Reproductive Pharmacology Flashcards
Name the drug groups used in reproductive pharmacology and name some drugs in each group
Sex steroid hormones - oestradiol, progesterone, testosterone
Inhibitors and antagonists - RU486, finasteride
Mixed agonists/antagonists - SERMs and SPRMs
Name some actions and side effects of oestradiol treatment
Actions - mildly anabolic, Na and water retention, increased HDL, decreased LDL, decreased bone reabsorption, increased blood coagulability
Side effects - breast tenderness, nausea, vomiting, water retention, thromboembolism, impaired glucose tolerance, endometrial hyperplasia and cancer, ovarian hyperplasia and cancer, breast hyperplasia and cancer
Name some actions and side effects of progesterone treatment
Actions - secertory endometrium, anabolic, increased mineral bone density, fluid retention, mood changes, maintains pregnancy
Side effects - weight gain, fluid retention, acne, nausea, vomiting, irritability, depression, PMS, lack of concentration
Name some actions and side effects of testosterone
Testosterone stimulates male characterists, body hair, deep voice, anabolism and aggression
Side effects - adverse effects on lipid profiles, mainly HDL/LDL ratio -> risk of atherosclerosis
Name some drugs that increase the production of CYP450s that metabolise oral contraceptives
Antiepileptics, e.g. carbamezapine, phenytoin
Some antibiotics, e.g. rifampicin, rifabutin
Some natural products, e.g. St John’s Wort
Name some steroids that are used in hormone replacement therapy
Oestradiol, e.g. valerate, enanthate, micronized oestradiol
Premarin
Medroxyprogesterone acetate
Norethisterone
Levonorgestrel
Name some risks with HRT use
Risk of endometrial and ovarian cancer - unopposed oestrogen (ERT)
Risk of breast cancer - unopposed oestrogen (HRT)
Risk of VTE - HRT has adverse effects on thromboembolism profile
Risk of stroke - associated with oral oestrogen (not transdermal)
What is RU486 and what is it also know as. When is it used
RU486/Mifepristone is a progesterone and glucocorticoid receptor antagonist
Used in termination of pregnancy - myometrium becomes sensitive to prostaglandin-induced contractions
Name some SERMs and name a SPRM
SERMs: tamoxifen, raloxifene, clomiphene
SPRM: ulipristal acetate
Describe the action of tamoxifen
Tamoxifen is metabolised in liver to active metabolites which compete with oestrogen receptors
In breast it is an ER antagonist while in endometrium it is an ER agonist
Some women may not have any effects as there are different isoforms in different women that metabolise tamoxifen differently
Describe the action of clomiphene and where it is used
Clomiphene competes for ER binding and leads to ovulation through increased production of anterior pituitary hormones
Causes production of FSH to promote follicular development and cause ovulation
Used in treatment of anovulation
Describe the action of ulipristal acetate and when it is used
Ulipristal acetate is a selective progesterone receptor modulator
It is used for emergency contraception as it is thought to delay/inhibit ovulation
Used for treatment of uterine fibroids
