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semester 4 - CPT & Prescribing > 8. Sex steroids > Flashcards

8. Sex steroids Flashcards

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1
Q

What are sex steroid hormones synthesised from?

A

Cholesterol

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2
Q

What receptors do steroid hormones have?

A
  • Classic nuclear receptors
  • Exert effects through gene transcription
  • But also a membrane receptor for oestrogen
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3
Q

what are the 3 main sex steroid hormones?

A

Oestrogens, progestagens, androgens

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4
Q

What are the major effects of oestradiol?

A

Stimulates growth of the endometrium and breast; stimulates production of Progesterone receptor (PR).

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5
Q

What are the major effects of progesterone?

A

Stimulates growth of the endometrium and breast; maintains pregnancy; inhibits production of ER(oestrogen receptor).

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6
Q

What are the major effects of testosterone?

A

Stimulates male characteristics; hairy body; deep voice; anabolism; aggression.

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7
Q

What are the actions of oestrogen?

A
  • Mild anabolic
  • Sodium and water retention
  • Raises HDL, lowers LDL
  • Decrease bone resorption (oestrogen decreases osteoclast function)
  • Impair glucose tolerance
  • Increase blood coagulability
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8
Q

What are the side effects of oestrogen?

A
  • Breast tenderness
  • Nausea, vomiting
  • Waterretention
  • Increased blood coagulability
  • Thromboembolism
  • Impaired glucose tolerance
  • Endometrial hyperplasia & cancer
  • Ovarian metaplasia & cancer
  • Breast hyperplasia & cancer
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9
Q

What are the actions of progesterone?

A
  • Secretory endometrium
  • Anabolic
  • Increases bone mineral density
  • Fluid retention
  • Mood changes
  • Maintains pregnancy
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10
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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11
Q

What are the actions of testosterone?

A
  • Male secondary sex characteristics
  • Anabolic
  • Voice changes
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12
Q

What are the side effects of testosterone?

A

Metabolic - adverse effects on lipid profiles particularly the HDLC/LDL-C ratio hence increased risk of atherosclerotic disease in males
• Acne
• Increases aggression

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13
Q

describe the role of oestrogen and progesterone in the menstrual cycle

A
  • Ovulation occurs due to the LH surge
  • Oestrogen and progesterone have differing effects on endometrial tissue and on cervical mucus
  • oestrogen promotes thin watery mucus for stern transport and progesterone promotes thick cervical mucus to block any further sperm from entering
  • Oestrogen and progesterone together produces suppression of the HPO axis
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14
Q

What are the pharmacokinetics of oestrogen?

A
  • Natural and synthetic oestrogens well absorbed in the GI tract
  • Also readily absorbed from skin and mucous membranes
  • Metabolism - liver
  • Excretion - in the urine as glucuronides and sulfates
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15
Q

What are the pharmacokinetics of progesterone?

A
  • Injected progesterone is bound to albumin with some stored in adipose tissue
  • Metabolised in the liver
  • Metabolites excreted in the urine conjugated to glucuronic acid
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16
Q

WHat are COCP and POP metabolised by?

A

CYP enzymes

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17
Q

what are Adverse effects of the combined pill?

A

• small Risk of thromboembolism

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18
Q

what increases the risk of thromboembolism with COCP?

A
  • Smoking increases this risk substantially
  • Also for long-term use in women over 35
  • Also consider other risk factors such as obesity and hypertension
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19
Q

Give examples of drugs that reduce efficacy of oral contraceptives and how?

A
  • anti-epileptics such as carbamazepine or phenytoin;
  • some antibiotics such as rifampicin and rifabutin and
  • some natural products such St John’s Wort

All increase production of hepatic CYP450 so speed up metabolism of drug

20
Q

What increases absorption of oestrogen?

A

Soya protiens - also reduce oestrogen storage in adipose tissue and decrease its half life

21
Q

What is HRT prescribed for?

A
  • symptoms of menopause: e.g. hotflushes /sweats and vaginal dryness / dyspareunia
  • osteoporosis - both oestrogen and progesterone limit bone resorption
    (should not be given for heart disease)
22
Q

what is menopause and what causes symptoms?

A

• Ovarian follicle supply depleted
• Consequently ovarian sex steroid production stops
• End of female reproductive capacity
• ALSO
Loss of oestrogen and progesterone leads to a range of systemic effects as symptoms of menopause

23
Q

which steroids are used for HRT?

