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1st Repro > Male Repro Pharmacology > Flashcards

Male Repro Pharmacology Flashcards

1
Q

What takes Testosterone to DHT?

A

5 alpha reductase

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2
Q

What takes testosterone to estradiol?

A

aromatase

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3
Q

There are two forms of 5-reductase:
Type I is found predominantly in:
Type II is found predominantly in :

A

Type I is found predominantly in nongenital skin, liver and bone,
Type II is found predominantly in urogenital tissue in men and genital skin in men and women

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4
Q

Dihydrotestosterone (DHT) and estradiol are active metabolites of testosterone. Their production can be inhibited by blocking

A

5 reductase and aromatase, respectively.

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5
Q

Why is some conversion of testosterone to estradiol important in men?

A

for the regulation of epiphyseal growth plate closure, also increases bone densitiy and libido

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6
Q

responsible for hair follicles and prostate hyperplasia

A

DHT

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7
Q

important for internal genitalia, skeletal muscle, erythropoiesis

A

testosterone

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8
Q

Androgens have varying actions in different tissues. Mechanisms to account for these differences are

A

the higher affinity with which DHT binds to and activates the androgen receptor compared to testosterone and the tissue-specific transcription factors

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9
Q

Testosterone has a high first pass effect thus many pharmaceutical androgen preparations are designed to

A

bypass hepatic catabolism.

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10
Q

How is Testesterone administered?

A

Transderm patch, gels and buccal tablet

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11
Q

Esterifying a fatty acid to the 17 hydroxyl group of testosterone creates a compound that is more lipophilic than testosterone itself. The ester hydrolyzes in vivo and results in serum testosterone concentrations that range from higher than normal in the first few days after the injection to low normal just before the next injection

A

Cypionate; testosterone ester

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12
Q

This ester is hydrolyzed resulting in slow testosterone release

A

Cypionate

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13
Q

We add a alkyl group to the 17 position to retard hepatic catabolism in this preparation of testosterone

A

Stanozolol

(causes hepatotoxicity!)

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14
Q

What is the main use of therapeutic androges, specifically testosterone

A

Male hypogonadism, testosterone deficiency is the principal indication for androgens.

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15
Q

What is the most important aspect of monitoring testosterone treatment for efficacy?

A

Measuring serum testosterone concentrations

You need to monitor for beneficial and deleterious effects.

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16
Q

What are adverse effects of the use of androgens?

A

acne, gynecomastia and more aggressive sexual behavior

***make sure to pay attention to growth hormone status of pt

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17
Q

What blood disorder are androgens used for?

A

Blood dyscrasias: use Danazol as adjunctive tx for hemolytic anema and idiopathic thrombocytopenic purpura refractory to first line agents

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18
Q

What specific agents do we use to tx Angioedema?

A

17-alkylated androgens; Stanozolol or danazol to stimulate hepatic synthesis of esterase inhibitor

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19
Q

Two examples of using androgens as therapy in women

A

Women w/ low serum testosterone

Using Danazol to tx endometriosis and fibrocystic breast disease

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20
Q

Big use of testosterone in men

A

male senescence; often see decreasing testosterone with age

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21
Q

What type of pts do we need to be careful of or inform increased risk when prescribing testosterone?

A

Those with pre-exsisting heart disease; see increase risk of myocardial infarct

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22
Q

Commonly used doping drugs

A

DHEA, stanozol, testosterone, androstendione

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23
Q

Adverse effects of Androgen Abuse

A

low endogenous testoerone and sperm production (low fertility) via suppressing gonadotropin secreation

smaller nuts

high dose–> erythrocytosis

Gynecomastia

24
Q

s are the only androgens that cause hepatotoxicity. These androgens are also more likely than to affect serum lipid concentrations by decreasing HLD and increasing LDL

A

17-Alkylated androgen

25
Q

What can happen in women and children that take androgens

A

virilization: increased facial adn body hirutism adn male pattern hair loss + acne

26
Q

What are some weird private part side effects of androgen abuse?

A

boys; phallic enlargement, girls have clit enlargment

27
Q

What happens to growth on androgen abuse?

