pharmacology Flashcards

1
Q

uses of oestrogen replacement therapy

A

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

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2
Q

what are the benefits of postmenopausal hormone therapy

A
  • 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?
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3
Q

what are the risks of postmenopausal oestrogen hormone therapy

A
  • breast tenderness
  • nausea
  • fluid retention
  • increased risk of breast/uterine cancer
  • increased risk of thromboembolism/stroke
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4
Q

what are the 4 ways oestrogen causes cellular effects

A
  • 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)
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5
Q

what are the effects of oestrogen and progesterone in the breast

A

oestrogen –> growth

progesterone –> differentiation

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6
Q

increased risk of breast cancer is associated with what receptors

A

oestrogen and progesterone positive in the breast

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7
Q

what are the two partial agonists of oestrogen (SERM)

A

tamoxifen

raloxifene

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8
Q

what are the effects of tamoxifen

A

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

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9
Q

what are the effects of raloxifene

A

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

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10
Q

what is fulvestrant

A

antagonist to oestrogen receptors throughout the body

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11
Q

when is tamoxifen used

A

palliative treatment of metastatic breast cancer and adjuvant after lumpectomy

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12
Q

adverse effects of tamoxifen

A
  • endometrial hyperplasia, polyps and cancer
  • thromboembolic events
  • thrombocytopaenia
  • ocular toxicity
  • menopausal symptoms
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13
Q

why are aromatase drugs useful for treating breast cancer

A

because its activity is high in breast adipose mesenchymal tissue

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14
Q

what are the effects of aromatase inhibitors

A
  • improved disease free survival after tamoxifen
  • reduced incidence of contralateral breast cancer
  • number of thromboembolic events
  • incidence of endometrial cancer
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15
Q

what are the adverse effects of aromatase inhibitors

A
  • increased bone loss and fracture risk
  • increased arthralgia
  • potential poorer lipid profile, hepatic steatosis and metabolic syndrome with long-term use
  • menopausal signs
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16
Q

where are the major places that DHT act in males

A

prostate
seminal vesicles
epididymus
skin

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17
Q

which enzyme converts testosterone to DHT

A

5-alpha-reductase

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18
Q

what are the main actions of DHT

A

prostate development
external virilisation
sexual maturation

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19
Q

how does testosterone travel in the blood

A

bound to steroid hormone binding globulin

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20
Q

action of testosterone in the cell

A

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

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21
Q

what are the medical uses of androgens

A
  • hypogonadism in children
  • senile osteoporosis
  • speed recovery from surgery and chronic debilitating diseases
  • promotes skeletal growth in pituitary dwarfism
  • endometriosis
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22
Q

what are the non-therapeutic uses of androgen

A

increased lean body mass
muscle strength
aggressiveness

23
Q

adverse effects of androgens

A
  • 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
24
Q

what is the difference between cyproterone and flutamide

A

cyproterone (steroidal antagonist)

flutamide (non-steroidal antagonsit)

25
Q

adverse effects of cyrpoterone

A

cognitive changes
fatigue
oedema
reduced spermatogenesis

26
Q

adverse effects of flutamide

A
diarrhoea
anaemia
hepatic injury
oedema 
dizziness
blurred vision
27
Q

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

A

finasteride

28
Q

what is the use of finasteride

A

benign prostatic hypertrophy

29
Q

adverse effects of finasteride

A
  • impotence, decreased libido and ejaculation disorder
  • breast enlargement, tenderness
  • breast cancer?
30
Q

what are the principles of pharmacokinetics in pregnant and lactating women

A
  • 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)
31
Q

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

A
  • crossing capillary membrane
  • crossing lipid membrane
  • blood flow
  • pH differences between the compartments
  • protein binding
  • binding of other tissue compartments
32
Q

what are the cardiovascular changes of pregnancy

A
  • increased HR, SV, CO, BV and oxygen consumption

- decreased TPR and MAP

33
Q

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

A
  • drug dose
  • route of administration
  • maternal metabolism and excretion
  • maternal protein binding
  • maternal pH and ionisation of the drug
  • uterine blood flow
34
Q

what are the factors affecting uterine blood flow

A

change in pressure/resistance

35
Q

what things can decrease uterine blood flow

A
  • decreased blood pressure
  • hypovolaemia
  • aortocaval compression
  • vasoconstrictors - endogenous/exogenous
36
Q

functions of the placenta

A
(TIME)
T- transport of substances
I - immunological
M - metabolic
E - endocrine
37
Q

placental transfer of a drug depends on

A
  • molecular weight of the drug
  • lipid solubility
  • degree of ionisation
38
Q

what are the 4 types of human teratogens

A
  • environmental/physical agents
  • infections
  • maternal metabolic imbalance
  • drugs and chemicals
39
Q

main cause of maternal mortality

A

cardiac disease

40
Q

what is the risk of severe maternal morbidity

A

1:200

41
Q

what are the main 3 causes obstetric mortality

A
  • haemorrhage
  • infection
  • eclampsia
42
Q

what are the goals of acute management of obstetric haemorrhage

A
  • control the bleeding
  • restore adequate oxygen carrying capacity
  • maintain adequate tissue perfusion
43
Q

what are the 2 most important drugs for obstetric haemorrhage

A

oxytocin

ergometrine

44
Q

route of administration of oxytocin and ergometrine

A

both IV or IM

45
Q

function of oxytocin in haemorrhage

A

stimulates smooth muscle contraction

46
Q

function of ergometrine in haemorrhage

A

stimulates smooth muscle contraction as well as vascular SM contraction

47
Q

side effects of oxytocin administration

A

hypotension
tachycardia
water intoxication

48
Q

side effects of ergometrine administration

A

hypertension, nausea and vomiting

49
Q

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

A
IHD
CVD
heart failure
CKD
PVD
50
Q

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

A

magnesium sulphate

51
Q

route of administration of MgSO4

A

IV or IM

52
Q

side effects of MgSO4

A

respiratory and cardiac depression

53
Q

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

A

labetalol

54
Q

route of administration of labetalol

A

oral and IV