Week 4: Reproductive Pharmacology: Antiandrogens Flashcards Preview

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Flashcards in Week 4: Reproductive Pharmacology: Antiandrogens Deck (25)
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1
Q

Flutamide MOA

A

Competitive antagonist of androgen receptors

2
Q

Flutamide clinical use

A
  • Prostate carcinoma
  • Off-label treatment of androgen excess
3
Q

Flutamide side effects

A
  • Hot flash
  • decreased libido
  • diarrhea
  • vomiting
4
Q

Flutamide contraindications

A
  • There have been reports of hospitalization and rarely death due to liver failure in patients taking Flutamide
  • Serum transaminase levels should be measured monthly for the first 4 months of therapy and periodically thereafter
  • Liver function tests also should be obtained at the first signs and symptoms suggestive of liver dysfunction
5
Q

Finasteride MOA

A

5α-reductase inhibitor (which catalyzes the conversion of testosterone to DHT)

6
Q

Finasteride clinical uses

A
  • Benign prostatic hyperplasia
  • treatment of male pattern hair loss in men only
  • off-label use for female hirsutism (idiopathic and related to polycystic ovary syndrome
7
Q

Finasteride side effects

A
  • Orthostatic hypotension
  • dizziness
  • decreased libido
  • fatigue
  • jaundice
8
Q

Finasteride contraindications

A
  • Use with caution in patients with hepatic impairment
  • Should be avoided by women who are pregnant, who may become pregnant, unless effective forms of contraception are being used due to Pregnancy Risk factor classification X
9
Q

Ketoconazole MOA

A
  • Inhibitor of androgen synthesis as a result of inhibiting CYP17A1 (also called 17α-hydroxylase/17; 20-lyase; C 17-20 desmolase)
10
Q

Ketoconazole clinical uses

A
  • Steroid-responsive metatstatic prostate cancer
11
Q

Ketoconazole side effects

A
  • Orthostatic hypotension
  • Dizziness
  • fatigue
  • jaundice
  • nausea
  • vomiting
12
Q

Ketoconazole contraindications

A

Rare:

  • causes reversible (although can be fatal) hepatotoxicity
  • can cause elevated plamsa concentrations of certain drugs and may prolong QT interval, sometimes resulting in life-threatening ventricular dysrhythmias
  • Multiple drug-interactions due to inhibition of CYP3A4, CYP1A2
  • CYP2C9
13
Q

Ketoconazole notes

A
  • An antifungal agent
  • Also inhibits cortisol synthesis due to CYP11B1 inhibition
14
Q

Ketoconazole notes

A
  • Antifungal agent
  • Also inhibits cortisol synthesis due to CYP11B1 inhibition
15
Q

Leuprolide MOA

A

Gonadotropin releasing hormone (GnRH) agonist

16
Q

Leuprolide clinical uses

A
  • advanced prostate cancer
  • endometriosis
  • uterine leiomyomata (fibroids)
  • central precocious puberty
  • off-label use in breast cancer
  • androgen excess
17
Q

Leuprolide side effects

A
  • Edema
  • headache
  • depression
  • hot flashes
  • allergic skin reaction
  • pain at injection site
18
Q

Leuprolide contraindications

A

For prostate cancer treatment

  • an initial rise in serum testosterone concentrations may cause “tumor flare” or worsening of symptoms during the first 2 weeks

In women:

  • similarly an initial increase in estradiol levels with a temporary worsening of symptoms may occur in women treated with leuprolide
19
Q

Leuprolide notes

A
  • Decreased bone density has been reported when used for more than 6 months
  • Use caution in patients with addition risk factors for bone loss
20
Q

Spironolactone MOA

A

Androgen receptor antagonist

21
Q

Spironolactone clinical uses

A

off-lable use for treatment of acne and hirsutism in females

22
Q

Spironolactone side effects

A
  • Side-effects at doses recommended for hirsutism and acne are minimal
  • Occasionally, polyuria, headaches, fatigue and gastritis may occur
  • some normal ovulatory women may experience menstrual irregularity
23
Q

Spironolactone contraindications

A

Spironolactone has the potential to induce hyperkalemia

24
Q

Spironolactone notes

A

Primarily used as a potassium-sparing diuretic

25
Q
A