Pharmacology Flashcards

1
Q

What are the clinical uses of antidepressant drugs

A

Moderate to severe depression
Dysthymia
Generalised anxiety disorder
Panic disorder, OCD, PTSD
Premenstrual dysphoric disorder
Bulimia nervosa
Neuropathic pain

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2
Q

What are the main classes of antidepressant

A

Monoamine oxidase inhibitors
Monoamine reuptake inhibitors which includes:
- tricyclics
- SSRI
- noradrenaline reuptake inhibitors
Atypicals

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3
Q

What are the monoamine neurotransmitters

A

Noradrenlaine
5-HT (serotonin)
Dopamine

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4
Q

How do most anti-depressants work

A

Altering the monoamine neurotransmission in some way
Most enhance their activity at the synapses

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5
Q

How might monoamines be affected in those with depression

A

There is a deficit in monoamine transmitters which causes depression - particularly serotonin and noradrenaline
Drugs that deplete stores of monoamines can induce low mood
CSF from depressed patients have reduced levels of monoamines or metabolites

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6
Q

Name some MAO inhibitors

A

Phenelzine - irreversible
Moclobemide - reversible

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7
Q

How do MAO inhibitors work

A

Irreversible (Phenelzine) or reversible (Moclobemide) inhibitors of monoamine oxidase A and B (enzymes)
MOA A and B are responsible for the metabolism of the monoamine neurotransmitters such as serotonin and noradrenaline
Therefore the inhibitors facilitate their release and storage

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8
Q

What are the side effects of MAO inhibitors

A

Prevents breakdown of dietary tyramine - cheese
Anticholinergic effects
Hypertensive crisis
Insomnia
Postural hypotension
Peripheral oedema

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9
Q

Name common tricyclic antidepressants

A

Imipramine
Amitriptyline - used for pain now and more sedating

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10
Q

How do the tricyclic antidepressants work

A

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

Named for the 3 rings in their chemical structure

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11
Q

What are the side effects of tricyclic anti-depressants

A

Anticholinergic - blurred vision, dry mouth, constipation, urinary retention
Sedation
Weight gain
Cardiovascular - Postural hypotension, dizziness tachycardia, arrhythmias

Cardiotoxic in overdose - arrhtymia and arrest
Also seizure and coma

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12
Q

Name common SSRIs

A

Fluoxetine
Citalopram / Escitalopram
Sertraline
Paroxetine

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13
Q

How do SSRIs work

A

Selectively inhibit reuptake of serotonin (5-HT) from the synaptic cleft.

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14
Q

List come common side effects of SSRIs

A

Nausea, V and diarrhoea
Increased risk of GI bleeding
Headache and dizziness
Insomnia
Worsened anxiety/agitation
Transient increase in self-harm / suicidal ideation in <25 years
Sweating / vivid dreams
Sexual dysfunction
Hyponatraemia (in elderly)
Discontinuation effects

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15
Q

How do SNRIs work

A

Dual monoamine reuptake inhibitors
They block the reuptake of noradrenaline and 5-HT (seratonin) into presynaptic terminals.
Therefore similar side effects to SSRIs

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16
Q

Name common SNRIs

A

Venlafaxine
Duloxetine

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17
Q

Name common atypical antidepressants

A

Mirtazapine - blocks alpha 2 adreno- and serotonin receptors
Bupropion - dopamine uptake inhibitor

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18
Q

What are the side effects of mirtazapine

A

Weight gain
Increased appetite
Sedation - best to take in the evening
Can be good if patient is complaining of lack of appetite and loss of sleep

Also presents with some SSRI side effects like nausea and sexual dysfunction due to serotonin blockage. Though generally less than other SSRIs

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19
Q

Do anti-depressants start working immediately

A

No
Most have a delayed onset of action of several weeks

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20
Q

Why do you need to be cautious when prescribing anti-depressants to young adults/ teenagers

A

There can be a transient increase in suicidal ideation, self harm and aggressive ideas in this age group when they take the medications

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21
Q

What is the aim of bipolar treatment

A

Acutely it is to treat the symptoms = reduce mood in mania and raise mood in depression

Long term it is to stabilise mood - prevent recurrence of mania or depression

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22
Q

How is lithium used

A

As first-line maintenance in bipolar - mood stabiliser
It reduces both the number and severity of relapses
Offers some protection against antidepressant-induced hypomania if on dual treatment

Can be used in acute mania as well
May be used in recurrent depressive disorder, or schizoaffective disorder

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23
Q

Do you need to monitor lithium doses

A

YES
Very narrow therapeutic index and can lead to toxicity
Also has a very long half life
Monitor blood levels - 12 hours post-dose
Check weekly when starting or changing dose
Levels are checked every 3-6 months once stable

