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Pharmacology Flashcards

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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
What are some side effects of antipsychotics used for bipolar disorder?
Sedation | Weight gain
26
What is the monoamine hypothesis?
Depression results from a functional deficit of monoamine transmitters - particularly serotonin and noradrenaline
27
How long should you trial an antidepressant before deciding it isn't working?
About 2-3 months
28
What factors may contribute to a patient not responding to medications?
May not be compliant Dosage too low Social factors Might not be the right drug for them
29
Why do some antidepressants work for some people and not for others?
Everyone has different genetics - one patient may have more of a serotonin problem and the other more a noradrenaline issue
30
How long should a patient be continued on antidepressants for?
At least 6 months from the resolution of symptoms NB - what makes you well keeps you well
31
What are some of the side effects of anticonvulsants which can be used in the management of bipolar disorder?
Sodium valproate is teratogenic Lamotrigine takes a long time to work and can cause Steven Johnson's syndrome Carbamazepine can be quite sedative
32
What investigations need to be routinely done for patients taking lithium?
Bloods Lithium levels 12 hours after dose Thyroid function, parathyroid function and renal function every 6 months
33
Which antidepressants are the worst in overdose?
Tricyclics are fatal in overdose SSRIs are not so bad in overdose
34
Why should tricyclics be avoided in patients with prostatism?
They cause urinary retention (anticholinergic effects)
35
Which class of antidepressants are useful in patients who are struggling to sleep?
Tricyclic antidepressants - these are sedative
36
Which drugs are most associated with weight gain?
Mirtazapine, tricyclics, lithium and antipsychotics
37
Why does lithium require monitoring?
It has a narrow therapeutic index
38
What drugs are used to treat anxiety disorders?
SSRIs (first line), other antidepressants Pregabalin (as mono therapy or to augment antidepressants) B-blockers and benzodiazepines for symptomatic relief
39
What drugs are used to treat OCD?
SSRIs/ clomipramine - tricyclic Antipsychotics
40
What is the mechanism of action of benzodiazepine? What are the pharmacological effects of this drug class?
Enhance the effect of GABA by allosteric modulation Relaxation Anticonvulsant effects Sedation
41
What are some of the side effects of benzodiazepines?
Sedation Psychomotor retardation / impaired coordination Dependency Alcohol interaction Aggression Anterograde amnesia
42
Give some examples of benzodiazepines
Diazepam (valium) Lorazepam Chlordiazepoxide
43
Which benzodiazepine is suitable for use in the community?
Diazepam (valium) this is because it has a longer half life than the others
44
What are some of the clinical uses of benzodiazepines?
Acute treatment of extreme anxiety Alcohol withdrawal Mania Delirium Status epilepticus Rapid tranquilisation
45
What is the mechanism of action of pregabalin, a drug which can be used in the management of anxiety?
Calcium channel blocker and GABA enhancer *NB only considered if the patient doesn't respond to other treatments
46
What specific symptoms are b-blockers useful for?
Physical symptoms such as palpitations and tremors
47
Give some examples of typical antipsychotics
Chlorpromazine, thioridazine, haloperidol
48
Give some examples of atypical antipsychotics
Olanzapine, quetiapine, aripiprazole, clozapine Amisulpramide
49
What is the mechanism of action of the antipsychotics?
Block dopamine D2 receptors, blocking dopaminergic transmission in the mesolimbic pathways
50
Which type of antipsychotic are more associated with extra-pyramidal side effects?
Typical antipsychotics
51
Which typical antipsychotic is associated with being the worst for causing extra- pyramidal side effects?
Haloperidol
52
What are the 4 main EPSE caused by typical antipsychotics?
Parkinsonism Acute dystonic reaction Akathisia Tardive dyskinesia
53
How can parkinsonism, an EPSE be managed?
Treatment with anticholinergics
54
How can acute dystonic reaction, an EPSE be managed?
IV anticholinergics - e.g prochlorperazine
55
How can akathisia, an EPSE be managed?
Reduce the dose or change to a different drug
56
When do patients develop tardive dyskinesia, an EPSE?
After long-term use of typical antipsychotics (years)
57
What is the main side effect of the atypical antipsychotics?
Metabolic syndrome
58
Both typical and atypicals may cause sedation. T/F?
True
59
Antipsychotics act by blocking dopamine receptors. what effect does this have on prolactin levels? How may this present?
