5.2.2 Oral Contraceptives Flashcards

(41 cards)

1
Q

What enzymes metabolise COCP and POP?

A

CYP450 in liver

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2
Q

What can affect COCP and POP contraceptives?

A

Efficacy is affected by enzyme inducing drugs which stimulate CYP450, therefore more breakdown of contraceptives

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3
Q

What drugs cannot be taken at the same time as COCP and POP?

A

Anti-epileptics
Carbamazepine or phenytoin

Antibiotics
Rifampicin and rifabutin

St John’s Wort

All increase production of CYP450

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4
Q

What natural products can enhance oestrogen absorption?

A

Soya protein

Enhances oestrogen absorption and reduces its storage in adipose and muscle

Half life reduced from 15 hours to 7 hours

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5
Q

What is the combined oral contraceptive pill (COCP)?

A

Pill containing synthetic oestrogen and progesterone

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6
Q

How long is the COCP taken for?

A

21 days with a 7 day break

7 placebo pills here
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7
Q

What does the COCP do?

A

Prevents ovulation

Reduces endometrial receptiveness to implantation

Thickens cervical mucus

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8
Q

What are the adverse effects of the COCP?

A

Increased risk of:
- VTE
- Stroke
- Breast cancer
- Cervical cancer

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9
Q

What are the contraindications of the COCP?

A
  • Smoker
  • Previous VTE
  • High BMI
  • Hypertension
  • IHD/stroke
  • Migraine
  • Breast cancer
  • Cirrhosis

Basically, things that put you at higher risk of clots, more oestrogen so breast cancer, cirrhosis as impaired oestrogen break down

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10
Q

What does the progestogen-only pill do?

A

Thickens cervical mucus

Reduced cilia activity in fallopian tubes

OVULATION IS NOT PREVENTED

Contains low-dose progestogen, taken daily with NO breaks

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11
Q

What are the advantages of the POP?

A

99% reliability

Can be used if COCP cannot

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12
Q

What are the disadvantages of the COCP?

A

No STI protection
Strict timing- user dependant
Menstrual irregularities
Increased risk of ectopic pregnancy (due to immotile cilia)

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13
Q

When is hormone replacement therapy offered?

A

Vasomotor or mood disorders

Urogenital symptoms

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14
Q

How is HRT given?

A

Oral or transdermal

Combined oestrogen and progesterone if woman has a uterus

Oestrogen alone if there is no uterus

Progesterone protects the endometrium from hyperplasia

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15
Q

What is the first line treatment for urogenital symptoms?

A

Low-dose vaginal oestrogen

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16
Q

What types of oestrogens are used in HRT?

A

Natural oestrogens
e.g. oestradiol

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17
Q

What types of progesterones are used in HRT?

A

Progesterone analogues
Testosterone analogues

Bioidentical- less side effects and risks

18
Q

What are the risks of using HRT?

A

Endometrial cancer (if oestrogen is unopposed)

Breast cancer

VTE- oral only

Stroke- oral only

CHD- if before 60

19
Q

Explain how HRT increases the risk of VTE

A

Increased:
- Activated protein C resistance
- Thrombin activation

Decreased:
- Anti-thrombin III activity
- Protein S levels
- Factor VII levels
- Tissue factor pathway inhibitor

20
Q

What is used to treat osteoporosis?

A

Bisphosphonates

21
Q

How do bisphophonates work?

A

Reduce bone turnover by controlling osteoclast activity

22
Q

When are bisphophonates used?

A

Prophylaxis and treatment of osteoporosis

Management of other diseases involving bone e.g. Paget’s disease of bone, malignancy

23
Q

Identify the pharmacokinetics of bisphophonates

A

Long half life
Poor gut absorption
Absorption affected by food, needs to be taken on an empty stomach

24
Q

What adverse reactions can occur when taking bisphophonates?

A

Upper GI effects
Oesophagitis- remain seated of standing for 30 minutes after taking

Hypocalcaemia
Check calcium and vitamin D levels prior to treatment

25
What is Mifepristone?
Progesterone and glucocorticoid receptor antagonist
26
What does Mifepristone do?
Acts as an anti-progesterone Sensitises myometrium to prostaglandin-induced contractions
27
When is mifepristone used?
Used for pregnancy termination and medical management of miscarriage
28
What do Selective Oestrogen Receptor Modulators (SERMs) do?
Interacts with oestrogen receptors as **agonists** or **antagonists** depending on the target tissue
29
What are some very important Selective Oestrogen Receptor Modulator examples?
**Tamoxifen**- Breast cancer **Raloxifene**- Prevention of osteoporosis in menopause and breast cancer
30
Where is tamoxifen metabolised?
Liver to active metabolites Active metabolites compete with oestrogen
31
What tissues does tamoxifen target?
Breast tissue Bone Hypothalamus Endometrium
32
Explain the action of tamoxifen in breast tissue
Antagonistically competes with oestrogen for binding sites Causes antioestrogenic and antitumour effects Slows cell cycling
33
Explain action of tamoxifen in bone
Stimulates oestrogen receptors instead of blocking them Exerts oestrogenic agonist effect, prevents osteoporosis in post-menopausal women
34
What is the action of tamoxifen on the hypothalamus?
Oesotrogen agonist Increases gonadotropin levels and can induce ovulation
35
How does tamoxifen act on the endometrium?
Oestrogen agonist **Can lead to endometrial hyperplasia**
36
What is clomiphene?
Non-steroidal ovulatory stimulatory Acts as a selective oestrogen receptor modulator (SERM)
37
When is clomiphene used?
Treatment of anovulation
38
How does clomiphene work?
Competes with oestrogen for receptor binding Leads to ovulation induction through increased production of LH and FSH
39
What is an example of a selective progesterone receptor modulator (SPRMS)?
Ulipristal acetate (Ella one)
40
How does ulipristal acetate (Ella one) work?
High-affinity binding to progesterone receptors Can be agonist or antagonist
41
When is Ellaone (ulipristal acetate) used?
Emergency contraception Inhibits or delays ovulation via suppression of the LH surge