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Clinical Pharmacology > 7) Sex Steroid Hormones > Flashcards

7) Sex Steroid Hormones Flashcards

1
Q

What is the function of GnRH?

A

Stimulates synthesis and secretion of LH and FSH

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2
Q

What is the function of FSH?

A

Follicle growth and oocyte maturation

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3
Q

What is the function of LH?

A

Ovulation and causes ruptured follicle to become corpus luteum

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4
Q

What is the function of oestrogen in the menstrual cycle?

A

Repair and growth of endometrium

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5
Q

What is the function of progesterone in the menstrual cycle?

A

Preparation of endometrium for implantation and promotes growth of mammary glands

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6
Q

How are the sex steroids transported?

A

Bound to sex hormone binding globulins (except progesterone) and albumin

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7
Q

What regulates sex hormone binding globulins?

A

Production upregulated by oestrogen

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8
Q

How can the sex steroids be stored?

A

In fatty tissue (adipocytes and brain), complex into plasma membrane

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9
Q

How are the sex steroids excreted?

A

Metabolites excreted in faeces and urine as glucuronides and sulphates

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10
Q

Describe the enterohepatic recirculation of oestrogen:

A

Oestrogen conjugated with glucuronide and into bile. Intestinal bacteria unconjugate oestrogen so it gets recycled into blood

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11
Q

How is sex steroid hormone binding to nuclear receptors regulated?

A

Co-factors stabilise the hormone-receptor complex

Integrators have the opposite effect

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12
Q

Describe the isoforms of steroid hormone receptors:

A

Oestrogen: ER alpha, ER beta
Progesterone: PR-A and PR-B
Androgen: AR1 and AR2

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13
Q

What are the 3 sex steroid hormones and their effects?

A

Oestradiol - stimulates growth of endometrium, breast and production of PR
Progesterone - maintains pregnancy, growth of endometrium and breast, inhibits production of ER
Testosterone - simulates male characteristics, anabolism, aggression

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14
Q

How are the sex steroids synthesised?

A

Synthesised from cholesterol
Oestradiol formation occurs in adrenal, adipose and gonads
Progesterone and testosterone in gonads

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15
Q

What molecule can be used as a pregnancy marker?

A

Estriol

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16
Q

What are the side effects of too much oestrogen?

A

Breast tenderness
Water retention (bloating)
Thromboembolism
Breast, ovary and endometrial hyperplasia + cancer

17
Q

What are the side effects of too much progesterone?

A 
Weight gain 
Acne
Irritability
Depression
PMS
18
Q

What are the side effects of too much testosterone?

A

Adverse effects on lipid profile to increased risk of atherosclerosis

19
Q

What are the types of COCP?

A

Monophasic - fixed oestrogen and progestin
Biphasic - oestrogen constant, progestin increases second half
Triphasic - oestrogen for first 14, progestin 1-7 and 14-21

20
Q

Describe the COCP:

A

Synthetic oestrogens and 1st to 4th generation progesterone

21
Q

How can the COCP be administered?

A

Oral, transdermal patch, implants

22
Q

What is the mechanism of action of the COCP?

A

Inhibits FSH and LH to prevent ovulation, also thickens cervical mucus and keeps endometrium atrophic

23
Q

What are the adverse effects of the COCP?

A

Venous thromboembolism
MI and HTN
Gallstones (increased cholesterol to liver)

24
Q

What potential drug interactions can occur with the COCP?

A

Inducers: rifampicin, carbamazepine, phenytoin, St John’s Wort

25
Q

What should be monitored when on the COCP?

A

BP, BMI, side effects

26
Q

Describe the POP:

A

28 days of progestin

27
Q

What can be used as emergency contraception up to 72 hours post coitus?

A

Levonorgestrel

28
Q

What can be used as emergency contraception up to 120 hours post coitus?

A

Ullipristal acetate - selective progesterone receptor modulator
Copper IUD

29
Q

When is hormone replacement therapy prescribed?

A

For hot flushes and vaginal dryness (symptoms of menopause)

30
Q

When is HRT contraindicated?

A

Heart disease

31
Q

What is the difference between ERT and HRT?

A

ERT - oestrogen replacement therapy

HRT - hormone (progesterone and oestrogen) replacement therapy

32
Q

What are the risks of ERT?

A

Increased risk or endometrial and ovarian cancer

33
Q

What are the risks of HRT?

A

Increased risk of breast cancer

Risk of stroke, risk of VTE

34
Q

What are the routes of administration for HRT?

A

Oral, transdermal, implant, transvaginal, nasal

35
Q

What is the mechanism of action of clomiphene and what is it used for?

A

Inhibits oestrogen by binding to ER in anterior pituitary causing decreased negative feedback and increased FSH and LH
Used for ovulation induction in IVF

36
Q

What is the mechanism of action of tamoxifen and what is it used for?

A

Binds to ER in breast and blocks oestrogen stimulated myoepithelial cell division
Decreases risk of breast cancer

37
Q

What is the mechanism of action of mifepristone and what is it used for?

A

Partial agonist at PR and sensitises uterus to prostaglandins
Used for medical termination of pregnancy or induction of labour

38
Q

Describe an androgen replacement therapy and its use:

A

Finasteride blocks 5-alpha reductase from catalysing testosterone -> 5DHT
Prevents hair loss and BPH

Clinical Pharmacology (24 decks)

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