MH- Pharmacology Flashcards

1
Q

Main side effects of TYPICAL antipsychotics

A

EPSE - dystonia (acute or tardive), akathisia (acute or tardive), tardive dyskinesia, parkinsonism (acute)

Anticholinergic effects - confusion, dry mouth, constipation, urinary retention, blurred vision

Hyperprolactinaemia - galactorrhoea, amenorrhoea, decreased libido, impotence, osteoporosis (W)

Weight gain but less metabolic syndrome than atypicals

Sedation

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2
Q

Main side effects of ATYPICAL antipsychotics

A

Metabolic syndrome/CV risk - weight gain, dyslipidaemia, hyperglycaemia, insulin resistance

Alpha-blockade - dizziness, postural hypotension, impotence

Sedation

Less EPSE than typical antipsychotics but can at high enough doses

QTc prolongation

Generally less anticholinergic side effects than typicals

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3
Q

What are some clinical considerations when choosing antipsychotics in older adults?

A
  1. Typicals cannot be used in PD or DLB due to increased risk of EPSE
  2. Atypicals can increase stroke risk in dementia patients
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4
Q

How can neuroleptic malignant syndrome & serotonin syndrome be distinguished?

A

NMS - SS

Antipsychotic - antidepressants

Muscle rigidity - tremor, myoclonic movements, seizure

Fever, pallor - sweating, flushing

No GIT symptoms - N+V, abdo pain, diarrhoea

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5
Q

What is neuroleptic malignant syndrome & how is it Rx?

A

Occurs when starting new or sudden increase in dose of antipsychotic -
Can lead to rhabdomyolysis & AKI

Change in mental state - agitation, confusion
Global, severe muscle rigidity
Autonomic dysfunction - labile BP, tachycardia, fever
Pallor
Raised CK & WCC
Rx - stop medication, supportive care (esp. rehydration), often ICU support, can use dopamine agonists & muscle relaxant

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6
Q

What is serotonin syndrome & how is it Rx?

A

Overstimulation of serotonin pathways - usually by accidental combination of 2+ antidepressants

Change in mental state - agitation, delirium, confusion, disorientation
Sweating, flushing, labile BP
N+V, diarrhoea, abdominal pain

Rx - stop medications, supportive care, sedation with benzo +/- antidote (anticholinergic with serotonin receptor antagonist properties)

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7
Q

What are the 4 EPSE, clinical features & Rx?

A
  1. Dystonia (Acute or Tardive) - muscle spasms, abnormal posturing & torsion (i.e. neck movements & tongue protrusion) - particularly eyes and larynx. Benzotropine (anticholinergic)
  2. Tardive dyskinesia - constant, purposeless movements usually of facial muscles i.e. lip smacking, grimacing. No good Rx, switch drugs, clozapine better for it
  3. Akathisia (acute or tardive) - restlessness where patient feels need to move but it does not help it (unlike in restless leg syndrome), crawling sensation. Propranolol or diazepam
  4. Parkinsonism - cogwheel rigidity, bradykinesia, resting tremor, abnormal gait. Benzotropine
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8
Q

What is the effect on positive, negative & cognitive features of psychosis with typical vs. atypical antipsychotics?

A

Typical - mainly only reduce positive symptoms of psychosis (delusions, hallucinations)

Atypical - reduce positive symptoms but may also affect negative and cognitive features

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9
Q

What are the characteristics (advantages/disadvantages) and any common uses/indications of HALOPERIDOL?

A

Least sedating antipsychotic - commonly used for delirium
Worst for EPSE - avoid in PD, DLB
Antiemetic effect - commonly used in pal care nausea

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10
Q

What are the characteristics (advantages/disadvantages) and any common uses/indications of OLANZAPINE?

A

Very efficacious but worst for weight gain and risk of metabolic syndrome
Rapid onset and very sedating - commonly used in ED setting/acute behaviour disturbance
Mood stabilising characteristics

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11
Q

What are the characteristics (advantages/disadvantages) and any common uses/indications of QUETIAPINE?

A

Most sedating
Most associated with QTc prolongation
Less weight gain

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12
Q

What are the characteristics (advantages/disadvantages) and any common uses/indications of RISPERIDONE?

A

Less associated weight gain
Not sedating
Most associated with hyperprolactinaemia - monitor prolactin levels
Good choice if view to change from oral to depot injection
Used in BPSD - most effective/evidence, on PBS

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13
Q

What considerations need to be made with antipsychotics and dementia?

A

Increase risk of stroke in dementia patients - esp. if they have other stroke risk factors

Only use if they have intractable aggression/psychosis that is not manageable with environmental/psychosocial methods

Only use if low-moderate risk of stroke

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14
Q

What are the side effects/toxicity of CLOZAPINE?

