Antipsychotics Flashcards
(118 cards)
1
Q
When were antipychotics introduced?
A
1950s
2
Q
Antipsychotics do not only treat the symptoms but also the cause
True or false?
A
False
Treat only the symptoms
3
Q
Name the two major classes of antipsychotics
A
Dopamine receptor antagonists (typical)
Serotonin-dopamine antagonists (atypical)
4
Q
How do dopamine antipsychotics work?
A
Blocks the D2 receptor -> improves positive symptoms
5
Q
Which dopamine pathways are most important for therapeutic effects?
A
Mesolimbic
Mesocortical
6
Q
Which transmitters are involved in dopamine antipsychotics?
A
5HT
NE
GABA
Glutamate
7
Q
How is the mesolimbic pathway related to psychosis?
A
Dopamine agonist hyperactivity -> psychotic symptoms
8
Q
How is the mesocortical pathway related to psychosis?
A
Dopamine agonist deficit -> negative and cognitive psychotic symptms
9
Q
Give causes of decreased dopamine agonists in the mesocortical pathway
A
Excito-toxicity of glutamate system
Secondary to inhibition by excess serotonin
D2 block by antipsychotics
10
Q
Which degenerative process could explain the worsening of negative psychotic symptoms over time?
A
Deficit of dopamine agonists in the mesocortical pathway
11
Q
Which nervous system is the nigrostriatal pathway part of?
A
Extrapyramidal nervous system
12
Q
What is the function of the nigrostriatal pathway?
A
Controls motor movements
13
Q
What is the effect of a dopamine agonist deficit in the nigrostriatal pathway?
A
Movement disorders
Extrapyramidal side effects (EPSE)
14
Q
What is the function of the tuberoinfinidbular pathway?
A
Controls prolactin secretion
15
Q
What is the effect of dopamine antagonists on the tuberoinfindibular pathway?
A
Inhibits prolactin
16
Q
What are indications for antipsychotics?
A
Psychotic disorders Dementia MDD augmentation OCD augmentation Tic disorders
17
Q
What element of dementia do antipsychotics assist with?
A
Behavioural symptoms
18
Q
Discuss the acute management of psychosis
A
Lorazepam 2-4mg imi w/
IM
- Haloperidol 5 – 10mg/2-4h (max 40mg/d)
• Olanzapine (not with BZ) 10mg 2-4h (max 30mg/d)
• Ziprasidone 10 – 20mg/4h (max40mg/d)
• Zuclopenthixol-acetate 50 – 100mg/ 72h (max
400mg over 2 weeks)
19
Q
Give another name for typical antipsychotics
A
1st generation antipsychotics
20
Q
Give another name for atypical antipsychotics
A
2nd generation antipsychotics
21
Q
Antagonism of which receptors is performed by 1st generation antipsychotics?
A
D2
M1
H1
Alpha-1
22
Q
Antagonism of which receptors is performed by 2nd generation antipsychotics?
A
5HT2A M1 H1 2HT2c Alpha-1
23
Q
Agonism of which receptor is performed by 2nd generation antipsychotics?
A
5HT1A
24
Q
Give common examples of 1st generation antipsychotics
A
Haloperidol
Chlorpromazine
25
Give common examples of 2nd generation antipsychotics
Clozapine
Risperidone
Olanzapine
26
Name the drug classes of 1st generation antipsychotics
```
Butyrophenone
Phenothiazines
Diphenylbutylpiperidine
Benzamide
Thioxanthines
```
27
Give examples of butyophenone
Haloperidol
28
Give examples of phenothiazines
Chlorpromazine
Trifluperazine
Fluphenazine
29
Give examples of diphenylbutylpiperidine
Pimozide
30
Give examples of benzamide
Sulpiride
31
Give examples of thioxanthenes
Flupenthixol
| Zuclopenthixol
32
What are the differences and similarities between 1st generation antipsychotics
Differ in molecular structure
Differ in potency
Differ in side effect profiles
Equal positive symptom efficacy
33
What is the dosage range for chlorpromazine?
200-800mg
34
What is the dosage range for haloperidol?
0.5-15mg
35
What is the dosage range for trifluoperazine?
2-15mg
36
What is the dosage range for pimozide?
1-12mg
37
When is the peak oral concentration of 1st generation antipsychotics?
1-4hrs
38
When is the peak parenteral concentration of 1st generation antipsychotics?
30-60min
39
How quickly does the antipsychotic effect take place with 1st generation antipsychotics?
D2 receptor block = immediate
| But effects takes weeks
40
What are the side effects of high potency 1st generation antipsychotics?
Increased EPSE
Decreased anti-Ach
Decreased anti-epileptic
41
What are the side effects of the D2 receptor block dueto 1st generation antipsychotics?
