Drugs used in infertility, child birth, abortion and osteoporosis.

Question 1

What is the main cause of infertility?

Answer 1

Hyperprolactinemia.

Prolactin is produced by lactotrophs in the AP - under negative control of dopamine from the hypothalamus - D2 receptors.

After pregnancy, suckling stimulates an increase in the release of prolactin to stimulate the breast to produce milk.
HIGH PROLACTIN LEVELS SUPPRESS NORMAL MENSTRUAL CYCLING.

So…if we can stimulate D2 receptors, d3 agonists (bromocriptine, cabergoline) then we will decrease prolactin levels.

Question 2

What treatments are there for infertility?

Answer 2

Antioestrogens.
Gonadotropins.
Recombinant chorionic gonadtropin (LH and FSH)
GnRH analogues (continuous)
GnRH antagonists.

Question 3

What is clomifene.

Answer 3

Antioestrogen.
Selective oestrogen receptor modulator.
Decreases negative feedback
Increase FSH.

Question 4

Give examples of GnRH analogues.

Answer 4

Buserelin and nafarelin.

Question 5

Give examples of GnRH antagonists.

Answer 5

Cetrorelix and ganirelix.

Question 6

Explain what happens in the uterus during labour.

Answer 6

Smooth muscle contracts spontaneously.
Myometrial cells in the fundus are the pace maker and they are regulated by sex hormones.
Weak contractions during follicular phase.
Strong contractions during luteal phase and mestruation.

Question 7

Explain 4 things that cause contraction of the uterus.

Answer 7

Parasympathetic innervation of M3 receptors.
Sympathetic innervation of alpha receptors.
Oxytocin.
PGE2 and PGF2 alpha.

Question 8

Oxytocin?

Answer 8

Induce or augment labour.

Treat post partum haemorrhage.

Question 9

Ergometrine?

Answer 9

Treat post partum haemorrhage.

Question 10

Carboprost?

Answer 10

Treat post partum haemorrhage.

Question 11

Oxytocin and ergometrine?

Answer 11

Management of 3rd stage of labour (passing the placenta)

Control bleeding from incomplete abortion.

Question 12

Dinoprostone (PGE2)

Answer 12

Vaginal cervical ripening.
Induction of labour.
Therapeutic abortion (2nd trimester)

Question 13

Gemoprost/misoprostol (PGE1 analogue)

Answer 13

Early abortion - up to 63 days.

Question 14

Name 3 classes of myometrial relaxants used to prevent labour.

Answer 14

Selective B2 agonists - salbutamol
Oxytocin antagonists - atosiban
COX inhibitors. - indomethacin.

Question 15

Explain the changes in hormone production with age

Answer 15

Menarche approx 9-16yrs.
Menopause - 42-60 years.
Increase LH and FSH, decrease oestrogen and preogesterone.
Oestrogen still produced by adipocytes.
Androgens from adrenal cortex converted to oestrogen.

Question 16

Name 5 classes (with eg) of symptoms of the menopause.

Answer 16

1) Urogential - vaginal dryness, Urinary tract infections, urinary incontinence, painful intercourse.
2) Vasomotor - hot flushes, sweating, palipitations.
3) Emotional - anxiety, depression, irritability.
4) Osteoporosis
5) CV diseases - oestrogen has a protective effect in reproductive years.

Question 17

What is osteoporosis?

Answer 17

Decrease in bone mineral density.
Increased risk of fractures.
More marked in women,
Accelerated at menopause.
CAUSED BY EXCESSIVE BONE RESORPTION IN RELATION TO BONE FORMATION.
Osteoclasts resorb bone.

Question 18

Explain SERM treatment for osteoporosis.

Answer 18

Selective Oestrogen Receptor Modulator.
Raloxifene.

Oestrogen antag in breast and endometrium.
Oestrogen agonist in bone, blood and lipid metabolism.
GOOD TREATMENT FOR OSTEOPOROSIS.
Increase bone mineral density, decrease fracture risk.

BUT - menopausal effects, venous thromboembolism.

Question 19

Strontium Ranalate?

Answer 19

Increase bone formation, substitues Ca++ in bone, decrease osteoclast activity, increase osteoblast proliferation.

Question 20

Name 2 Ca++ and vit D supplements.

Answer 20

Calciterol, ergocalciferol.

Question 21

Explain bisphosphates.

Answer 21

Substitute pyrophosphate in bone, inhibit bone turnover, decrease osteovlast activity and increase BMD, decrease fracture risk.

Side effects - GI disorders, hypocalcemia

eg Alendronate.

Question 22

Denosumab?

Answer 22

RANKL inhibitor. Humanised antibody. Binds to RANKL and decrease bone resorption.

Question 23

hPTH

Answer 23

Parathyroid hormone.
Normally causes resorption of the bone - but if intermittent, increases BMD and decreases fracture risk.

BUT - increases risk of thromboembolism,

Question 24

Explain hormone replacement therapy.

Answer 24

Prevents hot flushes, vaginitis, osteoporosis.
oestrogen given.
Salt and water retention.
decrease LDL, increase HDL.
increase coagulability of blood.

Question 25

Tibolone.

Answer 25

oestrogen, progesterone and weak anabolic anabolic activity.