PHARMACOLOGY

Question 1

what drug class is desogestrel, etonogestrel and levonorgestrel?

Answer 1

synthetic versions of progesterone

Question 2

describe desogestrel/etonogestrel/levonorgestrels mechanism of action?

Answer 2

they bind to the progesterone and oestrogen receptors present on the female reproductive tract, mammary gland, hypothalamus and pituitary. this slows the frequency of the release of GnRH from the hypothalamus and blunt the LH surge whilst also maintaining high levels of progesterone

Question 3

what are some indications of desogestrel/etonogestrel/levonorgestrel?

Answer 3

oral contraception

Question 4

what drug class is medroxyprogesterone acetate (MPA)?

Answer 4

a synthetic progestin

Question 5

what are the indications of medroxyprogesterone acetate (MPA)?

Answer 5

contraceptive, HRT and the treatment of endometriosis

Question 6

what is medroxyprogesterone acetates (MPA) mechanism of action?

Answer 6

it binds to the progesterone and oestrogen receptors present on the female reproductive tract, mammary gland, hypothalamus and pituitary. this slows the frequency of the release of GnRH from the hypothalamus and blunt the LH surge whilst also maintaining high levels of progesterone

Question 7

what drug class is norethisterone?

Answer 7

a synthetic progestational hormone

Question 8

what are the indications of norethisterone?

Answer 8

amenorrhea, functional uterine bleeding, endometriosis, contraception

Question 9

what is norethisterone’s mechanism of action?

Answer 9

it binds to the progesterone and oestrogen receptors present on the female reproductive tract, mammary gland, hypothalamus and pituitary. this slows the frequency of the release of GnRH from the hypothalamus and blunt the LH surge whilst also maintaining high levels of progesterone- its a more potent inhibitor of ovulation than progesterone

Question 10

what drug class is mefanamic acid?

Answer 10

an NSAID

Question 11

describe mefanamic acids mechanism of action?

Answer 11

it inhibits COX 1 and COX 2 enzymes which reduces the production of prostaglandin synthesis- this reduces pain, fever and inflammation

Question 12

what are the indications of mefanamic acid?

Answer 12

menstrual pain or any mild to moderate pain

Question 13

what drug class is tranexamic acid?

Answer 13

an antifibrinolytic drug

Question 14

what is tranexamic acids mechanism of action?

Answer 14

it competitively inhibits the activation of plasminogen to plasmin. this stops plasmin from degrading fibrin clots, fibrinogen and other plasma proteins. it also directly inhibits plasmin activity at higher doses

Question 15

what are the indications of tranexamic acid?

Answer 15

fibrinolysis, haemorrhage, menorrhagia (heavy periods)

Question 16

what drug class is oestradiol sulphate or oestradiol valerate?

Answer 16

these are salts of oestradiol and are oestrogen nuclear hormone receptor agonists

Question 17

where is oestradiol produced in humans?

Answer 17

cyclic ovaries and the placenta. also produced in adipose tissue in men and postmenopausal women

Question 18

describe the mechanism of action of either oestradiol sulphate/valerate?

Answer 18

it enters female organs, breasts, hypothalamus and pituitary and interacts with the oestradiol receptor. the receptor enters the nucleus and regulates gene transcription. this increases the hepatic synthesis of sex hormone-binding globulin, thyroid-binding globulin and suppresses FSH release from the anterior pituitary

Question 19

what are the indications of oestradiol sulphate and oestradiol valerate?

Answer 19

vasomotor symptoms
vulvar and vaginal atrophy due to menopause
hypoestrogenism due to hypogonadism, castration, or primary ovarian failure
prevention of postmenopausal osteoporosis.

Question 20

what drug class is oestriol?

Answer 20

a hydroxylated metabolite of oestradiol or estrone

Question 21

how is oestriol produced?

Answer 21

DHEA-S is produced by the adrenal cortex of the fetus which is converted to oestriol by the placenta. so only made during pregnancy

Question 22

what does is mean if unconjugated oestriol are abnormally low in a pregnant woman?

Answer 22

it may indicate a problem with the development of the child

Question 23

if oestriol binds to the oestrogen receptor, what’s its mechanism of action?

Answer 23

the same as oestradiol sulphate

Question 24

what are the indications of oestriol?

Answer 24

vaginal atrophy in postmenopausal women

can also be given for menopausal hot flushes

Question 25

what drug class is mestranol?

Answer 25

a synthetic derivative of oestradiol

Question 26

what are the indications of mestranol?

Answer 26

combined oral contraceptive pill

Question 27

what is mestranol mechanism of action?

Answer 27

it binds to the oestrogen receptor which moves into the cells nucleus and regulates gene transcription. this causes an increase in the hepatic synthesis of sex-hormone-binding globulin, thyroid-hormone binding globulin and suppresses FSH release from the anterior pituitary
the combination of oestrogen and progestin suppresses the hypothalamic-pituitary system, decreasing the secretion of GnRH