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CPT dorothy > 7 - Sex Hormones > Flashcards

7 - Sex Hormones Flashcards

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1
Q

What are three groups of drugs when considering sex hormones?

A
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2
Q

Why do drugs based on sex hormones take a while for a response?

A

They are steroid hormones so act through nuclear receptors so longer response

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3
Q

What are the actions and side effects of oestrogen?

A
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4
Q

What are the actions and side effects of progesterone?

A
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5
Q

What are the actions and side effects of testosterone?

A
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6
Q

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

A
  • Oral
  • Transdermal patch
  • Implants
  • Nasal
  • Vagina
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7
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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8
Q

What are some side effects of the combined pill?

A
  • Thromboembolic disease (higher in obese, hypertensives, smokers, long term users and over 35)
  • Mood swings
  • Decreased glucose tolerance
  • Mood swings
  • Hypertension
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9
Q

How are sex hormone drugs metabolised and excreted?

A
  • CYP450 in liver
  • Metabolites are excreted in faeces and urine as glucuronides and sulphates, respectively
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10
Q

What is the mechanism of action for the COCP and POP?

A

COCP:

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

POP: (low dose)

  • Thicken cervical mucous
  • Atrophy endometrium
  • High dose implant stops ovulation but this doesn’t
  • Need constant oestrogen as progestrone receptors only present when oestrogen around so not good if woman producing low oestrogen
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11
Q

What are some side effects of POP?

A
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12
Q

In the COCP, which progestins are prescribed?

A
  • Medroxyprogesterone acetate
  • Norethisterone
  • Levonorgesterel
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13
Q

In the COCP, which oestrogens are prescribed?

A

ethinylestradiol

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14
Q

How are sex hormones synthesised?

A

From cholesterol

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15
Q

What drug-drug interactions can occur with the POP and COCP?

A

Metabolised by CYP450 so the following enzyme inducing drugs can lower the drugs response:

  • Antiepileptics like carbamazepine and phenytoin

- Rifampicin and rifabutin

- St John’s Wort

- Soya protein for perimenopausal symptoms can enhance oestrogen absorption and reduce its storage in adipose so half life from 15 to 7 hours

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16
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
17
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
18
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
19
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

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

20
Q

Why is HRT prescribed?

A
  • Helps the symptoms of menopause e.g hot flushes, dyspareunia, genital atrophy
  • Helps osteoporosis
  • NOT cardioprotective
21
Q

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

A

- Oestrogen only: can only be given to a woman without a uterus (cause endometrial hyperplasia –> cancer)

- HRT: progesterone given with oestrogen as progesterone has antiproliferative effects on endometrium

22
Q

What are the side effects/risks of HRT?

A
  • Increased chance of breast cancer (mainly HRT)
  • Increased risk of endometrial and ovarian cancer in unopposed oestrogen
  • Risks of DVT and PE as oestrogen makes you hypercoagulable (only oral)

- Stroke and ischaemic heart disease

23
Q

What are the routes of administration for HRT?

A
  • Oral
  • Transdermal
  • Implant
  • Transvaginal
  • Nasal
24
Q

What is the mechanism of action of Mifepristone (RU486) and what class of drug is it?

A

- Antiprogesterone: Progesterone and glucocorticoid antagonist

  • Sensitises the myometrium to prostaglandin induced contraction

- Terminates pregnancy or labour induction

25
Q

What are anti-androgens used for?

A

- Cyproterone

  • Weak progestogenic effect
  • Partial agonist at the progesterone receptor, that competes with dihydrotestosterone
  • Used in COCP and can be used to treat advanced prostate cancer
26
Q

What class of drug is clomiphene and what is it used for?

A

- SERM: selective oestrogen receptor modulator

  • Varying effects depending what tissue it is in
  • Induces ovulation as prevents oestrogen binding to receptor on anterior pituitary and having negative feedback so increased FSH and LH
27
Q

What class of drug is Tamoxifen and what is it used for?

A

- SERM

  • Prodrug metabolised in the liver to become active

- Reduces breast cancer (or risk of) in ER positive cases as binds ER antagonist so binds to ER stopping myoepithelial growth

  • In endometrium it acts as ER agonist so can cause menopausal side effects and endometrial cancer
28
Q

Describe five effects/side effects of selective estrogen receptor modulators (SERM)

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
29
Q

What are two emergency contraceptives and what are their mechanisms of action?

A

- Levonorgestrel (up to 72 hours): progestogen. stops ovulation and/or prevents sperm fetilising an egg

- Ulipristal Acetate (up to 120 hours): selective progesterone receptor modulator. delays or inhibits ovulation and can be used to treat uterine fibroids

30
Q

What can SERMs be used for?

A
  • Breast cancer chemotherapy
  • Anovulation
  • HRT
31
Q

A man from ethiopia has a deficiency in CYP2D6, what effect would you expect to see if he was using codeine as an analgesic?

A

Decreased therapeutic effect, need an increase dose as it is a prodrug that needs metabolising to be active

32
Q

In a patient with hepatic disease, what affect will this have on the therapeutic action of tamoxifen?

A

Decreased as tamoxifen is a prodrug

33
Q

What hormones are involed in HRT that increase the risk of breast cancer when used in the short term?

A

Estradiol plus one of:

- Medroxyprogesterone

- Levonorgesterol

- Dydrogesterone

34
Q

What are the major effects of oestradiol, progesterone and testosterone??

A

CPT dorothy (25 decks)

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