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Clinical Pharmacology > Reproductive and Post Reproductive Pharmacology > Flashcards

Reproductive and Post Reproductive Pharmacology Flashcards

1
Q

What molecule are sex hormones synthesised from?

A

Cholesterol

(large aromatic ring makes them hydrophobic)

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2
Q

What are the 2 forms of oesterogen that are predominant in reproductive life and menopause respectively?

A

Reproductive life: Estradiol

Post Menopause: Estrone

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3
Q

What kind of receptors are steroid hormone receptors? How do they exert their effects

A

Nuclear receptors

Exert their effects by altering gene transcription

(there is also a membrane receptor for oestrogen)

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4
Q

What are the 3 broad classes of sex hormone drug groups?

A

Sex steroid hormones

  • Oestrogens
  • Progestegens
  • Androgens

Inhibitors & antagonists

  • RU486
  • Finasteride

Mixed agonists/ antagonists

  • SERMs and SPRMs
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5
Q

What are the major effects of Oestradiol?

A
  • Stimulates growth of the endometrium & breast
  • Stimulates production of progesterone receptor
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6
Q

What are the major effects of progesterone?

A
  • Stimulates growth of the endometrium & breast
  • Maintains pregnancy
  • Inhibits production of oestrogen receptors
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7
Q

What are the major effects of testosterone?

A
  • Stimulates male characteristics
  • Hairy body
  • Deep voice
  • Anabolism
  • Aggression
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8
Q

What are the main pharmacological actions of oestrogen?

A
  • Mildly anabolic
  • Sodium and water retention
  • Raises HDL and lowers LDL
  • Decreases bone resorption
    • good during reproductive life but no post menopause as lack of oestrogen increases bone resorption
  • Impairs glucose tolerance
  • Increased blood coagulability
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9
Q

What are some of the side effects of oestrogen on the body?

A
  • Breast tenderness
  • Nausea and vomiting
  • Water retention
  • Increased blood coagulability
  • Thromboembolism
  • Impaired glucose tolerance
  • Endometrial hyperplasia (may cause cancer)
  • Ovarian metaplasia (may cause cancer)
  • Breast hyperplasia (may cause cancer)
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10
Q

What are the main effects of progesterone on the body?

A
  • Secretory endometrium
  • Anabolic
  • Increases bone mineral density
  • Fluid retention
  • Mood Changes
  • Maintains pregnancy
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11
Q

What are some of the side effects of progesterone?

A
  • Weight gain
  • Fluid retention
  • Anabolic
  • Acne
  • Nausea and Vomiting
  • Irritabilty, Depression, PMS
  • Lack of concentration
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12
Q

Surge of what hormone causes ovulation?

A

LH

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13
Q

What is the combined effect of oestrogen and progesterone on the HPA?

A

inhibits the HPO axis to stop release of GnRH

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14
Q

What are the different routes that hormonal contraception can be given by?

A
  • Oral
  • Nasal
  • Transdermal
  • Implants
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15
Q

Describe the pharmacokinetics of oestrogen

A
  • Natural and synthetic oestrogens are well absorbed in the GI tract
  • Also, readily absorbed from skin and mucus membranes
  • Metabolised in the liver
  • Excreted in urine as glucoronides and sulfates
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16
Q

Describe the pharmacokinetics of progesterone

A
  • Injected progesterone binds to albumin and some is stored in adipose tissue
  • Metabolised in the liver
  • Excreted in urine as conjugated glucoronic acid
17
Q

What is the main adverse effect of the combined pill and what factors increase this risk?

A

Thromboembolism (Overall effect is however, small)

Increased risk by:

  • smoking
  • long term use in women >35
  • obesity
  • hypertension
18
Q

What drugs can reduce the efficacy of COCP and POP and why?

A

Both COCP and POP are metabolised by CYP450s

Efficacy of drug is reduced by anything that induces the activity of CYPS including..

