sex drugs Flashcards
sex steroid synthesis steps
cholesterol, progesterone, testosterone, estradiol
steroid hormone receptors
nuclear receptors, effect: gene transcription
estrogen has membrane receptor as well
oestradiol effect
Stimulates growth of the endometrium and breast;
stimulates production of PR.
Mild anabolic • Sodium and water retention
• Raises HDL, lowers LDL
• Decrease bone resorption
• Impair glucose tolerance
• Increase blood coagulability
progesterone effect
Stimulates growth of the secretory endometrium and breast;
maintains pregnancy;
inhibits production of ER.
• Anabolic • Increases bone mineral density • Fluid retention • Mood changes
testosterone effect:
Stimulates male characteristics;increased body hair; deep voice;
anabolism;
aggression.
Acne
Metabolic - adverse effects on lipid profiles particularly the HDL-C/LDL-C ratio hence increased risk of atherosclerotic disease in males
oestrogen side effects
- Breast tenderness • Nausea, vomiting • Water retention
- Increased blood coagulability • Thromboembolism
- Impaired glucose tolerance
- Endometrial hyperplasia & cancer • Ovarian metaplasia & cancer • Breast hyperplasia & cancer
progesterone side effects
- Weight gain • Fluid retention
- Anabolic
- Acne
- Nausea/vomiting
- Irritability Depression, PMS • Lack of concentration
oestrogen pharmacokinetics
absorbed well in gi tract,from skin and mucous membranes,
metabolized in liver,
exertion in urine as glucoronides and sulfates
progesterone pharmacokinetics
bound to albumin,
stored in adipose tissue,
metabolized in liver,
excreted in urine conjugated to glucoronic acid
COCP
thromboembolism small risk
but increases with smoking, long-term use, obesity and hypertension
^ COCP and POP
metabolised in the liver by CYP 450 enzymes
anti-epileptics such as carbamazepine or phenytoin; –
some antibiotics such as rifampicin and rifabutin and –
St John’s Wort
• because they all increase the production of hepatic CYP450
Soya protein products enhance oestrogen absorption, reducinng half-life
HRT oestradiol examples
Oestradiol
Medroxyprogesterone acetate
Unopposed oestrogen risk
developing endometrial and ovarian cancers
Opposed oestrogen risk
developing breast cancer
Bisphosphonates mechanism
for osteoporosis
reduce bone turnover by controlling osteoclast activity,
can’t attach to bone due to membrane dysfunction