HRT Flashcards
Why is Hormone Replacement Therapy used?
To combat symptoms such as
- Hot flushes/sweats
- Vaginal dryness/dyspareunia
- Osteoporosis
What the types of steroids used in HRT?
- Oestradiol
- Premarin
- Medroxyprogesterone acetate
- Norethisterone
- Levonorgestrel
- Combined HRT is used which includes oestrogen and progestin
What are the risk of HRT?
- Unopposed oestrogen (ERT): increases risk of developing endometrial and ovarian cancer
- Opposed oestrogen (HRT): increases risk of developing breast cancer
- Increased risk of stroke and ischaemic heart disease
- Increased risk of venous thromboembolism
What are the route of administration of HRT?
- Oral
- Transdermal
- Implant
- Transvaginal
- Nasal
What are the drugs type for HRT?
- Inhibitors and antagonists
- Anti progestins
- Anti androgens
- Mixed agonist/antagonists
- Androgen replacement therapy
What are the drug examples for Inhibitors and Antagonists?
Weak oestrogen that block receptors
- Clomiphene: ovulation induction
- Tamoxigen: reduces the risk of breast cancer
What is the mechanism of action of Clomiphene?
- Inhibits oestrogen binding to it ER in the anterior ituitary
- Inhibits negative feedback
- Results in increased FSH, LH expression
What is the mechanism of action of tamoxifen?
- Binds to ER in breast tissue and blocks oestrogen stimulated myoepithelial cell division
- Ovulation induction
What are examples of anti-progestins?
-Mifepristone
What is the mechanism of action of mifepristone?
- Partial agonist to progesterone receptor. To inhibit progesterone action
- Sensitises the uterus to prostaglandins
- Used for medical termination of pregnancy and induction of labour
What is an example of an anti-androgen?
-Cyproterone
Progesterone derivative
What is the mechanism of action of Cypterone?
- Weak progestogenic effect. Partial agonist at the progesterone receptor, that competes with dihydrotestosterone
- Used in combined contraceptive pill (Dianette)
- Can be used to treat advanced prostate cancer
What are some examples of Mixed agonist/antagonists?
- Selective estrogen receptor modulators (SERMs) such as Raloxifene
- Selective progesterone receptor modulators (SPRMs)
What is the mechanism of action of Raloxifene?
- Protects against osteoporosis
- Oestrogenic effects on bone, lipid metabolism & blood coagulation
- No proliferative effects on endometrium & breast
- Reduced risk of invasive breast cancer in post-menopausal women with osteoporosis
- Increases hot flushes (flashes) - sweating
What are some examples of androgen replacement therapy?
- Implants (testosterone)
- Intramuscular (Enenthate, Proprionate)
- Oral (Undecanoate, Mesterolone)
