Sex Steroid Hormone Pharmacology Flashcards Preview

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Flashcards in Sex Steroid Hormone Pharmacology Deck (46):
1

How are sex steroid hormones transported

Bound to SHBG and albumin
Binding protects against first pass metabolism
Progesterone does not bind to SHBG - majority undergo first pass metabolism
Oestrogen increases SHBG

2

What is enterohepatic recirculation of oestrogen

Oestrogen absorbed from GIT pass into liver
Conjugated and excreted into bile
Unconjugated by colonic flora
Absorbed from GIT pass into peripheral circulation

Thus antibiotics altering gut flora can affect oestrogen absorption

3

What type of receptors do sex steroid hormones act on

Intracellular receptors
Bind to DNA and alter gene transcription and protein synthesis

4

Give examples of sex steroid receptors

ER alpha, ER beta
PR A, PR B
AR 1, AR2

5

Why does progesterone activity require oestrogen to be present before

Oestrogen stimulates PR synthesis via ER binding
Action of progesterone requires presence of PR

6

What are the effects of oestrogen

Endometrial proliferation
Breast proliferation
PR synthesis
Na and water retention
Increased blood coaguability
Improve lipid profile: high HDL, low LDL
Reduce bone resorption
Impaired glucose tolerance

7

What are side effects of oestrogen

Breast tenderness
N+V
Fluid retention and bloating
Increased risk of VTE
Endometrial hyperplasia and cancer
Breast hyperplasia and cancer
Ovarian metaplasia and cancer

8

What are effects of progesterone

Endometrial maturation and glandular formation
Breast growth
Inhibit ER synthesis
Maintain pregnancy
Anabolic
Na and water retention
Mood changes

9

What are side effects of progesterone

N+V
Weight gain
Depression/PMS

10

What are effects of androgens

Deepening of voice
Male pattern hair growth
Aggression
Anabolic

11

What are side effects of androgens

Poor lipid profile: low HDL, high LDL
Increased risk of atherosclerotic disease
Increased risk of stroke

12

What are formulations of COCP

Monophasic
Biphasic
Triphasic

Progesterone dose increase in phases during the cycle

13

What is mechanism of action of COCP

Inhibit ovulation
Progesterone at High dose inhibits positive feedback - thus inhibit LH surge

14

What are side effects of COCP

Impaired glucose tolerance
Hypertension
Increase risk of VTE
Increased risk of IHD and stroke
Increased risk of breast cancer
Increased risk of cervical cancer

15

What are drug interactions of COCP

CYP450 inducers: causes contraceptive failure
Soya proteins: decreases T1/2 by increasing oestrogen absorption and decreasing storage in adipose

16

What is mechanism of action of POP

Thicken cervical mucus
(Low dose progesterone)

17

Give examples of IM progesterone injection

Medroxy Progesterone Acetate

18

What is mechanism of action of IM progesterone injection

Inhibit ovulation
Thicken cervical mucus
12 weeks

19

Give examples of intradermal progesterone depot

Etonogestrel

20

What is mechanism of action of etonogestrel

Inhibit ovulation
Thicken cervical mucus

21

What is levonorgestrel

Progesterone receptor modulator

22

What are indications of levonorgestrel

Emergency contraceptive - 72hrs UPSI
Intrauterine system

23

What is mechanism of action of levonorgestrel

Emergency: inhibit ovulation and implantation

IUS: inhibit endometrial proliferation, thicken cervical mucus

24

What is Ulipristal acetate

Selective progesterone receptor modulator

25

What are indications of ulipristal acetate

Emergency contraception - within 120hrs UPSI

26

What is mechanism of action of Ulipristal acetate

Inhibit ovulation

27

What are the types of hormone replacement therapy

HRT: oestrogen and progesterone
ERT: oestrogen only

28

What is mechanism of action of HRT

Relieve post menopausal symptoms:
Flushing
Atrophic vaginitis
Osteoporosis

29

What are side effects of HRT

ERT: Increased risk of endometrial cancer
Increased risk of breast cancer
Increased risk of VTE (oral admin only)
Increased risk of stroke
Improved lipid profile (but NOT used for purpose of preventing CVD)

30

What are contraindications of HRT

ERT in women wo hysterectomy

31

Give examples of oestrogen receptor blockers

Clomiphene
Tamoxifen
Raloxifene

32

What is mechanism of action of Clomiphene

ER Antagonist at hypothalamus and pituitary
Inhibit negative feedback
Increase GnRH and LH/FSH release
Increase oestrogen and progesterone release

33

What are indications of clomiphene

Infertility
(Induce ovulation)

34

What is mechanism of action of tamoxifen

Selective oestrogen receptor modulator
ER Agonist at bone and endometrium
ER Antagonist at Breast
Inhibit proliferation of myoepithelial cells in breast

35

What are indications of Tamoxifen

Oestrogen receptor positive breast cancer

36

What is mechanism of action of Raloxifene

Selective oestrogen receptor modulator
Agonist at bone and endometrium
Antagonist at Breast

37

What are indications of Raloxifene

Osteoporosis
Breast cancer

38

What are examples of anti-progestins

Mifepristone

39

What is mechanism of action of Mifepristone

Progesterone receptor Partial agonsist
Acts as an antagonist in high levels of progesterone

40

What are indications of Mifepristone

Terminate pregnancy
Induce labour

41

Give examples of anti-androgens

Cyproterone

42

What is mechanism of action of cyproterone

Act as partial agonist at Progesterone receptor
Have weak progesteronergic effect

43

What are indications of cyproterone

In COCP

44

Give examples of testosterone replacement therapy

Finasteride

45

What is mechanism of action of Finasteride

5alpha reductase inhibitor
Inhibit breakdown of testosterone to 5alpha-DHT

46

What are indications of Finasteride

Male hair loss
BPH