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Flashcards in systemic drugs: CNS Deck (110):

what are the 3 types of CNS drugs

- mental health
- anti epileptics
- drugs used in parkinson's disease


what are the 3 types of mental health drugs

- antidepressants
- Anxiolytics and hypnotics (sedatives)
- Antipsychotics


which types of drugs are used to treat short term anxiety



which types of drugs help people to sleep

hypnotics (sedatives)


how much of the adult population does mental health problems affect

1/3rd of the adult population in the UK


Mental health problems can often be _________ to _________

Mental health problems can often be difficult to diagnose


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

- Mixed anxiety and depression
- general anxiety


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

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


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

between 60-100 of new cases


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

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


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

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


what do the NICE guidelines make recommendations for with depression

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


what do the NICE guidelines base their classification on depression as

symptoms as mild, moderate or severe


describe Subthreshold depressive symptoms

fewer than five symptoms of depression


describe Mild depression

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


describe Moderate depression

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


describe severe depression

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


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

from mild depression when theres more than 5 symptoms


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

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


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

- '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


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

antidepressant drugs and psychological therapies can be offered


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

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


why are antidepressants a suitable treatment in moderate to severe depression

as they are as effective as psychological intervention


what 4 things does the choice of antidepressant drug depend on

- past experience of treatment
- patient choice
- side effects
- in more severe depression, the risk of suicide


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

- selective serotonin reuptake inhibitors (SSRIs)
- because they are as effective as tricyclic antidepressants (TCAs) and much safer in overdose


why must a antidepressant drug be safer in overdose

because a suicidal patient is likely to kill themselves an overdose


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

an algorithm for pharmacotherapy of depression


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

- 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


what chemical action is depression associated with

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


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

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


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

- dopamine
- nor-adrenaline
- serotonin

antidepressants target serotonin


what is another word for serotonin

5 hydroxytripamine (5-HT)


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

elevation of normal mood


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



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

- 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


name 4 selective serotonin reuptake inhibitors (SSRIs)

- Citalopram (Cipramil)
- Escitalopram (Cipralex)
- Fluoxetine (Prozac)
- Paroxetine (Seroxat)


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

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


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

Tricyclic antidepressants

they used to be the mainstay of treatment of depressive illness


what is a problem with Tricyclic antidepressants

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


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

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


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

- allow single daily dose regime
- often given at night
- their sedative effect may be helpful (as depressed can't often sleep)


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

they're not good in the case of an overdose


what is the mechanism of Tricyclic antidepressants

- 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


what is the difference between SSRIs and TCA antidepressants

- 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


name 4 Tricyclic antidepressants (TCAs)

- Amitriptyline
- Clomipramine (Anafranil)
- Imipramine
- Lofepramine (Gamanil)


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

Serotonin and Noradrenaline reuptake inhibitors


what is the mechanism of Serotonin and Noradrenaline reuptake inhibitors

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


name 2 Serotonin and Noradrenaline reuptake inhibitors

- Venlafaxine
- Duloxetine


which antidepressant drug is not prescribed often anymore and why

- 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


what do Monoamine Oxidase Inhibitors do

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


what do Monoamine Oxidase Inhibitors have a role in

in atypical and treatment resistant depressions


what is the mechanism of Monoamine Oxidase Inhibitors

- 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


what is monoamine oxidase A

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


what makes Monoamine Oxidase Inhibitors different

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


name 3 Monoamine Oxidase Inhibitors

- Phenelzine (Nardil)
- Isocarboxazid
- Moclobemide (Manerix)


what are hypnotics used for

the short-term management of insomnia


why are prescribers reluctant to give hypnotics for long term use

because tolerance to their effects occurs in 1-3 nights


what are Anxiolytics indicated for

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


when should the use of Anxiolytics be avoided

Using these drugs to treat short-term mild anxiety


when will antidepressants be more appropriate to treat anxiety

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


what are the 2 classes of hypnotics

- Benzodiazepines - Short half-life
- Non-benzodiazepine


name 2 Benzodiazepines - Short half-life hypnotics



name a Non-benzodiazepine hypnotic

Zopiclone e.g. Zimovane


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

- Benzodiazepines - Short half-life


name the class of Anxiolytics

- Benzodiazepines - Long half-life


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

- Diazepam (Valium)
- Lorazepam
- Oxazepam


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

- 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)


