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Therapeutics > systemic drugs: CNS > Flashcards

systemic drugs: CNS Flashcards

1
Q

what are the 3 types of CNS drugs

A
  • mental health
  • anti epileptics
  • drugs used in parkinson’s disease
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2
Q

what are the 3 types of mental health drugs

A
  • antidepressants
  • Anxiolytics and hypnotics (sedatives)
  • Antipsychotics
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3
Q

which types of drugs are used to treat short term anxiety

A

Anxiolytics

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4
Q

which types of drugs help people to sleep

A

hypnotics (sedatives)

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5
Q

how much of the adult population does mental health problems affect

A

1/3rd of the adult population in the UK

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6
Q

Mental health problems can often be _________ to _________

A

Mental health problems can often be difficult to diagnose

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7
Q

what is the most common problem, experienced by 9% of adults in Britain
and what is this followed by, experienced by 5% of people

A
  • Mixed anxiety and depression

- general anxiety

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8
Q

One person in _____ will have a ___________ illness at any one time e.g. ______________ or ___________ __________ disorder

A

One person in 250 will have a psychotic illness at any one time e.g. schizophrenia or bipolar affective disorder

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9
Q

how many people with depression will the average GP see every year

A

between 60-100 of new cases

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10
Q

> ____% of patients with depression are cared for in __________ ______

A

> 80% of patients with depression are cared for in primary care

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11
Q

what do you need to distinguish between in order to diagnose depression

A

distinguish between “normal” mood changes which occur during everyday life and symptoms which are sufficiently prolonged or persistent to require more active management

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12
Q

what do the NICE guidelines make recommendations for with depression

A

recommendations for the treatment and management of depression based on the classification of symptoms as mild, moderate or severe

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13
Q

what do the NICE guidelines base their classification on depression as

A

symptoms as mild, moderate or severe

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14
Q

describe Subthreshold depressive symptoms

A

fewer than five symptoms of depression

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15
Q

describe Mild depression

A

few, if any, symptoms in excess of the five required to make the diagnosis and symptoms result in only minor functional impairment

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16
Q

describe Moderate depression

A

Symptoms or functional impairment are between ‘mild’ and ‘severe’

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17
Q

describe severe depression

A

Most symptoms and the symptoms markedly interfere with functioning. Can occur with or without psychotic symptoms

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18
Q

from which severity of depression does quality of life start to get affected

A

from mild depression when theres more than 5 symptoms

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19
Q

what do GPs use to help them with quantifying the extent of depression and what else does this help them with

A

they use a patient health questionnaire about their symptoms which provides as a validated scale in order to put a number on depression
it also helps them make a decision about treatment

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20
Q

what 2 things is recommended to do for patients with mild depression before putting them on anti depressant drugs

A
  • ‘Watchful waiting’ is recommended, who in the opinion of the healthcare professional may recover with no intervention, or for patients who do not want an intervention
  • Guided self-help or exercise may also help many patients with mild depression
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21
Q

what treatments is used on a patient with mild depression, who fails to produce an adequate response to ‘watchful waiting’ or guided self help/exercise

A

antidepressant drugs and psychological therapies can be offered

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22
Q

why will you just want to monitor the impact of mild depression on a patient with ‘watchful waiting’

A

to see whether the depression is just transient or due to an event

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23
Q

why are antidepressants a suitable treatment in moderate to severe depression

A

as they are as effective as psychological intervention

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24
Q

what 4 things does the choice of antidepressant drug depend on

A
  • past experience of treatment
  • patient choice
  • side effects
  • in more severe depression, the risk of suicide
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25
Q

which anti depressant drugs are recommended as suitable for first line use and why

A
  • selective serotonin reuptake inhibitors (SSRIs)

- because they are as effective as tricyclic antidepressants (TCAs) and much safer in overdose

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26
Q

why must a antidepressant drug be safer in overdose

A

because a suicidal patient is likely to kill themselves an overdose

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27
Q

what can be used as a guidance of what anti depressant drug to prescribe

A

an algorithm for pharmacotherapy of depression

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28
Q

what is the therapeutic aims of a antidepressant drug and how does it do this

A
  • to maximise the concentration of monoamines e.g. 5-HT serotonin (this is how the drugs work)
  • can be done by preventing the breakdown of monoamine inside the presynaptic membrane
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29
Q

what chemical action is depression associated with

A

reduced levels of the monoamines in the brain e.g. 5-HT (serotonin)

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30
Q

how does the anti depressant drug selective serotonin reuptake inhibitors (SSRIs) work

