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5: Y5 - ESA 5 - Pharmacology NEW > Sex Hormones and HRT > Flashcards

Sex Hormones and HRT Flashcards

1
Q

What are the sex hormones?

A
  • Progesterone
  • Oestrogen
  • Testosterone
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2
Q

What are the sex hormones derived from?

A

Cholesterol

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3
Q

What do many of the sex hormones share?

A

Anabolic pathways

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4
Q

What can synthetic sex hormones be produced to do?

A

Act on the receptors with good effect

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5
Q

How can useful drugs be produced from sex hormones?

A

By minor modifications of parent groups

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6
Q

What drugs are used in contraception and HRT?

A

Oestrogen and progesterone

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7
Q

Are progesterone and oestrogen receptor intra- or extracellular?

A

Intra

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8
Q

What is affected when oestrogen and progesterone bind to their receptors?

A

Gene transcription

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9
Q

Where are oestrogen and progesterone receptors found at particularly high levels of expression?

A

In the female tract

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10
Q

What are the actions of progesterone around the body?

A
  • Secretory function of endometrium
  • Anabolic effects
  • Increased bone density
  • Fluid retention
  • Mood changes
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11
Q

What are the side effects of progesterone?

A
  • Weight gain
  • Fluid retention
  • Acne
  • Nausea and vomiting
  • Irritability
  • Lack of concentration
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12
Q

What are the actions of oestrogen around the body?

A
  • Mild anabolic effects
  • Sodium and water retention
  • Raise HDL, lower LDL
  • Decrease bone reabsorption
  • Improve blood coagulability
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13
Q

What are the side effects of oestrogen?

A
  • Nausea and vomiting
  • Water retention
  • Risk of thromboembolism
  • Impaired glucose tolerance
  • Endometrial hyperplasia and cancer risk
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14
Q

What does the COCP contain?

A

A variety of synthetic oestrogens in combination with 1st-4th generation progesterone

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15
Q

How does the COCP work?

A

By acting with the endocrine system to prevent ovulation, and the reproductive tract to cause cervical mucus thickening and endometrial thickening

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16
Q

What are the adverse effects of the COCP?

A

Quite minor

  • Increased risk of DVP
  • Raising of blood pressure
  • Increased risk of gallstones
  • Decreased glucose tolerance
  • Increased risk of stroke
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17
Q

How are COCPs metabolised?

A

They undergo metabolism in both phase I and II hepatic pathways

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18
Q

What is the result of COCPs undergoing metabolism in phase I and II hepatic pathways?

A

They are affected by CYP inducers

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19
Q

What are the CYP inducers?

A
  • Phenytoin
  • Carbamazapine
  • Barbituates
  • Rifampicin
  • Alcohol
  • Sulphonylureas
20
Q

What effect can broad-spectrum antibiotics have on the COCP?

A

It can reduce the efficacy of the COCP

21
Q

Why does the use of broad-spectum antibiotics reduce the efficacy of COCP?

A

The effect they have on intestinal flora will reduce their re-uptake into the circulation by lowering enterohepatic recycling

22
Q

What risk factors need to be evaulated before commencing on COCP?

A
  • BMI
  • Blood pressure
  • Migraines
  • Smoking history
23
Q

What advice is given to a patient taking COCP?

A
  • Taking it every day
  • Any missed days will require use of other contraceptives for 7 days
  • Any vomiting or diarrhoea may make COCP ineffective
  • Blood pressure checks needed every 3-6 months
24
Q

What is the main action of the progesterone only pill (POP)?

A

Thickening of cervical mucus

25
Q

What are the secondary actions of the POP?

A
  • Endometrial thickening
  • Endocrinological effects
26
Q

What are the disadvantages of the COCP compared with the POP?

A
  • Much narrower window of use
  • Much less reliable
  • More side effects than COCP
27
Q

What side effect may occur with POP?

A

Spotting

28
Q

In whom is the POP indicated?

A
  • Risk factors for venous thromboemboli
  • Smokers
  • Hypertensive

These women are not suitable for COCP

29
Q

What progestorone implants provide long term contraception?

A
  • Intramuscular implant
  • Subcutaneous deposition
  • Intra-uterine device
30
Q

How long to progesterone implants provide contraception for?

A

Between 3 months and 5 years

31
Q

What is hormone replacement therapy used for?

A
  • To prevent the symptoms of the menopause
  • Limit the early effects of osteoporosis
32
Q

Give a symptom of the menopause that can be prevented using HRT

A

Hot flushes/sweats

33
Q

Should HRT be used to prevent IHD?

A

No

34
Q

How can HRT be administered?

A
  • Orally
  • Transdermally
  • Implant
  • Transvaginaly
35
Q

What risks does HRT carry?

A
  • Increased risk of endometrial cancer and ovarian cancer
  • Increased risk of breast cancer
  • Increased risk of stroke
  • Increased risk of DVT
36
Q

What should be done before starting any woman on HRT?

A

All the side effects should be discussed, and baseline investigations should be undertaken

37
Q

What properties do the selective oestrogen receptor modulators (SERMs) exhibit?

A

Mixed agonist/antagonist properties

38
Q

What is the specific outcome of SERMs dependant on?

A
  • Tissue specific expression of oestrogen receptors
  • Genes associated with receptors
  • Presence of transcription factors
39
Q

Give three examples of SERMs

A
  • Clomiphene
  • Tamoxifen
  • Raloxifene
40
Q

What is clomiphene?

A

An oestrogen antagonist acting on the pituitary

41
Q

What does clomiphene do?

A

Induces ovulation

42
Q

How does clomiphene induce ovulation?

A

By inhibiting negative feedback

43
Q

What properties do tamoxifen and raloxifene have?

A

Differing agonist/antagonist tissue profiles

44
Q

How do tamoxifen and raloxifene have differing agonist/antagonist tissue profiles?

A

By acting as anti-oestrogenic in breast tissue, but oestrogenic in endometrium

45
Q

What effect does tamoxifen and raloxifene have on breast cancer risk?

A

Reduces it by 50%

46
Q

What effect does tamoxifen and raloxifene have on endometrial cancer risk?

A

It increases it

47
Q

What effect does tamoxifen and raloxifene have on oestroporosis risk?

A

Decreases it

5: Y5 - ESA 5 - Pharmacology NEW (17 decks)

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