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Pharmacology Flashcards

1
Q

What is the mechanism of action of the monoamine oxidase inhibitors?

A

Inhibit monoamine oxidase

Monoamine oxidase breaks down serotonin and noradrenaline in the brain - so inhibiting the enzyme inhibits breakdown

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2
Q

What are some of the side effects of the monoamine oxidase inhibitors?

A

Cheese reaction
Insomnia
Postural hypotension
Peripheral oedema

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3
Q

What is the “cheese reaction”

A

A side effect of monoamine oxidase inhibitors

Hypertensive crisis caused by inhibition of MAO-A in the gut which prevents the breakdown of dietary tyramine
(tyramine exists in wine and cheese)

Patients need to avoid these foods

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4
Q

With which drug class are patients required to have a restricted diet?

A

Monoamine oxidase inhibitors

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5
Q

Give some examples of tricyclic antidepressants

A

Imipramine
Dosulepin
Amitriptyline
Lofepramine

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6
Q

What is the mechanism of action of tricyclic antidepressants?

A

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

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7
Q

What are some of the side effects of tricyclic antidepressants?

A 
Anticholinergic effects
(blurred vision, dry mouth, constipation, urinary retention)

Antihistaminergic effects
(sedation and weight gain)

Cardiac effects
(postural hypotension, tachycardia)

Fatal arrhythmias with overdose

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8
Q

Give some examples of selective serotonin re-uptake inhibitors (SSRIs)

A

Fluoxetine
Citalopram
Sertraline
Paroxetine

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9
Q

What is the mechanism of action of the SSRIs?

A

Selective inhibition of the re-uptake of serotonin (5-HT)

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10
Q

What are some of the side effects of SSRIs?

A 
Nausea 
Headache 
Sweating 
Vivid dreams 
Worsening of anxiety 
Sexual dysfunction 
Hyponatraemia

*relatively safe in overdose compared to the others

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11
Q

With which drug class is there a transient increase in the risk of self-harm in patients <25 years old?

A

Selective serotonin reuptake inhibitors

*This drug class should be avoided in adolescence

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12
Q

Give some examples of dual reuptake inhibitors (SNRIs)

A

Venlafaxine

Duloxetine

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13
Q

What is the mechanism of action of the SNRIs?

A

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

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14
Q

Which drug class lack major receptor-blocking actions and therefore have fewer side effects than tricyclics?

A

Dual reuptake inhibitors

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15
Q

Give some examples of atypical antidepressants

A

Mirtazapine

Bupropion

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16
Q

Give some examples of antidepressants which are noradrenaline selective?

A

Reboxetine
Desipramine
Protriptyline

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17
Q

Give some examples of antidepressants which are 5-HT selective

A

Fluoxetine
Citalopram
Sertraline
Paroxetine

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18
Q

What is the gold standard medication for bipolar disorder?

A

Lithium

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19
Q

What is the mechanism of action of lithium?

A

Blocks phosphatidylinositol pathway

or

inhibits Glycogen Synthase Kinase 3β

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20
Q

What are some of the side effects of lithium?

A 
Dry mouth/ strange taste 
Weight gain 
Sedation
Polydipsia/ polyuria 
Tremor 
GI upset 
Ankle swelling

Hypothyroidism
Reduced renal function

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21
Q

What medication should not be taken in combination with lithium?

A

NSAIDs

Diuretics

ACE. I/ ARBs

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22
Q

Give some examples of anticonvulsants which are used long term as mood stabilisers for bipolar disorder

A

Valproate, lamotrigine, carbamazepine

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23
Q

Which drug which can be used as a mood stabiliser in bipolar disorder should not be given to women of child bearing age?

A

Valproate

  • teratogenic
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24
Q

Give some examples of antipsychotics which are used long term as mood stabilisers for bipolar disorder

A

Quetiapine
Aripiprazole
Olanzapine
Lurasidone

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25
Q

What are some side effects of antipsychotics used for bipolar disorder?

A

Sedation

Weight gain

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26
Q

What is the monoamine hypothesis?

A

Depression results from a functional deficit of monoamine transmitters - particularly serotonin and noradrenaline

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27
Q

How long should you trial an antidepressant before deciding it isn’t working?

A

About 2-3 months

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28
Q

What factors may contribute to a patient not responding to medications?

A

May not be compliant
Dosage too low
Social factors
Might not be the right drug for them

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29
Q

Why do some antidepressants work for some people and not for others?

A

Everyone has different genetics - one patient may have more of a serotonin problem and the other more a noradrenaline issue

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30
Q

How long should a patient be continued on antidepressants for?

A

At least 6 months from the resolution of symptoms

NB - what makes you well keeps you well

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31
Q

What are some of the side effects of anticonvulsants which can be used in the management of bipolar disorder?

