Antipsychotics Flashcards
What are the three atypical antipsychotics available as a depot?
risperidone
olanzapine
aripiprazole
What is the test dose of haloperidol
25mg
What is the test dose of zuclopenthixol
100mg
What is the test dose of flupentixol
20mg
What is the test dose of pipothiazine
25mg
What is the test dose of fluphenazine
12.5mg
Which antipsychotic is associated with post-injection syndrome
olanzapine
What are the features of post injection syndrome?
Sedation
Confusion, disorientation
Agitation, anxiety, aggression
Extrapyramidal symptoms, dysarthria, ataxia
Dizziness, weakness
Hypertension
Convulsion
What causes post injection syndroe?
accidental injury into a blood vessel on administration
When are patients most likely to deteriorate on a depot?
immediately after a depot
What drug is suggested by Maudsley for management of akathisia?
propranolol
In who is dystonia more common?
Young males
Neuroleptic naïve
High potency drugs e.g. haloperidol
In who is pseudo-parkinsonism more common in ?
elderly females
those with preexisting neuro damage e.g. stroke
What is the prevalence of akathisia?
25%
In whom is tardive dyskinesia more common?
Elderly women
Affective illness
If EPSE early on in treatment
How long does it take for dystonia to develop?
Hours or minutes within commencing antipsychotics
How long does it take for pseudoparkinsonism to develop?
days to weeks after antipsychotic started
How long does it take for akathisia to develop?
hours to weeks
How long does it take for tardive dyskinesia to develop?
months to years
What is the treatment of dystonia?
Anticholinergic drugs
Switch to different AP
Botox
What is the treatment of pseudoparkinsonism?
reduce dose
switch to different AP
Anticholinergics
What is treatment of akathisia?
Reduce dose
Switch to different AP
Propranolol
Mirtazapine
Anticholinergic drugs - trihexyphenidyl, procyclidine
Cyproheptadine
Benzos - diazepam or clonazepam
Clonidine
What is treatment of tardive dyskinesia?
Stop anticholinergic
Reduce dose
Switch to atypical AP
Tetrabenazine
Ginkgo biloba
Other than APs, what else can cause EPSEs?
SSRIs
TCAs
Schizophrenia if never received medication
Withdrawal of APs
Anti-emetics - metoclopramide and prochlorperazine
Lithium
CCBs - particularly flunarizine and cinnarizine
What is dystonia
Prolonged and unintentional muscular contractions of voluntary or involuntary muscles
What is a lifethreatening complication of EPSEs
Laryngeal dystonia
What is torticollis?
Cervical muscle spasms resulting in a twisted posturing of the neck
What is trismus
lock jaw
What is opisthotonus?
Arched posturing of the head trunk and extremities
What are oculogyric crises
involuntary contraction of one or more of the extraocular muscles, which may result in a fixed gaze with diplopia
What causes EPSEs?
Antagonism of dopaminergic D2 receptors in basal ganglia
What are the suggested mechanisms of weight gain caused by APs?
5HT2a and 5-HT2c antagonism
D2 and D3 antagonism
H1 and M3 antagonism
Hyperprolactinemnia
Increased serum leptin (leading to leptin desensitisation)
Ghrelin
What is the hardest EPSE to treat?
Akathasia
Which 2 APs confer a high risk of weight gain?
Clozapine and olanzapine
Which four APs confer a moderate risk of weight gain?
Chlorpromazine
Quetiapine
Risperidone
Paliperidone
What APs are advised to switch to for weight gain?
Aripiprazole
Ziprasidone
Lurasidone
What AP is recommended for AP induced weight gain as augmentation?
Aripiprazole
What are potential medical treatments of AP induced weight gain ?
Metformin
Orlistat
Liraglutide (for clozapine induced weight gain)
Topiramate
What is the cause of hyperprolactinaemia?
Dopamine inhibits prolactin so dopamine antagonists increase prolactin levels
What are the features of hyperprolactinaemia?
Galactorrhoea
Menstrual difficulties
Gynaecomastia
Hypogonadism
Sexual dysfunction
What does longstanding hyperprolactinaemia increase the risk of ?
Osteoporosis
Breast cancer
What APs are prolactin sparing?
Clozapine
Aripiprazole
Asenapine
Quetiapine
What APs cause a minor change in prolactin?
Lurasidone
Olanzapine
Ziprasidone
What APs cause a major change in prolactin?
All the typical antipsychotics
Risperidone
Amisulpride
Paliperidone
Sulpiride
How often should prolactin be measured when on APs?
Before starting AP
Measure at 3 months if sx present
If no symptoms present measure annually
What antipsychotic is most likely to cause EEG changes?
Clozapine
What antipsychotic is least likely to cause EEG changes?
Quetiapine
Give examples of typical APs
Chlorpromazine
Flupenthixol
Zuclopenthixol
Perphenazine
Trifluoperazine
Sulpiride
Haloperidol
Give examples of atypical APs
Clozapine
Risperidone
Olanzapine
Quetiapine
Ziprasidone
Amisulpride
Give examples of third generation APs
Aripiprazole
Brexpiprazole
Cariprazine
What is the main mechanism of action of typical APs?
D2 antagonism
What are the other effects of typical APs?
Antagonism of M1, H1 and alpha-1 receptors
What are the mechanisms of action of atypical APs?
D2 antagonism
5-HT2a antagonism
5-HT1a agonism
Rapid D2 dissociation
What are other mechanisms of action for atypical APs?
Antagonism of M1, H1 and alpha 1 receptors
Give an example of a phenothiazine with an aliphatic side chain
Chlorpromazine
Give an example of phenothiazine with a piperidine side chain?
Thioridazine
Pipothiazine
Give an example of a phenothiazine with a piperazine side chain?
Trifluoperazine
Fluphenazine
Give an example of a butyrophenones?
Haloperidol
What are the structural characteristics of butyrophenones?
Butyrophenone structure with a tertiary amine
Give examples of thiaxanthenes?
Flupenthixol
Zuclopenthixol
Give an example of a diphenylbutylpiperidine?
pimozide
What is the class and structure of clozapine?
Dibenzodiazepine
Two benzene rings and a diazepine ring
What class is risperidone?
Benzoxasole
What structure is olanzapine
thienobenzodiazepine with a benzodiazepine and thiophene ring
Give the structure of quetiapine
Dibenzothiazepine with a benzothiazepine ring
Give examples of substituted benzamides
Sulpiride
Amisulpride
What is the hypothesis for what causes tardive dyskinesia?
post-synaptic dopamine D2 receptor super sensitivity due to chronic blockade of receptors
What are non-modifiable risk factors for tardive dyskinesia?
advancing age
female sex
ethnicity - african and white descent
Longer illness duration
LD and brain damage
Negative sx in schizophrenia
mood disorders
What are modifiable risk factors in tardive dyskinesia?
Diabetes
Smoking
Alcohol and substance misuse
FGA vs SGA treatment
Higher antipsychotic dose
Anticholinergic co-treatment
Akathisia
Which antipsychotics have a lower propensity for TD?>
Clozapine - best
Quetiapine
Olanzapine
Aripiprazole
Which APs are highest risk of postural hypotension
Quetiapine and clozapine
Which APs have lowest risk of hypotension?
Lurasidone
Asenapine
What APs should be tried if postural hypotension is a problem?
Amisulpride
Aripiprazole
Haloperidol
Sulpiride
Trifluoperazine
