Drugs affecting reproductive function Flashcards
(30 cards)
what’s the most potent oestrogen
oestradiol (what HRT and the pill gives you)
what do effects of oestrogen depend on
stage of sexual maturity
give oestrogen to primary hypogondism patient
stimulates secondary characteristics and accelerate growth
give oestrogen to adult with amenorrhoea:
induce artifical menstrual cycle
name some therapeutic uses of oestrogens
- replacement therapy in primary ovarian failure (Turner’s) to promote sexual maturation
- replacement therapy for menopausal symptoms eg. flush, vaginal dryness and osteoporosis
- in contraception, in combo with progesterones
- prostate and breast cancer (rare)
2 natural
2 synthetic oestrogens
natural: oestradiol, estriol
synthetic: mestranol, ethinylestradiol, diethylstilbestrol
active state of oestrogen is what
unbound to albumin or sex-hormone binding globulin
unwanted effects of oestrogen
breast tenderness nausea vomiting anorexia retention of salt and water increased risk of TBE
what are SERMs
anti-oestrogens (selective oestrogen receptor modulators)
competitive antagonists or partial agonists
eg.
tamoxifen
ramloxifene (agonist in bone. antioestrogenic properties in uterus and breast)
clomiphene: treat infertility when too much neg feedback acting on hypothalamis. increases GnRH. facilitates ovulation.
interaction between oestrogen and progesterone on their Rs
oestrogen stimulates synthesis of PR
progesterone inhibits synthesis of oestrogen Rs
why do we not use progesterone?
what do we use instead?
too rapid clearance
synthetic derivatives: progestins
eg. medroxyprogesterone and hydroprogesterone
therapeutic uses of progestogens
- in oral COCP alone or in combo with oestrogen
- progesterone only injection or implantable contraception
- combined with oestrogen for replacement therapy in women WITH INTACT UTERUS to prevent: endometrial cancer, carcinoma, endometriosis
what’s the antiprogesterone?
when do we use it?
mifepristone
with prostaglandin analogues is chemical termination of pregnancy up to 9 weeks
oestrogen content of pill
20-50ug
mode of action of progestin only pill
primarily on cervical mucous which made inhospitable to soerm
also probs hinders implantation through effect on endometrium and motility and secretions of the fallopian tubes.
when might we use progestin only pill?
if oestrogen-containing is contraindicated
women whose blood pressure rises with combined
post-coital contraception
oral administration of levonogestrel
effective if taken within 72 hours and repeated 12 hours later
long acting progesterone only contraception
medroxyprogesterone acetate can be given IM as a contraceptive. 12 weeks!
Levonorgestrel implanted subcutaneously. capsule release progesterone slowly over 5 years. BAR
main androgen
testosterone
what makes testosterone
leydig cells in testes
adrenals and ovaries
MOA of intramuscular depot injections of testosterone
via nuclear receptors and control of gene expression
antiandrogens examples
and used for what
eg. flutamide, cyproterone
as part of treatment of prostatic cancer
dihydrotestosterone DHT synthesis inhibitors
used for what
eg. finasteride
used in benign hypertrophy
example of anabolic steroid
effects
nandrolone
increased protein synthesis and muscle development
therapy of aplastic anaemia
