pharmacology

Question 1

uses of oestrogen replacement therapy

Answer 1

hypogonadism in children
primary amenorrhoea (+progestin)
contraceptive (+progestin)
menopause (+progestin)

Question 2

what are the benefits of postmenopausal hormone therapy

Answer 2

• improved bone density
• relief from hot flushes, fatigue and vaginal dryness
• reverses atrophy of vulva, vagina and urethra
• improved sleep
• reduced incidence of colorectal cancers
• reduced incidence of CVD?
• reduced incidence of AD?

Question 3

what are the risks of postmenopausal oestrogen hormone therapy

Answer 3

• breast tenderness
• nausea
• fluid retention
• increased risk of breast/uterine cancer
• increased risk of thromboembolism/stroke

Question 4

what are the 4 ways oestrogen causes cellular effects

Answer 4

• crosses to cytoplasmic receptors –> homodimer –> SRE –> gene transcription
• crosses to cytoplasmic receptors –> heterodimer –> SRE –> gene transcription
• can bind to receptor on the cytoplasmic membrane
• bind to GPCR
  (last two account for rapid effects)

Question 5

what are the effects of oestrogen and progesterone in the breast

Answer 5

oestrogen –> growth

progesterone –> differentiation

Question 6

increased risk of breast cancer is associated with what receptors

Answer 6

oestrogen and progesterone positive in the breast

Question 7

what are the two partial agonists of oestrogen (SERM)

Answer 7

tamoxifen

raloxifene

Question 8

what are the effects of tamoxifen

Answer 8

stimulates uterus and CVS and bone but antagonist to breast and CNS

Question 9

what are the effects of raloxifene

Answer 9

stimulates bone and CVS, but antagonist to breast, uterus and CNS

Question 10

what is fulvestrant

Answer 10

antagonist to oestrogen receptors throughout the body

Question 11

when is tamoxifen used

Answer 11

palliative treatment of metastatic breast cancer and adjuvant after lumpectomy

Question 12

adverse effects of tamoxifen

Answer 12

• endometrial hyperplasia, polyps and cancer
• thromboembolic events
• thrombocytopaenia
• ocular toxicity
• menopausal symptoms

Question 13

why are aromatase drugs useful for treating breast cancer

Answer 13

because its activity is high in breast adipose mesenchymal tissue

Question 14

what are the effects of aromatase inhibitors

Answer 14

• improved disease free survival after tamoxifen
• reduced incidence of contralateral breast cancer
• number of thromboembolic events
• incidence of endometrial cancer

Question 15

what are the adverse effects of aromatase inhibitors

Answer 15

• increased bone loss and fracture risk
• increased arthralgia
• potential poorer lipid profile, hepatic steatosis and metabolic syndrome with long-term use
• menopausal signs

Question 16

where are the major places that DHT act in males

Answer 16

prostate
seminal vesicles
epididymus
skin

Question 17

which enzyme converts testosterone to DHT

Answer 17

5-alpha-reductase

Question 18

what are the main actions of DHT

Answer 18

prostate development
external virilisation
sexual maturation

Question 19

how does testosterone travel in the blood

Answer 19

bound to steroid hormone binding globulin

Question 20

action of testosterone in the cell

Answer 20

can bind to androgen receptor in the cytoplasm or can bind directly on receptors in the nucleus

Question 21

what are the medical uses of androgens

Answer 21

• hypogonadism in children
• senile osteoporosis
• speed recovery from surgery and chronic debilitating diseases
• promotes skeletal growth in pituitary dwarfism
• endometriosis

Question 22

what are the non-therapeutic uses of androgen

Answer 22

increased lean body mass
muscle strength
aggressiveness

Question 23

adverse effects of androgens

Answer 23

• increased LDL and decreased HDL
• female: acne, facial hair, etc
• male: priapsim, impotence, decreased spermatogenesis and gynaecomastia
• premature closure of epiphyseal plates, abnormal sexual maturation
• liver damage, increased aggression and psychotic epidodes

