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Pharm > Androgens > Flashcards

Androgens Flashcards

1
Q

What is the indication for testosterone?

A

Male hypogonadism

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2
Q

What are the adverse effects of testosterone?

A 
Acne
Increased risk prostate cancer
Increased risk BPH
Worsening of sleep apnea
Erythrocytosis -> increased risk VTE
Increased risk CVD (vHDL, ^LDL)
Hepatic dysfunction (oral derivatives)
Suppression of spermatogenesis
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3
Q

What are the contraindications for testosterone?

A

Prostate cancer
High level PSA
Untreated sleep apnea

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4
Q

Name the 4 androgen receptor antagonists that we have to know.

A

Flutamide
Bicalutamide
Nilutamide
Enzalutamide (2nd gen)

“Lutamides antagonize androgens”

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5
Q

What is the MoA for androgen receptor antagonists?

For testosterone?

A

ARA: Directly inhibits action of testosterone and DHT at the AR

T: Direct agonism of AR to restore T to nl level.

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6
Q

What are the indications for flutamide, bicalutamide, nilutamide, and enzalutamide? (androgen-receptor antagonists)
What are they used in combination w/?

Which of them can women use, and as tx for what?

A

Tx of advanced prostate cancer.
Used in combination with androgen deprivation therapy (e.g. GnRH agonist/antagonist)

Flutamide also used for tx of hyperandrogenism in women (King Fish’s sister plays the flute)

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7
Q

What are the adverse effects of androgen receptor antagonists?

What about rare SE’s?

A

Men- typical effects of androgen deprivation. (e.g. sexual dysfunction, gynecomastia, vasomotor responses)

Rare side effects:
1st Gen- Hepatotoxicity
2nd Gen (Enzalutamide) - increased seizure risk

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8
Q

Which of the androgen-receptor antagonists is most potent?

A

Enzalutamide (2nd gen)

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9
Q

Recall: list the GnRH agonists.

What is their MoA?

A

Leuprolide, Goserlin, Buserelin, Triptorelin, Naferelin (Lewd Pro [Jeremy] Lin agonizes the pussy)

Sustained activation of GnRH receptor inhibits release of gonadotropins (even though they’re agonists)

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10
Q

What are Leuprolide, Goserlin, Buserelin, Triptorelin, Naferelin (GnRH agonists) indicated for in males?

A

Advanced prostate cancer

Recall, in females: Controlled ovarian stimulation.
Palliative therapy of hormone-dependent tumors.
Suppression of inappropriate growth of hormone-dependent tissues (e.g. endometriosis & fibroids).
Tx of precocious puberty.
Suppression of endogenous puberty in gender dysmorphic adolescents.

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11
Q

Which GnRH antagonist is used in the tx of advanced prostate cancer?

Recall: what is the MoA?

A

Degarelix

Antagonize GnRH receptors, reduce gonadotropin release.

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12
Q

What are the adverse effects of both GnRH agonists and antagonists in males?

A 
Sexual dysfunction
Osteoporosis & bone fractures
Vasomotor responses (hot flashes)
Loss of lean body mass & increased fat mass
Fatigue
Anemia (>90%)
Gynecomastia
Decreased penis and testicular size
Emotional & cognitive changes

(basically makes you more like a woman)

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13
Q

Recall: what are the adverse effects of GnRH agonists and antagonists in females?

A 
Side effects associated with gonadal hormone deprivation, e.g.:
Hot flashes
Decreased bone density
Vaginal dryness/atrophy
Erectile dysfunction.
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14
Q

What type of drug is abiraterone?

What is its MoA?

Therefore, what are its adverse effects?

A

Androgen synthesis inhibitor

Inhibition of CYP17A1. Inhibits synthesis of testosterone (also affects cortisol, but not aldosterone)

Adrenocorticol insufficiency
Mineralocorticoid excess

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15
Q

Indications for abiraterone?

A

Hormone-resistant prostate cancer not responding to androgen deprivation therapy

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16
Q

What is the MoA for spironolactone?

A

Antagonist/weak partial agonist of androgen receptor

Also mineralocorticoid receptor antagonist- used as diuretic to treat HF

17
Q

What are indications for spironolactone?

A

Treatment of women with acne, hirsutism, or androgenic alopecia

18
Q

What are the adverse affects a/w spironolactone?

A

Menstrual irregularities
Breast tenderness
Orthostatic hypertension

19
Q

Who is contraindicated in the use of spironolactone?

A

Should not be used in men w/prostate cancer

20
Q

Name the 2 drugs that are 5alpha-reductase inhibitors.

What does this enzyme normally convert ?(inhibited by these drugs)

A

Finasteride
Dutasteride

Inhibits peripheral conversion of testosterone to DHT

21
Q

What are the indications for 5alpha-reductase inhibitors?

A

BPH
Male pattern baldness
Female hirsutism

(those w/hair loss use sterides)

22
Q

What is the adverse effect a/w dutasteride and finasteride?

A

Male sexual dysfunction

23
Q

When are 5alpha-reductase inhibitors contraindicated?

A

Pregnancy

Pharm (32 decks)

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