Antipsychotics Flashcards
What common property do all antipsychotics share?
they all reduce dopaminergic neurotransmission
How do typical anti-Ps work?
ability to block dopamine (D2) receptors.
They also have in, varying degrees, M1, Alpha-1 and H1 receptor blockade.
How do atypical anti-Ps work?
Combination of the relatively lower D2 antagonism with the 5HT2A antagonism.
How does 5HT2A antagonism reduces EPSE
by increasing Dopamine in the nigrostriatal areas.
How does 5HT2A antagonism reduce negative symptoms
by improving Dopamine in the prefrontal cortex
How does 5HT2A antagonism have antidepressant effect
by increasing dopamine in the ventromedial prefrontal cortex.
What does 5HT2A antagonism do to hyperprolactinaemia
reduce it
Which phenothiazine has an aliphatic side chain
Chlorpromazine
Which Phenothiazines have a PiperiDine side chain
Thioridazine, pipothiazine
Which Phenothiazines have a PiperiZine side chain
Trifluoperazine, fluphenazine
Name a Butyrophenone
Haloperidol
Name a Thioxanthenes
Flupenthixol, zuclupenthixol
Example of DiphenylbutylPiperidines
Pimozide
Example of Dibenzodiazepines
Clozapine
Example of Benzoxasoles
Risperidone
Thienobenzodiazepines example?
Olanzapine
Dibenzothiazepines example?
Quetiapine
Examples of Substituted benzamides
Sulpiride, amisulpride
Example of Arylpiperidylindole (quinolone)
Aripiprazole
Which three atypicals are available in depot form
Risperidone (available as Risperdal Consta or Paliperidone)
Olanzapine
Aripiprazole (approved in the UK in Jan 2014)
Which depot may be more effective in preventing relapses than others
zuclopenthixol
When may post injection syndrome happen and what is risk of this
from accidental entry into a blood vessel on administration.The incidence of this is < 0.1% and almost all reactions occur within 1 hour of injection.
Which depot must be given under supervision for three hours after the injection is given.
Olanzapine depots
Symptoms of post injection syndrome
Sedation
Confusion, disorientation
Agitation, anxiety, aggression
Extrapyramidal symptoms, dysarthria, ataxia
Dizziness, weakness
Hypertension
Convulsion
AntiPs with highest associated risk of diabetes?
Clozapine and olanzapine
AntiPs recommended for patients with or with risk of developing diabetes?
Amisulpride, aripiprazole, and ziprasidone
Half life and steady state of aripiprazole?
75 hours, 2 weeks
Half life and steady state of olanzapine?
30 hours 1 week
Half life and steady state of risperidone?
Risperidone 20 hours 2-3 days (oral)
Half life and steady state of both amisulpride and clozapine?
12 hours 2-3 days
Half life and steady state of zuprasidone and quetiapine?
6 hours 2-3 days
Which antipsychotic shows most change to EEG of patients on it
Clozapine (47.1%)
What is the term for the point at which the amount of drug administered each day is exactly counterbalanced by the amount eliminated.
steady state
Which antipsychotics are least likely to cause postural hypotension?
Amisulpride
Aripiprazole
Haloperidol
Sulpiride
Trifluoperazine
What scale can be used to ask about sexual symptoms prior to commencing AntiP
Arizona Sexual Experiences Scale (ASEX)
What is propensity for antiPs to cause sexual side effects related to?
effect on prolactin
Which antiP causes most sexual side effects and effect on prolactin
Risperidone, haloperidol
Which antiP causes sexual side effects but not related to prolactin
clozapine
Which antiP Causes a temporary increase in prolactin which then returns to normal within 6 weeks
olanzapine
If sexual side effects can consider adding 5-10 mg of what as can normalise prolactin level?
aripiprazole
The following are which type of side effects:
Galactorrhoea, gynecomastia, menstrual disturbance, lowered sperm count, reduced libido, Parkinsonism, dystonia, akathisia, tardive dyskinesia
Antidopaminergic effects/antimuscarinic
What type of SEs are Dry mouth, blurred vision, urinary retention, constipation
anticholinergic
Which type of SEs are Postural hypotension, ejaculatory failure
Antiadrenergic effects
What type of SE is Drowsiness
Histaminergic effects
Which antiP has highest risk of sudden death and why
Thioridazine has pronounced effects on K+ channels and materially prolongs the QTc interval
Which antiPs have moderate risk of weight gain
Chlorpromazine
Quetiapine
Risperidone
Paliperidone
Which antiPs have high risk of weight gain
clozapine, olanzapine
Apart from switching antiP if weight gain present, which additional measures may be taken?
Aripiprazole augmentation (for clozapine and olanzapine induced weight gain)
Metformin
Orlistat
Liraglutide (for clozapine induced weight gain)
Topiramate