Question 24

what is the difference between cyproterone and flutamide

Answer 24

cyproterone (steroidal antagonist)

flutamide (non-steroidal antagonsit)

Question 25

adverse effects of cyrpoterone

Answer 25

cognitive changes fatigue oedema reduced spermatogenesis

Question 26

adverse effects of flutamide

Answer 26

``` diarrhoea anaemia hepatic injury oedema dizziness blurred vision ```

Question 27

what is the drug name of a 5-alpha reductase inhibitor

Answer 27

finasteride

Question 28

what is the use of finasteride

Answer 28

benign prostatic hypertrophy

Question 29

adverse effects of finasteride

Answer 29

- impotence, decreased libido and ejaculation disorder - breast enlargement, tenderness - breast cancer?

Question 30

what are the principles of pharmacokinetics in pregnant and lactating women

Answer 30

- drug absorption (by woman and foetus) - drug distribution (by woman and foetus) - drug metabolism/biotransformation (by woman and foetus) - drug excretion (by woman and foetus)

Question 31

what are the factors affecting drug distribution in the pregnant women and foetus

Answer 31

- crossing capillary membrane - crossing lipid membrane - blood flow - pH differences between the compartments - protein binding - binding of other tissue compartments

Question 32

what are the cardiovascular changes of pregnancy

Answer 32

- increased HR, SV, CO, BV and oxygen consumption | - decreased TPR and MAP

Question 33

what are the maternal factors that determine transfer of drugs to the foetus

Answer 33

- drug dose - route of administration - maternal metabolism and excretion - maternal protein binding - maternal pH and ionisation of the drug - uterine blood flow

Question 34

what are the factors affecting uterine blood flow

Answer 34

change in pressure/resistance

Question 35

what things can decrease uterine blood flow

Answer 35

- decreased blood pressure - hypovolaemia - aortocaval compression - vasoconstrictors - endogenous/exogenous

Question 36

functions of the placenta

Answer 36

``` (TIME) T- transport of substances I - immunological M - metabolic E - endocrine ```

Question 37

placental transfer of a drug depends on

Answer 37

- molecular weight of the drug - lipid solubility - degree of ionisation

Question 38

what are the 4 types of human teratogens

Answer 38

- environmental/physical agents - infections - maternal metabolic imbalance - drugs and chemicals

Question 39

main cause of maternal mortality

Answer 39

cardiac disease

Question 40

what is the risk of severe maternal morbidity

Answer 40

1:200

Question 41

what are the main 3 causes obstetric mortality

Answer 41

- haemorrhage - infection - eclampsia

Question 42

what are the goals of acute management of obstetric haemorrhage

Answer 42

- control the bleeding - restore adequate oxygen carrying capacity - maintain adequate tissue perfusion

Question 43

what are the 2 most important drugs for obstetric haemorrhage

Answer 43

oxytocin | ergometrine

Question 44

route of administration of oxytocin and ergometrine

Answer 44

both IV or IM

Question 45

function of oxytocin in haemorrhage

Answer 45

stimulates smooth muscle contraction

Question 46

function of ergometrine in haemorrhage

Answer 46

stimulates smooth muscle contraction as well as vascular SM contraction

Question 47

side effects of oxytocin administration

Answer 47

hypotension tachycardia water intoxication

Question 48

side effects of ergometrine administration

Answer 48

hypertension, nausea and vomiting

Question 49

what are the morbidity short and long term conditions of pre eclampsia

Answer 49

``` IHD CVD heart failure CKD PVD ```

Question 50

what drug do you give mothers with severe pre-eclampsia to prevent and treat sdizures

Answer 50

magnesium sulphate

Question 51

route of administration of MgSO4

Answer 51

IV or IM

Question 52

side effects of MgSO4

Answer 52

respiratory and cardiac depression

Question 53

what is the most important drug to give a mother with preeclampsia

Answer 53

labetalol

Question 54

route of administration of labetalol

Answer 54

oral and IV