  • anti-epileptics e.g. carbamezepine / phenytoin
  • some antibiotics e.g. rifampicin and rifabutin
  • some over the counter e.g. St John’s Wort

All increase production of CYP450s

19
Q

What is the effect of soya protein products on oestrogen absorption?

A

Soya protein products enhance the absorption of eostrogen and reduces storage in adipose and muscle

Net effect: reduces t1/2 from 15 to ~7 hours

20
Q

What hormonal changes happen in the menopause?

A
  • Ovarian follicle supply is depleted
  • Consquently, ovarian sex steroid production stops
  • Loss of oestrogen and progesterone end reproductive capacity and have a range of systemic effects
21
Q

Why prescribe HRT? And for what reason should you not prescibe HRT

A
  • Prescribe to:* help with symptoms (hot flushes, swears and dyspareunia- painful sex) and to help prevent osteoporosis
  • Do not prescribe to*: prevent heart disease (used to be the case but no longer supported)
22
Q

What oestrogen steroids can be prescribed in HRT?

A
  • Synethtic derivatives e.g. ethinylestradiol
  • Premarin
23
Q

What progesterone steroids can prescribed as HRT?

A
  • Medroxyprogesterone acetate
  • Norethisterone
  • Levonorgestrel
24
Q

What is the main risk of unopposed oestrogen (ERT)?

A

Increases risk of developing endometrial & breast cancers

(in women who have uterus- better for those with TOTAL hysterectomy)

25
Q

What is the main risk of opposed oestrogen HRT?

(opposed= with progresterone)

A

Increases risk of developing breast cancer

26
Q

Explain the mechanism by which HRT can increase risk of venous theomboembolism?

A
  • Increased activity of activated protein C resistance (natural anticoagulant resistance)
  • Increased thrombin activation
  • Decreased activity of antithrombin III
  • Decreased levels of protein S
  • Decreased Factor VII
  • Decreased tissue factor pathway inhibitor (tissue factor activates the extrinsic pathway of clotting)
27
Q

What effect does HRT on lipid profiles?

A

Beneficial effect:

  • Increased HDL
  • Decreased oxo LDL
  • Decreased TAG
  • Decreased lipoprotein effect

Will not have an effect if patient already overweight

28
Q

What is the association between HRT and stroke?

A

Use of oral (not transdermal) oestrogen has a small increase in risk of stroke in women >60

29
Q

What is Mifepristone (RU486) used for? Explain its MoA

A

Used for the termination of pregnancy

  • Normal effect of progesterone makes myometrium quiescent
  • Mifepristone is a progesterone receptor antagonist
  • Acts as an anti-progesterone by sensitising the myometrium to prostaglandin induced contractions
30
Q

What is a SERM? Give 2 main examples

A

Selective Oestreogen Receptor Modulator

Have varying effects in differing tissues

e.g. tamoxifen, raloxifene

31
Q

What is clomiphene used to treat? Explain its MoA

A

Clompihene used to treat anovulation

MoA: Competes with oestrogen for the oestrogen receptor, once bound acts as a partial agonist

Pituitary thinks there is no oestrogen, increases oestrogen production for follicle stimulation

32
Q

What is tamoxifen used to treat? Explain how it works?

A

Used to treat breast cancer

A pro-drug, metabolised into active derivative in the liver

Competes with oestrogen binding to oestrogen receptor in breast

33
Q

What are the different effects of tamoxifen in different tissues?

A
  • Breast acts as an ER antagonist → cell cycle arrest
  • Endometrium acts as an ER agonist → promotes proliferation
34
Q

What are the 2 types of emergency contraception? How long can each be used for?

A
  • Progestogen: Levonorgestral
  • Progesterone Receptor Modulator: Ulipristal Acetate
35
Q

Explain how Ulipristal Acetate works (ellaOne)

A
  • Selective preogesterone receptor modulator
  • Primary mode of action as emergency contraception is to delay/ prevent ovulation
  • Also effective in treatment of uterine fibroids

Clinical Pharmacology (25 decks)

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