Also need to check thyroid and renal function every 6 months

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24
Q

What are the common side effects of lithium treatment

A

Dry mouth / strange taste
Nausea/vomiting and diarrhoea
Polydipsia and polyuria
Tremor - fine
Hypothyroidism - due to thyroid enlargement
Hyperparathyroidism
Long term reduced renal function
Nephrogenic diabetes insipidus
Weight gain
idiopathic intracranial hypertension
leucocytosis
hyperparathyroidism and resultant hypercalcaemia

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25
Q

What are the symptoms of lithium toxicity

A

Vomiting
Diarrhoea
Ataxia / coarse tremor
Drowsiness / altered conscious level
Convulsions
Coma

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26
Q

Which anti-convulsant drugs can be used as mood stabilisers

A

Valproic acid/ sodium valproate
Lamotrigine
Carbamazepine

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27
Q

What are the side effects of valproic acid

A

Drowsiness
Ataxia
CV effects
Induces liver enzymes
Hepatotoxicity
Teratogenicity - causes neural tube defects
Blood dyscrasia: Thrombocytopenia, leucopoenia, red cell hypoplasia.
Weight gain
Nausea, vomiting and diarrhoea.
Loss of hair
Headache, confusion and lethargy.
Pancreatitis

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28
Q

What are the side effects of carbamazepine

A

Drowsiness
Headache and diplopia
Ataxia
CV effects
Leucopenia
Hepatoxicity, liver failure and cholestatic jaundice.
Induces liver enzymes - interacts with other drugs
Teratogenicity: Spina bifida
Risk of SJS and TEN

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29
Q

What are the side effects of lamotrigine

A

Small risk of Stevens-Johnson syndrome
Flu-like symptoms
Aseptic meningitis
Ataxia and blurred vision

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30
Q

Which anti-psychotics can be used as mood stabilisers

A

Quetiapine
Aripiprazole
Olanzapine
Lurasidone

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31
Q

What are the side effects of the anti-psychotics used as mood stabilisers

A

Sedation
Weight gain
Metabolic syndrome
Extra-pyramidal side-effects (Aripiprazole)

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32
Q

Which herbal/complementary medicine can cause serotonin syndrome

A

St John’s Wort
Functions similarly to an MAOI
Higher risk if a conventional antidepressant is prescribed alongside it

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33
Q

Which anti-psychotic is most likely to cause extra pyramidal side effects

A

Chlorpromazine
First generation drugs acting on the D2 receptors will cause these symptoms

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34
Q

Women of child bearing age should not be prescribed sodium valproate - true or false

A

True
Unless other options are unavailable, AND adequate contraception (ideally depot or IUD) is in place.

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35
Q

Which anti-psychotic is most likely to cause weight gain

A

Clozapine
Olanzapine

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36
Q

How does acamprosate work to treat alcohol dependence

A

It acts on the neurotransmitter systems in the brain to reduce the reliance on and craving for alcohol
It helps to normalise the brain chemistry that has been disrupted by alcohol
Good for those who wish to control their drinking, but is not prepared to commit to abstinence from alcohol

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37
Q

List side effects of clozapine

A

Sialorrhoea - excessive salivation
Constipation - severe
Nausea and vomiting
Seizure
Weight gain
Hypotension - dose related
Neutropenia/agranulocytosis
Myocarditis and cardiomyopathy

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38
Q

How is dopamine involved in the treatment of psychotic disorders

A

Some evidence that an increase in dopamine level in the mesolimbic system contributes to psychotic disorders like schizophrenia
Many antipsychotics act on dopamine receptors - all act on D2
The more the dopamine receptor binding affinity, the better the therapeutic effect and clinical potency of the antipsychotic agent

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39
Q

What symptoms are associated with the mesolimbic pathway

A

Linked to positive symptoms – delusions, hallucinations, disorganized speech/thinking and disorganized or catatonic behaviour

40
Q

What symptoms are associated with the mesocortical pathway

A

Linked to negative symptoms – Alogia, affective flattening, avolition

41
Q

List examples of first generation antipsychotics

A

Chlorpromazine
Haloperidol
Trifluoperazine

Also called typical antipsychotics

42
Q

List examples of extra-pyramidal side effects that may be caused by anti-psychotics

A

Acute dystonia
Drug-induced parkinsonism
Akathisia - unpleasant state of motor restlessness
Tardive dyskinesia - most common is chewing and pouting of jaw

43
Q

List examples of second generation anti-psychotics

A

Clozapine
Risperidone
Olanzapine
Quetiapine
Aripiprazole

Also known as atypicals

44
Q

Which receptors do second generation anti-psychotics act on

A

Lower D2 receptor affinity.
Work on a variety such as D2,3,4 and 5-HT
High serotonin/dopamine binding ratio.

