Reproductive and post-reproductive health Flashcards

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1
Q

What are the different drug groups used in reproductive health?

A

Sex steroid hormones
Inhibitors and antagonists
Mixed agonist/antagonist

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2
Q

Give examples of sex steroid hormones

A

Oestrogens, progestogens and androgens

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3
Q

Give examples of inhibitors and antagonsists

A

RU486, finasteride

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4
Q

Give examples of mixed agonists/antagonists

A

Selective oesterogen receptor modulators

Selective progesterone receptor modulators

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5
Q

What are sex steroids synthesised from?

A

Cholestrol

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6
Q

What is the difference between Estrone and Estradiol?

A

Estone is more prevalent in post menopausal women whereas Estradiol is the more potent oestrogen present in reproductive life for follicular maturation

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7
Q

What are the receptors for steroid hormones? How do they exert their effects?

A

Classic nuclear receptors

Exert effects via gene transcription, as a transcription factor

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8
Q

What additional type of receptor does it have?

A

Membrane receptor for oestrogen

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9
Q

What are the major actions/effects of estradiol?

A
Stimulates growth of the endometrium and breast
Mild anabolic
Na and H20 retention 
Raises HDL and lowers LDL
Decreases bone reposition
Impairs glucose tolerance
Increased blood coagulability
Stimulates production of progesterone
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10
Q

What are the major actions/effects of progesterone?

A
Stimulates growth of the endometrium and breast
Anabolic
Increases bone mineral density
Fluid retention
Mood changes
Maintains pregnancy
Inhibits production of oestrogen
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11
Q

What are the major effects of testosterone?

A
Male characteristics
Body hair
Acne
Deep voice
Anabolism
Aggression
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12
Q

What are the side effects of oestrogen?

A
Breast tenderness
Nausea/vomiting
Water retention
Increased blood coagulability 
Thromboembolism
Impaired glucose tolerance
Emdometrial hyperplasia and cancer
Breast hyperplasia and cancer
Ovarian metaplasia
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13
Q

What are the side effects of progesterone?

A
Weight gain
Fluid retention
Anabolic 
Acne
Nausea/vomiting
Irritability, depression, PMS
Lack of concentration
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14
Q

What are the side effects of testosterone?

A

Adverse effects of lipid profiles especially the HDL-c/LDL-c ratio
Increased risk of atherosclerotic disease in males

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15
Q

Pharmacokinetics of oestrogen: What does it’s absorbability mean for administration?

A

Natural and synthetic oestrogen are well absorbed in the GI tract so can be given in oral root
OR via patches in skin because readily absorbed from skin and mucus membranes

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16
Q

Where is oestrogen metabolised and by what?

A

Liver by CYP450

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17
Q

How is oestrogen excreted?

A

In the urine as glucoronides and sulphates

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18
Q

Pharmacokinetics of progesterone: How is it transported in blood and where is it stored?

A

Injected progesterone if bound to albumin with some stored in adipose tissue

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19
Q

Where is progesterone metabolised and by what?

A

Liver by CYP450

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20
Q

How is progesterone excreted?

A

In urine conjugated to glucuronic acid

21
Q

What are some adverse effects of the combined pill?

A

Risk of thromboembolism

22
Q

What risk factors increase the likelihood of the adverse effects?

A

Smoking
Long term use after 35 years of age
Obesity
Hypertension

23
Q

What enzyme is involved in COCP and POP metabolism

A

CYP 450 in the liver

24
Q

What reduces the contraceptive efficacy?

A

Enzyme inducing drugs which increase production of CYP450

25
Q

What are some examples of enzyme inducing drugs?

A

Anti-epileptics e.g. carbamazepine or phenytoin
Antibiotics e.g. rifampicin and rifabutin
Natural products e.g. St Johns Wort- anti-depressant

26
Q

What are the effects of soya protein on oral contraceptives?

A

Enhance oestrogen absorption and reduce its storage in adipose and muscle so cause the T1/2 to bee reduced from 15 to 7 hrs

27
Q

Why prescribe hormone replacement therapy?

A

To relieve systemic symptoms that are a result of loss of oestrogen and progesterone
Osteoporosis

28
Q

What are the routes of HRT administration?

A
Oral
Transdermal
Implant
Transvaginal
Nasal
29
Q

Risks of taking unopposed oestrogen?

A

Increased risk of developing endometrial and ovarian cancers

30
Q

Risks of taking HRT: oestrogen and progesterone?

A

Increased risk of developing breast cancer

31
Q

Why is there an increased risk of venous thromboembolism?

A
Theres increased activated protein c resistance
Increased thrombin activation
Decreased anti thrombin 3 activity
Decreased protein s levels
Decreased factor 7 levels
Decreased TF pathway inhibitor
32
Q

What is Mifepristone (RU486)?

A

Progesterone receptor antagonist so acts as an anti-progesterone

33
Q

What effect does RU486 have?

A

Sensitising the myometrium to prostaglandin induced contarctions

34
Q

What is the use of RU486?

A

For the termination of pregnancy

35
Q

What is a SERM?

A

Selective estrogen receptor modulator, have varying effects in different tissues

36
Q

What are examples of drugs in the SERM class?

A

Tamoxifen
Raloxifene
Clomiphene

37
Q

What is Raloxifene?

A

Management og post-menopasual osteoporosis- stops acceleration of bone resorption

38
Q

What is clomiphene, what is its use?

A

Used in the treatment go anovulation

39
Q

What is the mechanism of action of Clomiphene

A

Competes with oestrogen for ER binding
Tricks the pituitary to think there is no oestrogen
This increases oestrogen production, and thus increased follicular development

40
Q

What is Tamoxifen?

A

Pro drug

41
Q

How is Tamoxifen made functional?

A

Metabolised in the liver to make active derivatives

42
Q

What is the mechanism of action of active Tamoxifen?

A

Competes with oestrogen for bidding to the ER

43
Q

Why is there so much person to person variability in Tamoxifen effects?

A

Metabolising enzymes come in various isoforms and so have varying metabolisms

44
Q

Where does Tamoxifen have converse effects?

A

Breast tissue and endometrial tissue

45
Q

What effect does Tamoxifen have on the endometrium?

A

Acts as ER agonist

46
Q

What effect does Tamoxifen have on the breast?

A

Acts as ER antagonist, causes the cell to arrest cycle

47
Q

What is Ulipristal acetate?

A

Selective progesterone receptor modulator

48
Q

What is Ulipristal acetate?

A

Used for emergency contraception and used for uterine fibroids

49
Q

What does Ulipristal acetate bind to?

A

Progesterone receptor