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Clinical Pharmacology > 5.2.2 Oral Contraceptives > Flashcards

5.2.2 Oral Contraceptives Flashcards

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
Q

What is Mifepristone?

A

Progesterone and glucocorticoid receptor antagonist

26
Q

What does Mifepristone do?

A

Acts as an anti-progesterone

Sensitises myometrium to prostaglandin-induced contractions

27
Q

When is mifepristone used?

A

Used for pregnancy termination and medical management of miscarriage

28
Q

What do Selective Oestrogen Receptor Modulators (SERMs) do?

A

Interacts with oestrogen receptors as agonists or antagonists depending on the target tissue

29
Q

What are some very important Selective Oestrogen Receptor Modulator examples?

A

Tamoxifen- Breast cancer

Raloxifene- Prevention of osteoporosis in menopause and breast cancer

30
Q

Where is tamoxifen metabolised?

A

Liver to active metabolites

Active metabolites compete with oestrogen

31
Q

What tissues does tamoxifen target?

A

Breast tissue
Bone
Hypothalamus
Endometrium

32
Q

Explain the action of tamoxifen in breast tissue

A

Antagonistically competes with oestrogen for binding sites

Causes antioestrogenic and antitumour effects

Slows cell cycling

33
Q

Explain action of tamoxifen in bone

A

Stimulates oestrogen receptors instead of blocking them

Exerts oestrogenic agonist effect, prevents osteoporosis in post-menopausal women

34
Q

What is the action of tamoxifen on the hypothalamus?

A

Oesotrogen agonist

Increases gonadotropin levels and can induce ovulation

35
Q

How does tamoxifen act on the endometrium?

A

Oestrogen agonist

Can lead to endometrial hyperplasia

36
Q

What is clomiphene?

A

Non-steroidal ovulatory stimulatory

Acts as a selective oestrogen receptor modulator (SERM)

37
Q

When is clomiphene used?

A

Treatment of anovulation

38
Q

How does clomiphene work?

A

Competes with oestrogen for receptor binding

Leads to ovulation induction through increased production of LH and FSH

39
Q

What is an example of a selective progesterone receptor modulator (SPRMS)?

A

Ulipristal acetate (Ella one)

40
Q

How does ulipristal acetate (Ella one) work?

A

High-affinity binding to progesterone receptors

Can be agonist or antagonist

41
Q

When is Ellaone (ulipristal acetate) used?

A

Emergency contraception

Inhibits or delays ovulation via suppression of the LH surge

Clinical Pharmacology (45 decks)

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