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IMSCP2 Pharmacology > Hormonal Contraception > Flashcards

Hormonal Contraception Flashcards

1
Q

What are the three natural oestrogens?

A

17β Oestradiol (E2)

  • Most abundant and potent oestrogen
  • Produced by ovarian granulosa cells

Oestrone (E1)

  • Produced by ovaries and adrenals

Oestriol (E3)

  • Only in pregnancy
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2
Q

What transports oestrogen in the blood?

A

Sex hormone binding globulin (SHBG)

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3
Q

What are the actions of oestrogen?

A

Development

  • Pubertal breast and genital development

Menstrual cycle regulation

  • Modulates FSH and LH release
  • Cyclical changes in breast and uterus

Metabolic

  • Increase bone mass
  • Improve HDL:LDL ration
  • Increases coagulability (increased stroke risk)
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4
Q

Where are oestrogen receptors expressed?

A

Redundantly in breast and reproductive system

Non-redundantly in CVS, bone and CNS

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5
Q

What secretes progesterone?

A

Corpus luteum

Placenta during pregnancy

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6
Q

What transports progesterone in blood?

A
  • Albumin
  • Corticosteroids binding globulin
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7
Q

Where can you find progesterone receptors?

A

Reproductive tract, breast and CNS.

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8
Q

Describe the action of progesterone on the body.

A

Action is to prepare for pregnancy.

Uterine/Cervical effects:

  • Decrease proliferation of endometrium
  • Blocks further sperm by thickening cervix and decreasing secretion

Other effects:

  • Glandular development in breast
  • Block ovulation through decreasing LH and GnRH release
  • Increase body temperature (CNS)
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9
Q

Two types of oral contraceptives

A
  1. Combined oral contraceptive (COC)
  2. Progestogen only contraceptive
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10
Q

What does the COC consist of ?

A

Contains synthetic oestrogen and synthetic progestogen

Synthetic oestrogen = ethinylestradiol

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11
Q

How is ethinylestradiol different from estradiol?

A

Addition of ethinyl group reduces the otherwise high first pass metabolism of estradiol.

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12
Q

Describe the mechanism of action of COCs

A

Inhibit ovulation by preventing release of FSH (oestrogen) and LH (progestogen) through negative feedback.

Also:

  • Thicken cervical mucous (progestogen effect) forming barrier to sperm
  • Thin endometrial lining (oestrogen + progestogen effect) to reduce sperm implantation.

Thus, COCs decrease likelihood of pregnancy by inhibiting ovulation, fertilisation and implantation.

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13
Q

Describe the efficacy of the pill, in theory and in real life.

A

If used properly, >99%.

EFfectiveness is reduced by:

  • Poor compliance
  • Vomiting or severe diarrhoea
  • Drugs that caused CYP3A4 induction
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14
Q

Two types of regimens for COC

A
  • 21 days OC + 7 days placebo
  • 21 days OC + 7 days no pill
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15
Q

What can occur durin the 7 hormone free days of the COC regimen?

A

Withdrawal bleeds

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16
Q

What is meant by monophasic, biphasic and triphasic formulations of COCs?

A

Monophasic = same daily dose of EE + progestogen for day 1 to 21

Biphasic = constant EE and increased progestogen in 2nd half of cycle

Triphasic = increased EE in middle of cycle to decrease breakthrough bleeding, plus gradual increase in progestogen over day 1-21.

17
Q

What are the side effects of COC?

A
  • Breakthrough bleeding (treated by increasing dose)
  • Nausea
  • Breast tenderness
  • Chloasma (pigmentation of face)
  • Depression, decreased libido
  • Increased clotting
18
Q

In what cases is COC contraindicated?

A
  • >35y.o.
  • Smoker
  • HTN
  • OBese
  • Genetic clotting abnormalities
  • Pregnancy / breast feeding
19
Q

What are the cancer-related risks and benefits of COC?

A

Oestrogen exposure increases the risk of breast cancer.

However, COC protects against:

  • Ovarian cancer
  • Endometrial cancer
  • Colorectal cancer
20
Q

Why might you use progestogen only OCs over COCs?

A

Contains no oestrogen, so useful when oestrogen is contraindicated

E.g. history of oestrogen-dependent cancer (breast)

21
Q

What is the mechanism of action of progestogen only OCs?

A

Inhibits ovulation due to inhibition of LH surge.

  • Thickening of cervix and decrease in cervical mucous impedes sperm penetration
  • Thinning endometrium decreases implantation
22
Q

What percentage of women still ovulation on OCs?

Why?

A

30-40%

  • REquires meticulous compliance - same time everyday, 28/28 days. Hard to do!
  • If you miss it by 3 hours, you need to use back-up contraception.
23
Q

What isthe most effective reversible contraceptive?

A

Long acting reversible contraceptive (LARC)

  • IUD
  • Progestogen implant

20x more effective than OCPs.

IMSCP2 Pharmacology (17 decks)

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