PHARMACOLOGY Flashcards
what drug class is desogestrel, etonogestrel and levonorgestrel?
synthetic versions of progesterone
describe desogestrel/etonogestrel/levonorgestrels mechanism of action?
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
what are some indications of desogestrel/etonogestrel/levonorgestrel?
oral contraception
what drug class is medroxyprogesterone acetate (MPA)?
a synthetic progestin
what are the indications of medroxyprogesterone acetate (MPA)?
contraceptive, HRT and the treatment of endometriosis
what is medroxyprogesterone acetates (MPA) mechanism of action?
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
what drug class is norethisterone?
a synthetic progestational hormone
what are the indications of norethisterone?
amenorrhea, functional uterine bleeding, endometriosis, contraception
what is norethisterone’s mechanism of action?
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
what drug class is mefanamic acid?
an NSAID
describe mefanamic acids mechanism of action?
it inhibits COX 1 and COX 2 enzymes which reduces the production of prostaglandin synthesis- this reduces pain, fever and inflammation
what are the indications of mefanamic acid?
menstrual pain or any mild to moderate pain
what drug class is tranexamic acid?
an antifibrinolytic drug
what is tranexamic acids mechanism of action?
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
what are the indications of tranexamic acid?
fibrinolysis, haemorrhage, menorrhagia (heavy periods)
what drug class is oestradiol sulphate or oestradiol valerate?
these are salts of oestradiol and are oestrogen nuclear hormone receptor agonists
where is oestradiol produced in humans?
cyclic ovaries and the placenta. also produced in adipose tissue in men and postmenopausal women
describe the mechanism of action of either oestradiol sulphate/valerate?
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
what are the indications of oestradiol sulphate and oestradiol valerate?
vasomotor symptoms
vulvar and vaginal atrophy due to menopause
hypoestrogenism due to hypogonadism, castration, or primary ovarian failure
prevention of postmenopausal osteoporosis.
what drug class is oestriol?
a hydroxylated metabolite of oestradiol or estrone
how is oestriol produced?
DHEA-S is produced by the adrenal cortex of the fetus which is converted to oestriol by the placenta. so only made during pregnancy
what does is mean if unconjugated oestriol are abnormally low in a pregnant woman?
it may indicate a problem with the development of the child
if oestriol binds to the oestrogen receptor, what’s its mechanism of action?
the same as oestradiol sulphate
what are the indications of oestriol?
vaginal atrophy in postmenopausal women
can also be given for menopausal hot flushes
what drug class is mestranol?
a synthetic derivative of oestradiol
what are the indications of mestranol?
combined oral contraceptive pill
what is mestranol mechanism of action?
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
