Reproductive and post-reproductive health Flashcards
What are the different drug groups used in reproductive health?
Sex steroid hormones
Inhibitors and antagonists
Mixed agonist/antagonist
Give examples of sex steroid hormones
Oestrogens, progestogens and androgens
Give examples of inhibitors and antagonsists
RU486, finasteride
Give examples of mixed agonists/antagonists
Selective oesterogen receptor modulators
Selective progesterone receptor modulators
What are sex steroids synthesised from?
Cholestrol
What is the difference between Estrone and Estradiol?
Estone is more prevalent in post menopausal women whereas Estradiol is the more potent oestrogen present in reproductive life for follicular maturation
What are the receptors for steroid hormones? How do they exert their effects?
Classic nuclear receptors
Exert effects via gene transcription, as a transcription factor
What additional type of receptor does it have?
Membrane receptor for oestrogen
What are the major actions/effects of estradiol?
Stimulates growth of the endometrium and breast Mild anabolic Na and H20 retention Raises HDL and lowers LDL Decreases bone reposition Impairs glucose tolerance Increased blood coagulability Stimulates production of progesterone
What are the major actions/effects of progesterone?
Stimulates growth of the endometrium and breast Anabolic Increases bone mineral density Fluid retention Mood changes Maintains pregnancy Inhibits production of oestrogen
What are the major effects of testosterone?
Male characteristics Body hair Acne Deep voice Anabolism Aggression
What are the side effects of oestrogen?
Breast tenderness Nausea/vomiting Water retention Increased blood coagulability Thromboembolism Impaired glucose tolerance Emdometrial hyperplasia and cancer Breast hyperplasia and cancer Ovarian metaplasia
What are the side effects of progesterone?
Weight gain Fluid retention Anabolic Acne Nausea/vomiting Irritability, depression, PMS Lack of concentration
What are the side effects of testosterone?
Adverse effects of lipid profiles especially the HDL-c/LDL-c ratio
Increased risk of atherosclerotic disease in males
Pharmacokinetics of oestrogen: What does it’s absorbability mean for administration?
Natural and synthetic oestrogen are well absorbed in the GI tract so can be given in oral root
OR via patches in skin because readily absorbed from skin and mucus membranes
Where is oestrogen metabolised and by what?
Liver by CYP450
How is oestrogen excreted?
In the urine as glucoronides and sulphates
Pharmacokinetics of progesterone: How is it transported in blood and where is it stored?
Injected progesterone if bound to albumin with some stored in adipose tissue
Where is progesterone metabolised and by what?
Liver by CYP450