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ESA4 - Clinical Pharmacology > Sex Steroids > Flashcards

Sex Steroids Flashcards

1
Q

What are the major effects of oestradiol?

A

Stimulates growth of the endometrium and breast, stimulates productions of progesterone receptors

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2
Q

What are the major effects of progesterone?

A

Stimulates growth of the endometrium and breast, maintains pregnancy, inhibits production of oestrogen receptors

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3
Q

What are the major effects of testosterone?

A

Stimulates male characteristics, body hair, deep voice, anabolism, aggression

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4
Q

What are sex steroids synthesised from?

A

Cholesterol

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5
Q

What are the actions of oestrogen?

A

Mild anabolic actions, sodium and water retention, raises HDL, lowers LDL, decreases bone resorption, impairs glucose tolerance, increases blood coagulability

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6
Q

What are the side effects of oestrogen?

A

Breast tenderness, nausea and vomiting, water retention, increased blood coagulability, thromboembolism, endometrial hyperplasia, ovarian metaplasia, breast hyperplasia

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7
Q

What are the actions of progesterone/progestin?

A

Secretory endometrium, anabolic actions, increases bone mineral density, fluid retention, mood changes, maintenance of pregnancy

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8
Q

What are the side effects of progesterone/progestin?

A

Weight gain, fluid retention, acne, nausea and vomiting, irritability, depression, PMS, lack of concentration

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9
Q

What are the adverse metabolic effects of testosterone?

A

Adverse effects on lipid profiles - HDL-C/LDL-C ratio

Hence increased risk of atherosclerotic disease in males

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10
Q

What would oestrogen drugs be bound to in the blood?

A

Sex hormone binding globule and albumin

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11
Q

True or False:

Progesterone is almost totally metabolised in one passage through the liver

A

True

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12
Q

Why are sex steroids easily stored in fatty tissue (adipocytes and brain)?

A

They are lipophilic

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13
Q

What two types do oral contaceptive pills exist as?

A

COCP - oestrogen + prostestin

POP - progestin only

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14
Q

What is meant by a monophasic combined pill?

A

Each tablet contains a fixed amount of oestrogen and progestin

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15
Q

What is meant by a biphasic combined pill?

A

Each tablet contains a fixed amount of oestrogen while the amount of progestin increases in the second half of the cycle

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16
Q

What is meant by a triphasic combined pill?

A

The amount of oestrogen may be fixed or variable, while the amount of progestin increases in 3 equal phases

17
Q

What is an example of a 1st generation progestin?

A

Norethynodrel

18
Q

What is an example of a 2nd generation progestin?

A

Levonorgestrel

19
Q

What is an example of a 3rd generation progestin?

A

Desogestrel

20
Q

What is an example of a 4th generation progestin?

A

Drospirenone (yasmin)

21
Q

What are some adverse effects of the pill?

A

Venous thromboembolism, MI, hypertension, headaches, mood swings, increase risk of stroke in women with focal migraine

22
Q

What drugs interact with the COCP?

A

Anti-epileptics such as carbamazepine
Rifampicin
St John’s Wort

All increase production of hepatic P450

23
Q

What are some risks of HRT?

A

Unopposed oestrogen increases risk of endometrial and ovarian cancers, opposed oestrogen increase risk of breast cancer, increased risk of stroke and IHD, increased risk of VTE

24
Q

What does tamoxifen do?

A

Binds to oestrogen receptor in breast tissue and locks oestrogen-stimulated myoepithelial cell division, also causes ovulation induction

Reduces risk of breast cancer

25
Q

Give an example of an anti-progestin

A

Mifepristone - partial agonist to progesterone receptor, inhibits progesterone action

Sensitises the uterus to prostaglandins - used in induction of labour

26
Q

What is an example of an anti-androgen?

A

Cyproterone - weak progestogenic effect

Partial agonist at the progesterone receptor that competes with dihydrotestosterone

Can be used to treat advanced prostate cancer

27
Q

What is a SERM? Give an example

A

Selective Estrogen Receptor Modulator

Example - raloxifene

Protects against oesteoporosis

ESA4 - Clinical Pharmacology (20 decks)

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