45
Q

List side effects of olanzipine

A

Sedation
Weight gain
Metabolic syndrome - dyslipidaemia
Dry mouth and constipation (anti-muscarinic)-

46
Q

What is risperidone used to treat

A

Schizophrenia
Acute treatment of mania

47
Q

Which ECG changes can be caused by antipsychotics

A

QT prolongation
Particularly haloperidol

48
Q

Anti-psychotics are used for which conditions

A

Schizophrenia
Mania
Other psychoses including psychotic depression and schizoaffective disorder
As augmenting agents in the treatment of obsessive-compulsive disorder and in the control of severely disturbed behaviour

49
Q

Clozapine is used in which conditions

A

It is licensed for treatment-resistant schizophrenia - used 3rd line if others have not worked
Can improve manic symptoms in treatment resistant bipolar disorder

50
Q

Those on clozapine must be monitored - true or false

A

True
Severe side effect profile so must be checked
e.g. FBC weekly for first 18 weeks due to neutropenia/agranulocytosis risk

51
Q

Which antipsychotics can cause SIADH

A

Haloperidol, risperidone, quetiapine, olanzapine and clozapine
Presents with mild hyponatreamia - confusion, cramps, nausea etc

52
Q

Which antipsychotics can cause an increase in prolactin

A

Risperidone and paliperidone are the worst
Olanzapine has a transient minimal effect

May present with galactorrhoea

53
Q

List common anti-cholinergic side effects

A

Dry mouth, blurred vision, urinary retention and constipation
Seen with chlorpromazine and clozapine

54
Q

What is Neuroleptic Malignant Syndrome

A

Life-threatening condition seen in some patients started on anti-psychotics - typically with sudden dose increases
Presents with hyperthermia, muscular rigidity, decreased conscious level and labile blood pressure
Acute onset

55
Q

Which drugs are used first line in the treatment of depression

A

SSRIs

56
Q

What are the contraindications for tricyclic antidepressant use

A

Arrhythmias
Recent MI
Heart block
Avoided in elderly due to cardiotixc events

Mania and hypomania - can causes manic switch

Acute porphyria

57
Q

In which types of depression are MAOIs mainly used

A

severe depression, treatment resistant depression and atypical depression

58
Q

Which antidepressant is the only one recommended for use in children and young people

A

Fluoxetine is the only one with the evidence that shows that benefits outweigh risks in the treatment of moderate to severe depression

59
Q

What is the risk of prescribing an antidepressant to a child or young person

A

Associated with an increase in suicidal behaviour, self‑harm or hostility, particularly at the beginning of treatment.

Must be closely monitored and is only used in extreme circumstances

60
Q

How does ECT work

A

It involves induction of seizure by applying an electrical stimulus to the brain
The exact mechanism of action is still under investigation - may induce changes in neurotransmitters, neuroplasticity and functional connectivity

61
Q

How is ECT carried out

A

The patient is given general anaesthesia and a muscle relaxant
Monitoring is performed throughout - ECG, EEG etc.
Electrodes are placed on the head - bilateral or unilateral
A short electrical impulse is passed through the head to induce a seizure
Patient is taken to recovery and are usually fine within an hour
Usually delivered 2 to 3 treatments per week

62
Q

There are no absolute contraindications for ECT - true or false

A

True

63
Q

What is ECT used for

A

Acute treatment of moderate to severe depression, mania or catatonia in patients who have failed in responding to other treatments
It is the most effective treatment for major depression

64
Q

List some of the potential side effects of ECT

A

Adverse effects relating to use of general anaesthesia.
Confusion, headache and nausea.
Cognitive impairment - usually short term and resolves but has been permanent in some patients
Memory loss of events prior to ECT
Cardiac arrhythmia

65
Q

Which drugs are used first line in treatment of anxiety disorders

A

SSRIs
Clomipramine for OCD

66
Q

How are benzodiazpeines used in anxiety

A

Used in the short term only for severe anxiety

67
Q

Which benzos are short and long acting

A

Short - lorazepam
Long - diazepam

68
Q

List side effects of benzodiazepines

A

Drowsiness and dizziness
Confusion (elderly)
Respiratory depression
Cognitive and psychomotor impairment.
Tolerance and cross-tolerance with alcohol.
Withdrawal and discontinuation symptoms
Addiction

69
Q

List some common anxiolytic drugs

A

Benzodiazepines - short-term
SSRIs - 1st line
Buspirone - rare
Pregabalin - GAD and social phobia
Beta Blockers - reduces physical symptoms