A

Decreases seizure threshold - increased risk of seizure

Agranulocytosis - increased risk of infection, esp. encapsulated bacteria, often present with sore throat

Non-specific resp symptoms - difficulty breathing, cough

Cardiac - tachycardia, myocarditis (usually first 4 weeks), can lead to cardiomyopathy, metabolic syndrome

Anticholinergic, metabolic syndrome, sedation, postural hypotention +++

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15
Q

What should be monitored when starting CLOZAPINE?

A
  1. Agranulocytosis - FBE (neutrophil count early, eosinophils later), weekly initially, then monthly
  2. Myocarditis - baseline ECG and/or ECHO, ongoing monitoring of CRP, troponins, vitals
  3. Metabolic syndrome - BMI, waist circumference, lipids, BGL/HbA1c
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16
Q

How does smoking affect CLOZAPINE?

A

Smoking increases hepatic clearance of clozapine, therefore run on lower serum levels

If suddenly stop smoking levels can rapidly increase, leading to toxicity

17
Q

Which antipsychotics have been shown to have some benefit on negative symptoms of schizophrenia?

A

Clozapine and olanzapine

18
Q

Describe the onset of effect of ANTIPSYCHOTICS

A

More immediate affect on calming/reducing agitation, however there is a delay in effect on disease/symptoms (disorder response) of ~2-4 weeks

19
Q

Describe the onset of effect of DEPRESSANTS

A

Delayed onset of disorder response - takes ~4-8 weeks

20
Q

How long should antidepressants be used in Rx of depression?

A

If first episode - continue for 6-12 months after stabilised/recovered

If 2 - 3+ episodes within 5 years should have 3-5 year maintenance therapy

If severe, psychotic features may require longer maintenance course

21
Q

How long should antipsychotics be used in Rx of schizophrenia?

A

First episode psychosis can begin to withdraw after 12 months if good effect

Relapse is common however, so need to monitor for early signs and reintroduce medication

If negative signs often require ongoing Rx

22
Q

What antidepressants are used 1st line and 2nd line in depression Rx?

A

1st = SSRI, SNRI, Mirtazipine

2nd = TCA, MAOI

23
Q

What are examples of, mechanism of action, S/E and uses of SSRIs?

A
  1. Sertraline, escitalopram, citalopram, fluoxetine, paroxetine
  2. Inhibits pre-synaptic reuptake of serotonin
  3. GIT upset and sexual dysfunction (common/prominent), weight gain (less so than others), dizziness, headache, sweating, insomnia, hyponatraemia
  4. Used first line for depression and can be beneficial in anxiety disorder Rx. Generally well tolerated
24
Q

What are common side effects generally of antidepressants?

A
Weight gain 
Insomnia 
GIT upset 
Anticholinergic effects 
Alpha-blockade effects 
Sexual dysfunction
25
Q

What are examples of, mechanism of action, S/E and uses of SNRIs?

A
  1. Venlafaxine, duloxitine
  2. Inhibits serotonin and NA reuptake
  3. Same as SSRIs + constipation, HTN, hypercholesterolaemia
  4. Can be used 1st line in depression, Venlafaxine 1st line in treatment resistant, particularly useful in melancholic or severe depression
26
Q

What is the mechanism of action, S/E and uses of Mirtazipine?

A
  1. Inhibits H1 receptors and presynaptic alpha2 and 5HT2 & 3 receptors
  2. Weight gain, increased appetite and sedation prominent. Also oedema and postural hypotension common
    Less sexual and GIT S/Es than SSRIs and SNRIs
  3. Commonly used to exploit side-effects - depression with weight loss and insomnia
27
Q

What are examples of, mechanism of action, S/E and uses of TCA?

A
  1. Amitriptyline, imipramine
  2. Blocks muscarinic, alpha and histamine receptors and some also block reuptake of NA and serotonin
  3. Usual (wt gain, insomnia, GIT upset, sexual dysfunction) + tachycardia, postural hypotension, anticholinergic side-effects and confusion/increased risk of delirium
  4. Efficacious but less well tolerated and toxic in overdose so used 2nd line
28
Q

What are examples of, mechanism of action, S/E and uses of MAOIs?

A
  1. Phenelzine
  2. Inhibits mitochondrial enzymes MAO-B and -A which metabolise NA, serotonin and dopamine
  3. Generally well tolerated and less side effects but risk of hypertensive crisis (requires dietary restriction and monitoring) so less commonly used
  4. Treatment resistant, melancholic and atypical depression