A

Sodium valproate is teratogenic

Lamotrigine takes a long time to work and can cause Steven Johnson’s syndrome

Carbamazepine can be quite sedative

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32
Q

What investigations need to be routinely done for patients taking lithium?

A

Bloods

Lithium levels 12 hours after dose

Thyroid function, parathyroid function and renal function every 6 months

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33
Q

Which antidepressants are the worst in overdose?

A

Tricyclics are fatal in overdose

SSRIs are not so bad in overdose

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34
Q

Why should tricyclics be avoided in patients with prostatism?

A

They cause urinary retention (anticholinergic effects)

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35
Q

Which class of antidepressants are useful in patients who are struggling to sleep?

A

Tricyclic antidepressants - these are sedative

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36
Q

Which drugs are most associated with weight gain?

A

Mirtazapine, tricyclics, lithium and antipsychotics

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37
Q

Why does lithium require monitoring?

A

It has a narrow therapeutic index

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38
Q

What drugs are used to treat anxiety disorders?

A

SSRIs (first line), other antidepressants

Pregabalin (as mono therapy or to augment antidepressants)

B-blockers and benzodiazepines for symptomatic relief

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39
Q

What drugs are used to treat OCD?

A

SSRIs/ clomipramine - tricyclic

Antipsychotics

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40
Q

What is the mechanism of action of benzodiazepine?

What are the pharmacological effects of this drug class?

A

Enhance the effect of GABA by allosteric modulation

Relaxation
Anticonvulsant effects
Sedation

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41
Q

What are some of the side effects of benzodiazepines?

A

Sedation

Psychomotor retardation / impaired coordination

Dependency

Alcohol interaction

Aggression

Anterograde amnesia

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42
Q

Give some examples of benzodiazepines

A

Diazepam (valium)

Lorazepam

Chlordiazepoxide

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43
Q

Which benzodiazepine is suitable for use in the community?

A

Diazepam (valium) this is because it has a longer half life than the others

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44
Q

What are some of the clinical uses of benzodiazepines?

A

Acute treatment of extreme anxiety

Alcohol withdrawal

Mania

Delirium

Status epilepticus

Rapid tranquilisation

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45
Q

What is the mechanism of action of pregabalin, a drug which can be used in the management of anxiety?

A

Calcium channel blocker and GABA enhancer

*NB only considered if the patient doesn’t respond to other treatments

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46
Q

What specific symptoms are b-blockers useful for?

A

Physical symptoms such as palpitations and tremors

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47
Q

Give some examples of typical antipsychotics

A

Chlorpromazine, thioridazine, haloperidol

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48
Q

Give some examples of atypical antipsychotics

A

Olanzapine, quetiapine, aripiprazole, clozapine

Amisulpramide

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49
Q

What is the mechanism of action of the antipsychotics?

A

Block dopamine D2 receptors, blocking dopaminergic transmission in the mesolimbic pathways

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50
Q

Which type of antipsychotic are more associated with extra-pyramidal side effects?

A

Typical antipsychotics

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51
Q

Which typical antipsychotic is associated with being the worst for causing extra- pyramidal side effects?

A

Haloperidol

52
Q

What are the 4 main EPSE caused by typical antipsychotics?

A

Parkinsonism

Acute dystonic reaction

Akathisia

Tardive dyskinesia

53
Q

How can parkinsonism, an EPSE be managed?

A

Treatment with anticholinergics

54
Q

How can acute dystonic reaction, an EPSE be managed?

A

IV anticholinergics - e.g prochlorperazine

55
Q

How can akathisia, an EPSE be managed?

A

Reduce the dose or change to a different drug

56
Q

When do patients develop tardive dyskinesia, an EPSE?

A

After long-term use of typical antipsychotics (years)

57
Q

What is the main side effect of the atypical antipsychotics?

A

Metabolic syndrome

58
Q

Both typical and atypicals may cause sedation. T/F?

59
Q

Antipsychotics act by blocking dopamine receptors. what effect does this have on prolactin levels?

How may this present?

A

Hyperprolactinaemia

Dopamine blocks prolactin production
- therefore drugs which block dopamine block the blockage or prolactin

This may present with gelactorrhea, gynaecomastia and osteoporosis

60
Q

Antipsychotics cause histamine blockage. How does this present?

A

Sedation and increased appetite

61
Q

Antipsychotics cause alpha adrenergic blockage. How does this present?

A

Dizziness

Postural hypotension

62
Q

Antipsychotics cause muscarinic blockage. How does this present?

A

Blurred vision

Dry mouth

Constipation

Urinary retention

63
Q

Clozapine is the most effective atypical antipsychotic so it is still used despite which serious side effects?