A

SSRIs restore the levels of 5-HT in the synaptic cleft by binding at the 5-HT re-uptake transporter preventing the re-uptake and subsequent degradation of 5-HT

so they prevent the breakdown of monoamine inside the presynaptic membrane by preventing its re-uptake into the presynaptic terminal, this maximises the amount of neurotransmitter in the cleft

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31
Q

what are the three types of monoamines/neurotransmitters found in the brain, and which one does anti depressants target

A
  • dopamine
  • nor-adrenaline
  • serotonin

antidepressants target serotonin

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32
Q

what is another word for serotonin

A

5 hydroxytripamine (5-HT)

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33
Q

what are high levels of the monoamines found in the brain associated with

A

elevation of normal mood

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34
Q

what are low levels of the monoamines found in the brain associated with

A

depression

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35
Q

how are levels of the 5-HT protein increased in the brain in order to prevent depression

A
  • the selection of SSRIs which is a 5-HT serotonin re-uptake protein
  • what happens is, serotonin is released, it binds onto the receptor and then is taken back up into the transporter. this process is cylindrical
  • but as the SSRI drug binds onto the re-uptake transporter (5-HT) protein means it blocks the re-uptake of serotonin AKA serotonin re-uptake inhibitors
  • therefore, in preventing the re-uptake, it elevates the levels of the 5-HT protein
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36
Q

name 4 selective serotonin reuptake inhibitors (SSRIs)

A
  • Citalopram (Cipramil)
  • Escitalopram (Cipralex)
  • Fluoxetine (Prozac)
  • Paroxetine (Seroxat)
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37
Q

what is a side affect of the serotonin reuptake inhibitor (SSRI) - Fluoxetine (Prozac)

A

it inhibits the enzyme which breaks down anti-muscarininc drugs e.g. the pupil remains dilated post tropicamide instillation

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38
Q

name an antidepressant drug which is used prior to using the SSRI type drugs

A

Tricyclic antidepressants

they used to be the mainstay of treatment of depressive illness

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39
Q

what is a problem with Tricyclic antidepressants

A

they have a high rate of side effects that may lead to lower compliance

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40
Q

Selection of a drug from within the class tends to be on the basis of ____________ ___________ ___________

A

Selection of a drug from within the class tends to be on the basis of adverse effect profile

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41
Q

what does the long half lives of Tricyclic antidepressants allow for and when are they usually taken and why

A
  • allow single daily dose regime
  • often given at night
  • their sedative effect may be helpful (as depressed can’t often sleep)
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42
Q

what is a disadvantage of Tricyclic antidepressants having a single daily dose regime

A

they’re not good in the case of an overdose

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43
Q

what is the mechanism of Tricyclic antidepressants

A
  • TCAs binding to 5-HT and noradrenaline re-uptake transporters prevents the re-uptake of these monoamines from the synaptic cleft and their subsequent degradation.
  • This leads to the accumulation of 5-HT and noradrenaline in the synaptic cleft and the concentration returns to within the normal range
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44
Q

what is the difference between SSRIs and TCA antidepressants

A
  • TCAs act on 2 types of re-uptake inhibitors, not just the serotonin re-uptake inhibitor like how the SSRIs do
  • TCAs also act on the re-uptake inhibitor of another monoamine - noradrenaline
  • this elevates the levels of serotonin, noradrenaline and also the 5-HT protein
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45
Q

name 4 Tricyclic antidepressants (TCAs)

A
  • Amitriptyline
  • Clomipramine (Anafranil)
  • Imipramine
  • Lofepramine (Gamanil)
46
Q

what are the latest group of anti depressant drugs, that are similar to TCAs

A

Serotonin and Noradrenaline reuptake inhibitors

47
Q

what is the mechanism of Serotonin and Noradrenaline reuptake inhibitors

A

Serotonin-Norepinephrine Reuptake Inhibitors- block re-uptakers of these neurotransmitters thereby increasing the concentration of these neurotransmitters at the synaptic cleft

48
Q

name 2 Serotonin and Noradrenaline reuptake inhibitors

A
  • Venlafaxine

- Duloxetine

49
Q

which antidepressant drug is not prescribed often anymore and why

A
  • Monoamine Oxidase Inhibitors
  • due to the dietary restrictions (foods containing tyramine), interactions and toxicity in overdose of this group of drugs
    and the affect it has on other drugs such as diagnostic agents e.g. pupil dilating drugs
50
Q

what do Monoamine Oxidase Inhibitors do

A

non-selectively and irreversibly inhibit monoamine oxidase (MAO-A and MAO-B)

