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Pharmacology > Sex Steroid Hormone Pharmacology > Flashcards

Sex Steroid Hormone Pharmacology Flashcards

(46 cards)

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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

20
Q

What is mechanism of action of etonogestrel

Study These Flashcards
A

Inhibit ovulation

Thicken cervical mucus

21
Q

What is levonorgestrel

Study These Flashcards
A

Progesterone receptor modulator

22
Q

What are indications of levonorgestrel

Study These Flashcards
A

Emergency contraceptive - 72hrs UPSI

Intrauterine system

23
Q

What is mechanism of action of levonorgestrel

Study These Flashcards
A

Emergency: inhibit ovulation and implantation

IUS: inhibit endometrial proliferation, thicken cervical mucus

24
Q

What is Ulipristal acetate

Study These Flashcards
A

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

Pharmacology (19 decks)

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