild reversible liver toxicity

27
Q

SE of GnRH agonists: Leuprolide, goserelin

A
  • Sexual dysfxn
  • Bone mineral density loss
  • Anemia
  • Fatigue
  • Initial surge in testosterone levels that can cause growth of prostate cancer
28
Q

SE of abiraterone (androgen biosynthetic inhibitor)

A
  • Adrenal insufficiency with concurrent infection or stress
  • Hepatotoxicity
  • HTN
  • Hypokalemia
  • Fluid retention
29
Q

SE of 5a-reductase inhibitors (Finasteride and Dutasteride)

A
  • Reduced DHT levels in male fetus can lead to abnoramlities in the external genitalia: contraindicated in pregnancy
  • Impotence and gynecomastic
  • Can lower PSA levels - possible false negatives with prostate cancer screening (PSA values should be doubled for comparison with normal ranges)
30
Q

Side effects of PDE5 inhibitors (Sildenafil, Vardenafil, Tadalafil, Avanafil)

A
  • Dyspepsia: inhibition of esophageal SM can reduce motility and worsen GERD
  • Headache, flushing, nasal congestion
  • Combination with nitrates/nitrites can cause dangerously low BP
  • Serious cardiac events (rare)
  • Priapism
  • Rare: sudden vision loss

Pharm exam 4 (15 decks)

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