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Pharmacology > Sex Steroid Hormone Pharmacology > Flashcards

Sex Steroid Hormone Pharmacology Flashcards

1
Q

How are sex steroid hormones transported

A

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

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2
Q

What is enterohepatic recirculation of oestrogen

A

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

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3
Q

What type of receptors do sex steroid hormones act on

A

Intracellular receptors

Bind to DNA and alter gene transcription and protein synthesis

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4
Q

Give examples of sex steroid receptors

A

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

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5
Q

Why does progesterone activity require oestrogen to be present before

A

Oestrogen stimulates PR synthesis via ER binding

Action of progesterone requires presence of PR

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6
Q

What are the effects of oestrogen

A 
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
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7
Q

What are side effects of oestrogen

A 
Breast tenderness
N+V
Fluid retention and bloating 
Increased risk of VTE 
Endometrial hyperplasia and cancer
Breast hyperplasia and cancer
Ovarian metaplasia and cancer
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8
Q

What are effects of progesterone

A 
Endometrial maturation and glandular formation
Breast growth 
Inhibit ER synthesis 
Maintain pregnancy
Anabolic
Na and water retention 
Mood changes
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9
Q

What are side effects of progesterone

A

N+V
Weight gain
Depression/PMS

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10
Q

What are effects of androgens

A

Deepening of voice
Male pattern hair growth
Aggression
Anabolic

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11
Q

What are side effects of androgens

A

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

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12
Q

What are formulations of COCP

A

Monophasic
Biphasic
Triphasic

Progesterone dose increase in phases during the cycle

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13
Q

What is mechanism of action of COCP

A

Inhibit ovulation

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

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14
Q

What are side effects of COCP

A 
Impaired glucose tolerance 
Hypertension 
Increase risk of VTE
Increased risk of IHD and stroke
Increased risk of breast cancer
Increased risk of cervical cancer
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15
Q

What are drug interactions of COCP

A

CYP450 inducers: causes contraceptive failure

Soya proteins: decreases T1/2 by increasing oestrogen absorption and decreasing storage in adipose

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16
Q

What is mechanism of action of POP

A

Thicken cervical mucus

Low dose progesterone

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17
Q

Give examples of IM progesterone injection

A

Medroxy Progesterone Acetate

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18
Q

What is mechanism of action of IM progesterone injection

A

Inhibit ovulation
Thicken cervical mucus
12 weeks

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19
Q

Give examples of intradermal progesterone depot

A

Etonogestrel

20
Q

What is mechanism of action of etonogestrel

A

Inhibit ovulation

Thicken cervical mucus

21
Q

What is levonorgestrel

A

Progesterone receptor modulator

22
Q

What are indications of levonorgestrel

A

Emergency contraceptive - 72hrs UPSI

Intrauterine system

23
Q

What is mechanism of action of levonorgestrel

A

Emergency: inhibit ovulation and implantation

IUS: inhibit endometrial proliferation, thicken cervical mucus

24
Q

What is Ulipristal acetate

A

Selective progesterone receptor modulator

25
Q

What are indications of ulipristal acetate

A

Emergency contraception - within 120hrs UPSI

26
Q

What is mechanism of action of Ulipristal acetate

A

Inhibit ovulation

27
Q

What are the types of hormone replacement therapy

A

HRT: oestrogen and progesterone
ERT: oestrogen only

28
Q

What is mechanism of action of HRT

A

Relieve post menopausal symptoms:
Flushing
Atrophic vaginitis
Osteoporosis

29
Q

What are side effects of HRT

A

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
Q

What are contraindications of HRT

A

ERT in women wo hysterectomy

31
Q

Give examples of oestrogen receptor blockers

A

Clomiphene
Tamoxifen
Raloxifene

32
Q

What is mechanism of action of Clomiphene

A

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

33
Q

What are indications of clomiphene

A

Infertility

Induce ovulation

34
Q

What is mechanism of action of tamoxifen

A

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

35
Q

What are indications of Tamoxifen

A

Oestrogen receptor positive breast cancer

36
Q

What is mechanism of action of Raloxifene

A

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

37
Q

What are indications of Raloxifene

A

Osteoporosis

Breast cancer

38
Q

What are examples of anti-progestins

A

Mifepristone

39
Q

What is mechanism of action of Mifepristone

A

Progesterone receptor Partial agonsist

Acts as an antagonist in high levels of progesterone

40
Q

What are indications of Mifepristone

A

Terminate pregnancy

Induce labour

41
Q

Give examples of anti-androgens

A

Cyproterone

42
Q

What is mechanism of action of cyproterone

A

Act as partial agonist at Progesterone receptor

Have weak progesteronergic effect

43
Q

What are indications of cyproterone

A

In COCP

44
Q

Give examples of testosterone replacement therapy

A

Finasteride

45
Q

What is mechanism of action of Finasteride

A

5alpha reductase inhibitor

Inhibit breakdown of testosterone to 5alpha-DHT

46
Q

What are indications of Finasteride

A

Male hair loss

BPH

Pharmacology (19 decks)

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