sex drugs Flashcards

1
Q

sex steroid synthesis steps

A

cholesterol, progesterone, testosterone, estradiol

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2
Q

steroid hormone receptors

A

nuclear receptors, effect: gene transcription

estrogen has membrane receptor as well

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3
Q

oestradiol effect

A

Stimulates growth of the endometrium and breast;
stimulates production of PR.
Mild anabolic • Sodium and water retention
• Raises HDL, lowers LDL
• Decrease bone resorption
• Impair glucose tolerance
• Increase blood coagulability

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4
Q

progesterone effect

A

Stimulates growth of the secretory endometrium and breast;
maintains pregnancy;
inhibits production of ER.
• Anabolic • Increases bone mineral density • Fluid retention • Mood changes

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5
Q

testosterone effect:

A

Stimulates male characteristics;increased body hair; deep voice;
anabolism;
aggression.
Acne
Metabolic - adverse effects on lipid profiles particularly the HDL-C/LDL-C ratio hence increased risk of atherosclerotic disease in males

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6
Q

oestrogen side effects

A
  • Breast tenderness • Nausea, vomiting • Water retention
  • Increased blood coagulability • Thromboembolism
  • Impaired glucose tolerance
  • Endometrial hyperplasia & cancer • Ovarian metaplasia & cancer • Breast hyperplasia & cancer
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7
Q

progesterone side effects

A
  • Weight gain • Fluid retention
  • Anabolic
  • Acne
  • Nausea/vomiting
  • Irritability Depression, PMS • Lack of concentration
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8
Q

oestrogen pharmacokinetics

A

absorbed well in gi tract,from skin and mucous membranes,
metabolized in liver,
exertion in urine as glucoronides and sulfates

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9
Q

progesterone pharmacokinetics

A

bound to albumin,
stored in adipose tissue,
metabolized in liver,
excreted in urine conjugated to glucoronic acid

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10
Q

COCP

A

thromboembolism small risk

but increases with smoking, long-term use, obesity and hypertension

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11
Q

^ COCP and POP

A

metabolised in the liver by CYP 450 enzymes
anti-epileptics such as carbamazepine or phenytoin; –
some antibiotics such as rifampicin and rifabutin and –
St John’s Wort
• because they all increase the production of hepatic CYP450
Soya protein products enhance oestrogen absorption, reducinng half-life

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12
Q

HRT oestradiol examples

A

Oestradiol

Medroxyprogesterone acetate

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13
Q

Unopposed oestrogen risk

A

developing endometrial and ovarian cancers

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14
Q

Opposed oestrogen risk

A

developing breast cancer

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15
Q

Bisphosphonates mechanism

A

for osteoporosis
reduce bone turnover by controlling osteoclast activity,
can’t attach to bone due to membrane dysfunction

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16
Q

Bisphosphonates examples

A

Alendronic acid, zoledronic acid, pamidronate disodium

17
Q

Bisphosphonates

A

long T1/2 life,
poor gut absorption, affected by food, taken on empty stomach.
esophagitis, hypocalcaemia

18
Q

Mifepristone mechanism

A

Progesterone receptor antagonist
Sensitising the myometrium to prostaglandin-induced contractions
Used for termination of pregnancy

19
Q

Selective Estrogen Receptor Modulator mechanism, examples

A

pure agonists and pure antagonists
depends on specific tissue
Tamoxifen, raloxifen, clomiphene,

20
Q

clomiphene mechanism

A

treatment of anovulation
Competes with oestrogen for ER binding
ovulation induction through increased production of anterior pituitary hormones

21
Q

tamoxifen mechanism

A

prodrug,
In endometrium, acts as ER agonist
• In breast, acts as ER antagonist causing cells to arrest the cell cycle

22
Q

Ulipristal acetate

mechanism

A
  • Selective Progesterone receptor modulator
  • emergency contraception: delay or inhibition of ovulation
  • treatment of uterine fibroids