PHARMACOLOGY

Question 1

What drug class is ethinylestradiol?

Answer 1

a synthetic derivative of oestradiol (an oestrogen hormone)

Question 2

describe the mechanism of ethinylestradiol and oestradiol?

Answer 2

they interact with the oestrogen receptor which then enters the nucleus and regulates gene transcription. this leads to an increase in hepatic synthesis of sex hormone binding globulin, thyroid-binding globulin and suppresses FSH release from anterior pituitary.

Question 3

where can we find oestrogen receptors?

Answer 3

female organs
breasts
hypothalamus
pituitary gland

Question 4

what has too much oestradiol been linked to?

Answer 4

acne
constipation
loss of sex drive
depression

Question 5

what has too little oestradiol been linked to?

Answer 5

retards bone growth and development

Question 6

in males, what are proper oestradiol levels important for?

Answer 6

bone maintenance, nitric oxide production and brain function

Question 7

what drug class is testosterone?

Answer 7

a steroid sex hormone

Question 8

describe the mechanism of action of testosterone?

Answer 8

free testosterone is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor or be reduced to DHT by 5 alpha-reductase. DHT undergoes a structural change and moves into the cells nucleus and binds to hormone response elements which influences transcriptional activity of certain genes, producing androgen effects.

Question 9

what drug class is nandrolone?

Answer 9

an anabolic steroid

Question 10

what is the mechanism of action of nandrolone?

Answer 10

it binds to androgen receptors but, unlike testosterone, it is broken down by 5 alpha-reductase into dihydronandrolone (instead of DHT like testosterone is)

Question 11

what are the effects of nandrolone?

Answer 11

increases production and urinary excretion of erythropoietin. it may also have direct action on bone marrow

Question 12

what drug class is sildanefil (aka viagra)?

Answer 12

a PDE5 inhibitor

Question 13

what is sildanefil’s mechanism of action?

Answer 13

inhibition of PDE5 (an enzyme that promotes breakdown of cGMP) in the corpus cavernosum located around the penis causes smooth muscle relaxation and increased blood flow into the corpus cavernosum= an erection

Question 14

what drug class is alprostadil?

Answer 14

a synthetic version of prostaglandin PGE-1

Question 15

describe alprostadils mechanism of action?

Answer 15

it binds to EP1 and EP2 receptors, leading to either an increase in cAMP and activation of protein kinase A, or activation of phospholipase C. this acts to locally relax the trabecular smooth muscle of the copora cavernosa and the cavernosal arteries= erection

Question 16

what is an indication of aprostadil?

Answer 16

erectile dysfunction

Question 17

what drug class is bicalutamide?

Answer 17

an oral non-steroidal anti-androgen

Question 18

what is bicalutamide mechanism of action?

Answer 18

binds to androgen receptor which prevents testosterone from reaching cancer cells which aids the slowing of growth of the cancer

Question 19

what are the indications of bicalutamide?

Answer 19

prostate cancer

Question 20

what drug class is finasteride?

Answer 20

an orally active testosterone 5-alpha reductase inhibitor

Question 21

desribe finasterides mechanism of action?

Answer 21

it inhibits type 2 5-alpha reductase so testosterone cant be converted to DHT. this means we get a significant decrease in serum and tissue DHT concentrations and an increase in serum testosterone concentrations. decreases in DHT leads to a reduction in prostate size.

Question 22

what are the indications of finasteride?

Answer 22

benign prostatic hyperplasia

Question 23

what drug class is goserelin?

Answer 23

a decapeptide analogue of luteinizing hormone-releasing hormone (a superagonist)

Question 24

describe goserelin mechanism of action?

Answer 24

it stimulates the release of LH which causes increases in serum androgen and oestradiol initially. but chronic administration can cause down-regulation of LHRH receptors, inhibiting LH secretions this decreases testicular production of androgen in men and can inhibit the growth of androgen-dependant prostate cancer.

Question 25

what are the indications of goserelin?

Answer 25

androgen-dependant prostate cancer