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CPT8 - Sex-Steroid Pharmacology Flashcards

(4 cards)

1
Q

3 features of pharmacokinetics of oestrogen and progesterone

Absorption
Metabolism
Excretion

A
  1. ) Oestrogen
    - absorption: GI tract and skin/mucous membranes
    - metabolism: liver
    - excretion: urine as glucuronides and sulfates
  2. ) Progesterone
    - absorption: when injected, it is bound to albumin while some is stored in adipose tissue
    - metabolism: liver
    - excretion: urine conjugated to glucuronic acid
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2
Q

4 features of pharmacokinetics of oral contraceptives (COCP and POP)

Metabolism
Enzyme Inducing Drugs x3
Soya Proteins
Adverse Effects of COCP

A
  1. ) Metabolism - liver by CYP450 enzymes
    - therefore efficacy is reduced by enzyme inducing drugs because they ↑production of hepatic CYP450s
  2. ) Enzyme Inducing Drugs
    - anti-epileptics: carbamazepine or phenytoin
    - antibiotics: rifampicin and rifabutin
    - natural products: St John’s Wort
  3. ) Soya Proteins - ↑oestrogen absorption
    - also ↓storage in adipose and muscle
    - causes half-life to reduce from 15 to 7 hours
  4. ) Adverse Effects of COCP - thromboembolism
    - smoking increases risk substantially as well as:
    - long term use in women over 35
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3
Q

4 features of hormone replacement therapy (HRT)

Usage
Administration Routes x5
Risks x3
Other Benefits x5

A
  1. ) Usage - prescribed for symptoms of menopause
    - e.g. hot flushes, dyspareunia, osteoporosis
    - it is NOT prescribed for heart disease
  2. ) Routes of Administration
    - oral, transdermal, implant, transvaginal, nasal
  3. ) Risks of HRT
    - endometrial/ovarian (ERT) and breast (HRT) cancer
    - venous thromboembolism
    - oral oestrogen associated w/ ↑ risk of stroke
  4. ) Other Benefits of HRT - ↓risk of CVD
    - ↑HDL, ↓LDL, ↓triglycerides, ↓lipoproteins
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4
Q

5 other drugs acting on the reproductive sytstem

Mifepristone (RU486)
SERMs
Clomiphene
Tamoxifen
Ulipristal Acetate
A
  1. ) Mifepristone (RU486) - progesterone antagonist
    - sensitises myometrium to prostaglandin-induced contractions
    - used for termination of pregnancy
  2. ) SERMs - mixed ER agonists and antagonists
    - have varying effects in differing tissues
    - raloxifene used for post-menopausal osteroporosis
  3. ) Clomiphene - SERM used to treat anovulation
    - ER antagonist in the hypothalamus, preventing negative FB of oestrogen so ↑GnRH
    - induces ovulation by ↑production of FSH and LH
  4. ) Tamoxifen - SERM used to treat breast cancer
    - pro-drug: activated by metabolism in the liver
    - ER antagonist in the breast
    - ER agonist in endometrium (↑ endometrial cancer)
  5. ) Ulipristal Acetate - emergency contraception
    - selective progesterone receptor modulator (SPRM)
    - delays/inhibits ovulation
    - also used to treat uterine fibroids
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