```
Antipsychotic effect
Worse negative symptoms
Movement disorders
ESPE
Hyperprolactinaemia
```
42
What are the side effects of the muscarinic cholinergic block due to 1st generation antipsychotics
Mitigates D2 block effects -> less ESPE
43
Name 2nd generation antipsychotics
```
Clozapine
Risperidone
Olanzapine
Quetiapine
Aripriazole
Ziprasidone
Palperidone
Amisulpiride
Sulpiride
```
44
Give the trade name for clozapine
Leponex
45
Give the trade name for risperidone
Risperdal
46
Give the trade name for olanzapine
Zyprexa
47
Give the trade name for quetiapine
Seroquel
48
Give the trade name for ariprizaole
Ablify
49
Give the trade name for ziprasidone
Geodon
50
Give the trade name for palperidone
Invega
51
Give the trade name for amisulpiride
Solian
52
Give the trade name for sulpiride
Eglonyl
53
What kind of antagonist is amisulpiride?
Selective D2/3 antagonist
54
What is the effect of 5HT1A agonism by 2nd generation antipsychotics?
Increased dopamine agonist release in prefrontal cortex -> decreased glutamate release
55
Which 2nd generation antipsychotics commonly cause 5HT1A agonism?
Ziprasidone
Quetiapine
Clozapine
56
What is the dosage range for olanzepine?
5-20mg
57
What is the dosage range for clozapine?
100-800mg
58
What is the dosage range for risperidone?
1-8mg
59
What is the dosage range for paliperidone?
3-12mg
60
What is the dosage range for quetiapine?
300-800mg
61
What is the dosage range for amisulpiride?
100-800mg
62
Give indications for 2nd generation antipsychotics`
```
Severe EPSE
Tardive dyskinesia
1st episode in young person
Better for - symptoms
Treatment-resistance
NMS rechallenge
Unacceptable prolactin levels
Mood symptoms
Increased suicide risk
Behavioural symptoms in elderly
```
63
Which 2nd generation antipsychotic is preferred in treatment resistance?
Clozapine
64
What are side effects of 2nd generation antipsychotics?
Metabolic disturbances
65
What options are there when patient is experiencing side effects?
Reduce dose
Switch medications
Treat side effect
66
Name advantages of 1st generation antipsychotics
Effective
| Affordable
67
Name disadvantages of 1st generation antipsychotics
```
EPSE
Tardive dyskinesia
Limited - symptom effectiveness
Neurocognitive symptoms
20% no treatment response
```
68
Name advantages of 2nd generation antipsychotics
Fewer EPSE
Effective with - symptoms
Effective with neurocognitive deficits
Mood problems assoc w/ schizophrenia
69
Name disadvantages of 2nd generation antipsychotics
Cardiac conduction abnormalities
Metabolic syndrome
High cost
Limited availability
70
What are metabolic side effects of 2nd generation antipsychotics?
```
Dyslipidaemias
Hyperglycemia
Insulin resistance
Obesity
Hypertension
Pro-inflammatory state
Pro-thrombotic state
```
71
Name risk factors for acute dystonia in antipsychotic treatment
Young
Males
High potency
72
What abnormal movements are seen in acute dystonia?
```
Torticollis
Trismus
Tongue protrusion
Dysphagia
Laryngopharyngeal spasm
Oculogyric crisis
```
73
What is the treatment for acute dystonia in antipsychotic treatment
Biperidine 5mg IVI/IMI
74
What is the cause of EPSE in antipsychotic treatment?
Dopamine agonist receptor blocked -> increased acetylcholine
75
What is the treatment for parkinsonism in antipsychotic treatment?
```
Anticholinergics
- orphenadrine 50mg po 1-3x/d
- biperidine 2mg 1-3x/d
Lower dose
Replace with serotonin dopamine agonist (SDA)
```
76
What is akathisia?
Akathisia is a movement disorder characterized by a feeling of inner restlessness and inability to stay still.
77
What is the treatment for akathisia in antipsychotic treatment?
```
Propanolol 10-30mg tds
BZDs
Lower dosage
Change to low potency typical
Change to SDA
```
78
What drug class does propanolol belong to?
Beta blocker
79
Tardive dyskinesia due to antipsychotic treatment is reversible/irreversible
Irreversible
80
Name risk factors for tardive dyskinesia in antipsychotic treatment
Female
Elderly
Increased dosage
81
What is the cause of tardive dyskinesia in antipsychotic treatment?
Upregulation of D2 receptors in the nigrostriatal pathway
82
How can you treat tardive dyskinesia in antipsychotic treatment?
Reduce dose
Stop anticholinergics
Try clozapine
Try SDA
83
What are the features of neuroleptic malignant syndrome
Advanced parkinsonism
| Catatonia
84
Which neurotransmitters are blocked in neuroleptic malignant syndrome?
GAMA
NE
5HT
Ach
85
Neuroleptic malignant syndrome is potentially lethal
| True or false?