Hyperprolactinaemia Dopamine blocks prolactin production - therefore drugs which block dopamine block the blockage or prolactin This may present with gelactorrhea, gynaecomastia and osteoporosis
60
Antipsychotics cause histamine blockage. How does this present?
Sedation and increased appetite
61
Antipsychotics cause alpha adrenergic blockage. How does this present?
Dizziness Postural hypotension
62
Antipsychotics cause muscarinic blockage. How does this present?
Blurred vision Dry mouth Constipation Urinary retention
63
Clozapine is the most effective atypical antipsychotic so it is still used despite which serious side effects?
Agranulocytosis Myocarditis Also causes metabolic syndrome and hyper salivation
64
How should patients taking clozapine be monitored?
FBCs weekly for the first 6 months, then very 2 weeks e.t.c
65
A patient presents with a sore throat. They are known to be taking clozapine, how should they be managed?
STOP CLOZAPINE AND CHECK FBC FOR AGRANULOCYTOSIS
66
What drugs can make the symptoms of schizophrenia worse?
Drugs which release dopamine into the brain E.g amphetamines and apomorphine
67
What is the assumed neurochemical basis of schizophrenia?
Over-activity of dopamine pathways in the brain
68
Why is haloperidol contraindicated in patients with Parkinson's? What medication can be used instead to manage psychosis?
Haloperidol is contraindicated because it can cause EPSE. Quetiapine can be used instead.
69
What drugs can be used in the management of Alzheimer's?
Acetylcholinesterase inhibitors Memantine
70
What is the mechanism of action of the acetylcholinesterase inhibitors, which can be used in the management of Alzheimer's?
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
Give some examples of acetylcholinesterase inhibitors which can be used in the management of Alzheimer's disease
Donepezil, rivastigmine, galantamine
72
What are some of the side effects of the acetylcholinesterase inhibitors which can be used in the management of Alzheimer's disease?
Bradycardia, muscle cramps, nausea, diarrhoea and headaches Contraindicated in patients with asthma and COPD
73
What is the mechanism of action of memantine, a drug which can be used in the management of Alzheimer's disease?
Antagonist of NMDA receptors which bind glutamate
74
When can memantine be prescribed?
For patients with moderate Alzheimer's or patients that can't tolerate acetylcholinesterase inhibitors
75
What medications can be used in the management of ADHD?
STIMULANTS Methylphenidate (ritalin), dexamfetamine and lisdexamfetamine NON-STIMULANTS Atomoxetine, antidepressants e.t.c
76
What is the mechanism of action of methylphenidate (ritalin) which can be used in the management of ADHD?
Improves dopaminergic neurotransmission in networks involved in executive functioning e.g prefrontal cortex
77
What are some of the possible side effects or methylphenidate (ritalin)?
Appetite and sleep reduction Dysphoria Anxiety Tics
78
What is the mechanism of action of atomexetine, a medication which can be used in the management of ADHD?
Noradrenergic and dopaminergic agonist
79
Which anticonvulsants are most useful in patients with bipolar disorder who are primarily manic/ hypomanic vs primarily depressed?
Primarily manic/ hypomanic - sodium valproate Primarily depressed - lamotrigine
80
What tests should be done before starting a patient on sodium valproate
LFTs U&Es Platelets
81
What are some of the signs of lithium toxicity?
Blurred vision Coarse tremor Ataxia Drowsiness
82
If clozapine has been missed for >48 hours, what is the most appropriate management?
Restarted at the starting dose of 12.5mg
83
What is the role of D1 receptors?
Stimulate cAMP
84
What is the role of D2 receptors?
Inhibit adenyl cyclase, inhibit Ca2+ channels and open K+ channels
85
Which EPSE is most associated with dysphonia?
Akathisia | akathisia is the EPSE associated with causing internal restlessness
86
What are some of the side effects of clozapine?
``` Weight gain Hyper-salivatino Constipation Seizures Agranulocytosis ```
87
Which EPSE are most receptive to treatment with anticholinergics?
Parkinsonism and acute dystonic reaction
88
Which antipsychotic is most associated with a risk of causing myocarditis and should therefore only be started in hospital?
Clozapine
89
Which pathways in the brain are responsible for motivation and reward systems?