A

• Oestradiol: e.g. valerate, enanthate, micronised oestradiol, ethinyl estradiol, etc.
(1-2 mg/day)
• Premarin® (0.625-1.25 mg/day)
• Medroxyprogesterone acetate (Provera®) (2.5 mg/day) • Norethisterone (1 mg/day)
• Levonorgestrel (1.5 mg/day)

24
Q

what are the routes of administration of HRT?

A 
ORAL 
TRANSDERMAL
IMPLANT 
TRANSVAGINAL 
NASAL
25
Q

WHat are the risks of HRT?

A

▪ Unopposed oestrogen (ERT): increases risk of developing endometrial and ovarian cancers
▪ Opposed oestrogen (HRT): increases risk of developing breast cancer
▪ Increase risk of venous thromboembolism
▪ Cardiovascular disease
▪ Increased risk of stroke

26
Q

What are the effects of HRT on thromboembolism profile?

A
  • Increased activated protein C resistance
  • increased thrombin activation,
  • decreased anti-thrombin III activity,
  • decreased protein S levels,
  • decreased Factor VII levels and
  • decreased tissue factor pathway inhibitor (but only for oral delivery systems)
27
Q

What are the effects of HRT on lipid profile?

A

Beneficial effect on lipid profile

  • increased HDL-C,
  • decreased oxoLDL-C,
  • decreased triglyceride,
  • decreased lipoprotein(a)
28
Q

what drugs are used to treat osteoporosis?

A

Bisphosphonates

29
Q

what is the action of bisphosphates?

A
  • Class of drugs that reduce bone turnover

* Act by controlling osteoclast activity

30
Q

what are bisphosphates used for?

A
  • Prophylaxis and treatment of osteoporosis
  • Other uses include management of other diseases involving bone
  • e.g. Paget’s disease of bone, malignancy
31
Q

What are the pharmacokinetics of bisphosphates?

A
  • Long biological half life
  • Poor gut absorption
  • Absorption affected by food
  • Therefore must be taken on an empty stomach
32
Q

what re the ADRs of bisphosphates?

A

• Upper GI effects
- Oesophagitis
- Stress the importance of remaining seated or standing for 30 minutes after taking
• Hypocalcaemia
- Check calcium and Vit D levels prior to initiating treatment

33
Q

what is an example of a bisphosphate?

A

alendrotnic acid

34
Q

What is Mifepristone (RU486)?

A

Progesterone (and glucocorticoid) receptor antagonist

35
Q

What is Mifepristone (RU486) used for?

A

Sensitising the myometrium to prostaglandin-induced contractions

  • Used for termination of pregnancy
  • progestogen usually cause inactivity of myometrium and prevents contractions
36
Q

What are SERMs?

A

• Selective Estrogen Receptor Modulator
• SERMs are distinct in having varying effects in differing tissues
i.e. are not pure agonists/antagonists

37
Q

What are 3 SERMs?

A

• Tamoxifen • Raloxifene • Clomiphene

38
Q

what can raloxifene be used for?

A

treatment of osteoporosis - has oestrogen effects on bone without harmful effects of breast and endometriun

39
Q

What is clomiphene used for?

A
  • Clomiphene used in the treatment of anovulation
40
Q

what is the action of clomiphene?

A
  • Competes with oestrogen for ER binding (in anterior pituitary, preventing negative feedback)
  • Leads to ovulation induction through increased production of anterior pituitary hormones
41
Q

Where is tamoxifen metabolized?

A

Liver - it is a prodrug, it has little affinity for ER

42
Q

What is tamoxifen used for?

A

To treat and prevent recurrence of ER-positive breast cancer

- ER antagonist in the breast, puts cells in cell cycle arrest

43
Q

describe the converse effects of tamoxifen in breast tissue and endometrium

A
  • In endometrium, acts as ER agonist

* In breast, acts as ER antagonist

44
Q

What is the risk of using tamoxifen?

A

It is an ER agonist in the endometrium, risk of endometrial cancer

45
Q

Give an example of a selective progesterone receptor modulator?

A

Ulipristal acetate

46
Q

What is ulipristal acetate used for?

A
  • used for emergency contraception (morning after pill)

- (effective for the treatment of uterine fibroids)

47
Q

How does ulipristal acetate work?

A

primary mode of action is thought most likely to be delay or inhibition of ovulation
- suppression of LH surge?

semester 4 - CPT & Prescribing (25 decks)

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