sex drugs

Question 1

sex steroid synthesis steps

Answer 1

cholesterol, progesterone, testosterone, estradiol

Question 2

steroid hormone receptors

Answer 2

nuclear receptors, effect: gene transcription

estrogen has membrane receptor as well

Question 3

oestradiol effect

Answer 3

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

Question 4

progesterone effect

Answer 4

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

Question 5

testosterone effect:

Answer 5

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

Question 6

oestrogen side effects

Answer 6

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

Question 7

progesterone side effects

Answer 7

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

Question 8

oestrogen pharmacokinetics

Answer 8

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

Question 9

progesterone pharmacokinetics

Answer 9

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

Question 10

COCP

Answer 10

thromboembolism small risk

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

Question 11

^ COCP and POP

Answer 11

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

Question 12

HRT oestradiol examples

Answer 12

Oestradiol

Medroxyprogesterone acetate

Question 13

Unopposed oestrogen risk

Answer 13

developing endometrial and ovarian cancers

Question 14

Opposed oestrogen risk

Answer 14

developing breast cancer

Question 15

Bisphosphonates mechanism

Answer 15

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

Question 16

Bisphosphonates examples

Answer 16

Alendronic acid, zoledronic acid, pamidronate disodium

Question 17

Bisphosphonates

Answer 17

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

Question 18

Mifepristone mechanism

Answer 18

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

Question 19

Selective Estrogen Receptor Modulator mechanism, examples

Answer 19

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

Question 20

clomiphene mechanism

Answer 20

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

Question 21

tamoxifen mechanism

Answer 21

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

Question 22

Ulipristal acetate

mechanism

Answer 22

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