51
Q

what do Monoamine Oxidase Inhibitors have a role in

A

in atypical and treatment resistant depressions

52
Q

what is the mechanism of Monoamine Oxidase Inhibitors

A
  • Monoamine oxidase A is an enzyme involved in the metabolism of the monoamines 5-HT and noradrenaline
  • It converts monoamines into their corresponding carboxylic acid
  • MAOI inhibit monoamine degradation and result in greater stores being available for release
53
Q

what is monoamine oxidase A

A

an enzyme involved in the metabolism of the monoamines 5-HT and noradrenaline
It converts monoamines into their corresponding carboxylic acid

54
Q

what makes Monoamine Oxidase Inhibitors different

A

rather than blocking the re-uptake like most drugs, these prevent the breakdown of monoamines
as once they’re taken up, they tend to be broken down by an enzyme which acts on the monoamines

55
Q

name 3 Monoamine Oxidase Inhibitors

A
  • Phenelzine (Nardil)
  • Isocarboxazid
  • Moclobemide (Manerix)
56
Q

what are hypnotics used for

A

the short-term management of insomnia

57
Q

why are prescribers reluctant to give hypnotics for long term use

A

because tolerance to their effects occurs in 1-3 nights

58
Q

what are Anxiolytics indicated for

A

short-term relief (two to four weeks) of anxiety that is severe, disabling or causing unacceptable distress to the patient

59
Q

when should the use of Anxiolytics be avoided

A

Using these drugs to treat short-term mild anxiety

60
Q

when will antidepressants be more appropriate to treat anxiety

A

In those instances where the patient has chronic anxiety, that is lasting more than four weeks

61
Q

what are the 2 classes of hypnotics

A
  • Benzodiazepines - Short half-life

- Non-benzodiazepine

62
Q

name 2 Benzodiazepines - Short half-life hypnotics

A

Nitrazepam

Flurazepam

63
Q

name a Non-benzodiazepine hypnotic

A

Zopiclone e.g. Zimovane

64
Q

which type of hypnotics are very addictive and only given as short term

A
  • Benzodiazepines - Short half-life
65
Q

name the class of Anxiolytics

A
  • Benzodiazepines - Long half-life
66
Q

name 3 types of - Benzodiazepines - Long half-life, used to treat anxiety

A
  • Diazepam (Valium)
  • Lorazepam
  • Oxazepam
67
Q

what is the mechanism of Benzodiazepines, in the action of inducing sleep or reducing anxiety

A
  • act by enhancing the action of GABA at GABAA receptors.
  • These receptor complexes have been identified as having specific benzodiazepine binding sites on them.

GABA is released from the pre synaptic neuron and it binds to GABA receptors on the post synaptic membrane. the drug which acts on the GABA receptors pretenciates the action of GABA (that induces sleep or reduces anxiety)

68
Q

what are two other words for Antipsychotics

A
  • neuroleptics
    or
  • major tranquillisers
69
Q

what 4 conditions are the use of Antipsychotics indicated in

A
  • schizophrenia
  • mania
  • psychotic depression
  • and may be useful for short-term sedation in aggression or agitation
70
Q

Antipsychotics also have important ___________ effects in _____________

A

Antipsychotics also have important prophylactic effects in schizophrenia

71
Q

what are Antipsychotics divided into

A

“typical” and “atypical”

72
Q

what is another name for “typical” Antipsychotics

A

conventional

73
Q

where do “typical” Antipsychotics act/work on

A

primarily at dopamine receptors

74
Q

what are the 3 side effects of “typical” Antipsychotics

A
  • sedation
  • extrapyramidal effects e.g. Parkinsonian, restlessness, dystonia
  • anticholinergic effects
75
Q

name 3 “typical” Antipsychotics

A
  • Phenothiazines e.g. chlorpromazine (Largactil)
  • Thioxanthenes e.g.flupentixol (Depixol)
  • Butyrophenones e.g. haloperidol (Serenade)
76
Q

what is a side effect of the “typical” Antipsychotic - Phenothiazines e.g. chlorpromazine (Largactil)

A

they deposit into the retina and can cause pigmentary changes

77
Q

what do “Atypical” antipsychotics act on

A

other receptors as well as dopamine

78
Q

what is the advantage of “Atypical” antipsychotics over “typical” Antipsychotics

A

they are less likely than typical antipsychotics to cause movement disorders as a side effect