A

Agranulocytosis

Myocarditis

Also causes metabolic syndrome and hyper salivation

64
Q

How should patients taking clozapine be monitored?

A

FBCs weekly for the first 6 months, then very 2 weeks e.t.c

65
Q

A patient presents with a sore throat. They are known to be taking clozapine, how should they be managed?

A

STOP CLOZAPINE AND CHECK FBC FOR AGRANULOCYTOSIS

66
Q

What drugs can make the symptoms of schizophrenia worse?

A

Drugs which release dopamine into the brain

E.g amphetamines and apomorphine

67
Q

What is the assumed neurochemical basis of schizophrenia?

A

Over-activity of dopamine pathways in the brain

68
Q

Why is haloperidol contraindicated in patients with Parkinson’s?

What medication can be used instead to manage psychosis?

A

Haloperidol is contraindicated because it can cause EPSE.

Quetiapine can be used instead.

69
Q

What drugs can be used in the management of Alzheimer’s?

A

Acetylcholinesterase inhibitors

Memantine

70
Q

What is the mechanism of action of the acetylcholinesterase inhibitors, which can be used in the management of Alzheimer’s?

A

Inhibit the re-uptake of acetylcholine, meaning there is more in the synaptic space

(NB the disease is not due to acetylcholine deficiency, but increasing it does help)

71
Q

Give some examples of acetylcholinesterase inhibitors which can be used in the management of Alzheimer’s disease

A

Donepezil, rivastigmine, galantamine

72
Q

What are some of the side effects of the acetylcholinesterase inhibitors which can be used in the management of Alzheimer’s disease?

A

Bradycardia, muscle cramps, nausea, diarrhoea and headaches

Contraindicated in patients with asthma and COPD

73
Q

What is the mechanism of action of memantine, a drug which can be used in the management of Alzheimer’s disease?

A

Antagonist of NMDA receptors which bind glutamate

74
Q

When can memantine be prescribed?

A

For patients with moderate Alzheimer’s or patients that can’t tolerate acetylcholinesterase inhibitors

75
Q

What medications can be used in the management of ADHD?

A

STIMULANTS
Methylphenidate (ritalin), dexamfetamine and lisdexamfetamine

NON-STIMULANTS
Atomoxetine, antidepressants e.t.c

76
Q

What is the mechanism of action of methylphenidate (ritalin) which can be used in the management of ADHD?

A

Improves dopaminergic neurotransmission in networks involved in executive functioning e.g prefrontal cortex

77
Q

What are some of the possible side effects or methylphenidate (ritalin)?

A

Appetite and sleep reduction

Dysphoria

Anxiety

Tics

78
Q

What is the mechanism of action of atomexetine, a medication which can be used in the management of ADHD?

A

Noradrenergic and dopaminergic agonist

79
Q

Which anticonvulsants are most useful in patients with bipolar disorder who are primarily manic/ hypomanic vs primarily depressed?

A

Primarily manic/ hypomanic - sodium valproate

Primarily depressed - lamotrigine

80
Q

What tests should be done before starting a patient on sodium valproate

A

LFTs
U&Es
Platelets

81
Q

What are some of the signs of lithium toxicity?

A

Blurred vision

Coarse tremor

Ataxia

Drowsiness

82
Q

If clozapine has been missed for >48 hours, what is the most appropriate management?

A

Restarted at the starting dose of 12.5mg

83
Q

What is the role of D1 receptors?

A

Stimulate cAMP

84
Q

What is the role of D2 receptors?

A

Inhibit adenyl cyclase, inhibit Ca2+ channels and open K+ channels

85
Q

Which EPSE is most associated with dysphonia?

A

Akathisia

akathisia is the EPSE associated with causing internal restlessness

86
Q

What are some of the side effects of clozapine?

A 
Weight gain 
Hyper-salivatino 
Constipation 
Seizures 
Agranulocytosis
87
Q

Which EPSE are most receptive to treatment with anticholinergics?

A

Parkinsonism and acute dystonic reaction

88
Q

Which antipsychotic is most associated with a risk of causing myocarditis and should therefore only be started in hospital?

89
Q

Which pathways in the brain are responsible for motivation and reward systems?

A

Mesolimbic and cortical dopamine pathways

90
Q

How does alpha-adrenergic blockade (S/E of antipsychotics) present?

A

Dizziness

Lightheadedness

Postural hypotension

91
Q

Which antipsychotic is most associated with causing metabolic syndrome and should therefore be avoided in people with diabetes?

A

Olanzapine

92
Q

Which pathway in the brain is responsible for prolactin release?