A

stunts linear growth

**can see death dt cardiac disease

28
Q

GnRH analogs inhibit testosterone secretion by ________ After a transient stimulation of gonadotropin secretion, they down-regulate the GnRH receptor and inhibit gonadotropin secretion.

A

inhibiting LH secretion.

29
Q

is a GnRH analog. Continuous administration results in suppression of ovarian and testicular steroidogenesis due to decreased levels of LH and FSH with subsequent decrease in testosterone (male) and estrogen (female) levels.

A

Leuprolide

30
Q

Used for the treatment of advanced prostate cancer; management of endometriosis; central precocious puberty.

A

Leuprolide

31
Q

Side effects of Leuprolide?

A

side effects related to the suppression of gonadal steroidogenesis including hot flashes, headache, vaginal dry

32
Q

Androgen receptor antagonists have limited efficacy when used alone because they increase LH secretion which stimulates higher serum testosterone concentrations.

A

Flutamide

33
Q

hey are used in conjunction with a GnRH analog for treating metastatic prostate cancer.

A

Flutamide

34
Q

a nonsteroidal, competitive inhibitor of the androgen receptor, also has been used to treat hirsutism in women

A

Flutamide

35
Q

What are the side effects of Flutamide?

A

side effects including galactorrhea (9% to 42%), breast tenderness, gynecomastia, hot flashes, impotence, libido decreased, tumor flare.
It also has a black box warning of **hepatic failure. **

36
Q

5alpha-reductase antagonist, especially the type II; block the conversion of testosterone to dihydrotestosterone, especially in the male external genitalia.

A
37
Q

used to treat benign prostate hyperplasia and for the treatment of male pattern baldness

A

Finasteride

38
Q

Side effects of Finasteride

A

impotence and decreased libido.

39
Q

given as an intracavernous injection or urethral suppository for the treatment of impotence

A

Alprostadil

40
Q

dilates the cavernosal arteries, allowing blood flow to and entrapment in the lacunar spaces of the penis; an erection will last for 1-3 hours and is sufficient for sexual intercourse.

A

Alprostadil

41
Q

Side effects of alprostadil include

A

penile pain and urethral burning.

42
Q

They improve erectile function (penile engorgement) in patients with erectile dysfunction, PDE5 inhibitors

A

Sildenafil , Vardenafil , Tadalafil

43
Q

What is the mechanism of Alprostadil?

A

PGE1 causes dilation of cavernosal arteries; see erection will last for 1-3 hours

44
Q

What is the mechanism of PDE5 inhibitors and NO

A

Carpus cavernosum nerves adn vascular endothelial cells make NO during sexual arousal. NO stimulates formation of cyclic GMP (cGMP) which relaxes the corpus cavernosum smooth muscle causing engorgement and erection: cGMP is metabolized by PDE thus get accumulation over time

45
Q

Which PDE5 inhibitor lasts the longest?

A

Tadalafil; lastsup to 36 hours; causes headace, dyspepsia and backpain

46
Q

Sildenafil and Vardenafil are what type of drugs?

A

PDE5 inhibitors; last up to 5 hours; cause headache and flushing

47
Q

Common side effects of PDE5

A

headache, flushing, visual distrubance

48
Q

What pts should not take PDE5 inhibitors?

A

Those on nitrates; the combination with organic nitrate vasodilator can cause severe hypotension: use in caution with

49
Q

FDA approved to tx pulmonary hypertension

A

Sildenafil

50
Q

is responsible for male pattern balding, prostate hyperplasia plus other physiology.

A

DHT

51
Q

induces fusion of the epiphysis plus other physiological responses.

A

Estradiol

52
Q

17-alpha alkylated testosterones including_____, are not easily metabolized by the liver and are given orally. They are hepatotoxic.

A

stanozolol

53
Q

Used in conjunction with flutamide, an androgen receptor antagonist for treating metastatic prostate cance

A

leuprolide

54
Q

is a 5-alpha reductase inhibitor. It is used to treat benign prostate hyperplasia and male pattern baldness.

A

Finasteride

55
Q

selective inhibitors of cGMP specific phosphodiesterase 5

(PDE5). They enhance the effects of NO. Used to treat erectile dysfunction.

A

Sildenafil, Vardenafil and Tadalafi

1st Repro (16 decks)

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