Sex Hormones And HRT Flashcards
What is the most potent form of oestrogen?
Oestradiol
What hormone is inv. in androstenedione to oestrone conversion?
Also in testosterone to oestradiol?
Aromatase
2 clinical uses of HRT
Primary ovarian failure (eg turners)
Menopause symptom control (flushes)
Oestrogen metabolic actions
Mild anabolic Na+ retention (water retention) Increased HDLs, Impair glucose tolerance Increased blood coagulability Decreased bone resorption
Side effects of giving oestrogens
N&V
Water retention
Increased thromboembolic risk
Endometrial hyperplasia risk
Actions of progesterone
Secretory endometrium, Thicken/acidify cervical mucus Anabolic Increased basal temp Increased fluid retention (Mood changes)
Side effects of progesterone
Weight gain, fluid retention Acne, PMS, depression Reduced libido Reduced concentration Breakthrough bleeding
Clinical uses of progesterone
W oestrogen in COCP
As POP or implant
In HRT (to prevent endometrial hyperplasia)
Endometriosis
HIGH dose - in levonorgestrel (emergency contraception)
What are the sex steroids derived from? Where do they act?
Cholesterol. Nuclear receptors
COCP important pharmacokinetics
CYP450 metabolism
Common COCP ADRs
Weight gain, acne, irritability, headaches
Serious ADRs of COCP
VTE, stroke, MI, hypertension
Disadvantages of POP compared to COCP
No anti ovulatory (less effective) and poor cycle control
So irregular bleeding common
Emergency contraception: up to 72 hours
Levonorgestrel
A high dose of progesterone
Emergency contraception: up to 120 hours (5 days)
Ullipristal acetate (prog. Receptor modulator)
Risks of HRT
High risk endometrial/ovarian cancer w unopposed oestrogen
Increases lipids and thrombosis risk increased (MI, stroke, IHD)
What can anti oestrogens can be used for clinically? Give an eg drug
Fertility treatment (eg clomiphene) Blocks oestrogen receptors so less negative feedback (as compete w body's own oestrogen) makes the body think it need to produce lots of oestrogen so high GnRH and ovary stimulation etc. ovulation induction
Tamoxifen. Indication, MoA and ADR
Oestrogen receptor positive breast cancer
Competes w oestrogen for nuclear receptor then blocks transcription of oestrogen responsive genes
Hot flushes (as less oestrogen effects make you feel menopausey)
Anti progesterones can be used in what clinical scenario
Give the example drug
Induces labour, can be used in Medical termination of pregnancy
Mife pristone
Give an eg Anti androgen
Cyproterone
Anti androgens block testosterone/progesterone
Give 3 clinical uses
Precocious puberty in males
Hirsuitism in females
Adjuvant therapy in prostate cancer
Name a SERM
Raloxifene
What can you use SERMs for?
Allow you to increase oestrogen effects in protective scenarios eg on bone in osteoporosis treatment, without inducing unwanted effects eg proliferator of endometrium leading to cancer risk
