021015 male pharm

Question 1

testosterone has a high first pass effect: true or false

Answer 1

true

most preps are designed to bypass hepatic catabolism (transdermal patch, gels)

Question 2

testosterone esters (cypionate)

Answer 2

has esterified fatty acid-lipophilic analog of testosterone

the ester is hydrolyzed resulting in slow testosterone release. lasts 1 week, IM injection

Question 3

17 alpha alklyated compounds

Answer 3

stanozolol (oral)
has alkyl group added to testosterone to retard hepatic catabolism

causes hepatotoxicity

Question 4

uses of androgens

Answer 4

MALE HYPOGONADISM (due to testosterone deficiency)

male senescence
athletic performance abuse
women w low serum testosterone (to enhance libido and sk musc to fat ratio)
etc

Question 5

adverse effects of androgens

Answer 5

similar to those in puberty-acne, gynecomastia, more aggressive sexual behavior

Question 6

what should be considered in using androgens?

Answer 6

height and growth hormone status, b/c you don’t want to limit long bone growth via estrogen

Question 7

risks of testosterone therapy

Answer 7

in men with pre-existing heart disease-risk of cardiovascular events

Question 8

how does testosterone therapy impact spermatogenesis?

Answer 8

it decreases sperm count

Question 9

testosterone precursors

Answer 9

androstenedione
dehydroepiandrosterone (DHEA)

weak androgens
no longer manufactured

Question 10

adverse effects of androgen abuse

Answer 10

decreased endogneous testosterone and sperm production

decreased testicular size (after many years)

high doses-erythryocytosis

gynecomastia (testos is converted to estrogen)

17 alkylated androgens-HEPATOTOXIC

in women and children-virilization (increased hirsutism, male pattern hair loss, acne)

phallic enlargement, clitoral enlargement

stunting of linear growth (in children)

cardiac dis

Question 11

antiandrogens and androgen antagnoists

Answer 11

leuprolide
finasteride
flutamide

Question 12

inhibitors of androgen synthesis

Answer 12

GnRH analog-leuprolide (continuous GnRH)

Question 13

5alpha-reductase inhibitor

Answer 13

finasteride

Question 14

androgen receptor antagonist

Answer 14

flutamide (competitive inhibitor of androgen receptor)

Question 15

uses of leuprolide

Answer 15

tx of advanced prostate cancer
endometriosis
central precocious puberty

Question 16

androgen receptor antagonists’ efficacy

Answer 16

alone, have limited efficacy because they increase LH secretion and endogenous androgen production. they are used in CONJUNCTION with GnRH analog

Question 17

use of flutamide

Answer 17

metastatic prostate cancer

hirsutism in women

Question 18

use of finasteride

Answer 18

BPH

male pattern baldness

Question 19

tx for erectile dysfxn

Answer 19

alprostadil (PGE1)

sildenafil, vardenafil, tadalafil (PDE5 inhibitors)

Question 20

MOA of alprostadil

Answer 20

dilation of cavernosal arteries

Question 21

PDE5 inhibitors-MOA

Answer 21

cGMP is normally metabolized by PDE, so inhibition of cyclic GMP specific PDE5 causes accumulation of cGMP

cGMP relaxes the corpus cavernosum smooth muscle resulting in engorgement and erection

Question 22

which PDE5 inhibitor can be active for up to 36 hrs

Answer 22

tadalafil

Question 23

what are PDE5 inhibitors contraindicated in?

Answer 23

in pts taking nitrates (combo can cause extreme hypotension)