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Year 2 - endocrinology > Oral contraceptives > Flashcards

Oral contraceptives Flashcards

1
Q

Describe the bioavailabilty of oestradiol

A

Oestradiol is well absorbed but has a low bioavailability (extensive first-pass metabolism)

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2
Q

What are some forms of oestrogen contraceptives/HRT?

A
  • Oestrone sulphate (‘conjugated’ oestrogen)
  • Oestriol
  • Ethinyl oestradiol (the ethinyl group protects the molecule from first-pass metabolism)
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3
Q

What does a lack of oestrogen lead to?

A

Increased chance of osteoporosis and fracture

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4
Q

What can oestrogen contribute towards?

A

Breast growth (cancer) and CVS problems (VTE, stroke)

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5
Q

Describe the absorption and metabolism of progesterone

A

Progesterone is poorly absorbed and rapidly metabolised in the liver

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6
Q

How can progesterone be administered?

A

IM injection or depot preparation

Oral - norethisterone

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7
Q

What is the combined oral contraceptive?

A

This is a combination of an oestrogen (ethinyl oestradiol) and a progestogen (levonorgestrel or norethisterone)

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8
Q

What are the mechanisms via which the oral contraceptive suppresses ovulation?

A
  • Feedback of oestrogen and progestogens on the hypothalamus and pituitary
  • Progestogens thicken cervical mucus
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9
Q

How long is the COC taken for?

A

Taken for 21 days (or 12 weeks) and is then stopped for 7 days.

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10
Q

What are the side effects of oestrogens?

A
  • Nausea.
  • Breast (oestrogen dependant cancers)
  • Headache
  • Endometrium (causes proliferative effects)
  • Increased weight (water retention and fat deposition)
  • CVS problems (increased risk of fatal stroke and VTE (thrombosis moved to lungs))
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11
Q

When are progesterone only pills used?

A

When oestrogens are not a good idea – i.e. CVS problems, history of thrombosis, smokers, migraine

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12
Q

How are progesterone only pills administered?

A
  • Long-acting preparations may be given by deep IM injection or via intra-uterine system
  • Oral
    They have short half lives and short duration of activity. For long acting use intrauterine
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13
Q

What are some emergency contraceptives?
How are they taken (doses)?
SE?

A

Levonorgestrel – combined E+P or P-only

  • 2 doses 12 hours apart beginning ASAP within 72 hours of intercourse
  • May cause nausea and vomiting

Copper IUD - Exclude pregnancy first. It works by affecting sperm viability and function

Ulipristal – up to 120 hours after intercourse
- Delays ovulation up to 5 days with anti-progestin activity. Impairs implantation

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14
Q

What is menopause and the age of onset?

A

Permanent cessation of menstruation resulting from the loss of ovarian follicular activity

Average age: 51 (45-55)

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15
Q

What is climacteric menopause?

A

The period of transition from predictable ovarian function through the postmenopausal years

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16
Q

What is premature ovarian failure/insufficiency and causes?

A

Menopause occurring before the age of 40 and occurs in 1% of women
- May be autoimmune or secondary to surgery, chemotherapy or radiation

17
Q

Describe the levels of GnRH, LH, FSH and oestradiol in normal women

A

GnRH - high
LH/FSH - high
Oestradiol - high

18
Q

Describe the levels of GnRH, LH, FSH and oestradiol in menopausal women

A

GnRH - high
LH/FSH - high
Oestradiol - low

19
Q

What are the symptoms of menopause?

A
  • Hot flushes
  • Sleep disturbance
  • Depression
  • Urogenital atrophy
  • Decreased libido
  • Joint pain (lack of oestradiol)
    disappear with time
20
Q

What are the complications of menopause?

A

Osteoporosis:

  • Oestrogen deficiency leads to loss of bone matrix.
  • Loss of 1-3% of bone mass/year and have 10x increase risk of fracture.

Cardiovascular disease:
- Women are protected from CVS disease before the menopause but have the same risk as men by the age of 70.

21
Q

What is the HRT for menopause?

A
  • HRT – oestrogen + progesterone – to prevent endometrial hyperplasia
  • Can be given oral, transdermal, transvaginal
  • HRT can be cyclical: oestrogen given every day, and progesterone is given for the last 12-14 days
  • Or HRT can be continuous combined: continuous oestrogen and progestogens, all the time
22
Q

Which menopausal women are given oestrogen only treatment and why are they given HRT?

A

Women that have had hysterectomies (as no endometrium!)

Control symptoms – i.e. control vasomotor symptoms of hot flushes.

23
Q

What is used in the treatment & prevention of postmenopausal osteroporosis?
Give examples

A

SERMs – Selective Oestrogen Receptor Modulators:

E.G. Raloxifene (Tissue-selective – oestrogenic in bone and anti-oestrogenic in breast and uterus)
Reduces risk of: vertebral fractures and breast cancer.
Increases risk of: fatal stroke, VTE.
Does not affect vasomotor symptoms.

24
Q

Which drug can be used in breast cancer treatment?

A

Tamoxifen (anti-cancer drug):
Anti-oestrogenic in breast tissue.
Used to treat oestrogen-dependant breast tumours and metastatic breast cancers.

25
Q

What are the side effects of HRT?

A
  • breast cancer
  • coronary heart disease
  • deep vein thrombosis
  • stroke
  • gallstones

The absolute risk of complications for healthy symptomatic postmenopausal women in their 50s taking HRT for five years is very low

26
Q

Give examples of oestrogen preparations for HRT

A
  • Oral estradiol (1mg)
  • Oral conjugated equine oestrogen (0.625 mg)
  • Transdermal (patch) oestradiol (50 microgram/day)
  • Intravaginal – relevant for dyspareunia
27
Q

HRT and CHD and cancer etc.

A
  • Oestrogen alone has beneficial effects on lipid profile & endothelial function, but synthetic progestins negate these effects of estrogen
  • If you give oestrogen to younger women they experience the beneficial effects of oestrogens
  • Adverse effects arise when oestrogen is given to women over 60
  • Slightly more cases of breast cancer, stroke, DVT and CHD in women on combined HRT
  • Women’s Health Initiative (WHI) trials report an increased risk of CHD events in HRT treatment
  • But mean age of these participants: 63 – not the age of menopause presentation
28
Q

What is tibolone?
Effects?
SE?

A
  • A synthetic prohormone with oestrogenic, progestogenic & weak androgenic actions
  • It reduces fracture risk
  • It promotes an increased risk of stroke (RR: 2.2), and possibly an increased risk of breast cancer
  • Used in HRT
29
Q

What is raloxifene?
Effects?
SE?

A

Selective oestrogen receptor modulator

  • Oestrogenic in bone: reduces risk of vertebral fractures
  • Anti-oestrogenic in breast & uterus: reduces breast cancer risk
  • It does not reduce vasomotor symptoms, and it carries an increased risk of VTE & fatal stroke

Year 2 - endocrinology (18 decks)

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