79
Q

name 5 “Atypical” antipsychotics

A
  • Amisulpride (Solian)
  • Clozapine (Clozaril)
  • Olanzapine (Zyprexa)
  • Quetiapine (Seroquel)
  • Risperidone (Risperdal)
80
Q

what is psychosis induced by

A

increased levels of dopamine activity

81
Q

what do most antipsychotic drugs block

A

postsynaptic dopamine receptors (D2 in particular)

82
Q

other than blocking post synaptic dopamine receptors, what 3 other receptors do antipsychotic drugs affect

A
  • cholinergic
  • histaminergic
  • serotoninergic receptors
83
Q

what is the aim of antipsychotics and what is their side effect as a consequence

A
  • to reduce dopamine levels in the brain in order to target the psychosis
  • but might produce symptoms like parkinson’s disease
84
Q

when do symptoms of Schizophrenia develop

A

develop in early adult life

85
Q

how many people will develop Schizophrenia in their lifetime

A

1 in 100 people

86
Q

which types of antipsychotics are usually better tolerated

A

atypical

better tolerated than typical

87
Q

what can be problematic with atypical antipsychotics

A

adverse effects such as:

  • weight gain
  • hyperglycaemia and
  • occasional diabetes
88
Q

Schizophrenia can be __________ with medication, but never really _________

A

Schizophrenia can be controlled with medication, but never really cured

89
Q

what does Bipolar affective disorder cause

A

dramatic mood swings – from extremely “high” and/or irritable (mania) to sad and hopeless (depression), and then back again, usually with periods of normal mood in between

90
Q

what 2 things are drugs for Bipolar affective disorder used for

A

to control acute attacks and also to prevent their recurrence

91
Q

which 2 drugs can be used to control the acute attack of Bipolar affective disorder

A
  • Benzodiazepines

- Antipsychotics

92
Q

which drug can be used for prophylaxis of Bipolar affective disorder

A

Lithium (Priadel)

93
Q

for what 2 reasons are drug for Bipolar affective disorder used

A
  • acute attack
    and
  • Prophylaxis
94
Q

what is the objective of epileptic treatments

A

to prevent the recurrence of epileptiform events (seizures)§

95
Q

which three ways can someone have epilepsy

A
  • born with
  • develop later in life
  • acquired - from brain trauma or stroke
96
Q

describe an epileptiform event

A

a sudden, excessive depolarisation of cerebral neurones which may remain localised (focal epilepsy) or spread (generalised epilepsy)

97
Q

what do anti-epileptic agents do and which 3 ways do they do this

A

prevent depolarisation of neurones by:

  • inhibition of excitatory neurotransmitters
  • direct membrane stabilisation
  • stimulation of inhibitory neurotransmitters
98
Q

name 2 common antiepileptics

A
  • Carbamazepine (Tegretol)
  • Lamotrigine (Lamictal)
  • Sodium Valproate (Epilim)
99
Q

what are Antiepileptics associated with

A

ocular advise effects

100
Q

name 2 Antiepileptics with significant OARs

A
  • Vigabatrin (Sabril)

- Topiramate (Topamax)

101
Q

what is parkinson’s disease

A

involves progressive degeneration of pigmented cells in the substantia nigra leading to a deficiency of the neurotransmitteer dopamine

102
Q

name 3 symptoms of parkinson’s disease

A
  • hypokinesia (difficulty in initiating movement)
  • rigidity
  • tremor
103
Q

what is parkinson’s disease an imbalance of and what does this result in

A

imbalance of dopaminergic and cholinergic activity within the extra-pyramidal system, resulting in:

  • reduced dopaminergic activity
  • Increased cholinergic activity
104
Q

what does drug therapy do for parkinson’s disease

A

does not prevent progression but improves quality of life

105
Q

what is the treatment aim of parkinson’s disease

A

to restore dopaminergic activity or reduce cholinergic activity

106
Q

what is the downside to parkinson’s disease drugs

A

their effectiveness decreases overtime

107
Q

what are the 2 types of drugs for parkinson’s disease

A
  • dopamine receptor agonists

- antimuscarinics

108
Q

name 5 dopamine receptor agonists (drugs) used to treat parkinson’s

A
  • Bromocriptine
  • Carbergoline
  • Lisuride
  • Pergolide
  • Ropinrole
109
Q

what are the 3 antimuscarinics (drugs) used to treat parkinson’s

A
  • Benzatropine
  • Orphenadrine
  • Procyclidine
110
Q

name the 4 types/categories of drugs that can be used to treat depression

A
  • selective serotonin reuptake inhibitors (SSRIs)
  • tricyclic antidepressants (TCAs)
  • serotonin and noradrenaline reuptake inhibitors
  • monoamine oxidase inhibitors

Therapeutics (19 decks)

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