70
Q

In which form is lithium usually given

A

Normally as lithium carbonate

71
Q

Can lithium be used in pregnancy and breastfeeding

A

Not safe in first trimester due to risk of Ebstein’s heart anomaly
Not advisable in breastfeeding mums either - can affect the baby

72
Q

The adverse effects of lithium are dependent on the serum concentration - ture or false

A

True

73
Q

Which tests must be done before starting lithium treatment

A

Serum electrolyte, urea and creatinine, thyroid function and ECG
UandE and TFTs are rechecked every 6 months

74
Q

Valproate is used in the treatment of which conditions

A

As a mood stabiliser in mania, rapid cycling bipolar and as maintenance in bipolar

75
Q

Carbamazepine is used in the treatment of which conditions

A

Prophylaxis of bipolar disorder which has been unresponsive to lithium
Acts as a mood stabiliser

76
Q

Which drugs does carbamazepine increase the metabolism of

A

Psychotropic medications – antidepressants, antipsychotics, valproate etc.
Oral contraceptive agents leading to failure.
Anticoagulants

77
Q

Lamotrigine is used in the treatment of which conditions

A

Has a modest antidepressant activity
Used as a adjunct in bipolar - can prevent depressive relapse

78
Q

How do you treat acute mania

A

STOP antidepressant medication.
Atypical Antipsychotics: Risperidone, quetiapine, olanzapine etc.
Mood Stabilisers: Lithium and Valproate

79
Q

How do you treat alcohol withdrawal

A

Use benzodiazepines - typically chlordiazepoxide on a reducing schedule (dose dependent on severity of withdrawal)
Can also use diazepam
Carbemazepine can be effective

Also give Pabrinex to avoid development of Wernicke’s encephalopathy

80
Q

How does disulfiram work to reduce alcohol dependence

A

It inhibits aldehyde dehydrogenase resulting in the accumulation of acetaldehyde in the body
Therefore when you drink on top of it it makes you sick - flushing, hypotension, palpitation and nausea and vomiting

81
Q

How is methadone used

A

It is a long acting opioid that aims to wean people off IV opioid use to reduce harm

82
Q

How is naltrexone used

A

It is an opiate antagonist, effective in the treatment of alcohol and opiate
dependence
Reduces craving and relapses in alcohol dependent people

83
Q

Which drugs can be used for symptom relief in dementia

A

Donepezil
Galantamine
Memantine

84
Q

How does memantine work in symptom control in dementia

A

It is an NMDA receptor antagonist
It stops excitatory cell death in Alzheimer’s and vascular dementia

85
Q

How do donepezil/galantamine work in symptom control in dementia

A

The are acetylcholinesterase inhibitors
Prevent metabolisation of ACh so increase the duration of action
Cholinergic neurons are lost in Alzheimers so there is a decrease in ACh

86
Q

How can you treat acute dystonia caused by antipsychotic drugs

A

Procyclidine

87
Q

Anti-psychotic drugs can increase the risk of stroke in the elderly - true or false

A

True
Increased risk of stroke and VTE

88
Q

Which atypical anti-psychotic has the best side-effect profile

A

Aripiprazole
Particularly good for those who have experienced raised prolactin on other drugs

89
Q

List the major side effects of clozapine

A

Agranulocytosis and neutropenias - need regular FBC
Reduced seizure threshold
Constipation
Myocarditis - need a baseline ECG
Hypersalivation

90
Q

How does smoking affect the action of clozapine

A

Smoking can reduce the amount of clozapine in the body
If someone suddenly stops smoking their levels can go up risking side effects
If they start smoking or smoke more, levels may go down
Dose adjustments may be needed

91
Q

List symptoms of benzodiazepine withdrawal

A

Insomnia
irritability
anxiety
tremor
loss of appetite
tinnitus
perspiration
perceptual disturbances
seizures

92
Q

Describe the action of benzodiazepines

A

They enhance the action of GABA - main inhibitory neurotransmitter - buy increasing the frequency of chloride channels

93
Q

What is the SSRI of choice post-MI

A

Sertraline

94
Q

What is the SSRI of choice in children and adolescents

A

Fluoxetine

95
Q

Which SSRI is at higher risk of QT prolongation

A

Citalopram

96
Q

List the symptoms that may be experienced on discontinuation of SSRIs

A

increased mood change
restlessness
difficulty sleeping
unsteadiness
sweating
gastrointestinal symptoms: pain, cramping, diarrhoea, vomiting
paraesthesia

97
Q

What are the risks of using SSRIs in pregnancy

A

Use during the first trimester gives a small increased risk of congenital heart defects
Paroxetine has an increased risk of congenital malformations, particularly in the first trimester

Use during the third trimester can result in persistent pulmonary hypertension of the newborn