Pharmacology of Mood Stabilisers Flashcards

1
Q

what drugs most effectively diffuse across blood brain barrier?

A

hydrophobic / lipophillic

water soluble = dont get through BBB

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2
Q

what are clinical uses for antidepressant drugs?

A
depression (mod - severe)
dysthymia 
GAD
panic disorder, OCD, PTSD
premenstrual dysphoric disorder
bulimia nervosa 
neuropathic pain
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3
Q

what are three main types of antidepressant drugs?

A

monoamine oxidase inhibitors
monoamine reuptake inhibitors
atypical drugs (post-synaptic receptor effects)

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4
Q

what are four different kinds of monoamine reuptake inhibitors?

A

tricyclics
other non selective reuptake inhibitors
selective serotonin reuptake inhibitors
noradrenaline reuptake inhibitors

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5
Q

give 3 examples of monoamine neurotransmitters?

A

noradrenaline
5-HT
dopamine

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6
Q

give 3 examples of monoamine reuptake inhibitors?

A

phenelzine
imipramine
fluoxetine

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7
Q

what area of cortex does 5-HT control mood, sleep, feeding behaviour and sensory perception?

A

rostral

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8
Q

what area of cortex does 5-HT control analgesia?

A

caudal raphe

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9
Q

what converts the following reactions?

a) tryptophan -> 5-OH-tryptophan
b) 5-OH-tryptophan -> 5-HT

A

a) tryptophan hydroxylase

b) L-AA decarbocylase

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10
Q

what areas of cortex does noradrenalin control arousal and emotion?

A

local ceeruleus

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11
Q

what converts the following reactions?

a) tyrosine -> DOPA
b) DOPA -> DA
c) DA -> NA

A

a) tyrosine hydroxylase
b) L-AA decarboxylase
c) DA B-hydroxylase

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12
Q

what is the mode of action of monoamine oxidase inhibitors?

A

irreversible (phenelzine) or reversible (moclobemide) inhibitors of MAO-A and B (these normally break down neurotransmitter)

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13
Q

what are side effects of monoamine oxidase inhibitors?

A

cheese reaction / hypertensive crisis

potentiates effects of other drugs (barbiturates) by decreasing metabolism

insomnia

postural hypotension

peripheral oedema

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14
Q

how do monoamine oxidase inhibitors cause this “cheese reaction” / hypertensive crisis?

A

inhibit MAO-A in gut preventing breakdown of dietary tyramine (can’t eat cheese if on these)

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15
Q

what should be avoided in 57 year old man with ischaemic HD who has become depressed following MI?

A

tricyclics (imipramine) - these are cardiotoxic

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16
Q

give examples of tricyclic antidepressants?

A

imipramine
dosulepin
amitriptyline
lofepramine

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17
Q

what is mode of action of tricyclic antidepressants?

A

block the reuptake of monoamines (mainly norarenaline and 5-HT) into presynaptic terminals

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18
Q

what are common side effects of tricyclics?

A

anticholinergic - blurred vision, dry mouth, constipation, urinary retention

sedation

weight gain

CV - postural hypotension, tachycardia, arrhythmias

cardiotoxic in overdose

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19
Q

what are examples of selective serotonin reuptake inhibitors?

A

fluoxetine
citalopram / escitalopram
sertraline

20
Q

what is mode of action of SSRI?

A

selectively inhibit reuptake of serotonin (5-HT) from synaptic cleft

21
Q

what are common side effects of SSRIs?

A
nausea 
headache 
sweating / vivid dreams 
worsened anxiety 
sexual dysfunction 
hyponatraemia (in elderly)
increase in self harm / suicidal ideation
22
Q

do SSRIs have discontinuation effects?

A

yes but these are self limiting

23
Q

give examples of other monoamine reuptake inhibitors (dual reuptake or SNRIs)

A

venlafaxine

duloxetine

24
Q

what is mode of action of other monoamine reuptake inhibitors?

A

block the reuptake of monoamines (noradrenaline and 5-HT) into presynaptic terminals

25
Q

what are side effects of other monoamine reuptake inhibitors?

A

similar to SSRIs

lack major receptor blocking actions so more limited range of side effects than tricyclics

26
Q

give examples of an atypical antidepressant drug (mixed receptors effects)?

A

mirtazapine (blocks a2, 5-HT2 and 5-HT3)

27
Q

what are side effects of atypical antidepressants?

A

weight gain and sedation

28
Q

what is benefit of mirtazapine if given with SSRIs?

A

can block serotenergic side effects

29
Q

what is example of dopamine uptake inhibitor which only available in USA?

A

bupropion

30
Q

what is the aim of acute BPAD treatment?

A

reduce mood in episodes of mania

raise mood in episodes of depression

31
Q

what is the aim of long term BPAD treatment?

A

to stabilise mood and prevent recurrence of both mania and depression (prophylaxis)

32
Q

lithium is normally given in what form?

A

lithium carbonate

note - different forms have different bioavailablity so be careful about doses if salt has changed

33
Q

what is the thought mode of action of lithium?

A

may block phosphatidylinositol pathway (second messenger system) or inhibit glycogen synthase kinase 3B

34
Q

why must 12 hour post-dose blood levels be monitored?

A

due to narrow therapeutic index

35
Q

how is lithium metabolised?

A

it is an element - it is not metabolised

36
Q

what will the effect of dehydration be on lithium levels?

A

they will be increased

37
Q

what are the side effects of lithium?

A
dry mouth / strange taste 
polydipsia and polyuria 
tremor 
hypothyroidism 
long term reduced renal function
nephrogenic diabetes insipidus 
weight gain
38
Q

what are toxic effects of lithium?

A
vomiting 
diarrhoea 
ataxia / coarse tremor 
drowsiness 
convulsions 
coma
39
Q

what mood stabiliser should be absolutely avoided in pregnant bipolar woman?

A

valproic acid - do not even give in childbearing age

40
Q

what types of anticonvulsants can be used as mood stabilisers?

A

valproic acid
lamotrigine
carbamazepine

41
Q

is the mode of action of anticonvulsants as mood stabilisers clear?

A

no - perhaps block overactive pathways

42
Q

what are side effects of valproate and carbamazepine?

A

drowsiness
ataxia
cardiovascular effects
induces liver enzymes

43
Q

what is main side effect of valproate?

A

teratogenicity (neural tube defects)

44
Q

what does lamotrigine have a very small risk of?

A

stevens-johnson syndrome

45
Q

which antipsychotics can be used as mood stabilisers?

A

quetiapine
aripiprazole
olanzapine
lurasidone

46
Q

what is mode of action of antipsychotics as mood stabilisers?

A

dopamine antagonism + 5-HT antagonism

47
Q

what are side effects of antipsychotics?

A

sedation, weight gain, metabolic syndrome

extra-pyramidial side effects (aripiprazole)