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Clinical Pharmacology and Therapeutics > Sex Steroid Hormones, Oral Contraceptives, and HRT > Flashcards

Sex Steroid Hormones, Oral Contraceptives, and HRT Flashcards

1
Q

What % of sex steroid hormones are bound to SHBG and albumin?

A

98%

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2
Q

Why are they bound to SHBG?

A

To protect against liver metabolism of free hormones

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3
Q

What causes SHBG to be produced?

A

Oestrogens upregulate SHBG production

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4
Q

Where are sex steroids stored within the body and why?

A

Within fatty tissue as they are lipophilic

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5
Q

How are sex stroid metabolites excreted?

A

In faeces as glucuronide, and urine as sulphates

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6
Q

What are the oestrogen receptors in the body?

A

ERα and ERβ

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7
Q

Apart from ERα and ERβ, are there other oestorgen receptors?

A

Not in normal physiology, but there can be in cancer

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8
Q

What are the progesterone receptors in the body?

A

PR-A and PR-B

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9
Q

What are the androgen receptors in the body?

A

AR-1 and AR-2

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10
Q

Where do AR-1 receptors exist within the body?

A

Testes, penis, and prostate

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11
Q

Where do AR-2 receptors exist within the body?

A

Liver, bone, and hair follicles

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12
Q

What happens when oestrogen binds to an oestrogen receptor?

A

Oestrogen response element responds to stimulus by starting processes like transcription. Response is regulated by co-factors and integrators.

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13
Q

In terms of the response to oestrogen, how do cofactors and integrators act?

A

Co-factors act to stabilise the process so more transcription takes place.

Integrator are mainly negative in action.

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14
Q

Why are oestrogen receptors alpha and beta, but androgen and progesterone A&B/1&2?

A

ERs are generated from different genes on different chromosomes, but ARs and PRs are isoforms generated from alternate splicing of genes

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15
Q

When does steroid receptor expression vary?

A

Throughout the menstrual cycle

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16
Q

When in the menstrual cycle are more ER alpha receptors expressed?

A

Proliferative phase

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17
Q

When in the menstrual cycle are more ER beta receptors expressed?

A

Secretory phase

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18
Q

When in the menstrual cycle are more AR receptors expressed?

A

Late secretory phase

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19
Q

When in the menstrual cycle are more PR receptors expressed?

A

More in glands in proliferative phase, but more in stroma in secretory phase

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20
Q

What are synthetic progestagens called?

A

Progestins

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21
Q

What drug classes can we use to target steroid hormone receptors?

A
  • Natural/synthetic sex steroid hormones i.e. agonists
  • Inhibitors and Antagonists
  • Mixed agonists/antagonists
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22
Q

Name some examples of inhibitors and antagonists of steroid hormone receptors.

A

Clomiphene
Finesteride
RU 486

Actually these are all partial agonists, technically speaking.

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23
Q

Name some examples of mixed agonist/antagonists of steroid hormone receptors.

A

SERMs (selective oestrogen receptor modulators)
SPRMs
SARMs

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24
Q

What is the major effect of oestradiol in the body?

A

Stimulates endometrial and breast growth, and progesterone receptor production.

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25
Q

What is the major effect of progesterone in the body?

A

Stimulates endometrial and breast growth, and inhibits oestrogen receptor production. Maintains pregnancy.

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26
Q

What is the major effect of testosterone in the body?

A

Stimulates male characteristics (hair, voice, anabolism, agression).

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27
Q

What are sex steroid hormones synthesised from?

A

Cholesterol

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28
Q

Where does sex steroid hormone production occur?

A

Adrenal gland, adipose tissue, and gonads.

29
Q

What are the 3 main endogenous oestrogens?

A

Estradiol
Estrone
Estriol

30
Q

Which oestrogen is at high levels during pregnancy? Why is tis useful?

A

Estriol - we can use it as a marker for good pregnancy progression.

31
Q

What can we use progesterone derivatives for?

A

Delaying the onset of labour to prevent preterm birth

32
Q

What is the most commonly presecribed testosterone derivative, and what are they for?

A 
Levonogestrel = morning after pill
Desogestrel = POP
Norgestrel = OCP
33
Q

Aside form its action in the menstrual cycle, what other effects does oestrogen have on the body?

A 
Mild anabolic effect
Na2+ and water retention
HDL increase, LDL decrease
Decreases bone resorption
Impairs glucose tolerance
Increases blood coagulability
34
Q

What side effects can oestrogen cause?

A 
Breast tenderness
N&V
Water retention
Increases blood coagulability
Thromboembolism
Impairs glucose tolerance
35
Q

Aside form its action in the menstrual cycle, what other effects does progesterone have on the body?

A

Anabolic
Fluid retention
Increase bone mineral density
Mood changes

36
Q

What side effects can progesterone cause?