True
86
Name features of neuroleptic malignant syndrome
```
Diaphoresis
Autonomic instability
Tremor
Dysphagia
Mutism
Incontinence
Leukocytosis
Delirium
Increased CK
```
87
What is the management of neuroleptic malignant syndrome?
1. Stop all antipsychotics
2. Admit to medical ward/high care
3. Exclude other serious conditions
4. Supportive measures
- cool pt off
- hydration
- monitor vitals
- NG tube
5. Diazepam/lorazepam
6. DVT prophylaxis
7. Beware renal failure
8. Dantrolene/bromocriptine
9. ECT if no response
10. Rechallenge with low dose atypical + ECT
88
Why should you avoid anticholinergics in neuroleptic malignant syndrome?
DVT prophylaxis
89
Name anticholinergic side effects in neuroleptic malignancy syndrome
```
Dry mouth
Blurred vision -> dry eyes
Constipation
Urinary retention
Cognitive dysfunction
```
90
What are the anticholinergic side effects in neuroleptic malignancy syndrome due to?
Muscarinic antagonism
91
What are the cardiovascular side effects in neuroleptic malignancy syndrome due to?
Alpha-1 antagonism
| Muscarinic antagonism
92
Name the cardiovascular side effects in neuroleptic malignancy syndrome
```
Postural hypotension
Tachycardia
ECG changes - prolonged QT interval
Arrythmias
Cardiomyopathy
```
93
What side effect can clozapine have on the heart?
Cardiomyopathy
94
Name the neurological side effects in neuroleptic malignancy syndrome
Lowers the seizure threshold
95
What are the neurological side effects in neuroleptic malignancy syndrome due to?
D2 antagonism
96
Name the cognitive side effects in neuroleptic malignancy syndrome
Sedation
Headaches
Decreased concentration
Depression
97
What are the cognitive side effects in neuroleptic malignancy syndrome due to?
Histaminergic antagonism
98
Name the sexual side effects in neuroleptic malignancy syndrome
Decreased libido
Anorgasmio
Erectile dysfunction
Ejaculation inhibition
99
What are the sexual side effects in neuroleptic malignancy syndrome due to?
D2 antagonism
Alpha-1 antagonism
Muscarinic antagonism
100
Name the endocrine side effects in neuroleptic malignancy syndrome
```
Sexual dysfunction
Galactorrhoea
Increased weight
SIAHD
Incr/decr glucose
```
101
What does SIAHD stand for?
Syndrome of inappropriate antidiuretic hormone secretion
102
What are the endocrine side effects in neuroleptic malignancy syndrome due to?
Increased prolactin
103
Name the hypersensitivity side effects in neuroleptic malignancy syndrome
Photosensitivity
Skin reactions
Aganulocytosis
104
Name the ocular side effects in neuroleptic malignancy syndrome
Retinitis pigmentosa
105
Name the gastrointestinal side effects in neuroleptic malignancy syndrome
Weight gain
Metabolic syndrome
Constipation
Sialorrhoea
106
What are the gastrointestinal side effects in neuroleptic malignancy syndrome due to?
5HT2c antagonism
| H1 antagonism
107
Name indications for clozapine
Treatment resistant schizophrenia
Introlerable EPS
Tardive dyskinesia
108
Why should you monitor WBC when taking clozapine?
Aganulocytosis risk
109
What is agranulocytosis?
An acute condition involving a severe and dangerous leukopenia, most commonly of neutrophils.
110
What are the dangers of clozapine?
Myocarditis
Toxic megacolon
Seizures (high doses)
Metabolic syndrome
111
Name common side effects of clozapine
Hypersalivation
Constipation
Weight gain
Sedation
112
Until when should depot preparations not be used in antipsychotic treatment?
Until response to oral medication demonstrated
113
Name the depot preparations of antipsychotic treatment
- Flupentixol decanoate 10 - 60mg 2-4 weekly
- Fluphenazine decanoate 6.25 - 50mg 2-4
weekly
- Zuclopenthixol decanoate 100 - 400mg 2-
4weekly
- Risperidone 25-50mg 2 weekly
- Paliperidone
114
What should be taken into consideration when prescribing antipsychotic treatment?
```
Prominent current symptoms
Comorbid conditions
Past therapeutic response
Adverse effects
Patient choice
Patient expectations
Gradual dose increased
Lowest effective dose
Sufficient time (4-6w)
Prolonged use of prophylactic treatment
```
115
How can you give antipsychotic medication in a patient who is non-compliant?
Long acting depot injections
116
Why is zuclopenthixol-acetate best in the chronic psychosis management?
Late action
| Long duration
117
Explain oculogyric crisis
A dystonic reaction to certain drugs or medical conditions characterized by a prolonged involuntary upward deviation of the eyes.
118
How can temporal lobe epilepsy resemble schizophrenia?
Presents with psychotic aggression and hallucinations