Mesolimbic and cortical dopamine pathways
90
How does alpha-adrenergic blockade (S/E of antipsychotics) present?
Dizziness Lightheadedness Postural hypotension
91
Which antipsychotic is most associated with causing metabolic syndrome and should therefore be avoided in people with diabetes?
Olanzapine
92
Which pathway in the brain is responsible for prolactin release?
Tuberoinfundibular dopamine pathway
93
Prolonged QT is a side effect more associated with which type of antipsychotics?
Typicals
94
Which dopamine pathway is responsible for the extra-pyramidal motor system?
Nigrastriatal dopamine pathway
95
Which receptors do typicals and antitypical antipsychotics mainly block?
Typicals - D2 Atypical - block more 5HT2 (serotonin) than D2 (dopamine)
96
Why are atypical antipsychotics less likely to cause EPSE than typical antipsychotics?
Atypical antipsychotics block more 5-HT2A (serotonin) than D2 (dopamine) receptors
97
Which dopamine pathway is responsible for the control of prolactin release?
Tuberoinfundibular dopamine pathway
98
What is the role of dopamine (D2) receptors in the brain?
Inhibition of adenylyl cyclase Opening of potassium channels
99
How are SSRIs eliminated from the body?
Hepatic metabolism
100
Which class of antidepressants should SSRIs NOT Be given alongside?
MOAIs Together can cause serotonin syndrome (excess levels of serotonin)
101
Which class of antidepressants increase bleeding risk and shouldn't be used in conjunction with aspirin?
SSRIs *they interact with serotonin receptors on platelets
102
Why is venlafaxine not used first line?
It has a short half life - can cause serotonin withdrawal syndrome when patients come off it
103
Which medication that can help with sleep should be avoided in the elderly? What can be used as an alternative?
Zopiclone - *Can cause falls Melatonin can be used instead
104
Tricyclics work by increasing the concentration of which neurotransmitters in the synaptic cleft?
Serotonin Noradrenaline Dopamine (they are non-specific)
105
What are the symptoms of discontinuation syndrome which can occur following withdrawal of an SSRI?
Headache Sweating and shivering Increased anxiety GI symptoms
106
In elderly patients prone to falls, which antidepressant drug class should you try ad stick to?
SSRIs - Don't cause sedation or lower BP
107
What are some of the symptoms of hypertensive crisis caused by intake of foods containing tyramine in a patient taking an MAOI?
Anxiety Headache Dyspnoea Nosebleeds
108
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?
Fluoxetine
109
Depression causes what to happen to levels of cortisol in the body?
Causes cortisol levels to be chronically increased
110
Which SSRI is especially associated with prolongation of the QT interval?
Citalopram
111
Nasal congestants shouldn't be taken alongside which class of antidepressants?
MOAIs
112
Which two antidepressants used together are referred to as 'california rocket fuel'?
Mirtazapine and venlafaxine
113
Lithium should be avoided in both pregnancy and breastfeeding
True
114
Which tests should be done every 6 months in a patient taking lithium?
TFTs Parathyroid function Renal function
115
Which tests should be done every 3 months in a patient taking lithium?
Plasma lithium levels U&Es
116
Why is it important to test renal function in patients taking lithium?
There is a risk of nephrogenic DI and reduced glomerular function
117
When a patient is first commenced on lithium, how often should U&Es be formed?
Every 5 days until the therapeutic dose is reached
118
What tests should be done before starting a patient on sodium valproate?
Platelet count LFTs
119
What drug is used to treat benzodiazepine overdose and works as a GABA antagonist?
Flumazenil
120
Which mood stabiliser drug does EUPD typically respond well to?
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
Why can tricyclic drugs cause fatal arrhythmias?
They affect sodium channels in the heart
122
What is the role of GABA?
Inhibitory neurotransmitter Role is for passage of CL- ions into the cell to cause hyper polarisation.
123
What risk to the baby is there with SSRIs when used in the third trimester of pregnancy?
Risk of PPH of the newborn
124
What is the big risk of using antipsychotics in the elderly?
Increased risk of stroke and VTE
125
What is first line for delirium tremens/ alcohol withdrawal?
Oral chlordiazepoxide
126
SSRIs + NSAIDs (e.g aspirin) increases the risk of GI bleed, what medication should be given to counter this?
PPI
127
Triptans should be avoided with which antidepressant class?
SSRIs

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