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(LUSUMA) Clinical Pharmacology & Therapeutics > S5) Sex Hormones > Flashcards

S5) Sex Hormones Flashcards

1
Q

Identify three drug groups of consideration when considering sex hormones

A
  • Sex steroid hormones
  • Inhibitors and antagonists
  • Mixed agonists / antagonists
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2
Q

What are the major effects of oestradiol?

A
  • Stimulates growth of the endometrium and breast
  • Stimulates production of PR
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3
Q

What are the major effects of progesterone?

A
  • Stimulates growth of the endometrium and breast
  • Maintains pregnancy
  • Inhibits production of ER
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4
Q

What are the major effects of testosterone?

A

Stimulates male characteristics – hairy body, deep voice, anabolism, aggression

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5
Q

Identify five effects of oestrogen

A
  • Sodium and water retention
  • ↑ HDL, ↓ LDL
  • Decrease bone resorption
  • Impair glucose tolerance
  • Increase blood coagulability
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6
Q

Identify five side effects of oestrogen

A
  • Breast tenderness
  • Nausea & vomiting
  • Water retention
  • Increased blood coagulability
  • Thromboembolism
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7
Q

Identify five effects of progesterone

A
  • Secretory endometrium
  • Increases bone mineral density
  • Fluid retention
  • Mood changes
  • Maintains pregnancy
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8
Q

Identify five side effects of progesterone

A
  • Weight gain
  • Fluid retention
  • Acne
  • Nausea/vomiting
  • Irritability
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9
Q

Identify four effects / side effects of testosterone

A
  • Male secondary sex characteristics
  • Acne
  • Voice changes
  • Increases aggression
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10
Q

What are the different routes of administration for sex steroid hormones?

A
  • Oral
  • Transdermal patch
  • Implants
  • Nasal
  • Vagina
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11
Q

How are sex steroids transported in the blood?

A
  • Transport bound to SHBG (except progesterone) and albumin
  • SHBG production upregulated by oestrogens – protects against hepatic metabolism
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12
Q

Sex steroid hormones are metabolised in the liver.

Explain how this occurs for progesterone

A

Liver metabolism – progesterone almost totally metabolised in one passage through liver

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13
Q

Storage of sex steroid hormones increases half life.

Describe how they are stored.

A
  • Sex steroids easily stored in fatty tissue (adipocytes and brain) as they are lipophilic
  • They complex into the plasma membrane just like cholesterol
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14
Q

How are sex steroid hormones excreted?

A

Metabolites are excreted in faeces and urine as glucuronides and sulphates, respectively

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15
Q

Sex steroids are effective by binding to nuclear receptors.

Which receptors are used by the following sex steroid hormones:

  • Oestrogens
  • Progestagens
  • Androgens
A
  • Oestrogens – ERα and ERβ
  • Progestagens – PR-A and PR-B
  • Androgens – AR-1 and AR-2
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16
Q

In the COCP, which oestrogens are prescribed and what are their half lives?

A
  • Ethinylestradiol (T1/2 ~ 15 hours)
  • Mestranol (T1/2 8-24 hours)
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17
Q

In the COCP, which progestins are prescribed?

A
  • Levonorgestrel
  • Norethisterone
  • Desogestrel
18
Q

What is the mode of action of the COCP?

A
  • Suppression of ovulation (inhibits FSH, LH)
  • Thickens cervical mucus (more viscous)
  • Prevents secretory phase in endometrium (remains atrophic)
19
Q

Identify five adverse effects of the COCP

A
  • Venous thromboembolism
  • Myocardial infarction
  • Hypertension
  • Decrease glucose tolerance
  • Mood swings
20
Q

What is the mode of action of the progestin only pill?

A
  • Thicken cervical mucous
  • Atrophy endometrium
21
Q

How can the management for missed pill advice change?

A

Management depends on:

  • How many pills have been missed (a missed pill is when it’s more than 24 hours)
  • When the pill was missed (time in pack)
  • The type of combined pill
22
Q

What advice can one give a female patient who has missed one pill?

A
  • Take the last pill immediately, even if this means taking two pills in one day
  • Continue taking the rest of the pack as normal
  • Take seven day pill free break as normal or take (inactive) pills
23
Q

What advice can one give a female patient who has missed two pills anywhere in the pack or started a new pack two or more days late (48 hours or more)?