what are two other words for Antipsychotics

- neuroleptics
- major tranquillisers


what 4 conditions are the use of Antipsychotics indicated in

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


Antipsychotics also have important ___________ effects in _____________

Antipsychotics also have important prophylactic effects in schizophrenia


what are Antipsychotics divided into

"typical" and "atypical"


what is another name for "typical" Antipsychotics



where do "typical" Antipsychotics act/work on

primarily at dopamine receptors


what are the 3 side effects of "typical" Antipsychotics

- sedation
- extrapyramidal effects e.g. Parkinsonian, restlessness, dystonia
- anticholinergic effects


name 3 "typical" Antipsychotics

- Phenothiazines e.g. chlorpromazine (Largactil)
- Thioxanthenes e.g.flupentixol (Depixol)
- Butyrophenones e.g. haloperidol (Serenade)


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

they deposit into the retina and can cause pigmentary changes


what do "Atypical" antipsychotics act on

other receptors as well as dopamine


what is the advantage of "Atypical" antipsychotics over "typical" Antipsychotics

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


name 5 "Atypical" antipsychotics

- Amisulpride (Solian)
- Clozapine (Clozaril)
- Olanzapine (Zyprexa)
- Quetiapine (Seroquel)
- Risperidone (Risperdal)


what is psychosis induced by

increased levels of dopamine activity


what do most antipsychotic drugs block

postsynaptic dopamine receptors (D2 in particular)


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

- cholinergic
- histaminergic
- serotoninergic receptors


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

- to reduce dopamine levels in the brain in order to target the psychosis
- but might produce symptoms like parkinson's disease


when do symptoms of Schizophrenia develop

develop in early adult life


how many people will develop Schizophrenia in their lifetime

1 in 100 people


which types of antipsychotics are usually better tolerated

better tolerated than typical


what can be problematic with atypical antipsychotics

adverse effects such as:
- weight gain
- hyperglycaemia and
- occasional diabetes


Schizophrenia can be __________ with medication, but never really _________

Schizophrenia can be controlled with medication, but never really cured


what does Bipolar affective disorder cause

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


what 2 things are drugs for Bipolar affective disorder used for

to control acute attacks and also to prevent their recurrence


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

- Benzodiazepines
- Antipsychotics


which drug can be used for prophylaxis of Bipolar affective disorder

Lithium (Priadel)


for what 2 reasons are drug for Bipolar affective disorder used

- acute attack
- Prophylaxis


what is the objective of epileptic treatments

to prevent the recurrence of epileptiform events (seizures)§


which three ways can someone have epilepsy

- born with
- develop later in life
- acquired - from brain trauma or stroke


describe an epileptiform event

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


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

prevent depolarisation of neurones by:
- inhibition of excitatory neurotransmitters
- direct membrane stabilisation
- stimulation of inhibitory neurotransmitters


name 2 common antiepileptics

- Carbamazepine (Tegretol)
- Lamotrigine (Lamictal) 
- Sodium Valproate (Epilim)


what are Antiepileptics associated with

ocular advise effects


name 2 Antiepileptics with significant OARs

- Vigabatrin (Sabril)
- Topiramate (Topamax)


what is parkinson's disease

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


name 3 symptoms of parkinson's disease

- hypokinesia (difficulty in initiating movement)
- rigidity
- tremor


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

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


what does drug therapy do for parkinson's disease

does not prevent progression but improves quality of life


what is the treatment aim of parkinson's disease

to restore dopaminergic activity or reduce cholinergic activity


what is the downside to parkinson's disease drugs

their effectiveness decreases overtime


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

- dopamine receptor agonists
- antimuscarinics


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

- Bromocriptine
- Carbergoline
- Lisuride
- Pergolide
- Ropinrole


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

- Benzatropine
- Orphenadrine
- Procyclidine


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

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