A 
Weigh gain
Fluid retention
Acne
Anabolic
N&V
Irritability
PMS
Depression
Lack of concentration
37
Q

What metabolic effect does testosterone have, and why is this important?

A

Adverse effect on HDL/LDL ratio so there is a higher risk of atherosclerotic disease in males and gender-reassigned females

38
Q

What are the 2 types of OCPs?

A

COCP

POP

39
Q

What 3 types of COCP are there?

A

Monophasic
Biphasic
Triphasic

40
Q

Tell me about monophasic, biphasic, and triphasic COCPs.

A

Monophasic - every tablet has the same amount of O and P.
Biphasic - every tablet has the same amount of O, but P increased for second half of cycle.
Triphhasic - O fixed then variable, P increases in 3 equal phases.

41
Q

How are oestrogens reccommended to be started?

A

At lowest dose, and if that is ineffective, increase the dose.

42
Q

How does the COCP work?

A

Suppresses ovulation by inhibiting FSH and LH.
Increased viscosity of cervical mucus.
Prevents secretory phase of endometrium (remains atrophic).

43
Q

What are the risks associted with COCP?

A 
VTE
MI
HTN
Impaired glucose tolerance
Stroke in women with focal migraines
Headaches
Mood swings
Cholestatic jaundice
Gallstones
44
Q

What is important about oestrogen and progesterone metabolism wrt COCP?

A

It is metabolised by CP450 in the liver so may become ineffective if inducers are taken alongside COCP.

45
Q

Tell me about the POP.

A

28 days of progestin (different forms).

Works best if started at begining of follicular phase/start of menstrual bleed.

46
Q

What is the depot?

A

Medroxy progesterone acetate

Given every 12 weeks

47
Q

What is Nexplanon?

A

A brand of etonogestrel used as the implant in females as contraception.

48
Q

What are the 3 kinds of emergency contraception?

A

Levonogestrel
Ulipristal acetate (EllaOne)
Cu2+ IUD

49
Q

What is ulipristal acetate and how does it work?

A

SPRM - suprresses LH surge and prevents ovulation.

50
Q

When can EllaOne be taken?

A

Up to 120 hours post-coitus

51
Q

When can levonogestrel be taken?

A

Up to 72 hours post-coitus

52
Q

How does the Cu2+ IUD work?

A

Copper is toxic to the blastocyst, acts as a spermicide, and prevents endometrial attachment by altering the uterine and tubal environment.

53
Q

What is HRT/ORT prescribed for?

A

Symptoms of hot flushes, vaginal dryness, or if the pt is at risk of developing osteoporosis.

54
Q

Who is HRT contraindicated in?

A

Anyone with heart disease

55
Q

How can HRT be administered?

A 
Oral
Transdermal
Implant
Transvaginal
Nasal
56
Q

Which agents are used in HRT?

A

Oestradiol or Premarin

+/- medroxyprogesterone acetate/Norethisterone/Levonorgestrel

57
Q

What are the risks of HRT?

A

Unopposed oestrogen in ERT increases risk of developing endometrial/ovarian cancer.
Opposed oestrogen in HRT increases risk of developing breast cancer.
Increased risk of VTE and stroke

58
Q

What are the benefits of HRT/ERT (aside from the aim of treatment)?

A

Beneficial effect on risk of IHD, as well as higher HDL, lower LDL, TAG and lipoproteins.

59
Q

What does clomiphene do?

A

Weak oestrogen/partial agonist:

  • Induces ovulation
  • Inhibits Oestrogen binding in anterior pituitary so LH and FSH expression increases
60
Q

What is clomphene used for?

A

Female infertility

61
Q

What does tamoxifen do?

A

Weak oestrogen/partial agonist:

  • Reduces risk of breast cancer in ER positive women by blocking receptor to prevent cell division.
  • Induces ovulation
62
Q

Tell me about antiprogestins.

A

Partial PR agonists to prevent progesterone action. Sensitises uterus to prostaglandins.

63
Q

What are antiprogestins used for?

A

Medical termination of pregnancy

Induction of labour

64
Q

What is Mifepristone (RU 486)?

A

Antiprogestin

65
Q

Tell me about antiandrogens.

A

Progesterone derivatives that compete with dihydrotestosterone.

66
Q

What is finasteride?

A

5 alpha reductase inhibitor used for BPH and androgenetic alopecia in men

67
Q

What is the main SERM?

A

Raloxifene

68
Q

What is raloxifene used for?

A
  • Post-menopausal osteoporosis (Rx and Prevention)

- Breast cancer chemoprevention

69
Q

How does raloxifene work?

A

Oestrogenic effect on bone, lipid metabolism, and coagulation.

Clinical Pharmacology and Therapeutics (26 decks)

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