Sex Hormones Flashcards
How do sex hormones travel in the blood and why is this the case
All bound to SHBG or albumin, except progesterone
They are lipophilic so have a tendency to enter adipose and brain tissue
What increases SHBG production
Increased oestrogen
Where are sex hormones metabolised and what into?
In liver Into glucuronides (enter faeces) or sulphates (enter urine)
Describe enterohepatic recirculation of oestrogen
Oral oestrogens pass from gut to liver and are conjugated with glucuronide to enter bile
Colonic bacteria unconjugate oestrogen so it reenter the circulation (peripheral rather then hepatic portal)
How do oral ABx decrease oral oestrogen’s efficacy
Decrease gut flora so less unconjugation of oestrogen and more is excreted before it has entered the peripheral circulation
What are the SH receptors
ER alpha and beta
PR A and B
AR 1 and 2
Classification and examples of progestins
Progesterone derived: medroxyprogesterone acetate
Testosterone derived: levonorgestrel, desogestrel, norgestrel
Examples of mixed agonist/antagonist sex hormone drug groups
Uses?
SERM - hormone receptor positive breast cancer , raloxifene protects against osteoporosis
SPRM - <120 hour emergency contraception
SARM - PCOS
Side effects of oestrogen drugs
Breast tenderness VTE/MI/stroke Ovarian/endometrial/breast cancer Vomiting Fluid retention = bloating
Side effects of progestin drugs
Acne Irritability Weight gain Fluid retention Depression
Side effects of testerone drugs
Hirsuitism Acne Deeper voice Menstrual dysfunction Weight gain
Formulation of COCP
21 days of oestrogen and progestin
7 days of placebo or no tablets
How do oestrogen and progestin work together in a COCP
Oestrogen increases expression of progesterone receptor
Side effects of COCP
VTE/MI/stroke
Cholestatic jaundice and gall stones
Lower glucose tolerance
Mood swings
Examples of things that decrease COCP efficacy
CYP450 inducers: Carbamazepine Phenytoin Rifampicin St. John's wort
