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PHARMACOLOGY FRCA > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

why is thiopentone stored at a pH of 11

A

to promote its ionised form to make it lipid soluble. otherwise it would precipitate out of solution

it is an acid with pKa 7.6

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2
Q

what type of molecule (acid or base) is thiopentone, propofol and etomidate?

A

thio and propofol = weak acids

etomidate = weak base

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3
Q

Is fentanyl an acid or base?

A

weak base

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4
Q

what is the pKa of fentanyl and morphine, what does this mean?

A

both weak bases
fentanyl = 8.4
morphine = 7.9

therefore bases ionise below pH so at pH 7.4 more fentanyl will be ionised

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5
Q

what amine group does morphine have?

A

tertiary amine

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6
Q

what is the pka of the carbonate/bicarb buffer system?

A

6.4

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7
Q

what type of drug is meperidine ?

A

opioid, weak base
Aka pethidine

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8
Q

are NSAIDs acids or bases?

A

all weak acids

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9
Q

what is the pka of paracetamol ? is it an acid or base?

A

9.4
weak acid

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10
Q

what is the pka of remifentanil?

A

7.1

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11
Q

which is the only volatile agent NOT to exist as a stereoisomer?

A

sevoflurane

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12
Q

for levobupivacaine, ropivacaine and etomidate which isomer R or S is the clinically useful one?

A

bupivacaine and ropivacaine - S

Etomidate - R

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13
Q

how does sugamadex work pharmacodynamically?

A

Chelating agent - encapsulates roc

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14
Q

which drugs work by neutralisation

A

antacids
protamine

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15
Q

What is meant by an ionotrophic receptor

A

ligand gated
ion channel

NOT the same as VG ion channel

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16
Q

what 2 factors does drug potency depend on?

A

affinity and efficacy

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17
Q

which value represents drug affinity and potency?

A

kd = affinity
EC50 = potency

the lower for each , the more potent/higher affinity.

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18
Q

what is efficacy?

A

Efficacy is an inherent property of an agonist and reflects its ability to activate the receptor and produce a maximal biological response

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19
Q

which value from the drug response curve defines efficacy

A

Emax

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20
Q

define intrinsic activity

A

Intrinsic activity (IA) is the drug’s maximal efficacy as a fraction of the maximal efficacy produced by a full agonist.

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21
Q

what type of intracellular receptors are oestrogen and thyroxine

A

oestrogen - type 1 - cytoplasmic
thyroxine - type 2 - nuclear

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22
Q

how do intracellular receptors work?

A

intrinsic transcriptional activity, bind via zinc fingers

23
Q

what activates thyroid receptors?

A

can be active with or without ligand.
ligand = T3/T4

when active it binds to thyroid response element (not transcription activating domain)

24
Q

how are anticholinesterases divided?

A

Anticholinesterases are divided into short-, medium- and long-acting.

25
Q

what test is diagnostic for myasthenia gravis?

A

Tensilon test

26
Q

how is neostigmine hydrolysed?

A

same way as ACh just takes much longer

27
Q

how long do long acting anticholinergics last

A

weeks due to covalent bonds

28
Q

what is SLUDGE syndrome of cholinergic overdose characterised by?

A

salivation
lacrimation
urination
defacation
GI upset
emesis

29
Q

where is carbonic anhydrase found?

A

renal tubules
pancreatic
parietal cells
RBC
ciliary epithelium of eye

30
Q

where are COX1 and 2 found

A

COX 1 all cells
COX 2 - inflammatory cells

31
Q

how are mono-oxidase enzymes classified?

A

They are classified as MAO-A, RIMA or MAO-B

32
Q

where are mono oxidase enzymes found?

A

attached to mitochondria.

33
Q

which family are mono-oxidase enzymes from?

A

flavoprotein

34
Q

which MOA is found from birth?

A

MOA-A

35
Q

how do MAO work?

A

remove amine

36
Q

where are MAO found?

A

brain, liver, lung and placenta

37
Q

what does MAO-A breakdown?

A

MAO-A breaks down MANS (melatonin, adrenaline, noradrenaline and serotonin

38
Q

which drugs should MAO be avoided with?

A

never in combination with SSRI/SNRIs - increased levels in brain of NT –> hypertensive crisis

39
Q

which other conditions can MAO be used in?

A

depression
prophylaxis migraines
parkinsons

40
Q

which drug causes red man syndrome?

A

vancomycin

41
Q

what law do michelias menton kinetics obey?

A

law of mass action

42
Q

which part of the liver contains high levels of CYP450

A

Centrilobular hepatocytes (zone 3) contain high concentration of CYP 450 enzymes.

43
Q

what is the main mechanism of CYP450 enzyme induction

A

increase in gene expression - takes some time to develop

44
Q

how does dexamethasone affect CYP450

A

inducer

45
Q

how doe rifampicin, paroxetine and erythromycin effect…

diltiazam, warfarin, betablockers

A

Rifampicin induces CYP2C9 with a risk of inadequate anticoagulation by warfarin.

Paroxetine inhibits CYP2D6, reducing the metabolism of beta-blockers.

Erythromycin inhibits CYP3A4, reducing the metabolism of diltiazem.

46
Q

what type of drug reaction is sux apnoea?

A

Type B - Bizzare

47
Q

what type of drug reaction is hypoglycaemia with aspirin?

A

type A

48
Q

what are the different methods for defining drug reaction?

A

Type A and B - understandble / bizzare - i.e. reasoning
coombs - immunologicals
DOTS - timing, dose and susceptibility

49
Q

what are pseudoallergic reactions?

A

present like allergy due to histamine release
not immune mediated

50
Q

what is innate tolerance?

A

Innate tolerance describes a lack of sensitivity to a drug the first time it is administered

51
Q

how can tolerance be classified

A

Acquired tolerance can be subdivided into three main categories: pharmacokinetic, pharmacodynamic and behavioural tolerance

52
Q

which drugs show tachyphylaxis?

A

ephedrine
hydralazine

53
Q

define summation, synergism and potentiation…

A

summation - effects are additive
synergism - combined effect is more that added affect of each alone
potentiation - one increases effect of another but doesnt have an effect itself

54
Q

which herbal meds interact with NSAIDs?

A

garlic, ginger, ginseng, gingco, st johns

PHARMACOLOGY FRCA (13 decks)

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