A
  • Take the last pill immediately, even if this means taking two pills in one day
  • Continue taking the rest of the pack as normal
  • Use extra contraception for the following seven days
24
Q

What advice can one give a female patient if there are seven or more pills left in the pack after the last missed pill?

A

If there are seven or more pills left in the pack after the last missed pill – finish the pack and take seven-day pill-free break as normal or, take (inactive) pills

25
Q

What advice can one give a female patient if there are less than seven pills left in the pack after the last missed pill?

A

If there are less than seven pills left in the pack after the missed pill – finish the pack and start a new pack the next day; this means missing out the pill-free break or not taking your inactive pills

26
Q

Which emergency contraception can be provided up to 72 hours post coitus?

A

Up to 72 hours post coitus – Levonorgestrel 1.5mg

27
Q

Which emergency contraception can be provided up to 120 hours post coitus?

A
  • Ullipristal acetate 30mg – selective progesterone receptor modulator
  • Cu2+ IUD – prevents blastocyst attachment to endometrium
28
Q

Identify two types of hormonal regimes

A
  • Oestrogen replacement therapy (ERT)
  • Hormone replacement therapy (HRT)
29
Q

What are the indications for HRT?

A
  • Symptoms: hot flushes, sweats, vaginal dryness, dyspareunia
  • Osteoporosis
30
Q

What are the contraindications for HRT?

A

Heart disease

31
Q

Identify five types of steroids used in HRT and their dosing regimen

A
  • Oestradiol (1-2 mg/day)
  • Medroxyprogesterone acetate (2.5 mg/day)
  • Norethisterone (1 mg/day)
  • Levonorgestrel (1.5 mg/day)
32
Q

What are the routes of administration for HRT?

A
  • Oral
  • Transdermal
  • Implant
  • Transvaginal
  • Nasal
33
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
  • Increased risk of stroke and ischaemic heart disease
  • Increase risk of venous thromboembolism
34
Q

In terms of sex hormones, what are inhibitors/oestrogens?

A

Inhibitors/oestrogens are weak oestrogens that block receptors

35
Q

The inhibitor/antagonist, clomiphene, acts by ovulation induction.

Explain how this occurs as well as its result

A
  • Inhibits oestrogen binding to its ER in the anterior pituitary
  • Inhibits negative feedback
  • Results in increased FSH, LH expression
36
Q

The inhibitor/antagonist, tamoxifen reduces risk of breast cancer.

Explain how this occurs

A
  • Binds to ER in breast tissue and blocks oestrogen-stimulated myoepithelial cell division
  • Causes ovulation induction
37
Q

The inhibitor/antagonist, mifepristone (RU486) is an anti-progestin.

Explain its mechanism of action and its uses.

A
  • Partial agonist to progesterone receptor, inhibits progesterone action
  • Sensitises the uterus to prostaglandins
  • Used for medical termination of pregnancy and induction of labour
38
Q

The inhibitor/antagonist, cyproterone is an anti-androgen.

Describe its mechanism of action and uses

A
  • Weak progestogenic effect
  • Partial agonist at the progesterone receptor, that competes with dihydrotestosterone
  • Used in combined contraceptive pill and can be used to treat advanced prostate cancer
39
Q

How can androgen replacement therapy be administered?

A
  • Implants e.g. Testosterone
  • Intramuscular e.g. Enenthate, Proprionate
  • Oral e.g. Undecanoate, Mesterolone
40
Q

Describe the effects of finasteride?

A
  • Prevents hair loss
  • Male pattern baldness
  • Benign prostatic hyperplasia
41
Q

What is a contraindication of finasteride?

A

Finasteride is not approved for use in women, especially due to risks of birth defects in a foetus

42
Q

Describe five effects/side effects of selective estrogen receptor modulators

A
  • Protects against osteoporosis
  • Oestrogenic effects on bone, lipid metabolism & blood coagulation
  • No proliferative effects on endometrium & breast
  • Reduced risk of invasive breast cancer in postmenopausal women with osteoporosis
  • Increases hot flushes (flashes) – sweating

(LUSUMA) Clinical Pharmacology & Therapeutics (29 decks)

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