Reproductive Drugs Flashcards
how are most sex hormones made ?
steroid hormones- cholesterol
what is the steps of synthesis of cholesterol ?
cholesterol –> progesterone –> testosterone –> estradiol
how do steroid hormones work ?
nuclear receptors through gene transcription
What steroid hormone has a plasma membrane receptor ?
Oestrogen
what is the effect of oestrodiol ?
stimulate growth of endometrium and breast, releases progesterone receptor
what is the effect of progesterone?
stimulate growth of endometrium and breast, maintains pregnancy . inhibits oestrogen receptor
secretions of endometrium , mood change , increase bone density
what is the effect of oestrogen ?
Anabolic sodium and water retention raises HDL, lowers LDL decrease bone resorption - maintains high density reduce bone resorption increase coagulation
what are side effects of oestrogen ?
breast tenderness nausea / vomiting water retention thromboembolism decreased glucose tolerance endometrial/ breast hyperplasia and cancer ovarian metaplasia
what are the side effects of progesterone ?
weight gain , fluid retention, Acne, nausea/ vomiting, depression , PMS and lack of concentration
what are the effects of testosterone ?
anabolic, acne , voice changes , aggression , increased HDL/LDL ratio
State 3 facts about the pharmokinetics of oestrogen
A- absorbed in GI tract and mucous membranes and Skin
D
M- Liver
E- urine = glucuronides and sulfates
State 3 facts about the pharmokinetics of progesterone ?
A- Injected
D- Bound to albumin and adipose
M- Liver
E- urine via conjugated glucuronic acid
what is a risk factors of COCP?
Thromboembolism
Name some CYP450 inducers
carbamazepine , phenytoin
st john’s wort
rifampicin
what does soya do to oestrogen ?
increase absorption , reduce storage in adipose, T1/2 reduced to 7 hours from 15
when should you give HRT?
Menopause symptoms - hot flushes, Dyspareunia
osteoporosis , genital atrophy
not for Heart diease
name 2 oestradiol drugs
Valerate , enanthate and premarin
what are the route of administration for HRT?
Oral, transdermal, transvaginal, implant and nasal
what is the main side effect of unopposed oestrogen therapy ?
Risk of endometrial/ ovarian cancers
- highly proliferative
what is the main side effect of opposed oestrogen therapy ?
increases risk of breast cancer
why does oral HRT lead to thromboemoblsim ?
increased resistance to protein C (anticoagulant)
increased thrombin , decreased anti thrombin 3 , decreased protein s , decreased factor 7 and decreased TF inhibitor
what is the CV effect of HRT?
Increase HDL , reduce oxLDL and TAG and Lipop A
does not happen if patient is obese
What Administration of HRT leads to increased risk of stroke ?
Oral
what is Mifepristone ?
progesterone and glucocorticoid receptor antagonist
what is the uses for Mifepristone ?
sensitising the myometrium to prostaglandin induced contraction
termination of pregnancy
what is a SERM ?
Selective estrogen receptor modulator
agonists and antagonists mix
what is Clomiphene treated for ? how does it work?
anovulation
competes binding with oestrogen
leads to increased FSH,LH Production = ovulation
what is tamoxifen ?
pro drug SERM metabolised in liver
what does tamoxifen do at each site ?
active metabolites –>
Endometrium = ER agonist
Breast= ER antagonist = cells arrest in cell cycle
what is Ulipristal acetate and what is it used for ?
Selective progesterone receptor modulator
emergency contraception - MOA is delay of ovulation
used for fibroids as well .