A

Tuberoinfundibular dopamine pathway

93
Q

Prolonged QT is a side effect more associated with which type of antipsychotics?

94
Q

Which dopamine pathway is responsible for the extra-pyramidal motor system?

A

Nigrastriatal dopamine pathway

95
Q

Which receptors do typicals and antitypical antipsychotics mainly block?

A

Typicals - D2

Atypical - block more 5HT2 (serotonin) than D2 (dopamine)

96
Q

Why are atypical antipsychotics less likely to cause EPSE than typical antipsychotics?

A

Atypical antipsychotics block more 5-HT2A (serotonin) than D2 (dopamine) receptors

97
Q

Which dopamine pathway is responsible for the control of prolactin release?

A

Tuberoinfundibular dopamine pathway

98
Q

What is the role of dopamine (D2) receptors in the brain?

A

Inhibition of adenylyl cyclase

Opening of potassium channels

99
Q

How are SSRIs eliminated from the body?

A

Hepatic metabolism

100
Q

Which class of antidepressants should SSRIs NOT Be given alongside?

A

MOAIs

Together can cause serotonin syndrome (excess levels of serotonin)

101
Q

Which class of antidepressants increase bleeding risk and shouldn’t be used in conjunction with aspirin?

A

SSRIs

*they interact with serotonin receptors on platelets

102
Q

Why is venlafaxine not used first line?

A

It has a short half life - can cause serotonin withdrawal syndrome when patients come off it

103
Q

Which medication that can help with sleep should be avoided in the elderly? What can be used as an alternative?

A

Zopiclone - *Can cause falls

Melatonin can be used instead

104
Q

Tricyclics work by increasing the concentration of which neurotransmitters in the synaptic cleft?

A

Serotonin

Noradrenaline

Dopamine

(they are non-specific)

105
Q

What are the symptoms of discontinuation syndrome which can occur following withdrawal of an SSRI?

A

Headache

Sweating and shivering

Increased anxiety

GI symptoms

106
Q

In elderly patients prone to falls, which antidepressant drug class should you try ad stick to?

A

SSRIs

  • Don’t cause sedation or lower BP
107
Q

What are some of the symptoms of hypertensive crisis caused by intake of foods containing tyramine in a patient taking an MAOI?

A

Anxiety

Headache

Dyspnoea

Nosebleeds

108
Q

SSRIs may cause a transient increase in the risk of self-harm in adolescents, if they have to be used, which one should you choose?

A

Fluoxetine

109
Q

Depression causes what to happen to levels of cortisol in the body?

A

Causes cortisol levels to be chronically increased

110
Q

Which SSRI is especially associated with prolongation of the QT interval?

A

Citalopram

111
Q

Nasal congestants shouldn’t be taken alongside which class of antidepressants?

112
Q

Which two antidepressants used together are referred to as ‘california rocket fuel’?

A

Mirtazapine and venlafaxine

113
Q

Lithium should be avoided in both pregnancy and breastfeeding

114
Q

Which tests should be done every 6 months in a patient taking lithium?

A

TFTs

Parathyroid function

Renal function

115
Q

Which tests should be done every 3 months in a patient taking lithium?

A

Plasma lithium levels

U&Es

116
Q

Why is it important to test renal function in patients taking lithium?

A

There is a risk of nephrogenic DI and reduced glomerular function

117
Q

When a patient is first commenced on lithium, how often should U&Es be formed?

A

Every 5 days until the therapeutic dose is reached

118
Q

What tests should be done before starting a patient on sodium valproate?

A

Platelet count

LFTs

119
Q

What drug is used to treat benzodiazepine overdose and works as a GABA antagonist?

A

Flumazenil

120
Q

Which mood stabiliser drug does EUPD typically respond well to?

A

Lamotrigine

  • Lamotrigine is also used for bipolar II
  • Bipolar II and EUPD are often seen as similar as they both involve ups and downs
121
Q

Why can tricyclic drugs cause fatal arrhythmias?

A

They affect sodium channels in the heart

122
Q

What is the role of GABA?

A

Inhibitory neurotransmitter

Role is for passage of CL- ions into the cell to cause hyper polarisation.

123
Q

What risk to the baby is there with SSRIs when used in the third trimester of pregnancy?

A

Risk of PPH of the newborn

124
Q

What is the big risk of using antipsychotics in the elderly?

A

Increased risk of stroke and VTE

125
Q

What is first line for delirium tremens/ alcohol withdrawal?

A

Oral chlordiazepoxide

126
Q

SSRIs + NSAIDs (e.g aspirin) increases the risk of GI bleed, what medication should be given to counter this?

127
Q

Triptans should be avoided with which antidepressant class?

PSYCHIATRY (11 decks)

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